CA2925363C - Composition, especially in the form of a lubricant gel comprising a local anaesthetic and polyhexanide - Google Patents
Composition, especially in the form of a lubricant gel comprising a local anaesthetic and polyhexanide Download PDFInfo
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- CA2925363C CA2925363C CA2925363A CA2925363A CA2925363C CA 2925363 C CA2925363 C CA 2925363C CA 2925363 A CA2925363 A CA 2925363A CA 2925363 A CA2925363 A CA 2925363A CA 2925363 C CA2925363 C CA 2925363C
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- 239000000203 mixture Substances 0.000 title claims abstract description 381
- 239000000314 lubricant Substances 0.000 title claims abstract description 58
- VAZJLPXFVQHDFB-UHFFFAOYSA-N 1-(diaminomethylidene)-2-hexylguanidine Polymers CCCCCCN=C(N)N=C(N)N VAZJLPXFVQHDFB-UHFFFAOYSA-N 0.000 title claims abstract description 51
- 229920002413 Polyhexanide Polymers 0.000 title claims abstract description 51
- 229940093158 polyhexanide Drugs 0.000 title claims abstract description 49
- 230000003444 anaesthetic effect Effects 0.000 title abstract description 9
- 230000002421 anti-septic effect Effects 0.000 claims abstract description 47
- 238000000034 method Methods 0.000 claims abstract description 42
- 239000004480 active ingredient Substances 0.000 claims abstract description 26
- 238000001839 endoscopy Methods 0.000 claims abstract description 24
- 238000002627 tracheal intubation Methods 0.000 claims abstract description 21
- 150000003839 salts Chemical class 0.000 claims abstract description 18
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 15
- 239000003589 local anesthetic agent Substances 0.000 claims description 35
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 25
- 239000003755 preservative agent Substances 0.000 claims description 22
- 210000004877 mucosa Anatomy 0.000 claims description 20
- 238000004659 sterilization and disinfection Methods 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 16
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 13
- 229920002678 cellulose Chemical class 0.000 claims description 13
- 235000010980 cellulose Nutrition 0.000 claims description 13
- 229960004194 lidocaine Drugs 0.000 claims description 13
- 239000000126 substance Substances 0.000 claims description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 12
- 239000002585 base Substances 0.000 claims description 12
- 150000005846 sugar alcohols Polymers 0.000 claims description 12
- -1 alkylene glycols Chemical class 0.000 claims description 10
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims description 10
- 239000004615 ingredient Substances 0.000 claims description 10
- 239000001913 cellulose Chemical class 0.000 claims description 8
- 229960005015 local anesthetics Drugs 0.000 claims description 8
- 238000004806 packaging method and process Methods 0.000 claims description 8
- 210000003708 urethra Anatomy 0.000 claims description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 7
- 230000000069 prophylactic effect Effects 0.000 claims description 7
- 206010016717 Fistula Diseases 0.000 claims description 6
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 6
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 6
- 230000003890 fistula Effects 0.000 claims description 6
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 6
- 239000002253 acid Substances 0.000 claims description 5
- 150000001408 amides Chemical class 0.000 claims description 5
- 229960005274 benzocaine Drugs 0.000 claims description 5
- 238000011109 contamination Methods 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- 229920002125 Sokalan® Chemical class 0.000 claims description 4
- 229910001860 alkaline earth metal hydroxide Inorganic materials 0.000 claims description 4
- 229940064004 antiseptic throat preparations Drugs 0.000 claims description 4
- 239000000872 buffer Substances 0.000 claims description 4
- 239000003205 fragrance Substances 0.000 claims description 4
- 239000008213 purified water Substances 0.000 claims description 4
- 238000009736 wetting Methods 0.000 claims description 4
- 150000008044 alkali metal hydroxides Chemical class 0.000 claims description 3
- 150000002148 esters Chemical class 0.000 claims description 3
- 229960004393 lidocaine hydrochloride Drugs 0.000 claims description 3
- YECIFGHRMFEPJK-UHFFFAOYSA-N lidocaine hydrochloride monohydrate Chemical compound O.[Cl-].CC[NH+](CC)CC(=O)NC1=C(C)C=CC=C1C YECIFGHRMFEPJK-UHFFFAOYSA-N 0.000 claims description 3
- ZKMNUMMKYBVTFN-HNNXBMFYSA-N (S)-ropivacaine Chemical compound CCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C ZKMNUMMKYBVTFN-HNNXBMFYSA-N 0.000 claims description 2
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 claims description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- 239000004606 Fillers/Extenders Substances 0.000 claims description 2
- 239000006057 Non-nutritive feed additive Substances 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 235000012216 bentonite Nutrition 0.000 claims description 2
- 239000011230 binding agent Substances 0.000 claims description 2
- 239000007853 buffer solution Substances 0.000 claims description 2
- 229960003150 bupivacaine Drugs 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 150000007942 carboxylates Chemical class 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 239000000975 dye Substances 0.000 claims description 2
- 239000003995 emulsifying agent Substances 0.000 claims description 2
- 239000003906 humectant Substances 0.000 claims description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims description 2
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 claims description 2
- 229960002409 mepivacaine Drugs 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 239000011785 micronutrient Substances 0.000 claims description 2
- 235000013369 micronutrients Nutrition 0.000 claims description 2
- 239000011707 mineral Substances 0.000 claims description 2
- 235000010755 mineral Nutrition 0.000 claims description 2
- 239000006174 pH buffer Substances 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Chemical class 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 claims description 2
- 229960001807 prilocaine Drugs 0.000 claims description 2
- 229960001549 ropivacaine Drugs 0.000 claims description 2
- 125000005624 silicic acid group Chemical class 0.000 claims description 2
- 235000012239 silicon dioxide Nutrition 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims description 2
- 239000002562 thickening agent Substances 0.000 claims description 2
- 239000011573 trace mineral Substances 0.000 claims description 2
- 235000013619 trace mineral Nutrition 0.000 claims description 2
- 229940088594 vitamin Drugs 0.000 claims description 2
- 235000013343 vitamin Nutrition 0.000 claims description 2
- 239000011782 vitamin Substances 0.000 claims description 2
- 229930003231 vitamin Natural products 0.000 claims description 2
- 229920001285 xanthan gum Polymers 0.000 claims description 2
- VTUSIVBDOCDNHS-UHFFFAOYSA-N Etidocaine Chemical compound CCCN(CC)C(CC)C(=O)NC1=C(C)C=CC=C1C VTUSIVBDOCDNHS-UHFFFAOYSA-N 0.000 claims 1
- 229960003976 etidocaine Drugs 0.000 claims 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims 1
- 229960004919 procaine Drugs 0.000 claims 1
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 claims 1
- 229960002372 tetracaine Drugs 0.000 claims 1
- 230000002485 urinary effect Effects 0.000 claims 1
- 239000000645 desinfectant Substances 0.000 abstract description 8
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 4
- 239000000470 constituent Substances 0.000 abstract description 2
- 230000009471 action Effects 0.000 description 34
- 239000000499 gel Substances 0.000 description 24
- 208000002193 Pain Diseases 0.000 description 20
- 230000036407 pain Effects 0.000 description 15
- 208000027418 Wounds and injury Diseases 0.000 description 10
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 description 9
- 229960003260 chlorhexidine Drugs 0.000 description 9
- 230000000052 comparative effect Effects 0.000 description 9
- 230000006378 damage Effects 0.000 description 9
- 230000000694 effects Effects 0.000 description 9
- 238000011835 investigation Methods 0.000 description 9
- 238000012360 testing method Methods 0.000 description 9
- 208000014674 injury Diseases 0.000 description 8
- 206010061217 Infestation Diseases 0.000 description 7
- 230000002906 microbiologic effect Effects 0.000 description 7
- 239000000523 sample Substances 0.000 description 7
- 230000001954 sterilising effect Effects 0.000 description 7
- 230000000845 anti-microbial effect Effects 0.000 description 6
- 208000015181 infectious disease Diseases 0.000 description 6
- 229960001774 octenidine Drugs 0.000 description 6
- SMGTYJPMKXNQFY-UHFFFAOYSA-N octenidine dihydrochloride Chemical compound Cl.Cl.C1=CC(=NCCCCCCCC)C=CN1CCCCCCCCCCN1C=CC(=NCCCCCCCC)C=C1 SMGTYJPMKXNQFY-UHFFFAOYSA-N 0.000 description 6
- 238000003860 storage Methods 0.000 description 6
- 230000002411 adverse Effects 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 230000007774 longterm Effects 0.000 description 5
- 235000013772 propylene glycol Nutrition 0.000 description 5
- 230000009467 reduction Effects 0.000 description 5
- 230000009885 systemic effect Effects 0.000 description 5
- 206010040880 Skin irritation Diseases 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 150000002334 glycols Chemical class 0.000 description 4
- 230000007794 irritation Effects 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 230000014759 maintenance of location Effects 0.000 description 4
- 244000005700 microbiome Species 0.000 description 4
- 230000036556 skin irritation Effects 0.000 description 4
- 231100000475 skin irritation Toxicity 0.000 description 4
- 230000029663 wound healing Effects 0.000 description 4
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical class NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- 241000191967 Staphylococcus aureus Species 0.000 description 3
- 230000001580 bacterial effect Effects 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 210000000746 body region Anatomy 0.000 description 3
- 238000002405 diagnostic procedure Methods 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 238000009434 installation Methods 0.000 description 3
- 210000003734 kidney Anatomy 0.000 description 3
- 244000052769 pathogen Species 0.000 description 3
- 230000000704 physical effect Effects 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- 230000002195 synergetic effect Effects 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- 210000000626 ureter Anatomy 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 206010052428 Wound Diseases 0.000 description 2
- 230000003260 anti-sepsis Effects 0.000 description 2
- 239000012752 auxiliary agent Substances 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000000356 contaminant Substances 0.000 description 2
- 238000009109 curative therapy Methods 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 238000003780 insertion Methods 0.000 description 2
- 230000037431 insertion Effects 0.000 description 2
- 230000005923 long-lasting effect Effects 0.000 description 2
- 238000005461 lubrication Methods 0.000 description 2
- 230000000813 microbial effect Effects 0.000 description 2
- 230000001717 pathogenic effect Effects 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 238000011321 prophylaxis Methods 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- QTGIAADRBBLJGA-UHFFFAOYSA-N Articaine Chemical compound CCCNC(C)C(=O)NC=1C(C)=CSC=1C(=O)OC QTGIAADRBBLJGA-UHFFFAOYSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 102000003914 Cholinesterases Human genes 0.000 description 1
- 108090000322 Cholinesterases Proteins 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 229960003831 articaine Drugs 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 230000002238 attenuated effect Effects 0.000 description 1
- 229960000386 benzocaine hydrochloride Drugs 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
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- 230000008859 change Effects 0.000 description 1
- 229940048961 cholinesterase Drugs 0.000 description 1
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- 238000002425 crystallisation Methods 0.000 description 1
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- 238000006900 dealkylation reaction Methods 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
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- 238000003745 diagnosis Methods 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- JAADDQHUJDUAKW-UHFFFAOYSA-N ethyl 4-aminobenzoate;hydron;chloride Chemical compound Cl.CCOC(=O)C1=CC=C(N)C=C1 JAADDQHUJDUAKW-UHFFFAOYSA-N 0.000 description 1
- 230000002743 euphoric effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000013861 fat-free Nutrition 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 244000000058 gram-negative pathogen Species 0.000 description 1
- 244000000059 gram-positive pathogen Species 0.000 description 1
- 230000001632 homeopathic effect Effects 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
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- 230000036512 infertility Effects 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 210000000244 kidney pelvis Anatomy 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000001050 lubricating effect Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229910000000 metal hydroxide Inorganic materials 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
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- 210000002569 neuron Anatomy 0.000 description 1
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- 150000003904 phospholipids Chemical class 0.000 description 1
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Classifications
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
- A61L2300/40—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
- A61L2300/402—Anaestetics, analgesics, e.g. lidocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
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- A61L2400/10—Materials for lubricating medical devices
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Abstract
The present invention relates to a composition, especially pharmaceutical composition, preferably in the form of a lubricant gel and/or lubricant medium, preferably for use as a (local) antiseptic and/or (local) anaesthetic, especially for use in diagnostic and/or therapeutic (operative) interventions, preferably for use in catheterizations, preferably transurethral or suprapubic catheterizations, exploratory procedures, endoscopies, intubations and/or interventions to aid birth, wherein the composition in each case contains effective, especially pharmaceutical active, amounts of at least one local anaesthetic and polyhexanide and/or salts thereof, especially as antiseptic active ingredient and/or constituent (disinfectant).
Description
COMPOSITION, ESPECIALLY IN THE FORM OF A LUBRICANT GEL
The present invention relates to the field of medicine or medical technology. More particularly, the present invention relates to the field of medically useful catheters which can be especially in the form of bladder catheters and/or fistula catheters, and to the area of compositions or lubricants especially useful for facilitating or improving catheterization. The present invention also relates to the area of endoscopy, especially in connection with the medical use of endoscopies or medical probes.
More particularly, the present invention relates to a composition, more particularly a pharmaceutical composition, preferably, in the form of a lubricant gel and/or lubricant, which can be used as a (local) antiseptic and/or (local) anesthetic, and which can he used in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures or the like.
Furthermore, the present invention relates to the use of the composition according to the invention as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations.
Lastly, the present invention relates to containers, catheters, packaging units and kits which comprise the composition according to the invention.
As part of medical procedures for diagnostic, therapeutic or prophylactic purposes, it is frequently necessary to insert medical instruments, such as catheters, into the human or animal body via preferably natural body openings, but also via artificial or
The present invention relates to the field of medicine or medical technology. More particularly, the present invention relates to the field of medically useful catheters which can be especially in the form of bladder catheters and/or fistula catheters, and to the area of compositions or lubricants especially useful for facilitating or improving catheterization. The present invention also relates to the area of endoscopy, especially in connection with the medical use of endoscopies or medical probes.
More particularly, the present invention relates to a composition, more particularly a pharmaceutical composition, preferably, in the form of a lubricant gel and/or lubricant, which can be used as a (local) antiseptic and/or (local) anesthetic, and which can he used in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures or the like.
Furthermore, the present invention relates to the use of the composition according to the invention as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations.
Lastly, the present invention relates to containers, catheters, packaging units and kits which comprise the composition according to the invention.
As part of medical procedures for diagnostic, therapeutic or prophylactic purposes, it is frequently necessary to insert medical instruments, such as catheters, into the human or animal body via preferably natural body openings, but also via artificial or
- 2 -surgically established body openings. Examples of such procedures include catheterizations of the bladder, it being possible to carry out said catheterizations in a transurethral manner or a percutaneous or suprapubic manner, probings, endoscopies, intubations and obstetrical procedures.
In the area of urology, catheters are frequently used as part of diagnostic and therapeutic methods, for example in order to drain urine from the bladder or the kidneys or in order to introduce medicaments or contrast agents into the urogenital tract. A
distinction is made here between percutaneous, especially suprapubic, catheters, which are guided through the skin into the bladder or into the renal pelvis, and transurethral catheters, which are inserted along the urethra or through the urethra into the body or into the bladder. Percutaneous or suprapubic bladder and kidney catheters are primarily used for a prolonged catheter retention time or in cases in which the use of a transurethral catheter is too risky. By contrast, transurethral catheters are preferably used as disposable catheters in diagnostic methods or as long-term catheters generally with a retention time of a few days.
The advantage of transurethral catheters is that, when used properly, they are substantially more gentle for the patient, especially since injuries associated with the placement of the catheter are minimized.
Nevertheless, placement of a transurethral catheter -known as catheterization - is a process which is frequently described as very unpleasant or as even painful and in which there is additionally the risk of urogenital tract injuries. In the prior art, catheterization is facilitated by using auxiliary agents, such as lubricants for example. However, these are frequently merely unsatisfactory with respect to
In the area of urology, catheters are frequently used as part of diagnostic and therapeutic methods, for example in order to drain urine from the bladder or the kidneys or in order to introduce medicaments or contrast agents into the urogenital tract. A
distinction is made here between percutaneous, especially suprapubic, catheters, which are guided through the skin into the bladder or into the renal pelvis, and transurethral catheters, which are inserted along the urethra or through the urethra into the body or into the bladder. Percutaneous or suprapubic bladder and kidney catheters are primarily used for a prolonged catheter retention time or in cases in which the use of a transurethral catheter is too risky. By contrast, transurethral catheters are preferably used as disposable catheters in diagnostic methods or as long-term catheters generally with a retention time of a few days.
The advantage of transurethral catheters is that, when used properly, they are substantially more gentle for the patient, especially since injuries associated with the placement of the catheter are minimized.
Nevertheless, placement of a transurethral catheter -known as catheterization - is a process which is frequently described as very unpleasant or as even painful and in which there is additionally the risk of urogenital tract injuries. In the prior art, catheterization is facilitated by using auxiliary agents, such as lubricants for example. However, these are frequently merely unsatisfactory with respect to
- 3 -the improvement in catheterization that is sought after and with regard to ensuring lower adverse effects during the retention of the catheter in the body.
In order also to achieve a reduction in friction between medical instruments, such as catheters or probes or endoscopes, and skin or mucosa or the body opening, it has been found to be advantageous to use lubricants or lubricant gels as auxiliary agents, so as to prevent skin irritations, pain and injuries due to the procedure or the catheterization. Furthermore, in connection with procedures of the aforementioned type, it is advantageous when a disinfection of the skin or mucosa in the treated area is carried out simultaneously in order to prevent infections and inflammations.
In this connection, first-generation lubricants are predominantly based on fatty or oily substances, though this is disadvantageous in many respects, especially with respect to sterility and wetting properties.
Lubricants meanwhile typically consist of a fat-free gel which may optionally contain an antiseptic active ingredient and/or antiseptic ingredient for reducing the microbial count. Furthermore, it is possible for lubricants or lubricant gels to contain a local anesthetic in order to alleviate the pain during the procedure.
Although the lubricants or lubricant gels known from the prior art sometimes have improved wetting or lubricating properties with respect to oil- and fat-based lubricants used in the first-generation lubricants, they are not always optimal with regard to their action and use, especially with respect to efficacy or onset of action and tolerability.
Especially the action of the optionally used local anesthetic is not always sufficient, and so there is no
In order also to achieve a reduction in friction between medical instruments, such as catheters or probes or endoscopes, and skin or mucosa or the body opening, it has been found to be advantageous to use lubricants or lubricant gels as auxiliary agents, so as to prevent skin irritations, pain and injuries due to the procedure or the catheterization. Furthermore, in connection with procedures of the aforementioned type, it is advantageous when a disinfection of the skin or mucosa in the treated area is carried out simultaneously in order to prevent infections and inflammations.
In this connection, first-generation lubricants are predominantly based on fatty or oily substances, though this is disadvantageous in many respects, especially with respect to sterility and wetting properties.
Lubricants meanwhile typically consist of a fat-free gel which may optionally contain an antiseptic active ingredient and/or antiseptic ingredient for reducing the microbial count. Furthermore, it is possible for lubricants or lubricant gels to contain a local anesthetic in order to alleviate the pain during the procedure.
Although the lubricants or lubricant gels known from the prior art sometimes have improved wetting or lubricating properties with respect to oil- and fat-based lubricants used in the first-generation lubricants, they are not always optimal with regard to their action and use, especially with respect to efficacy or onset of action and tolerability.
Especially the action of the optionally used local anesthetic is not always sufficient, and so there is no
- 4 -satisfactory or sufficient alleviation of pain. In particular, there is frequently no optimal coordination with the other components of the lubricant, and so the efficiency of action of the local anesthetic as such is not always optimized especially with respect to its efficacy or availability at the site of action.
With respect too to antimicrobial or antiseptic properties, the lubricants of the prior art are not always satisfactory, this being linked especially to the antiseptic active ingredients and/or antiseptic ingredients that are typically used. For instance, chlorhexidine or octenidine are frequently used in the prior art as antiseptic components in lubricant gels or lubricants. However, a disadvantage in this case is the not always optimal tolerability. Although efficacy is altogether at least sufficient, it is not always optimal, since the onset of action is sometimes delayed and is, furthermore, frequently not sufficiently long-lasting.
Furthermore, especially the use of chlorhexidine is, under certain circumstances, associated with a development of resistances with respect to various microorganisms, and this is disadvantageous in many respects in view of the hospital microbes that frequently emerge. Sometimes, the mere use of chlorhexidine is enough to promote the development of further resistant microorganisms, and there is furthermore no effective protection against pathogens or microorganisms that are already resistant.
Chlorhexidine in particular exhibits no action or virtually no action in the case of certain microbes of the species Staphylococcus aureus, and this cannot be compensated for even by an increase in concentration of the active ingredient. Moreover, it is also barely possible to effectively control or break up biofilms
With respect too to antimicrobial or antiseptic properties, the lubricants of the prior art are not always satisfactory, this being linked especially to the antiseptic active ingredients and/or antiseptic ingredients that are typically used. For instance, chlorhexidine or octenidine are frequently used in the prior art as antiseptic components in lubricant gels or lubricants. However, a disadvantage in this case is the not always optimal tolerability. Although efficacy is altogether at least sufficient, it is not always optimal, since the onset of action is sometimes delayed and is, furthermore, frequently not sufficiently long-lasting.
Furthermore, especially the use of chlorhexidine is, under certain circumstances, associated with a development of resistances with respect to various microorganisms, and this is disadvantageous in many respects in view of the hospital microbes that frequently emerge. Sometimes, the mere use of chlorhexidine is enough to promote the development of further resistant microorganisms, and there is furthermore no effective protection against pathogens or microorganisms that are already resistant.
Chlorhexidine in particular exhibits no action or virtually no action in the case of certain microbes of the species Staphylococcus aureus, and this cannot be compensated for even by an increase in concentration of the active ingredient. Moreover, it is also barely possible to effectively control or break up biofilms
- 5 -using chlorhexidine Or octenidine. Furthermore, chlorhexidine and octenidine exhibit a certain cytotoxicity especially in the event of a high concentration or misuse, and this can be problematic especially with respect to wound healing or wound antisepsis. Wound healing in particular will be slowed by octenidine and chlorhexidine under such circumstances.
Therefore, the lubricants or lubricant gels known in the prior art are not always optimal with regard to their tolerability and their efficiency of action, especially in terms of wound antisepsis or antiseptic action and also pain alleviation.
Embodiments of the present invention provide improved compositions for use as lubricants or lubricant gels which are capable of preventing or at least reducing the above-described disadvantages of the lubricants or lubricant gels known in the prior art.
Embodiments of the present invention provide improved compositions in the form of lubricants or lubricant gels, which, with respect to the compositions of the prior art, exhibit improved antiseptic properties and also no adverse effects or at least reduced adverse effects and an improved or quickened onset of action.
Embodiments of the present invention provide compositions which exhibit improved pain-alleviating properties.
Embodiments of the claimed invention pertain to a composition in the form of a lubricant gel and/or a lubricant for use in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, wherein the composition comprises: (a) a pharmaceutically effective amount of at least one local anesthetic as "component (a)- and (b) a pharmaceutically effective amount of polyhexanide
Therefore, the lubricants or lubricant gels known in the prior art are not always optimal with regard to their tolerability and their efficiency of action, especially in terms of wound antisepsis or antiseptic action and also pain alleviation.
Embodiments of the present invention provide improved compositions for use as lubricants or lubricant gels which are capable of preventing or at least reducing the above-described disadvantages of the lubricants or lubricant gels known in the prior art.
Embodiments of the present invention provide improved compositions in the form of lubricants or lubricant gels, which, with respect to the compositions of the prior art, exhibit improved antiseptic properties and also no adverse effects or at least reduced adverse effects and an improved or quickened onset of action.
Embodiments of the present invention provide compositions which exhibit improved pain-alleviating properties.
Embodiments of the claimed invention pertain to a composition in the form of a lubricant gel and/or a lubricant for use in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, wherein the composition comprises: (a) a pharmaceutically effective amount of at least one local anesthetic as "component (a)- and (b) a pharmaceutically effective amount of polyhexanide
- 6 -and/or salts thereof as "component (b)", wherein the composition is at least substantially free of (poly)alkylene glycols; and wherein the composition has a physiologically compatible pH within the range from 5 to 7.5.
Embodiments of the claimed invention also pertain to a container containing a composition as disclosed herein.
Embodiments of the claimed invention also pertain to a packaging unit, containing such a container, wherein the container has been introduced into outer packaging providing protection against contamination.
Embodiments of the claimed invention also pertain to a catheter, wherein the catheter is provided with a composition as disclosed herein, and wherein the composition is applied to a segment of the catheter that is insertable and/or introducible into a body lumen.
Embodiments of the claimed invention also pertain to a kit comprising, as spatially separated components, a catheter and a composition as disclosed herein.
It is self-evident that, hereinafter, special designs, embodiments or the like which are only described in connection with one aspect of the invention, also apply accordingly with regard to the other aspects of the invention, without this requiring an explicit mention.
Furthermore, in the case of all below-mentioned relative or percentage amounts, especially weight-based amounts, it should be noted that they are to be selected by a person skilled in the art in the context of the present invention in such a way that the sum of - 6a -the particular ingredients, active ingredients, additives or excipients or the like is always 100% or
Embodiments of the claimed invention also pertain to a container containing a composition as disclosed herein.
Embodiments of the claimed invention also pertain to a packaging unit, containing such a container, wherein the container has been introduced into outer packaging providing protection against contamination.
Embodiments of the claimed invention also pertain to a catheter, wherein the catheter is provided with a composition as disclosed herein, and wherein the composition is applied to a segment of the catheter that is insertable and/or introducible into a body lumen.
Embodiments of the claimed invention also pertain to a kit comprising, as spatially separated components, a catheter and a composition as disclosed herein.
It is self-evident that, hereinafter, special designs, embodiments or the like which are only described in connection with one aspect of the invention, also apply accordingly with regard to the other aspects of the invention, without this requiring an explicit mention.
Furthermore, in the case of all below-mentioned relative or percentage amounts, especially weight-based amounts, it should be noted that they are to be selected by a person skilled in the art in the context of the present invention in such a way that the sum of - 6a -the particular ingredients, active ingredients, additives or excipients or the like is always 100% or
- 7 -100% by weight. This, however, is automatically understood by a person skilled in the art.
Apart from that, it is possible for a person skilled in the art to deviate from the below-specified numbers, ranges or amounts on the basis of the application or as determined by the individual case without departing from the context of the present invention.
Moreover, all below-stated parameter values or the like can be fundamentally determined or ascertained using standardized or explicitly specified methods of determination or else using methods of determination that are familiar per se to a person skilled in the art.
The present invention therefore provides - in a first aspect of the present invention - a composition, more particularly a pharmaceutical composition, preferably in the form of a lubricant gel and/or lubricant, preferably for use as a (local) antiseptic and/or (local) anesthetic, especially for use in diagnostic and/or therapeutic (surgical) procedures, preferably for use in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, wherein the composition contains in each case in effective amounts, more particularly in pharmaceutically effective amounts, (a) at least one local anesthetic ("component (a)") and (b) polyhexanide and/or the salts thereof ("component (b)"), more particularly as antiseptic active ingredient and/or antiseptic ingredient (disinfectant).
This is because, in the context of the present invention, the applicant has found that, surprisingly, the specific combination of polyhexanide as antiseptic active ingredient and/or antiseptic ingredient
Apart from that, it is possible for a person skilled in the art to deviate from the below-specified numbers, ranges or amounts on the basis of the application or as determined by the individual case without departing from the context of the present invention.
Moreover, all below-stated parameter values or the like can be fundamentally determined or ascertained using standardized or explicitly specified methods of determination or else using methods of determination that are familiar per se to a person skilled in the art.
The present invention therefore provides - in a first aspect of the present invention - a composition, more particularly a pharmaceutical composition, preferably in the form of a lubricant gel and/or lubricant, preferably for use as a (local) antiseptic and/or (local) anesthetic, especially for use in diagnostic and/or therapeutic (surgical) procedures, preferably for use in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, wherein the composition contains in each case in effective amounts, more particularly in pharmaceutically effective amounts, (a) at least one local anesthetic ("component (a)") and (b) polyhexanide and/or the salts thereof ("component (b)"), more particularly as antiseptic active ingredient and/or antiseptic ingredient (disinfectant).
This is because, in the context of the present invention, the applicant has found that, surprisingly, the specific combination of polyhexanide as antiseptic active ingredient and/or antiseptic ingredient
- 8 -(disinfectant) together with at least one local anesthetic leads to compositions, preferably for use as lubricant or lubricant gel in catheterizations or the like, which have significantly improved properties compared with lubricant or lubricant gels of the prior art, especially with respect to tolerability and to a rapid onset of action coupled with prolonged duration of action and, simultaneously, excellent pain-alleviating or analgesic properties.
Moreover, the inventive compositions as such are especially suited for prophylactic or therapeutic mucosa/skin disinfection, especially in connection with catheterizations, endoscopies or the like preferably carried out in the diagnosis and/or therapy.
The terms "pharmaceutical composition", "pharmaceutical preparation" or the like, as used in the context of the present invention, are to be understood in a very broad manner and do not refer only to pharmaceutical preparations or pharmaceuticals or drugs as such or in the narrower sense, but also to so-called medical devices, homeopathic substances, foodstuffs, food supplements or the like.
Moreover, the term "mucosa/skin disinfection" used according to the invention refers especially to a disinfection or microbe reduction of body regions in particular, such as skin or mucosa, wherein said disinfection or microbe reduction is present or is carried out during the preferably therapeutic or diagnostic use of catheters, endoscopes or the like and wherein said body regions are in contact with the catheters or endoscopes used, specifically especially for avoiding or reducing the formation of biofilms, for preventing infections or for preventing the transmission of, in particular, pathogenic microbes or pathogens from a medical instrument that is used, such
Moreover, the inventive compositions as such are especially suited for prophylactic or therapeutic mucosa/skin disinfection, especially in connection with catheterizations, endoscopies or the like preferably carried out in the diagnosis and/or therapy.
The terms "pharmaceutical composition", "pharmaceutical preparation" or the like, as used in the context of the present invention, are to be understood in a very broad manner and do not refer only to pharmaceutical preparations or pharmaceuticals or drugs as such or in the narrower sense, but also to so-called medical devices, homeopathic substances, foodstuffs, food supplements or the like.
Moreover, the term "mucosa/skin disinfection" used according to the invention refers especially to a disinfection or microbe reduction of body regions in particular, such as skin or mucosa, wherein said disinfection or microbe reduction is present or is carried out during the preferably therapeutic or diagnostic use of catheters, endoscopes or the like and wherein said body regions are in contact with the catheters or endoscopes used, specifically especially for avoiding or reducing the formation of biofilms, for preventing infections or for preventing the transmission of, in particular, pathogenic microbes or pathogens from a medical instrument that is used, such
- 9 -as a catheter, to the skin or mucosa in contact the As will be explained below, the composition according to the invention has further numerous advantages and particularities:
The compositions according to the invention dispense with the additional use of preservatives - especially as a result of the distinctly improved antiseptic or antimicrobial properties substantially caused by the use of polyhexanide. This further increases the tolerability of the compositions according to the invention, and so undesired systemic reactions or irritations and allergic reactions to any preserving agents can be ruled out or minimized.
In one embodiment according to the invention, the composition according to the invention is formed without any preserving agents or preservatives or is at least substantially free of preserving agents or preservatives.
Furthermore, the application and efficacy studies carried out by the applicant clearly show that the antiseptic or disinfectant polyhexanide, on the one hand, and the local anesthetic used according to the invention, more particularly lidocaine, on the other, are supplemented or intensified in a synergistic manner in terms of their efficacy. Firstly, an excellent antimicrobial performance action, more particularly a rapid onset of action and a long-lasting duration of action, is achieved; secondly, the use of the compositions according to the invention can also significantly alleviate or reduce pain during procedures, such as catheterizations, probings, endoscopies, intubations or obstetrical procedures.
The compositions according to the invention dispense with the additional use of preservatives - especially as a result of the distinctly improved antiseptic or antimicrobial properties substantially caused by the use of polyhexanide. This further increases the tolerability of the compositions according to the invention, and so undesired systemic reactions or irritations and allergic reactions to any preserving agents can be ruled out or minimized.
In one embodiment according to the invention, the composition according to the invention is formed without any preserving agents or preservatives or is at least substantially free of preserving agents or preservatives.
Furthermore, the application and efficacy studies carried out by the applicant clearly show that the antiseptic or disinfectant polyhexanide, on the one hand, and the local anesthetic used according to the invention, more particularly lidocaine, on the other, are supplemented or intensified in a synergistic manner in terms of their efficacy. Firstly, an excellent antimicrobial performance action, more particularly a rapid onset of action and a long-lasting duration of action, is achieved; secondly, the use of the compositions according to the invention can also significantly alleviate or reduce pain during procedures, such as catheterizations, probings, endoscopies, intubations or obstetrical procedures.
- 10 -Furthermore, the use as such of polyhexanide as antiseptic or as antiseptic active ingredient and/or antiseptic ingredient (disinfectant) is also advantageous in many respects. More particularly, the efficiency of action can be significantly improved because polyhexanide allows a particularly rapid onset of action, though the action additionally also lasts for an extremely long time. Furthermore, when using polyhexanide as mucosa disinfectant, there is no appreciable systemic resorption of the active ingredient, and so the risk of adverse effects occurring can be distinctly lowered. In this connection, it should also be emphasized that polyhexanide does not act cytotoxically, and this further increases the tolerability of the overall composition.
Moreover, the antiseptic or the antiseptic active ingredient and/or antiseptic ingredient (disinfectant) used according to the invention in the form of polyhexanide has a particularly broad spectrum of activity, i.e., it acts both against Gram-positive pathogens and against Gram-negative pathogens. This is particularly advantageous in that polyhexanide also has a good efficiency of action toward the so-called hospital microbes, such as Staphylococcus aureus.
Without wishing to be restricted to this theory here, the nonspecific mode of action or interaction of polyhexanide with the acidic membrane phospholipids of bacteria or microorganisms prevents resistances to polyhexanide from being able to be developed.
Moreover, the storage stability of the compositions according to the invention is increased by the purposeful use of polyhexanide, since this antiseptic active ingredient and/or antiseptic ingredient (disinfectant) as such already has an excellent
Moreover, the antiseptic or the antiseptic active ingredient and/or antiseptic ingredient (disinfectant) used according to the invention in the form of polyhexanide has a particularly broad spectrum of activity, i.e., it acts both against Gram-positive pathogens and against Gram-negative pathogens. This is particularly advantageous in that polyhexanide also has a good efficiency of action toward the so-called hospital microbes, such as Staphylococcus aureus.
Without wishing to be restricted to this theory here, the nonspecific mode of action or interaction of polyhexanide with the acidic membrane phospholipids of bacteria or microorganisms prevents resistances to polyhexanide from being able to be developed.
Moreover, the storage stability of the compositions according to the invention is increased by the purposeful use of polyhexanide, since this antiseptic active ingredient and/or antiseptic ingredient (disinfectant) as such already has an excellent
- 11 -microbial stability, and so a use of (additional) preserving agents is not required.
Furthermore, it is advantageous that the use of polyhexanide does not negatively influence wound healing; on the contrary, wound healing is even promoted as a result of the high antimicrobial activity of polyhexanide.
Furthermore, in the context of the present invention, it has been shown that, surprisingly, the compositions according to the invention can be improved in terms of their tolerability when the use of glycols, more particularly propylene glycol, is dispensed with, since they or it can lead to intolerabilities, such as mucosa irritations and allergic reactions. Therefore, in one embodiment according to the invention, the composition according to the invention can be at least substantially free of glycols, more particularly free of propylene glycols.
Moreover, the composition according to the invention has a specifically coordinated or adjusted viscosity and excellent lubrication or gliding properties, and so the composition according to the invention adheres to and wets the mucosa in an outstanding manner, allowing a problem-free gliding or insertion of medical instruments, such as catheters, probes, endoscopes or ultrasound probes. The body region in contact with the medical instrument, such as skin or mucosa, is thus protected from injuries to the greatest possible extent. The additional local anesthetic in conjunction with or in addition to the extraordinarily good adhesion and lubrication properties of the composition according to the invention - additionally results in the underlying procedures for the patients proceeding in an extremely gentle and pain-free manner.
Furthermore, it is advantageous that the use of polyhexanide does not negatively influence wound healing; on the contrary, wound healing is even promoted as a result of the high antimicrobial activity of polyhexanide.
Furthermore, in the context of the present invention, it has been shown that, surprisingly, the compositions according to the invention can be improved in terms of their tolerability when the use of glycols, more particularly propylene glycol, is dispensed with, since they or it can lead to intolerabilities, such as mucosa irritations and allergic reactions. Therefore, in one embodiment according to the invention, the composition according to the invention can be at least substantially free of glycols, more particularly free of propylene glycols.
Moreover, the composition according to the invention has a specifically coordinated or adjusted viscosity and excellent lubrication or gliding properties, and so the composition according to the invention adheres to and wets the mucosa in an outstanding manner, allowing a problem-free gliding or insertion of medical instruments, such as catheters, probes, endoscopes or ultrasound probes. The body region in contact with the medical instrument, such as skin or mucosa, is thus protected from injuries to the greatest possible extent. The additional local anesthetic in conjunction with or in addition to the extraordinarily good adhesion and lubrication properties of the composition according to the invention - additionally results in the underlying procedures for the patients proceeding in an extremely gentle and pain-free manner.
- 12 -The compositions according to the invention in the form of lubricants or lubricant gels are designed in such a way that they wet and adhere to the mucosae in an optimal manner and moreover have excellent lubricant properties. This makes it possible to carry out diagnostic or therapeutic procedures very much more easily and rapidly, and the risk of mucosa injuries in the region of the examined tissue or body part is simultaneously minimized, as mentioned above.
In the case of the below-specified substances which may be present in the composition according to the invention, reference is always made to the compounds which can be mixed into or added to the composition. It is possible here that the compounds are converted into other substances owing to reactions; more particularly, acid/base reactions are possible, i.e., the substances used may, for example, be protonated or deprotonated.
However, this is known per se to a person skilled in the art.
The polyhexanide used according to the invention has an antiseptic or antimicrobial action. Chemically, the active ingredient polyhexanide is generally polyhexamethylene biguanide (PHMB), which can be synonymously also referred to as poly(iminocarbonimidoyliminocarbonimidoylimino-1,6-hexanediyl) hydrochloride or polyhexanide and has in particular the molecular formula C81-117N5 and a molecular weight of 183.25 g/mol.
An advantage of polyhexanide is in particular its broad spectrum of activity, which is also directed against the difficult-to-treat hospital microbes, such as Staphylococcus aureus for example. Furthermore, polyhexanide acts even in extremely low concentrations, since it binds directly to the bacterial cell wall and damages said wall in such a way that the result is
In the case of the below-specified substances which may be present in the composition according to the invention, reference is always made to the compounds which can be mixed into or added to the composition. It is possible here that the compounds are converted into other substances owing to reactions; more particularly, acid/base reactions are possible, i.e., the substances used may, for example, be protonated or deprotonated.
However, this is known per se to a person skilled in the art.
The polyhexanide used according to the invention has an antiseptic or antimicrobial action. Chemically, the active ingredient polyhexanide is generally polyhexamethylene biguanide (PHMB), which can be synonymously also referred to as poly(iminocarbonimidoyliminocarbonimidoylimino-1,6-hexanediyl) hydrochloride or polyhexanide and has in particular the molecular formula C81-117N5 and a molecular weight of 183.25 g/mol.
An advantage of polyhexanide is in particular its broad spectrum of activity, which is also directed against the difficult-to-treat hospital microbes, such as Staphylococcus aureus for example. Furthermore, polyhexanide acts even in extremely low concentrations, since it binds directly to the bacterial cell wall and damages said wall in such a way that the result is
- 13 -typically cell death. This makes possible the effective use of this antiseptic even in low concentrations, lowering accordingly the risk of the occurence of adverse effects. Furthermore, polyhexanide has a low systemic resorption, leading equally to a minimization of adverse effects.
The term "local anesthetics", as used according to the invention, is generally understood in the context of the present invention to mean anesthetics having a locally confined action or for the purpose of local pain relief or anesthesia, and in particular the local anesthetics used in the context of the inventive use should not have any euphorigenic or habit-forming action. The chemical structure of the underlying local anesthetics is fundamentally similar. It generally comprises a lipophilic aromatic ring structure, an intermediate chain and a hydrophilic amino group.
Depending on the intermediate chain, a distinction is made between amino esters ("ester type") and amino amides ("amide type"). The amino esters are metabolized in tissue by a cholinesterase; the degradation of the amino amides takes place in the liver by N-dealkylation or hydrolysis. In particular - without wishing to be restricted to this theory - local anesthetics develop their action on the cell membrane of nerve cells, with the formation and conduction of sensations, such as temperature, pressure or pain, being attenuated or completely interrupted in a local manner.
With regard to the local anesthetic used according to the invention, it is possible in the context of the present invention to use a range of substances which are effective as local anesthetic and which are well known per se to a person skilled in the art. However, according to the invention, it is preferred when the local anesthetic is selected from the group of local anesthetics of the ester type, more particularly amino
The term "local anesthetics", as used according to the invention, is generally understood in the context of the present invention to mean anesthetics having a locally confined action or for the purpose of local pain relief or anesthesia, and in particular the local anesthetics used in the context of the inventive use should not have any euphorigenic or habit-forming action. The chemical structure of the underlying local anesthetics is fundamentally similar. It generally comprises a lipophilic aromatic ring structure, an intermediate chain and a hydrophilic amino group.
Depending on the intermediate chain, a distinction is made between amino esters ("ester type") and amino amides ("amide type"). The amino esters are metabolized in tissue by a cholinesterase; the degradation of the amino amides takes place in the liver by N-dealkylation or hydrolysis. In particular - without wishing to be restricted to this theory - local anesthetics develop their action on the cell membrane of nerve cells, with the formation and conduction of sensations, such as temperature, pressure or pain, being attenuated or completely interrupted in a local manner.
With regard to the local anesthetic used according to the invention, it is possible in the context of the present invention to use a range of substances which are effective as local anesthetic and which are well known per se to a person skilled in the art. However, according to the invention, it is preferred when the local anesthetic is selected from the group of local anesthetics of the ester type, more particularly amino
- 14 -esters, and local anesthetics of the amide type, more particularly amino amides, and also the mixtures or combination thereof, more particularly from lidocaine, mepivacaine, prilocaine, bupivacaine, articaine and ropivacaine and also the mixtures or combination thereof, particularly preferably lidocaine.
In the context of the present invention, particularly good results are achieved when the local anesthetic is lidocaine. In this case, the local anesthetic is one of the amide type, which has a good efficacy coupled with, simultaneously, a rapid onset of action. For further explanations regarding lidocaine, reference can, for example, be made to Rompp Chemielexikon [Rompp dictionary of chemistry], 10th edition, volume 3, 1997, Georg Thieme Verlag Stuttgart/New York, keyword:
"Lidocaine" and also to the particular literature cited therein, the entire content of which is hereby incorporated by reference.
Concerning the amount used of the local anesthetic or of component (a), this can vary within wide ranges.
However, in the context of the present invention, a particularly good efficacy has been demonstrated when the composition contains component (a) in an amount within the range from 0.1 to 10% by weight, more particularly within the range from 0.5 to 8% by weight, by preference within the range from 0.7 to 6% by weight, preferably within the range from 1 to 3% by weight, based on the composition.
Equally, it can be envisaged that the composition contains component (a) in an amount of at least 0.01%
by weight, more particularly at least 0.1% by weight, by preference at least 0.5% by weight, preferably at least 1% by weight, based on the composition. In this connection, it can also be envisaged that the composition contains component (a) in an amount of not
In the context of the present invention, particularly good results are achieved when the local anesthetic is lidocaine. In this case, the local anesthetic is one of the amide type, which has a good efficacy coupled with, simultaneously, a rapid onset of action. For further explanations regarding lidocaine, reference can, for example, be made to Rompp Chemielexikon [Rompp dictionary of chemistry], 10th edition, volume 3, 1997, Georg Thieme Verlag Stuttgart/New York, keyword:
"Lidocaine" and also to the particular literature cited therein, the entire content of which is hereby incorporated by reference.
Concerning the amount used of the local anesthetic or of component (a), this can vary within wide ranges.
However, in the context of the present invention, a particularly good efficacy has been demonstrated when the composition contains component (a) in an amount within the range from 0.1 to 10% by weight, more particularly within the range from 0.5 to 8% by weight, by preference within the range from 0.7 to 6% by weight, preferably within the range from 1 to 3% by weight, based on the composition.
Equally, it can be envisaged that the composition contains component (a) in an amount of at least 0.01%
by weight, more particularly at least 0.1% by weight, by preference at least 0.5% by weight, preferably at least 1% by weight, based on the composition. In this connection, it can also be envisaged that the composition contains component (a) in an amount of not
- 15 -more than 15% by weight, more particularly not more than 10% by weight, by preference not more than 8% by weight, preferably not more than 5% by weight, particularly preferably not more than 3% by weight, based on the composition.
The amount too of the polyhexanide used according to the invention as antiseptic can vary within wide ranges. In terms of the antiseptic or antimicrobial action, the best results are achieved according to the invention when the composition contains polyhexanide and/or the salts thereof in an amount within the range from 0.05 to 10% by weight, more particularly within the range from 0.1 to 8% by weight, by preference within the range from 0.5 to 5% by weight, preferably within the range from 0.75 to 3% by weight, particularly preferably within the range from 1 to 2%
by weight, based on the composition.
It can also be envisaged in the context of the present invention that the composition contains polyhexanide and/or the salts thereof in an amount of at least 0.05%
by weight, more particularly at least 0.1% by weight, by preference at least 0.5% by weight, preferably at least 0.75% by weight, particularly preferably at least 1% by weight, based on the composition. It can be equally envisaged with regard to the amount used of polyhexanide that the composition contains the polyhexanide in an amount of not more than 10% by weight, more particularly not more than 8% by weight, by preference not more than 5% by weight, preferably not more than 3% by weight, particularly preferably not more than 2% by weight, based on the composition.
Furthermore, in the context of the present invention, it has been demonstrated that, surprisingly, it is not only the active-ingredient amount of the two active ingredients as such that are used which is of
The amount too of the polyhexanide used according to the invention as antiseptic can vary within wide ranges. In terms of the antiseptic or antimicrobial action, the best results are achieved according to the invention when the composition contains polyhexanide and/or the salts thereof in an amount within the range from 0.05 to 10% by weight, more particularly within the range from 0.1 to 8% by weight, by preference within the range from 0.5 to 5% by weight, preferably within the range from 0.75 to 3% by weight, particularly preferably within the range from 1 to 2%
by weight, based on the composition.
It can also be envisaged in the context of the present invention that the composition contains polyhexanide and/or the salts thereof in an amount of at least 0.05%
by weight, more particularly at least 0.1% by weight, by preference at least 0.5% by weight, preferably at least 0.75% by weight, particularly preferably at least 1% by weight, based on the composition. It can be equally envisaged with regard to the amount used of polyhexanide that the composition contains the polyhexanide in an amount of not more than 10% by weight, more particularly not more than 8% by weight, by preference not more than 5% by weight, preferably not more than 3% by weight, particularly preferably not more than 2% by weight, based on the composition.
Furthermore, in the context of the present invention, it has been demonstrated that, surprisingly, it is not only the active-ingredient amount of the two active ingredients as such that are used which is of
- 16 -importance in terms of an optimization of action, but also the ratio used of the two active ingredients in relation to one another. A particularly good efficiency of action in terms of the antiseptic action, on the one hand, and the pain-alleviating action, on the other, is achieved in the context of the present invention when the composition contains component (a) and component (b) in a weight-based ratio of [(a): (b) within the range from 1:50 to 50:1, more particularly within the range from 1:20 to 20:1, by preference within the range from 1:10 to 10:1, preferably within the range from 1:5 to 5:1, particularly preferably from 1:3 to 3:1. This is because, by using the two active ingredients in a defined ratio in relation to one another, the action of local anesthetic, on the one hand, and antiseptic, on the other, during combined use goes beyond the particular individual action of the active ingredients during sole administration, and this can be judged to be evidence of the presence of a synergistic effect.
The composition according to the invention can be configured in an altogether variable manner. Preferred embodiments will be explained in detail below.
In one embodiment preferred according to the invention, it can be envisaged that the composition is water-based or water/alcohol-based, preferably water-based.
In this connection, it is advantageous when the composition contains water, more particularly purified water, in an amount within the range from 30 to 99% by weight, more particularly within the range from 40 to 98% by weight, preferably within the range from 50 to 97% by weight, particularly preferably within the range from 60 to 96% by weight, based on the composition.
Furthermore, it can be envisaged in the context of the present invention that the composition according to the
The composition according to the invention can be configured in an altogether variable manner. Preferred embodiments will be explained in detail below.
In one embodiment preferred according to the invention, it can be envisaged that the composition is water-based or water/alcohol-based, preferably water-based.
In this connection, it is advantageous when the composition contains water, more particularly purified water, in an amount within the range from 30 to 99% by weight, more particularly within the range from 40 to 98% by weight, preferably within the range from 50 to 97% by weight, particularly preferably within the range from 60 to 96% by weight, based on the composition.
Furthermore, it can be envisaged in the context of the present invention that the composition according to the
- 17 -invention contains at least one preferably polyhydric alcohol, especially selected from the group of polyvinyl alcohols, glycerol, glycols and the combinations thereof, preferably glycerol. However, in the context of the present invention, it has been found to be advantageous when the composition is at least substantially free of glycols, more particularly (poly)alkylene glycols. In particular, it can be envisaged in this connection that the composition according to the invention comprises at least substantially no propylene glycol. This is because (poly)alkylene glycols, especially propylene glycol, can lead to skin irritations and to reactions due to intolerability, and this is disadvantageous especially with respect to use on the mucosa, since the mucosa is particularly sensitive. Furthermore, dispensing with (poly)alkylene glycols, especially propylene glycol, at least substantially avoids a systemic resorption, especially an excessive systemic resorption, of the active ingredients used, i.e., of the local anesthetic and of the antiseptic, and this further increases the tolerability of the composition according to the invention.
Concerning the amounts used of the preferably polyhydric alcohol, these can vary within wide ranges.
Particularly good results are obtained according to the invention when the composition contains the preferably polyhydric alcohol in an amount within the range from 1 to 80% by weight, more particularly within the range from 5 to 70% by weight, by preference within the range from 10 to 60% by weight, preferably within the range from 15 to 50% by weight, based on the composition.
In a further embodiment according to the invention, it can be envisaged that the composition comprises a mix or a mixture of water and at least one preferably polyhydric alcohol. In this connection, it has been
Concerning the amounts used of the preferably polyhydric alcohol, these can vary within wide ranges.
Particularly good results are obtained according to the invention when the composition contains the preferably polyhydric alcohol in an amount within the range from 1 to 80% by weight, more particularly within the range from 5 to 70% by weight, by preference within the range from 10 to 60% by weight, preferably within the range from 15 to 50% by weight, based on the composition.
In a further embodiment according to the invention, it can be envisaged that the composition comprises a mix or a mixture of water and at least one preferably polyhydric alcohol. In this connection, it has been
- 18 -found to be advantageous when the proportion of water is at least 10% by weight, more particularly at least 30% by weight, by preference at least 50% by weight, based on the mix or the mixture. Equally, it can be envisaged with regard to this embodiment according to the invention that the weight-based ratio of water to alcohol in the composition is within the range from 9:1 to 1:5, more particularly within the range from 3:1 to 1:3, by preference within the range from 2:1 to 1:2, preferably within the range from 1.5:1 to 1:1.5.
Concerning, in addition, the role of the composition according to the invention as lubricant, it is preferred according to the invention when the composition is viscous or gel-like or is in the form of a lubricant gel or lubricant. The viscous or gel-like consistency ensures the suitability of the compositions according to the invention for reducing friction, i.e., the resistance between skin or mucosa, on the one hand, and medical instruments, on the other, is reduced, making an easy insertion possible without injuries or skin irritations occurring.
In this connection, it is advantageous when the composition comprises at least one gel-forming agent.
In the context of the present invention, the gel-forming agent can be selected from the group of bentonites, silicic acids, polyacrylic acids, carbomers, polyvinylpyrrolidones, cellulose and cellulose derivatives, xanthans and the mixtures thereof, by preference cellulose and cellulose derivatives, preferably modified celluloses, particularly preferably chemically modified celluloses, very particularly preferably methylcellulose, carboxymethylcellulose and/or hydroxyethylcellulose, even more preferably hydroxyethylcellulose.
Concerning, in addition, the role of the composition according to the invention as lubricant, it is preferred according to the invention when the composition is viscous or gel-like or is in the form of a lubricant gel or lubricant. The viscous or gel-like consistency ensures the suitability of the compositions according to the invention for reducing friction, i.e., the resistance between skin or mucosa, on the one hand, and medical instruments, on the other, is reduced, making an easy insertion possible without injuries or skin irritations occurring.
In this connection, it is advantageous when the composition comprises at least one gel-forming agent.
In the context of the present invention, the gel-forming agent can be selected from the group of bentonites, silicic acids, polyacrylic acids, carbomers, polyvinylpyrrolidones, cellulose and cellulose derivatives, xanthans and the mixtures thereof, by preference cellulose and cellulose derivatives, preferably modified celluloses, particularly preferably chemically modified celluloses, very particularly preferably methylcellulose, carboxymethylcellulose and/or hydroxyethylcellulose, even more preferably hydroxyethylcellulose.
- 19 -Concerning the amount used of the gel-forming agent, this can be varied within wide ranges. In particular, the amount of gel-forming agent is selected depending on the viscosity that the composition according to the invention is to have. In the context of the present invention, it has been found to be advantageous when the composition comprises the gel-forming agent in an amount within the range from 0.01 to 20% by weight, more particularly within the range from 0.1 to 10% by weight, by preference within the range from 0.5 to 5%
by weight, preferably within the range from 1 to 3% by weight, based on the composition.
Particularly effective gel-type structures or properties are obtained when the composition according to the invention has, at a temperature of 20 C, a dynamic viscosity within the range from 20 to 20 000 mPa-s, more particularly within the range from 50 to 15 000 mPars, by preference within the range from 100 to 10 000 mPa.s, preferably within the range from 500 to 8000 mPa.s, particularly preferably within the range from 1000 to 7000 mPa-s, even more preferably within the range from 2000 to 6000 mPa-s.
In the context of the present invention, it is thus possible, on the basis of the selected gel-forming agents and the usable amounts of the gel-forming agent, to specifically set the rheological properties of the composition according to the invention and to be able to tailor said properties so to speak.
Concerning the methods or procedures for determining the viscosity of the composition according to the invention, these as such are known to a person skilled in the art, and so no further information regarding this is required here. In particular, it is possible to use measuring instruments such as capillary viscometers, rotational viscometers, falling ball
by weight, preferably within the range from 1 to 3% by weight, based on the composition.
Particularly effective gel-type structures or properties are obtained when the composition according to the invention has, at a temperature of 20 C, a dynamic viscosity within the range from 20 to 20 000 mPa-s, more particularly within the range from 50 to 15 000 mPars, by preference within the range from 100 to 10 000 mPa.s, preferably within the range from 500 to 8000 mPa.s, particularly preferably within the range from 1000 to 7000 mPa-s, even more preferably within the range from 2000 to 6000 mPa-s.
In the context of the present invention, it is thus possible, on the basis of the selected gel-forming agents and the usable amounts of the gel-forming agent, to specifically set the rheological properties of the composition according to the invention and to be able to tailor said properties so to speak.
Concerning the methods or procedures for determining the viscosity of the composition according to the invention, these as such are known to a person skilled in the art, and so no further information regarding this is required here. In particular, it is possible to use measuring instruments such as capillary viscometers, rotational viscometers, falling ball
- 20 -viscometers or Brookfield viscometers to determine the viscosity. In particular, the above-specified viscosity values are based on a determination in accordance with DIN 53015 at room temperature (20 C) (e.g., using a falling ball viscometer, e.g., RheoTec Messtechnik GmbH, Germany).
Furthermore, the composition according to the invention typically has a physiologically compatible pH. In this connection, it is advantageous according to the invention when the composition has a pH within the range from 3 to 8.5, more particularly within the range from 4 to 8, by preference within the range from 5 to 7.5, preferably within the range from 6 to 7.
Furthermore, it is preferred in the context of the present invention when the composition has a physiologically compatible electrical conductivity, more particularly within the range from 1 to 20 mS/cm, by preference within the range from 2 to 15 mS/cm, preferably within the range from 3 to 13 mS/cm, particularly preferably within the range from 5 to 10 mS/cm.
Furthermore, it can be envisaged in the context of the present invention that the composition also contains at least one acid and/or base, more particularly for setting the pH, by preference for setting a physiologically compatible pH, preferably for forming a buffer system. The relevant buffer systems are well known to a person skilled in the art, and so there is no need for any further explanations in relation to this.
Moreover, it has been found to be advantageous when the composition preferably comprises at least one base. In this connection, it can be envisaged that the base is selected from the group of amines, carboxylates, alkali
Furthermore, the composition according to the invention typically has a physiologically compatible pH. In this connection, it is advantageous according to the invention when the composition has a pH within the range from 3 to 8.5, more particularly within the range from 4 to 8, by preference within the range from 5 to 7.5, preferably within the range from 6 to 7.
Furthermore, it is preferred in the context of the present invention when the composition has a physiologically compatible electrical conductivity, more particularly within the range from 1 to 20 mS/cm, by preference within the range from 2 to 15 mS/cm, preferably within the range from 3 to 13 mS/cm, particularly preferably within the range from 5 to 10 mS/cm.
Furthermore, it can be envisaged in the context of the present invention that the composition also contains at least one acid and/or base, more particularly for setting the pH, by preference for setting a physiologically compatible pH, preferably for forming a buffer system. The relevant buffer systems are well known to a person skilled in the art, and so there is no need for any further explanations in relation to this.
Moreover, it has been found to be advantageous when the composition preferably comprises at least one base. In this connection, it can be envisaged that the base is selected from the group of amines, carboxylates, alkali
- 21 -metal hydroxides and/or alkaline earth metal hydroxides and the mixtures and combinations thereof, more particularly alkali metal hydroxides and/or alkaline earth metal hydroxides, preferably sodium hydroxide.
The addition of acids or bases, especially of bases, allows the pH to be specifically set, and so the compositions according to the invention are physiologically highly compatible and, at the same time, the preferably used local anesthetic, preferably of the amide type, is present in protonated form, improving or ensuring the local action of the local anesthetic. Likewise, buffer systems are formed, and as a result, the pH of the composition according to the invention remains stable even during application.
Furthermore, according to a preferred embodiment of the present invention, it is envisaged that the composition according to the invention comprises at least substantially no preserving agent or no preservative.
More particularly, in the context of the present invention, it can be envisaged that the composition is at least substantially free of preserving agents or of preservatives. By dispensing with preserving agents, it is possible to even further increase the tolerability of the compositions. It is completely surprising here that the composition according to the invention has an excellent long-term stability even without the use of preserving agents, and that there is no microbiological infestation of the compositions even after a storage time of at least two years.
Furthermore, the composition according to the invention can contain at least one further active ingredient and/or ingredient, especjaliy selected from the group of skin protectants, antiseptics, local anesthetics, vitamins, trace elements, minerals, micronutrients and the combinations thereof.
The addition of acids or bases, especially of bases, allows the pH to be specifically set, and so the compositions according to the invention are physiologically highly compatible and, at the same time, the preferably used local anesthetic, preferably of the amide type, is present in protonated form, improving or ensuring the local action of the local anesthetic. Likewise, buffer systems are formed, and as a result, the pH of the composition according to the invention remains stable even during application.
Furthermore, according to a preferred embodiment of the present invention, it is envisaged that the composition according to the invention comprises at least substantially no preserving agent or no preservative.
More particularly, in the context of the present invention, it can be envisaged that the composition is at least substantially free of preserving agents or of preservatives. By dispensing with preserving agents, it is possible to even further increase the tolerability of the compositions. It is completely surprising here that the composition according to the invention has an excellent long-term stability even without the use of preserving agents, and that there is no microbiological infestation of the compositions even after a storage time of at least two years.
Furthermore, the composition according to the invention can contain at least one further active ingredient and/or ingredient, especjaliy selected from the group of skin protectants, antiseptics, local anesthetics, vitamins, trace elements, minerals, micronutrients and the combinations thereof.
- 22 -It can be equally envisaged that the composition according to the invention contains at least one customary pharmaceutical additive and/or excipient, which is preferably selected from the group of processing aids, stabilizers, emulsifiers, antioxidants, preservatives, humectants, pH setters, pH
buffer substances, thickeners, antiseptics, dyes, buffer substances, odorants, fragrances, extenders, binders, wetting substances and/or preservatives and the combinations thereof.
In general, the composition according to the invention is suitable for use in the area of medicine, medical technology, pharmacy and cosmetics.
More particularly, the composition according to the invention is suitable for use as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Equally, the composition according to the invention is suitable for use in prophylactic or therapeutic (mucosa) disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, endoscopies, probings, intubations and obstetrical procedures.
In summary, it should be emphasized that it is possible for the first time according to the invention, with respect to the composition according to the invention, to provide lubricants or lubricant gels as aids for therapeutic or diagnostic or prophylactic procedures, such as catheterizations, endoscopies, probings, intubations or obstetrical procedures, which lubricants
buffer substances, thickeners, antiseptics, dyes, buffer substances, odorants, fragrances, extenders, binders, wetting substances and/or preservatives and the combinations thereof.
In general, the composition according to the invention is suitable for use in the area of medicine, medical technology, pharmacy and cosmetics.
More particularly, the composition according to the invention is suitable for use as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Equally, the composition according to the invention is suitable for use in prophylactic or therapeutic (mucosa) disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, endoscopies, probings, intubations and obstetrical procedures.
In summary, it should be emphasized that it is possible for the first time according to the invention, with respect to the composition according to the invention, to provide lubricants or lubricant gels as aids for therapeutic or diagnostic or prophylactic procedures, such as catheterizations, endoscopies, probings, intubations or obstetrical procedures, which lubricants
- 23 -or lubricant gels are distinctly superior to the lubricants or lubricant gels of the prior art. The composition according to the invention has altogether an improved efficacy, more particularly an increased antiseptic action, specifically both with respect to the spectrum of activity and with respect to a rapid onset of action. Furthermore, the composition is improved in terms of its tolerability, since especially the antiseptic used has at least substantially no cytotoxic action and the risk of undesired adverse reactions or effects is thus minimized. Furthermore, the local anesthetic used, on the one hand, and the antiseptic, on the other, are complementary to one another in a synergistic manner, i.e., the combined use of both active ingredients, especially in defined ratios to one another, leads to a significant increase in action with regard to both active ingredients.
Furthermore, the composition according to the invention has viscosity and adhesion properties which are tailored or which are optimized with respect to the particular area of use, and so medical procedures, more particularly catheterizations, endoscopies, intubations, probings and obstetrical procedures, can be carried out more easily and more gently - especially with a reduced risk of injury.
The present invention further provides for - in a secondaspect of the present invention - the use of the composition according to the invention, as described above, as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention relates to the composition according to the invention as such, as
Furthermore, the composition according to the invention has viscosity and adhesion properties which are tailored or which are optimized with respect to the particular area of use, and so medical procedures, more particularly catheterizations, endoscopies, intubations, probings and obstetrical procedures, can be carried out more easily and more gently - especially with a reduced risk of injury.
The present invention further provides for - in a secondaspect of the present invention - the use of the composition according to the invention, as described above, as a (local) antiseptic and/or (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention relates to the composition according to the invention as such, as
- 24 -described above, for use as a (local) antiseptic and/or as a (local) anesthetic, especially in diagnostic and/or therapeutic (surgical) procedures, preferably in catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
For further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the first inventive aspect, said explanations also applying accordingly with regard to this aspect of the invention.
Equally, the present invention also relates to the use of the composition according to the invention for prophylactic and/or therapeutic mucosa/skin disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention also relates to the composition according to the invention as such, as described above, for use in prophylactic and/or therapeutic mucosa/skin disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, endoscopies, probings, intubations and/or obstetrical procedures.
In particular, the present invention also relates to the use of the composition according to the invention, as defined above, as lubricant and/or as lubricant gel especially in catheterizations, especially for a bladder catheter, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention also relates to the composition according to the invention as such, as
For further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the first inventive aspect, said explanations also applying accordingly with regard to this aspect of the invention.
Equally, the present invention also relates to the use of the composition according to the invention for prophylactic and/or therapeutic mucosa/skin disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention also relates to the composition according to the invention as such, as described above, for use in prophylactic and/or therapeutic mucosa/skin disinfection, especially in the context of catheterizations, preferably transurethral or suprapubic catheterizations, endoscopies, probings, intubations and/or obstetrical procedures.
In particular, the present invention also relates to the use of the composition according to the invention, as defined above, as lubricant and/or as lubricant gel especially in catheterizations, especially for a bladder catheter, probings, endoscopies, intubations and/or obstetrical procedures.
Therefore, the present invention also relates to the composition according to the invention as such, as
- 25 -defined above, for use in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, especially as a lubricant and/or as a lubricant gel in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, especially for a bladder catheter.
The use of the composition according to the invention especially in catheterization allows not only a comparatively gentle catheterization and lowers the risk of injuries in catheterization; on the contrary, a distinctly reduced occurrence of infections during the catheter retention time is also observed.
Moreover, the present invention relates to the use of the composition according to the invention, as defined above, for the curative and/or prophylactic treatment of infections, inflammations and/or pain which are associated with Or linked to catheterizations, probings, endoscopies, intubations and/or obstetrical procedures and which, in the case of catheterizations, occur especially in the region of the ureter and/or bladder.
Consequently, the present invention also relates to the composition according to the invention as such, as defined above, for use in the curative and/or prophylactic treatment of infections, inflammations and/or pain which are associated with or linked to catheterizations, probings, endoscopies, intubations and/or obstetrical procedures and which, especially in the case of catheterizations, occur in the region of the ureter and/or bladder.
In general, the composition according to the invention can be applied in the case of or in connection with catheterization, especially in the installation of a catheter, especially a bladder catheter.
The use of the composition according to the invention especially in catheterization allows not only a comparatively gentle catheterization and lowers the risk of injuries in catheterization; on the contrary, a distinctly reduced occurrence of infections during the catheter retention time is also observed.
Moreover, the present invention relates to the use of the composition according to the invention, as defined above, for the curative and/or prophylactic treatment of infections, inflammations and/or pain which are associated with Or linked to catheterizations, probings, endoscopies, intubations and/or obstetrical procedures and which, in the case of catheterizations, occur especially in the region of the ureter and/or bladder.
Consequently, the present invention also relates to the composition according to the invention as such, as defined above, for use in the curative and/or prophylactic treatment of infections, inflammations and/or pain which are associated with or linked to catheterizations, probings, endoscopies, intubations and/or obstetrical procedures and which, especially in the case of catheterizations, occur in the region of the ureter and/or bladder.
In general, the composition according to the invention can be applied in the case of or in connection with catheterization, especially in the installation of a catheter, especially a bladder catheter.
- 26 -It has been found to be particularly advantageous when the composition is applied into a body lumen, especially into the urethra, in the case of catheterization, especially before the installation of a catheter, especially a bladder catheter. Typically, it is envisaged that the composition according to the invention is installed before placement of the catheter into the urethra, though it is also possible to wet the catheter additionally during catheterization using the composition according to the invention.
Furthermore, it is possible according to the invention for the composition, in the case of catheterization, to be applied on the catheter before and/or during the installation of a catheter, especially a bladder catheter. It can be envisaged here that the composition is applied to the segment of a catheter that is insertable and/or introducible into a body lumen, especially into a urethra.
In turn, the present invention further provides - in a third aspect of the present invention - a container, especially an application apparatus, preferably in the form of a preferably sterile syringe, which contains the above-described composition according to the invention.
In the context of the present invention, it can be envisaged in this connection that the container is designed to accommodate a single dose of the composition.
In a preferred embodiment of the present invention, the container has a defined volume of from 3 to 30 cm3, more particularly from 3.5 to 20 cm3, preferably from 4 to 15 cm3, particularly preferably from 4.5 to 12 cm3, for accommodating the composition, especially for
Furthermore, it is possible according to the invention for the composition, in the case of catheterization, to be applied on the catheter before and/or during the installation of a catheter, especially a bladder catheter. It can be envisaged here that the composition is applied to the segment of a catheter that is insertable and/or introducible into a body lumen, especially into a urethra.
In turn, the present invention further provides - in a third aspect of the present invention - a container, especially an application apparatus, preferably in the form of a preferably sterile syringe, which contains the above-described composition according to the invention.
In the context of the present invention, it can be envisaged in this connection that the container is designed to accommodate a single dose of the composition.
In a preferred embodiment of the present invention, the container has a defined volume of from 3 to 30 cm3, more particularly from 3.5 to 20 cm3, preferably from 4 to 15 cm3, particularly preferably from 4.5 to 12 cm3, for accommodating the composition, especially for
- 27 -accommodating the composition according to the invention.
In a particular embodiment of the present invention, the container of the invention also comprises an application unit, especially in the form of a piece of tubing, for the application or administration of the composition to body lumen accommodating or adjacent to a catheter, especially a bladder catheter or kidney catheter, especially for the application and/or administration of the composition to the urethra or bladder.
For further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Moreover, the present invention further provides - in a fourth aspect of the present invention - a catheter, especially a bladder catheter or fistula catheter, the catheter being provided with or comprising the above-described composition according to the invention. It can be envisaged here that the composition is also applied to a segment of the catheter that is insertable or introducible into a body lumen, especially into the urethra.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
In turn, the present invention further provides - in a fifthaspect of the present invention -apackaging
In a particular embodiment of the present invention, the container of the invention also comprises an application unit, especially in the form of a piece of tubing, for the application or administration of the composition to body lumen accommodating or adjacent to a catheter, especially a bladder catheter or kidney catheter, especially for the application and/or administration of the composition to the urethra or bladder.
For further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Moreover, the present invention further provides - in a fourth aspect of the present invention - a catheter, especially a bladder catheter or fistula catheter, the catheter being provided with or comprising the above-described composition according to the invention. It can be envisaged here that the composition is also applied to a segment of the catheter that is insertable or introducible into a body lumen, especially into the urethra.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
In turn, the present invention further provides - in a fifthaspect of the present invention -apackaging
- 28 -unit, containing at least one container, as described above, and/or one catheter, as described above.
It can be envisaged here that the container or the catheter has been introduced into outer packaging providing protection against contamination.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Lastly, the present invention further provides - in a sixth aspect of the present invention - a kit, especially a catheterization system, comprising, on the one hand, a catheter, especially a bladder catheter or fistula catheter, as spatially separate components and, on the other hand, the above-described composition.
In the context of the present invention, it can be envisaged here that the composition has been introduced into a container according to the invention, as defined above.
In the kit according to the invention, the relevant components or constituents are spatially separate, but are functionally connected.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Further designs, modifications and variations of the present invention are readily identifiable and realizable for a person skilled in the art upon reading
It can be envisaged here that the container or the catheter has been introduced into outer packaging providing protection against contamination.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Lastly, the present invention further provides - in a sixth aspect of the present invention - a kit, especially a catheterization system, comprising, on the one hand, a catheter, especially a bladder catheter or fistula catheter, as spatially separate components and, on the other hand, the above-described composition.
In the context of the present invention, it can be envisaged here that the composition has been introduced into a container according to the invention, as defined above.
In the kit according to the invention, the relevant components or constituents are spatially separate, but are functionally connected.
With regard to further details concerning this aspect of the invention, reference can be made to the above explanations in relation to the other inventive aspects, said explanations also applying accordingly with regard to this aspect of the invention.
Further designs, modifications and variations of the present invention are readily identifiable and realizable for a person skilled in the art upon reading
- 29 -the description, without said person departing from the context of the present invention.
The present invention will be illustrated on the basis of the following exemplary embodiments, which, however, are intended in no case to limit the present invention.
The present invention will be illustrated on the basis of the following exemplary embodiments, which, however, are intended in no case to limit the present invention.
- 30 -Exemplary embodiments:
1. Providing compositions according to the invention and comparative compositions The efficacy of the compositions according to the invention is investigated by comparing compositions according to the invention that are provided by the applicant with various comparative compositions. Tables 1 and 2 show the recipes for compositions A and B according to the invention that are provided.
Table 1: Recipe of composition A according to the invention Component Amount in % by weight (based on the composition) Purified water 92-96 Lidocaine hydrochloride 1.5-3 Polyhexanide (0.3%) 0.5-3 Hydroxyethylcellulose 0.5-2.5 Sodium hydroxide solution 0.01-0.15 Table 2: Recipe of composition B according to the invention _____________ Component Amount in % by weight (based on the composition) Purified water 92-96 Benzocaine hydrochloride 1.5-3 Polyhexanide (0.3%) 0.5-3 Hydroxyethylcellulose 0.5-2.5 Sodium hydroxide solution 0.01-0.15 Comparative composition C differs from composition A according to the invention in that octenidine
1. Providing compositions according to the invention and comparative compositions The efficacy of the compositions according to the invention is investigated by comparing compositions according to the invention that are provided by the applicant with various comparative compositions. Tables 1 and 2 show the recipes for compositions A and B according to the invention that are provided.
Table 1: Recipe of composition A according to the invention Component Amount in % by weight (based on the composition) Purified water 92-96 Lidocaine hydrochloride 1.5-3 Polyhexanide (0.3%) 0.5-3 Hydroxyethylcellulose 0.5-2.5 Sodium hydroxide solution 0.01-0.15 Table 2: Recipe of composition B according to the invention _____________ Component Amount in % by weight (based on the composition) Purified water 92-96 Benzocaine hydrochloride 1.5-3 Polyhexanide (0.3%) 0.5-3 Hydroxyethylcellulose 0.5-2.5 Sodium hydroxide solution 0.01-0.15 Comparative composition C differs from composition A according to the invention in that octenidine
- 31 -hydrochloride is used as antiseptic instead of the polyhexanide used according to the invention.
Comparative composition D differs from composition A according to the invention in that chlorhexidine is used as antiseptic instead of the polyhexanide used according to the invention.
As described below, the four compositions provided are investigated in the context of application or efficacy studies with regard to their application properties and their efficacy in catheterizations.
2. Physical properties/stability properties of the compositions according to the invention:
After their preparation, compositions A and B
according to the invention are investigated with regard to their physical properties both before and after sterilization. The relevant results are shown in Tables 3 and 4 below.
Table 3: Properties of composition A according to the invention Composition A Before After sterilization sterilization Appearance Virtually Virtually colorless, clear, colorless, clear, viscous liquid viscous liquid pH 6.59 6.57 Viscosity [mPa-s] 2.764 (20 C) Polyhexanide 1.567 1.531 content (mg/100 ml) Lidocaine 2.031 2.000 hydrochloride content (mg/100 ml)
Comparative composition D differs from composition A according to the invention in that chlorhexidine is used as antiseptic instead of the polyhexanide used according to the invention.
As described below, the four compositions provided are investigated in the context of application or efficacy studies with regard to their application properties and their efficacy in catheterizations.
2. Physical properties/stability properties of the compositions according to the invention:
After their preparation, compositions A and B
according to the invention are investigated with regard to their physical properties both before and after sterilization. The relevant results are shown in Tables 3 and 4 below.
Table 3: Properties of composition A according to the invention Composition A Before After sterilization sterilization Appearance Virtually Virtually colorless, clear, colorless, clear, viscous liquid viscous liquid pH 6.59 6.57 Viscosity [mPa-s] 2.764 (20 C) Polyhexanide 1.567 1.531 content (mg/100 ml) Lidocaine 2.031 2.000 hydrochloride content (mg/100 ml)
- 32 -Unknown Not detectable Not detectable contaminants Table 4: Properties of composition B according to the invention Composition B Before After sterilization sterilization Appearance Virtually Virtually colorless, clear, colorless, clear, viscous liquid viscous liquid pH 6.66 6.63 Viscosity [mPa-s] 2.770 (20 C) Polyhexanide 1.543 1.510 content (mg/100 ml) Benzocaine 2.021 2.016 hydrochloride content (mg/100 ml) Unknown Not detectable Not detectable contaminants As shown by the above specifications, the compositions according to the invention have a good stability. Even after sterilization, there is virtually no change in appearance, pH and active-ingredient content. The compositions according to the invention also exhibit after sterilization a viscosity within the range envisaged according to the invention, said viscosity being optimal for the application due to said viscosity being unchanged.
Furthermore, the compositions according to the invention are investigated with regard to their long-term stability, i.e., their stability over a period of two years. It is apparent here that, even after a storage over a period of two years,
Furthermore, the compositions according to the invention are investigated with regard to their long-term stability, i.e., their stability over a period of two years. It is apparent here that, even after a storage over a period of two years,
- 33 -the optical properties remain unchanged, that especially no clouding or crystallization can be observed. Furthermore, the active-ingredient contents also remain at least substantially constant.
It has also been demonstrated in the context of the investigation of long-term stability that the compositions according to the invention do not exhibit any microbiological infestation or any bacterial contamination, even though the compositions according to the present invention are free of preserving agents. Altogether, the compositions according to the invention thus have an excellent long-term stability or storage stability.
3. Application and efficacy studies:
In the context of efficacy studies carried out by the applicant, the excellent action of compositions according to the present invention based on the inventive active-ingredient combination of polyhexanide, on the one hand, and a local anesthetic, on the other (cf. following "Composition A" (local anesthetic: lidocaine) and "Composition B" (local anesthetic: benzocaine)) is demonstrated with respect to comparative compositions based on octenidine and lidocaine as active-ingredient combination (cf. "Composition C") and based on chlorhexidine and lidocaine (cf.
following "Composition D"). In this connection, a distinctly improved efficacy both with respect to the reduction of infections and with respect to the pain-relieving properties is observed for the inventive combination based on the following composition A and composition B.
It has also been demonstrated in the context of the investigation of long-term stability that the compositions according to the invention do not exhibit any microbiological infestation or any bacterial contamination, even though the compositions according to the present invention are free of preserving agents. Altogether, the compositions according to the invention thus have an excellent long-term stability or storage stability.
3. Application and efficacy studies:
In the context of efficacy studies carried out by the applicant, the excellent action of compositions according to the present invention based on the inventive active-ingredient combination of polyhexanide, on the one hand, and a local anesthetic, on the other (cf. following "Composition A" (local anesthetic: lidocaine) and "Composition B" (local anesthetic: benzocaine)) is demonstrated with respect to comparative compositions based on octenidine and lidocaine as active-ingredient combination (cf. "Composition C") and based on chlorhexidine and lidocaine (cf.
following "Composition D"). In this connection, a distinctly improved efficacy both with respect to the reduction of infections and with respect to the pain-relieving properties is observed for the inventive combination based on the following composition A and composition B.
- 34 -The efficacy study carried out is ascertained on the basis of various investigation methods (i.e., subjective well-being of the patients, pathogen or bacterial content in a sample from the test subject after removal of the catheter).
In the context of the investigations explained below, to the test subjects prior to placement of the catheter, corresponding catheterization gels based on the above compositions are applied in each case to the ureter and the corresponding catheters are subsequently placed. For each investigation group or composition, ten test subjects are investigated, with the test subjects distributed across the groups ranging from 40 to 69 years of age. Each investigation group consists of 5 male and 5 female test subjects.
a) In the context of the first line of investigation, the test subjects give their subjective feeling on the basis of a grading system with grades from 1 to 6 (1 = very good to 6 = unsatisfactory). This investigation focuses especially on pain during placement of the catheter and on the sensation of pain at time t - 6 hours, 12 hours or 24 hours after catheterization.
With compositions A and B according to the invention, it is possible to observe a distinct improvement in pain symptoms. Both in the case of placement of the catheter and at the later times after catheterization, the pain symptoms can be significantly improved for the test subjects. In this connection, the use of lidocaine as local anesthetic is found to be slightly superior with respect to the use of benzocaine. Nevertheless, even
In the context of the investigations explained below, to the test subjects prior to placement of the catheter, corresponding catheterization gels based on the above compositions are applied in each case to the ureter and the corresponding catheters are subsequently placed. For each investigation group or composition, ten test subjects are investigated, with the test subjects distributed across the groups ranging from 40 to 69 years of age. Each investigation group consists of 5 male and 5 female test subjects.
a) In the context of the first line of investigation, the test subjects give their subjective feeling on the basis of a grading system with grades from 1 to 6 (1 = very good to 6 = unsatisfactory). This investigation focuses especially on pain during placement of the catheter and on the sensation of pain at time t - 6 hours, 12 hours or 24 hours after catheterization.
With compositions A and B according to the invention, it is possible to observe a distinct improvement in pain symptoms. Both in the case of placement of the catheter and at the later times after catheterization, the pain symptoms can be significantly improved for the test subjects. In this connection, the use of lidocaine as local anesthetic is found to be slightly superior with respect to the use of benzocaine. Nevertheless, even
- 35 -with the use of benzocaine, an excellent alleviation of pain can be achieved altogether. With comparative compositions C
and D, poorer results are achieved. The results ascertained for all groups are shown in Table 5 below:
Table 5: Results of the assessment of pain symptoms A(invention) B(invention) C(comparison) D(comparison) t = Oh 1.2 0.1 1.3 0.2 1.6 0.4 2.0 0.3 t = 6 h 1.4 0.3 1.5 0.1 1.9 0.5 2.6 0.1 t = 12 h1.7 0.1 1.8 0.3 2.2 0.3 2.9 0.5 t - 24 h2.0 0.2 2.1 0.2 2.4 0.6 3.3 0.2 h) In a second line of investigation, the catheter is removed after 72 hours and a sample from each test subject is subsequently investigated with respect to any microbiological infestation. The classification is likewise carried out on the basis of the above-described grading system with grades from 1 to 6 (1 = very low or no microbiological infestation to 6 = very severe microbiological infestation in the acquired sample). Corresponding mean values and the associated standard deviations are ascertained. Table 6 below shows the results ascertained for all groups. With regard to compositions A and B according to the invention, there is a significant reduction in microbiological infestation.
With comparative compositions C and D, especially composition D, poorer results are achieved.
Table 6: Results of the assessment of microbiological infestation
and D, poorer results are achieved. The results ascertained for all groups are shown in Table 5 below:
Table 5: Results of the assessment of pain symptoms A(invention) B(invention) C(comparison) D(comparison) t = Oh 1.2 0.1 1.3 0.2 1.6 0.4 2.0 0.3 t = 6 h 1.4 0.3 1.5 0.1 1.9 0.5 2.6 0.1 t = 12 h1.7 0.1 1.8 0.3 2.2 0.3 2.9 0.5 t - 24 h2.0 0.2 2.1 0.2 2.4 0.6 3.3 0.2 h) In a second line of investigation, the catheter is removed after 72 hours and a sample from each test subject is subsequently investigated with respect to any microbiological infestation. The classification is likewise carried out on the basis of the above-described grading system with grades from 1 to 6 (1 = very low or no microbiological infestation to 6 = very severe microbiological infestation in the acquired sample). Corresponding mean values and the associated standard deviations are ascertained. Table 6 below shows the results ascertained for all groups. With regard to compositions A and B according to the invention, there is a significant reduction in microbiological infestation.
With comparative compositions C and D, especially composition D, poorer results are achieved.
Table 6: Results of the assessment of microbiological infestation
- 36 -A(invention)B(invention) C(comparison) D(comparison) t = 72 h1.1 0.2 1.2 0.1 1.4 0.1 2.9 0.4 c) In a third line of investigation, the extent to which the various tested compositions cause skin irritations or intolerabilities is assessed. In this connection too, the classification is done on the basis of the above-mentioned grading scale from 1 to 6 (1 = no irritation or intolerabilities to 6 -very severe intolerabilities or irritations).
The corresponding mean values and the associated standard deviations are ascertained. Table 7 shows the relevant results ascertained for all groups. With regard to compositions A and B according to the invention, no intolerabilities whatsoever are observed. Comparative compositions C and D are, on average, tolerated less well by the test subjects.
Table 7: Assessment of tolerability A (invention) B (invention) C(comparison) D(comparison) 1.2 0.2 1.3 0.1 2.3 0.3 3.2 0.4 The above series of experiments show altogether the excellent efficacy of the compositions according to the invention based on polyhexanide, on the one hand, and a local anesthetic, especially lidocaine hydrochloride, on the other, with respect to the stated comparative compositions. In particular, in the context of the present invention, it has been demonstrated that using polyhexanide as antiseptic can significantly improve the tolerability of lubricants Or lubricant gels. Furthermore, an excellent
The corresponding mean values and the associated standard deviations are ascertained. Table 7 shows the relevant results ascertained for all groups. With regard to compositions A and B according to the invention, no intolerabilities whatsoever are observed. Comparative compositions C and D are, on average, tolerated less well by the test subjects.
Table 7: Assessment of tolerability A (invention) B (invention) C(comparison) D(comparison) 1.2 0.2 1.3 0.1 2.3 0.3 3.2 0.4 The above series of experiments show altogether the excellent efficacy of the compositions according to the invention based on polyhexanide, on the one hand, and a local anesthetic, especially lidocaine hydrochloride, on the other, with respect to the stated comparative compositions. In particular, in the context of the present invention, it has been demonstrated that using polyhexanide as antiseptic can significantly improve the tolerability of lubricants Or lubricant gels. Furthermore, an excellent
- 37 -antimicrobial action and an efficient pain alleviation are achieved.
Moreover, the compositions according to the invention have an excellent (storage) stability.
Even over a storage period of two years, there are no relevant changes in physical properties.
Concerning, in addition, specifically the microbial stability of the compositions according to the invention, this is ensured even without the use of an additional preserving agent.
Moreover, the compositions according to the invention have an excellent (storage) stability.
Even over a storage period of two years, there are no relevant changes in physical properties.
Concerning, in addition, specifically the microbial stability of the compositions according to the invention, this is ensured even without the use of an additional preserving agent.
Claims (97)
1. A composition in the form of a lubricant gel and/or a lubricant for use in catheterizations, probings, endoscopies, intubations and/or obstetrical procedures, wherein the composition comprises:
(a) a pharmaceutically effective amount of at least one local anesthetic as "component (a)"
and (b) a pharmaceutically effective amount of polyhexanide and/or salts thereof as "component (b)", wherein the composition is at least substantially free of (poly)alkylene glycols; and wherein the composition has a physiologically compatible pH within a range from 5 to 7.5.
(a) a pharmaceutically effective amount of at least one local anesthetic as "component (a)"
and (b) a pharmaceutically effective amount of polyhexanide and/or salts thereof as "component (b)", wherein the composition is at least substantially free of (poly)alkylene glycols; and wherein the composition has a physiologically compatible pH within a range from 5 to 7.5.
2. The composition of claim 1, wherein component (a) is a local anesthetic of the ester type, a local anesthetic of the amide type, or combinations or mixtures thereof.
3. The composition of claim 1, wherein component (a) is selected from the group consisting of benzocaine, procaine, tetracaine, lidocaine, etidocaine, prilocaine, mepivacaine, bupivacaine, S-ropivacaine, salts thereof, and combinations or mixtures thereof.
4. The composition of claim 1, wherein component (a) is lidocaine and/or salts thereof.
5. The composition of claim 1, wherein component (a) is lidocaine hydrochloride.
6. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount within a range from 0.1 to 10% by weight, based on the composition.
7. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount within a range from 0.5 to 8% by weight, based on the composition.
8. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount within a range from 0.7 to 6% by weight, based on the composition.
9. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount within a range from 1 to 3% by weight, based on the composition.
10. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount within a range from 0.01 to 15% by weight, based on the composition.
11. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount of not more than 15% by weight, based on the composition.
12. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount of not more than 10% by weight, based on the composition.
13. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount of not more than 8% by weight, based on the composition.
14. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount of not more than 5% by weight, based on the composition.
15. The composition of any one of claims 1 to 5, wherein the composition comprises component (a) in an amount of not more than 3% by weight, based on the composition.
16. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount within a range from 0.05 to 10% by weight, based on the composition.
17. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount within a range from 0.1 to 8% by weight, based on the composition.
18. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount within a range from 0.5 to 5% by weight, based on the composition.
19. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount within a range from 0.75 to 3% by weight, based on the composition.
20. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount within a range from 1 to 2%
by weight, based on the composition.
by weight, based on the composition.
21. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount of not more than 10% by weight, based on the composition.
22. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount of not more than 8% by weight, based on the composition.
23. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount of not more than 5% by weight, based on the composition.
24. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount of not more than 3% by weight, based on the composition.
25. The composition of any one of claims 1 to 15, wherein the composition comprises polyhexanide and/or salts thereof in an amount of not more than 2% by weight, based on the composition.
26. The composition of any one of claims 1 to 25, wherein the composition comprises component (a) and component (b) in a weight-based ratio of [(a):(b)] within a range from 1:50 to 50:1.
27. The composition of any one of claims 1 to 25, wherein the composition comprises component (a) and component (b) in a weight-based ratio of [(a):(b)] within a range from 1:20 to 20:1.
28. The composition of any one of claims 1 to 25, wherein the composition comprises component (a) and component (b) in a weight-based ratio of [(a):(b)] within a range from 1:10 to 10:1.
29. The composition of any one of claims 1 to 25, wherein the composition comprises component (a) and component (b) in a weight-based ratio of [(a):(h)] within a range from 1:5 to 5:1.
30. The composition of any one of claims 1 to 25, wherein the composition comprises component (a) and component (b) in a weight-based ratio of [(a):(b)] within a range from 1:3 to 3:1.
31. The composition of any one of claims 1 to 30, wherein the composition is water-based or water/alcohol-based.
32. The composition of claim 31, wherein the composition comprises purified water.
33. The composition of claim 31 or 32, wherein the composition comprises water in an amount within a range from 30 to 99% by weight, based on the composition.
34. The composition of claim 31 or 32, wherein the composition comprises water in an amount within a range from 40 to 93% by weight, based on the composition.
35. The composition of claim 31 or 32, wherein the composition comprises water in an amount within a range from 50 to 97% by weight, based on the composition.
36. The composition of claim 31 or 32, wherein the composition comprises water in an amount within a range from 60 to 96% by weight, based on the composition.
37. The composition of any one of claims 31 to 36, wherein the composition contains at least one polyhydric alcohol.
38. The composition of claim 37, wherein the polyhydric alcohol is selected from the group consisting of polyvinyl alcohols, glycerol and combinations thereof.
39. The composition of claim 37, wherein the polyhydric alcohol is glycerol.
40. The composition of claim 37, 38 or 39, wherein the composition comprises the polyhydric alcohol in an amount within a range from 1 to 80% by weight, based on the composition.
41. The composition of claim 37, 38 or 39, wherein the composition comprises the polyhydric alcohol in an amount within a range from 5 to 70% by weight, based on the composition.
42. The composition of claim 37, 38 or 39, wherein the composition comprises the polyhydric alcohol in an amount within a range from 10 to 60% by weight, based on the composition.
43. The composition of claim 37, 38 or 39, wherein the composition comprises the polyhydric alcohol in an amount within a range from 15 to 50% by weight, based on the composition.
44. The composition of any one of claims 1 to 30, wherein the composition comprises a mix or a mixture of water and at least one polyhydric alcohol, and wherein the proportion of water is at least 10% by weight, based on the mix or the mixture.
45. The composition of claim 44, wherein the proportion of water is at least 30% by weight, based on the mix or the mixture.
46. The composition of claim 44, wherein the proportion of water is at least 50% by weight, based on the mix or the mixture.
47. The composition of claim 44, 45 or 46, wherein a weight-based ratio of water to alcohol in the composition is within a range from 9:1 to 1:5.
48. The composition of claim 44, 45 or 46, wherein a weight-based ratio of water to alcohol in the composition is within a range from 3:1 to 1:3.
49. The composition of claim 44, 45 or 46, wherein a weight-based ratio of water to alcohol in the composition is within a range from 2:1 to 1:2.
50. The composition of claim 44, 45 or 46, wherein a weight-based ratio of water to alcohol in the composition is within a range from 1.5:1 to 1:1.5.
51. The composition of any one of claims 1 to 50, wherein the composition comprises substantially no propylene glycol.
52. The composition of any one of claims 1 to 51, wherein the composition is viscous or gel-like.
53. The composition of any one of claims 1 to 52, wherein the composition further comprises at least one gel-forming agent.
54. The composition of claim 53, wherein the at least one gel-forming agent is selected from the group consisting of bentonites, silicic acids, polyacrylic acids, carbomers, polyvinylpyrrolidones, cellulose and cellulose derivatives, xanthans, and mixtures thereof.
55. The composition of claim 53, wherein the at least one gel-forming agent is cellulose or cellulose derivatives.
56. The composition of claim 53, wherein the at least one gel-forming agent is modified celluloses.
57. The composition of claim 56, wherein the modified celluloses are chemically modified celluloses.
58. The composition of claim 53, wherein the at least one gel-forming agent is methylcellulose, carboxymethylcellulose and/or hydroxyethylcellulose.
59. The composition of claim 53, wherein the at least one gel-forming agent is hydroxyethylcellulose.
60. The composition of any one of claims 53 to 59, wherein the composition comprises the gel-forming agent in an amount within the range from 0.01 to 20% by weight, based on the composition.
61. The composition of any one of claims 53 to 59, wherein the composition comprises the at least one gel-forming agent in an amount within a range from 0.1 to 10% by weight, based on the composition.
62. The composition of any one of claims 53 to 59, wherein the composition comprises the at least one gel-forming agent in an amount within a range from 0.5 to 5% by weight, based on the composition.
63. The composition of any one of claims 53 to 59, wherein the composition comprises the at least one gel-forming agent in an amount within a range from 1 to 3% by weight, based on the composition.
64. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within the range from 20 to 20 000 mPa-s.
65. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within a range from 50 to 15 000 mPa-s.
66. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within a range from 100 to 10 000 mPa-s.
67. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within a range from 500 to 8000 mPa-s.
68. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within a range from 1000 to 7000 mPa-s.
69. The composition of any one of claims 1 to 63, wherein the composition has, at a temperature of 20°C, a dynamic viscosity within a range from 2000 to 6000 mPa-s.
70. The composition of any one of claims 1 to 69, wherein the physiologically compatible pH is within a range from 6 to 7.
71. The composition of any one of claims 1 to 70, wherein the composition has a physiologically compatible electrical conductivity within a range from 1 to 20 mS/cm.
72. The composition of any one of claims 1 to 70, wherein the composition has a physiologically compatible electrical conductivity within a range from 2 to 15 mS/cm.
73. The composition of any one of claims 1 to 70, wherein the composition has a physiologically compatible electrical conductivity within a range from 3 to 13 mS/cm.
74. The composition of any one of claims 1 to 70, wherein the composition has a physiologically compatible electrical conductivity within the range from 5 to 10 mS/cm.
75. The composition of any one of claims 1 to 74, wherein the composition further comprises at least one acid and/or base.
76. The composition of claim 75, wherein the at least one acid and/or base is for forming a buffer system.
77. The composition of claim 75 or 76, wherein the composition comprises at least one base.
78. The composition of claim 77, wherein the base is selected from the group consisting of amines, carboxylates, alkali metal hydroxides, alkaline earth metal hydroxides, and combinations thereof.
79. The composition of claim 77, wherein the base is an alkali metal hydroxide or an alkaline earth metal hydroxide.
80. The composition of claim 77, wherein the base is sodium hydroxide.
81. The composition of any one of claims 1 to 80, wherein the composition comprises no preserving agent.
82. The composition of any one of claims 1 to 81, wherein the composition comprises no preservatives.
83. The composition of any one of claims 1 to 80, wherein the composition is substantially free of preserving agents.
84. The composition of any one of claims 1 to 80 and 83, wherein the composition is substantially free of preservatives.
85. The composition of any one of claims 1 to 84, wherein the composition further comprises at least one further active ingredient and/or ingredient selected from the group consisting of skin protectants, antiseptics, local anesthetics, vitamins, trace elements, minerals, micronutrients, and combinations thereof.
86. The composition of any one of claims 1 to 85, wherein the composition further comprises at least one pharmaceutical additive and/or excipient selected from the group consisting of processing aids, stabilizers, emulsifiers, antioxidants, preservatives, humectants, pH setters, pH buffer substances, thickeners, antiseptics, dyes, buffer substances, odorants, fragrances, extenders, binders, wetting substances, and combinations thereof.
87. The composition of any one of claims 1 to 86 for use in prophylactic mucosa disinfection, therapeutic mucosa disinfection, diagnostic mucosa disinfection, or a combination thereof in the context of catheterizations, probings, endoscopies, intubations and/or obstetrical procedures.
88. The composition of claim 87, wherein the catheterizations comprise transurethral or suprapubic catheterizations.
89. A container, containing a composition as defined in any one of claims 1 to 88.
90. The container of claim 89, wherein the container is an application apparatus.
91. The container of claim 90, wherein the application apparatus is a sterile syringe.
92. A catheter, wherein the catheter is provided with a composition as defined in any one of claims 1 to 88, and wherein the composition is applied to a segment of the catheter that is insertable and/or introducible into a body lumen.
93. The catheter of claim 92, wherein the catheter is a bladder catheter or a fistula catheter, and wherein the segment of the catheter is insertable and/or introducible into a urethra or an artificial fistula for urinary diversion.
94. A packaging unit, containing at least one container as defined in claim 89, 90 or 91, wherein the container has been introduced into outer packaging providing protection against contamination.
95. The packaging unit of claim 94, further comprising a catheter as defined in claim 92 or 93, wherein the catheter has been introduced into outer packaging providing protection against contamination.
96. A kit, comprising, as spatially separated components, a catheter and a composition as defined in any one of claims 1 to 80.
97. The kit of claim 96, wherein the catheter is a bladder catheter or a fistula catheter.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102013112876.9 | 2013-11-21 | ||
| DE102013112876 | 2013-11-21 | ||
| DE102014100274.1 | 2014-01-13 | ||
| DE102014100274.1A DE102014100274A1 (en) | 2013-11-21 | 2014-01-13 | Composition, in particular in the form of a gel, and its use |
| PCT/EP2014/002492 WO2015074730A1 (en) | 2013-11-21 | 2014-09-16 | Composition, especially in the form of a lubricant gel comprising a local anaesthetic and polyhexanide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2925363A1 CA2925363A1 (en) | 2015-05-28 |
| CA2925363C true CA2925363C (en) | 2018-04-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2925363A Expired - Fee Related CA2925363C (en) | 2013-11-21 | 2014-09-16 | Composition, especially in the form of a lubricant gel comprising a local anaesthetic and polyhexanide |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP3035915B1 (en) |
| CA (1) | CA2925363C (en) |
| DE (1) | DE102014100274A1 (en) |
| DK (1) | DK3035915T3 (en) |
| ES (1) | ES2697402T3 (en) |
| WO (1) | WO2015074730A1 (en) |
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|---|---|---|---|---|
| DE102017105010A1 (en) * | 2017-02-24 | 2018-08-30 | Farco-Pharma Gmbh | Composition, in particular gel, for use in the genitourinary tract |
| WO2019059856A1 (en) | 2017-09-22 | 2019-03-28 | Turkuaz Sağlik Hi̇zmetleri̇ Medi̇kal Temi̇zli̇k Ki̇myasal Ürünler Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ | Obstetrics gel and production method |
| EP3524055A1 (en) * | 2018-02-08 | 2019-08-14 | BCSK Biocid GmbH | Antibacterial and spermicidal lubricant |
| US11534577B2 (en) * | 2018-06-28 | 2022-12-27 | Adapta Medical, Inc. | Catheters having low viscosity lubricant |
| US12290512B2 (en) | 2018-12-27 | 2025-05-06 | José António PACHECO DOS SANTOS DIAS | Gel composition with an anaesthetic effect of short and long term duration |
| CA3140207C (en) | 2019-06-13 | 2025-05-13 | Hollister Incorporated | Reusable urinary catheter products |
| AU2020304005B2 (en) | 2019-06-25 | 2025-12-04 | Hollister Incorporated | Reusable urinary catheter products |
| EP4062952B1 (en) * | 2021-03-23 | 2024-01-31 | Wellspect AB | Reusable hydrophilic urinary catheter assembly |
| CN113855863A (en) * | 2021-09-08 | 2021-12-31 | 深圳市盛康泰医疗器械有限公司 | Body cavity instrument lubricating liquid and preparation method thereof |
| EP4245294B1 (en) * | 2022-03-16 | 2025-03-12 | Pharmazeutische Fabrik Montavit Ges.m.b.H. | Catheter slide with enhanced stability |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5611464A (en) * | 1995-05-30 | 1997-03-18 | Ciba Geigy Corporation | Container for preserving media in the tip of a solution dispenser |
| EP3025704B1 (en) * | 2005-03-10 | 2019-01-16 | 3M Innovative Properties Company | Methods of reducing microbial contamination |
| EP2415487B1 (en) * | 2010-08-02 | 2014-10-08 | angioclinic AG | An ultrasonic couplant composition |
| RU2427379C1 (en) * | 2010-09-20 | 2011-08-27 | Закрытое акционерное общество "Институт прикладной нанотехнологии" | Diabetic foot prevention and care composition |
| EP2540322A1 (en) * | 2011-07-01 | 2013-01-02 | angioclinic AG | Ultrasonic couplant spray |
| DE202013000446U1 (en) * | 2012-10-04 | 2013-10-07 | Maria Clementine Martin Klosterfrau Vertriebsgesellschaft Mbh | Composition, in particular pharmaceutical composition, in particular for administration in hoarseness and sore throat |
-
2014
- 2014-01-13 DE DE102014100274.1A patent/DE102014100274A1/en not_active Withdrawn
- 2014-09-16 ES ES14776998T patent/ES2697402T3/en active Active
- 2014-09-16 DK DK14776998.8T patent/DK3035915T3/en active
- 2014-09-16 EP EP14776998.8A patent/EP3035915B1/en active Active
- 2014-09-16 CA CA2925363A patent/CA2925363C/en not_active Expired - Fee Related
- 2014-09-16 WO PCT/EP2014/002492 patent/WO2015074730A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| CA2925363A1 (en) | 2015-05-28 |
| DK3035915T3 (en) | 2018-12-17 |
| WO2015074730A1 (en) | 2015-05-28 |
| ES2697402T3 (en) | 2019-01-23 |
| DE102014100274A1 (en) | 2015-05-21 |
| EP3035915B1 (en) | 2018-08-22 |
| EP3035915A1 (en) | 2016-06-29 |
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| Date | Code | Title | Description |
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| EEER | Examination request |
Effective date: 20160608 |
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| MKLA | Lapsed |
Effective date: 20210916 |