RU2005119159A - Диспергируемые фармацевтические композиции - Google Patents
Диспергируемые фармацевтические композиции Download PDFInfo
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- RU2005119159A RU2005119159A RU2005119159/15A RU2005119159A RU2005119159A RU 2005119159 A RU2005119159 A RU 2005119159A RU 2005119159/15 A RU2005119159/15 A RU 2005119159/15A RU 2005119159 A RU2005119159 A RU 2005119159A RU 2005119159 A RU2005119159 A RU 2005119159A
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- Prior art keywords
- composition
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- methyl
- fatty acids
- salts
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- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- 239000000203 mixture Substances 0.000 claims 20
- -1 5- (3-pyridyl) -thiophen-2-yl Chemical group 0.000 claims 11
- 235000014113 dietary fatty acids Nutrition 0.000 claims 6
- 239000000194 fatty acid Substances 0.000 claims 6
- 229930195729 fatty acid Natural products 0.000 claims 6
- 150000004665 fatty acids Chemical class 0.000 claims 6
- 239000003921 oil Substances 0.000 claims 5
- 235000019198 oils Nutrition 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000000126 substance Substances 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 208000035143 Bacterial infection Diseases 0.000 claims 4
- 230000000844 anti-bacterial effect Effects 0.000 claims 4
- 239000008365 aqueous carrier Substances 0.000 claims 4
- 208000022362 bacterial infectious disease Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N monopropylene glycol Natural products CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 235000019808 microcrystalline wax Nutrition 0.000 claims 3
- 239000004200 microcrystalline wax Substances 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- 229930186147 Cephalosporin Natural products 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 125000005907 alkyl ester group Chemical group 0.000 claims 2
- ZBHXIWJRIFEVQY-IHMPYVIRSA-N ceftiofur Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1CSC(=O)C1=CC=CO1 ZBHXIWJRIFEVQY-IHMPYVIRSA-N 0.000 claims 2
- 229960005229 ceftiofur Drugs 0.000 claims 2
- 229940106164 cephalexin Drugs 0.000 claims 2
- AVGYWQBCYZHHPN-CYJZLJNKSA-N cephalexin monohydrate Chemical compound O.C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=CC=C1 AVGYWQBCYZHHPN-CYJZLJNKSA-N 0.000 claims 2
- 229940124587 cephalosporin Drugs 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 239000012530 fluid Substances 0.000 claims 2
- 125000005456 glyceride group Chemical group 0.000 claims 2
- 238000001802 infusion Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000002480 mineral oil Substances 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 235000015112 vegetable and seed oil Nutrition 0.000 claims 2
- 239000008158 vegetable oil Substances 0.000 claims 2
- FMZXNVLFJHCSAF-DNVCBOLYSA-N (6R,7R)-3-[(4-carbamoyl-1-pyridin-1-iumyl)methyl]-8-oxo-7-[(1-oxo-2-thiophen-2-ylethyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound C1=CC(C(=O)N)=CC=[N+]1CC1=C(C([O-])=O)N2C(=O)[C@@H](NC(=O)CC=3SC=CC=3)[C@H]2SC1 FMZXNVLFJHCSAF-DNVCBOLYSA-N 0.000 claims 1
- YWKJNRNSJKEFMK-PQFQYKRASA-N (6r,7r)-7-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-3-(5,6,7,8-tetrahydroquinolin-1-ium-1-ylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound N([C@@H]1C(N2C(=C(C[N+]=3C=4CCCCC=4C=CC=3)CS[C@@H]21)C([O-])=O)=O)C(=O)\C(=N/OC)C1=CSC(N)=N1 YWKJNRNSJKEFMK-PQFQYKRASA-N 0.000 claims 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims 1
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical group O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 claims 1
- RRJHESVQVSRQEX-SUYBPPKGSA-N O-formylcefamandole Chemical compound CN1N=NN=C1SCC1=C(C(O)=O)N2C(=O)[C@@H](NC(=O)[C@H](OC=O)C=3C=CC=CC=3)[C@H]2SC1 RRJHESVQVSRQEX-SUYBPPKGSA-N 0.000 claims 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims 1
- 239000005642 Oleic acid Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 238000006136 alcoholysis reaction Methods 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- RRYMAQUWDLIUPV-BXKDBHETSA-N cefacetrile Chemical compound S1CC(COC(=O)C)=C(C(O)=O)N2C(=O)[C@@H](NC(=O)CC#N)[C@@H]12 RRYMAQUWDLIUPV-BXKDBHETSA-N 0.000 claims 1
- NBFNMSULHIODTC-CYJZLJNKSA-N cefadroxil monohydrate Chemical compound O.C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=C(O)C=C1 NBFNMSULHIODTC-CYJZLJNKSA-N 0.000 claims 1
- 229960001065 cefadroxil monohydrate Drugs 0.000 claims 1
- FLKYBGKDCCEQQM-WYUVZMMLSA-M cefazolin sodium Chemical compound [Na+].S1C(C)=NN=C1SCC1=C(C([O-])=O)N2C(=O)[C@@H](NC(=O)CN3N=NN=C3)[C@H]2SC1 FLKYBGKDCCEQQM-WYUVZMMLSA-M 0.000 claims 1
- 229960003408 cefazolin sodium Drugs 0.000 claims 1
- GCFBRXLSHGKWDP-XCGNWRKASA-N cefoperazone Chemical compound O=C1C(=O)N(CC)CCN1C(=O)N[C@H](C=1C=CC(O)=CC=1)C(=O)N[C@@H]1C(=O)N2C(C(O)=O)=C(CSC=3N(N=NN=3)C)CS[C@@H]21 GCFBRXLSHGKWDP-XCGNWRKASA-N 0.000 claims 1
- 229960004682 cefoperazone Drugs 0.000 claims 1
- 229950009592 cefquinome Drugs 0.000 claims 1
- 229960002588 cefradine Drugs 0.000 claims 1
- VAAUVRVFOQPIGI-SPQHTLEESA-N ceftriaxone Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1CSC1=NC(=O)C(=O)NN1C VAAUVRVFOQPIGI-SPQHTLEESA-N 0.000 claims 1
- 229960004755 ceftriaxone Drugs 0.000 claims 1
- JFPVXVDWJQMJEE-IZRZKJBUSA-N cefuroxime Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 JFPVXVDWJQMJEE-IZRZKJBUSA-N 0.000 claims 1
- 229960001668 cefuroxime Drugs 0.000 claims 1
- 229940047526 cephalexin monohydrate Drugs 0.000 claims 1
- 150000001780 cephalosporins Chemical group 0.000 claims 1
- RDLPVSKMFDYCOR-UEKVPHQBSA-N cephradine Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CCC=CC1 RDLPVSKMFDYCOR-UEKVPHQBSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229950008631 eperezolid Drugs 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims 1
- 230000001983 lactogenic effect Effects 0.000 claims 1
- TYZROVQLWOKYKF-ZDUSSCGKSA-N linezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCOCC1 TYZROVQLWOKYKF-ZDUSSCGKSA-N 0.000 claims 1
- 229960003907 linezolid Drugs 0.000 claims 1
- 235000020778 linoleic acid Nutrition 0.000 claims 1
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims 1
- 150000004668 long chain fatty acids Chemical class 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000004396 mastitis Diseases 0.000 claims 1
- 239000002609 medium Substances 0.000 claims 1
- YGZIWEZFFBPCLN-UHFFFAOYSA-N n,3-bis(2-chloroethyl)-4-hydroperoxy-2-oxo-1,3,2$l^{5}-oxazaphosphinan-2-amine Chemical compound OOC1CCOP(=O)(NCCCl)N1CCCl YGZIWEZFFBPCLN-UHFFFAOYSA-N 0.000 claims 1
- SIMWTRCFFSTNMG-AWEZNQCLSA-N n-[[(5s)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCN(C(=O)CO)CC1 SIMWTRCFFSTNMG-AWEZNQCLSA-N 0.000 claims 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims 1
- 235000021313 oleic acid Nutrition 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000004685 tetrahydrates Chemical class 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0046—Ear
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0041—Mammary glands, e.g. breasts, udder; Intramammary administration
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gynecology & Obstetrics (AREA)
- Tropical Medicine & Parasitology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pregnancy & Childbirth (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dispersion Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (18)
1. Фармацевтическая композиция, содержащая наполнитель, который включает в себя (а) амфипатическое масло, которое диспергирует в воде и не растворяется в этаноле, (b) микрокристаллический воск и (с) фармацевтически приемлемый неводный носитель; указанный наполнитель содержит устойчиво диспергированное в нем антибактериальное вещество в количестве, эффективном против бактерий.
2. Композиция по п.1, в которой антибактериальное вещество представляет собой оксазолидинон, выбранный из группы, состоящей из эперезолида, линезолида, N-((5S)-3-(3-фтор-4-(4-(2-фторэтил)-3-окси-1-пиперазинил)фенил-2-окси-5-оксазолидинил)метил)ацетамида, (S)-N-((3-(5-(3-пиридил)-тиофен-2-ил)-2-окси-5-оксазолидинил)метил)ацетамида и гидрохлорида (S)-N-((3-(5-(4-пиридил)пирид-2-ил)-2-окси-5-оксазолидинил)метил)ацетамида.
3. Композиция по п.1, в которой антибактериальное вещество представляет собой цефалоспорин, выбранный из группы, состоящей из цефтиофура и его солей, цефалексина, цефрадина, цефквинома, цефацетрила, цефалониума, цефуроксима, цефазидима, цефоперазона, цефеметкарбоксилата натрия, гептагидрата цефема, ди- и тригидрата цефалоспорина, моногидрата цефадроксила, моногидрата цефазолина натрия, цефиксимина, цефтаксима, цефтизоксима, цефтриаксона, о-формилцефамандола, солей производных 3-ацетоксиметил-7-(иминоцетамидо)-цефалоспорановой кислоты, моногидрата 7-(D-α-амино-α-(п-гидроксифенил)ацетамино)-3-метил-3-цефем-1-карбоновой кислоты, гидрохлорида син-7-((2-амино-1-тиазолил)(метоксиимино)ацетил)амино)-3-метил-3-цефем-4-карбоновой кислоты, кристаллических аддитивных солей цефемовой кислоты, (пивалоилокси)метил-7-бета-(2-(2-амино-4-тиазолил)ацетамидо)-3-(((1-(2-(диметиламино)этил)-1Н-тетраазол-5-ил)тио)метил)-3-цефем-4-карбоксилата, цефалексина, моногидрата цефалексина, тетрагидрата 7-(D-2-нафтиглициламино)-3-метил-3-цефем-4-карбоновой кислоты, их таутомеров, стереоизомеров, энантиомеров, солей, гидратов и пролекарств и их комбинаций.
4. Композиция по п.1, в которой антибактериальное вещество выбрано из группы, состоящей из цефтиофура и его фармацевтически приемлемых солей и их комбинаций.
5. Композиция по п.1-4, в которой амфипатическое масло является полигликолилированным глицеридом, полученным в результате реакции алкоголиза природных триглицеридов с полиэтиленгликолями.
6. Композиция по п.5, в которой полигликолилированный глицерид содержит основной компонент жирных кислот, олеиновой кислоты или линолевой кислоты.
7. Композиция по пп.1-4 и 6, в которой неводный носитель выбран из группы, состоящей из растительных масел, минеральных масел, жирных кислот с длиной цепи от средней до длинной и их сложных алкиловых эфиров, сложных пропиленгликолевых диэфиров жирных кислот с длиной цепи от средней до длинной, сложных моно-, ди- и триглицериловых эфиров жирных кислот, полиэтиленгликолей и их комбинаций.
8. Композиция по п.5, в которой неводный носитель выбран из группы, состоящей из растительных масел, минеральных масел, жирных кислот с длиной цепи от средней до длинной и их сложных алкиловых эфиров, сложных пропиленгликолевых диэфиров жирных кислот с длиной цепи от средней до длинной, сложных моно-, ди- и триглицериловых эфиров жирных кислот, полиэтиленгликолей и их комбинаций.
9. Композиция по пп.1-4 и 6, в которой амфипатическое масло составляет приблизительно от 0,01 до 99%, предпочтительно от 1 до 80% и более предпочтительно приблизительно от 3 до 25% мас./об. композиции.
10. Композиция по п.5, в которой амфипатическое масло составляет приблизительно от 0,01 до 99%, предпочтительно от 1 до 80% и более предпочтительно приблизительно от 3 до 25% мас./об. композиции.
11. Композиция по п.1, в которой микрокристаллический воск составляет приблизительно от 0,01 до 50%, предпочтительно приблизительно от 1 до 40% и более предпочтительно приблизительно от 3 до 15% мас./об. композиции.
12. Композиция по п. 1, в которой неводный носитель составляет приблизительно от 0,5 до 99%, предпочтительно приблизительно от 10 до 95% и более предпочтительно от 40 до 90% мас./об. композиции.
13. Изделие производства, содержащее контейнер или устройство для доставки, имеющее проницаемую для кислорода стенку и содержащее внутри себя композицию по п.1.
14. Изделие по п. 13, в котором композиция характеризуется длительной химической и/или физической стабильностью по сравнению с другой подобной же стандартной композицией, в которой отсутствует один или оба из компонентов, выбранных из амфипатического масла и микрокристаллического воска.
15. Способ лечения или предупреждения бактериальной инфекции у субъекта, включающий в себя введение композиции по любому из пп.1-12 в содержащий жидкость орган субъекта через естественное наружное отверстие органа, причем при упомянутом введении композиция диспергирует в указанной жидкости.
16. Способ по п.15, при котором указанная бактериальная инфекция присутствует в вымени лактогенного животного и при котором указанное введение осуществляют с помощью интрамаммарной инфузии.
17. Способ по п.16, при котором указанная бактериальная инфекция проявляется как мастит.
18. Способ по п.15, при котором указанная бактериальная инфекция присутствует в ухе и при котором указанное введение осуществляют с помощью ушной инфузии или инъекции.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2627429C2 (ru) * | 2012-02-27 | 2017-08-08 | Байер Нью Зиленд Лимитед | Составы с контролируемым высвобождением и способы их использования |
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