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WO2008148573A2 - Médicaments contenant une combinaison de principes actifs pour traiter les symptomes allergiques - Google Patents

Médicaments contenant une combinaison de principes actifs pour traiter les symptomes allergiques Download PDF

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Publication number
WO2008148573A2
WO2008148573A2 PCT/EP2008/004567 EP2008004567W WO2008148573A2 WO 2008148573 A2 WO2008148573 A2 WO 2008148573A2 EP 2008004567 W EP2008004567 W EP 2008004567W WO 2008148573 A2 WO2008148573 A2 WO 2008148573A2
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WO
WIPO (PCT)
Prior art keywords
allergic
dexpanthenol
combination
drug
treatment
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2008/004567
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German (de)
English (en)
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WO2008148573A3 (fr
Inventor
Marianne Petersen-Braun
Sabine Rabini
Sabine GLÄSER
Klaus Kluthe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Consumer Care AG
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Bayer Consumer Care AG
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Filing date
Publication date
Application filed by Bayer Consumer Care AG filed Critical Bayer Consumer Care AG
Priority to RU2009148577/15A priority Critical patent/RU2472499C2/ru
Priority to EP08773373A priority patent/EP2164481A2/fr
Priority to BRPI0812750-6A2A priority patent/BRPI0812750A2/pt
Publication of WO2008148573A2 publication Critical patent/WO2008148573A2/fr
Publication of WO2008148573A3 publication Critical patent/WO2008148573A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents

Definitions

  • the invention relates to combinations comprising at least one active ingredient comprising pantothenic acid and pantothenic acid derivatives, in particular dexpanthenol, and at least one antiallergic active ingredient for the treatment of allergic symptoms of the skin or mucous membrane, medicaments containing them and their preparation.
  • the available for an anti-allergic therapy drugs are generally symptomatic, since a causal therapy could be effected only by complete antigenic deficiency.
  • a causal therapy could be effected only by complete antigenic deficiency.
  • drugs from the drug class of antihistamines and from the class of corticosteroids are used.
  • mediators eg histamine
  • mast cells and basophilic granulocytes plays a central role.
  • mediators eg histamine
  • the released mediators cause increased permeability of vessels, spastic contractions of smooth muscle, and - by activation of other cell types of the immune system - local inflammatory reactions.
  • Antihistamines prevent the occurrence or effects of mediators of allergic reactions (prostaglandins, especially PGD2, and histamine) and have an antagonistic effect on the migration of eosinophilic granulocytes in atopic patients.
  • the allergic reaction can be counteracted by administration of anti-inflammatory and immunosuppressive corticosteroids (glucocorticoids). Based on this, the use of these drug classes in the symptomatic therapy of allergic diseases.
  • the symptoms caused by allergic reactions mainly affect the skin, the mucous membranes, especially the mucous membranes of the respiratory tract (nasal cavity, paranasal sinuses, oral cavity, pharynx, larynx, trachea, bronchi, bronchioles), the bronchi, the gastrointestinal tract, the conjunctiva of the eye as well as the vascular system.
  • the mucous membranes of the respiratory tract e.g.
  • Antihistamines and glucocorticoids are approved as both oral (ie systemic) and topical drugs for the treatment of allergic symptoms. Indeed the therapeutic efficacy of the known antihistamines and glucocorticoids is often inadequate, and an increase in the dose is not justifiable due to the associated risk of side effects. Frequently it comes in the symptomatic anti-allergic therapy using drugs from the classes of antimutamines and glucocorticoids to unwanted side effects, such. As skin dryness, skin atrophy, susceptibility of the skin or mucous membrane for fungal infections and bacterial and viral infections.
  • pantothenic acid and its derivatives eg dexpanthenol
  • amino acid glycine cause an inhibition of the release of mediators from mast cells and thereby the allergic reaction can be alleviated.
  • dexpanthenol is used as a component in topical medicines.
  • EP 1159958 A1 describes a nasal ointment containing dexpanthenol as a nourishing ingredient.
  • DE 10005936 A1 discloses a cream for external use in the nose area, which contains a combination of allantoin and dexpanthenol.
  • DE 19541919 A1 describes a pharmaceutical preparation for the treatment of acute rhinitis which comprises a sympathomimetic with 2-imidazoline structure (eg oxymetazoline) suitable for topical use in combination with a pantothenol derivative, e.g. As dexpanthenol contains.
  • the combination with dexpanthenol alleviated the side effects caused by the sympathomimetic.
  • the object underlying the present invention was to provide medicaments for the therapeutic treatment of allergic symptoms of the skin or mucosa, which have improved efficacy and / or a lower side-effect potential.
  • this object is achieved by a combination comprising at least one active ingredient from the pantothenic acid and pantothenic acid derivatives group, preferably dexpanthenol, and at least one anti-allergic active ingredient from the
  • Anti-inflammatory drugs corticosteroids, synthetic mast cell degranulation inhibitors and leukotriene
  • pantothenic acid and pantothenic acid derivatives comprising group, in particular dexpanthenol, the efficacy of the co-administered with the drug combination
  • the combinations according to the invention are advantageously suitable for the treatment of allergic symptoms or diseases of the skin, the mucous membranes, especially the respiratory tract and in particular the nose, or even the conjunctiva.
  • a combination of hydrocortisone with dexpanthenol is particularly advantageous for the treatment of allergic symptoms or diseases because of its anti-inflammatory properties.
  • the combinations according to the invention are furthermore advantageous, since they have a reduced side-effect potential.
  • pantothenic acid derivatives includes in particular dexpanthenol, DL-panthenol, salts of pantothenic acid (eg Na-pantothenate, Ca-pantothenate), esters of pantothenic acid (eg ethyl, methyl ester), panthenol-ether (e.g. Ethyl or methyl ether), panthenol thioether and panthenyl triacetate.
  • the relative proportion of dexpanthenol (or of the pantothenic acid derivative and / or pantothenic acid) can be varied within wide ranges, depending on the respective desired effects.
  • the dexpanthenol content is 0.1 to 95 wt .-%, in particular 0.5 to 50 wt .-%, particularly preferably 0.5 to 30 wt .-%, each based on the total amount of active ingredient.
  • the mentioned synergistic effect is observed in particular when the weight ratio of dexpanthenol (or pantothenic acid derivative) to said at least one anti-allergic active ingredient is in the range from 1: 100 to 100: 1, preferably in the range from 50: 1 to 1: 50, more preferably in the range of 1:10 to 10: 1.
  • the active ingredient combination additionally contains glycine.
  • the additional administration of glycine can achieve a further increase in therapeutic efficacy.
  • Glycine in a proportion of 0.1 to 25 wt .-%, in particular 0.5 to 10 wt .-%, each based on the total active ingredient content, in the active ingredient combination.
  • Active hypoallergenic active substances which are used according to the invention in combination with dexpanthenol (or with pantothenic acid and / or pantothenic acid derivatives) are, in particular, active substances from the active substance class of the antihistamines and from the active substance class of the corticosteroids.
  • the corticosteroids used according to the invention are generally glucocorticoids.
  • the combination according to the invention comprises at least one active ingredient from pantothenic acid and pantothenic acid derivatives group, preferably dexpanthenol, and at least one active ingredient from the drug class of antihistamines and / or at least one active ingredient from the class of corticosteroids.
  • Antihistamines histamine HI receptor antagonists, histamine H2 receptor antagonists
  • Antihistamines are substances that antagonize the action of the released histamine on the Hl receptor (or the H2 receptor), thereby eliminating the effect of histamine on Hl receptors, especially on the peripheral vessels.
  • Suitable antihistamines in connection with the present invention are, in particular, the following active substances: ketotifen, thonzylamine, mepyramine, thenalidine, tripelennamine, chlorpyramine, promethazine, tolpropamine, dimetindene, clemastine, bamipine, loratadine, isothipendyl, diphenhydramine, diphenhydramine methyl bromide, chlorphenoxamine, pheniramine, diphenylpyraline , Dioxopromethazine, dimenhydrinate, thiethylperazine and meclozin, azelastine, levocabastine, astemizole, mebhydroline, terfenadine, mequitazine, cetirizine, emedastine, mizolastine, olopatadine, epinastine and antazoline.
  • antihistamines are: bamipin, clemastine, chlorphenoxamine, azelastine, terfenadine, loratadine.
  • the relative proportion of the antihistamine (or antihistamines) is determined in a manner known to those skilled in the art, depending on the pharmacological properties and the nature of the particular dosage form used.
  • corticosteroids are basically all glucocorticoid drugs into consideration, whose therapeutic efficacy in the treatment of allergic diseases or symptoms is known.
  • the following active substances are contemplated: triamcinolone, dexamethasone, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, hydrocortisone buteprate, prednisolone, betamethasone, methylprednisolone, clobetasone, flumetasone, fluocortin, fluperolone, fluorometholone, flupredniden, desonide, triamcinolone, alclometasone, dexamethasone , clocortolone, betamethasone, Fluclorolon, desoximetasone, fluocinolone, fluocortolone, diflucortolone, fludroxycortide, fluocinonide, budesonide, d
  • the invention further includes embodiments which provide that the drug combination contains at least one synthetic antiallergic drug not selected from the group consisting of anti-viral and corticosteroids.
  • active substances from the group comprising synthetic mast cell degranulation inhibitors and leukotriene receptor antagonists come into consideration.
  • Mast cell degranulation inhibitors also referred to as mast cell stabilizers, are substances that inhibit the release of histamine from mast cells.
  • exemplary and preferred representatives of this class of drugs are cromoglycic acid, spaglumic acid, nedocromil and lodoxamide.
  • Leukotriene receptor antagonists are substances that inhibit leukotriene synthesis and / or leukotriene effects. Leukotrienes are involved in the development and chronicity of allergic inflammatory symptoms. Exemplary and preferred representatives of this class of drugs are montelukast, pranlukast, ibudilast and zafirlukast.
  • active substances exemplified in the preceding paragraphs do not provide a complete and exhaustive list of active substances from the classes of the antihistamines, glucocorticoids, synthetic mast cell degranulation inhibitors and leukotriene receptor Antagonists dar.
  • the mention of these substances is only illustrative of these classes of drugs.
  • other active ingredients from the mentioned classes of active substances can be used in the context of the invention.
  • the active substances according to the invention can also be used in the form of their pharmaceutically acceptable salts.
  • Pharmaceutically acceptable salts of the compounds of the invention may be acid addition salts of the compounds with mineral acids, carboxylic acids or sulfonic acids. Particularly preferred are e.g. Salts with hydrochloric, hydrobromic, sulfuric, phosphoric, methanesulfonic, ethanesulfonic, toluenesulfonic, benzenesulfonic, naphthalenedisulfonic, acetic, propionic, lactic, tartaric, citric, fumaric, maleic, oxalic, succinic, butyric, decanoic, aspartic or benzoic acids.
  • salts with customary bases can also be mentioned as salts, for example alkali metal salts (for example sodium or potassium salts), alkaline earth salts (for example calcium or magnesium salts) or ammonium salts derived from ammonia or organic amines such as, for example, diethylamine, triethylamine, ethyldiisopropylamine, procaine, Dibenzylamine, N-methylmorpholine, dihydroabiethylamine, 1-ephenamine or methylpiperidine.
  • alkali metal salts for example sodium or potassium salts
  • alkaline earth salts for example calcium or magnesium salts
  • ammonium salts derived from ammonia or organic amines such as, for example, diethylamine, triethylamine, ethyldiisopropylamine, procaine, Dibenzylamine, N-methylmorpholine, dihydroabiethylamine, 1-ephenamine or methylpiperidine.
  • the combination of active substances according to the invention comprises a) dexpanthenol and at least one antiWstaminic, or b) dexpanthenol, glycine and at least one antihistamine, or c) dexpanthenol and at least one corticosteroid, or d) dexpanthenol, glycine and at least one corticosteroid, or e) dexpanthenol, at least an antihistamine and at least one corticosteroid, or f) dexpanthenol, glycine, at least one antihistamine and at least one corticosteroid, or g) dexpanthenol and at least one group comprising the synthetic mast cell degranulation inhibitor and leukotriene receptor antagonists, or h) dexpanthenol, glycine and at least one drug selected from the group consisting of synthetic mast cell degranulation inhibitors and leukotriene receptor antagonists.
  • the active substance combinations described above may optionally additionally comprise at least one further active substance which is not selected from the abovementioned groups of the antiallergic active ingredients.
  • the said further active ingredient may preferably consist of selected from the group consisting of herbal active substances, plant extracts (eg evening primrose oil, borage oil, St.
  • vitamins
  • Jojoba oil, aloe vera, lanolin, vegetable oils and fats) and sunscreen substances (UV-A filter, UV-B filter, broadband filter).
  • sunscreen substances UV-A filter, UV-B filter, broadband filter.
  • Particularly advantageous is the addition of substances or mixtures of substances with anti-inflammatory effect, such as. Coal tar solution, sodium bituminosulfonate, ammonium bituminosulfonate, tretinoin, evening primrose oil, borage oil, St. John's wort extract, aloe vera extract, witch hazel extract, marigold extract, chamomile extract, vitamin E and its salts, bisabolol, allantoin, glycyrrhic acid and salts and polidocanol.
  • the proportion of the said further active ingredient (s) can be chosen freely, this proportion is preferably 0.05 to 50 wt .-%, in particular 0.1 to 20 wt .-%, each based on the drug.
  • Combination within the meaning of the invention is understood to mean not only administration forms which contain all components in a common administration form (so-called fixed combinations), and combination packages which contain the components separated from one another in a single package ("kit”) but also simultaneously or staggered components, if used to treat the same disease / symptom.
  • the active substances of the medicaments and pharmaceutical formulations according to the invention are particularly suitable for being formulated in a fixed combination. It is known that the application reliability (compliance) in patients depends crucially on the factors number of dosage forms per application time, and optionally on the size and weight of the (solid peroral) dosage form. Therefore, both the number of different medicines to be taken separately should be as small as possible (the advantage of a fixed combination) and, if necessary, the size and weight of a solid oral dosage form should be kept as small as possible without compromising therapeutic potency. This makes the application as comfortable as possible for the patient designed. By implementing fixed combinations, the highest possible patient compliance is provided and the safety and reliability of the therapy are decisively improved.
  • the medicaments according to the invention preferably contain the active ingredient combination according to the invention in the form of a "fixed combination"; This means that all active ingredients which form the respective active ingredient combination are present together in a dosage form and administered together.
  • the active compound combinations according to the invention in the form of medicaments are generally administered locally (i.e., topically) to those areas of the skin or mucous membrane which are affected by allergic symptoms.
  • the medicaments according to the invention are preferably formulated as solid, semi-solid, liquid or gaseous dosage forms for topical application to the skin or mucous membrane, in particular as powder, powder, plaster, dust aerosol, granules, lozenge, lozenge, chewing gum, gel, ointment, lotion, paste, Shampoo, emulsion, suspension, solution, gargle, juice, syrup, oil, aerosol or inhalant.
  • the following dosage forms are particularly suitable: eye ointments, eye sprays, eye tablets, eye drops, eye lotions, eye baths, eye salves.
  • the following dosage forms are considered: nose drops, nasal sprays, nose creams, creams, lozenges, suspensions or solutions, tinctures, lotions, emulsions, nose powder, powders, gels, nasal douche, nasal irrigation, aerosols, inhalants.
  • the invention also includes dosage forms for the external treatment of the nose (eg, ointments, gels, creams).
  • the following dosage forms are particularly suitable: aerosol, inhalant (suspensions, solutions), throat spray, oral spray, powder for inhalation, drops, tablets, lozenges, Pastilles, capsules, syrups, tinctures, gargles.
  • aerosol, inhalant suspensions, solutions
  • throat spray oral spray
  • powder for inhalation drops, tablets, lozenges, Pastilles, capsules, syrups, tinctures, gargles.
  • dosage forms are considered: gels, ointments, solutions, powders, creams, sprays, emulsions, suspensions, tinctures, lotions.
  • Suitable adjuvants are, for example: particulate carriers (eg talc, zinc oxide, starch, starch derivatives, diatomaceous earth); gel-forming substances (eg gelatin, tragacanth, cellulose derivatives, alginates, polyacrylic acid); Humectants (eg, urea, glycerol, propylene glycol), pressure-sensitive adhesives (eg, polyacrylates, as well as tackifier resins); Ointment bases (eg vaseline, fats, cellulose derivatives, polyacrylic acid, polyethylene glycols); Emulsifiers (eg wool wax, sorbitan esters, monoglycerides); Preservatives (e.g., benzalkonium chloride), antioxidants (e.g., butylhydroxyanisole), thickening agents (e.g., hydroxypropylmethylcellulose), pH corrigents; Binders (eg polyvinylpyrrolidone, starch, hydroxypropylmethylcellulose
  • Liquid dosage forms are also prepared by standard methods with pharmaceutically acceptable excipients and either contain the active ingredients dissolved or suspended. Typical application volumes of these pharmaceutical preparations are between 1 and 10 ml.
  • auxiliaries in these liquid formulations are: solvents (eg water, alcohol, natural and synthetic oils such as medium-chain triglycerides), solubilizers (eg glycerol, glycol derivatives), wetting agents (eg polysorbate, sodium lauryl sulfate ), as well as other auxiliaries needed for the preparation of pharmaceutical formulations of the desired properties For example, viscosity increasing agents, pH adjuvants, sweeteners and flavors, antioxidants, stabilizers and / or preservatives.
  • solvents eg water, alcohol, natural and synthetic oils such as medium-chain triglycerides
  • solubilizers eg glycerol, glycol derivatives
  • wetting agents eg polysorbate, sodium lauryl sulfate
  • dosage forms may be used which enable a delayed or controlled release of active ingredient.
  • Dosage forms with controlled or protracted release of active ingredient eg depot preparations and sustained-release preparations, as well as therapeutic systems
  • active ingredient eg depot preparations and sustained-release preparations, as well as therapeutic systems
  • composition of the drugs by known means, for example by means of
  • Envelopes, embedding or microencapsulation, drug release from the drug can be controlled.
  • the delayed or controlled release may optionally affect only one, several or all active ingredient components of the fixed drug combination.
  • the total active ingredient content in the medicaments according to the invention is preferably in the range from 0.05 to 70% by weight, in particular in the range from 0.1 to 50% by weight, particularly preferably in the range from 0.5 to 15% by weight. , in each case based on the total weight of a drug.
  • the active substances can be present in the medicaments in particular in particulate, dispersed, dissolved, suspended or emulsified form.
  • the medicaments according to the invention are medicaments for intranasal, intraocular or dermal application, or medicaments for inhalation
  • the medicaments of the invention are particularly suitable for the treatment of allergic
  • Symptoms of the nasal mucosa, conjunctiva, skin, oral mucosa, mucous membrane of the pharynx, or lower respiratory tract eg, trachea, bronchi,
  • the present invention comprises dermal dosage forms containing dexpanthenol in combination with a Hl antihistamine.
  • Preferred dosage forms are ointments, creams and gels.
  • Preferred HIV antihistamines are bamipine, clemastine fumarate and chlorphenoxamine HCl.
  • the dexpanthenol content is preferably in the range of 0.5 to 20 wt .-%, in particular from 5 to 15 wt .-%.
  • the proportion of the antihistamine is preferably in the range of 0.01 to 10 wt .-%, in particular from 0.01 to 5 wt .-%.
  • the invention comprises administration forms for intranasal or nasal administration which contain dexpanthenol in combination with a HI-antihistamine.
  • Preferred administration forms are sprays, in particular dosing sprays, or solutions.
  • Preferred Hl antihistamines are azelastine HCl and cromolyn sodium.
  • the dexpanthenol content is preferably in the range from 0.5 to 20% by weight, in particular from 5 to 15% by weight.
  • the proportion of the anti-micro-amine is preferably in the range from 0.01 to 10% by weight, in particular from 0.01 to 5% by weight.
  • the administration is carried out by means of a dosing spray, wherein with each dosing a volume of 0.05 to 0.2 ml is administered.
  • the invention includes dermal dosage forms containing dexpanthenol in combination with a corticosteroid.
  • Preferred dosage forms are ointments, creams, gels, solutions and suspensions.
  • Preferred corticosteroids are hydrocortisone, beclomethasone 17,21-dipropionate and dexamethasone.
  • the dexpanthenol content is preferably in the range of 0.5 to 20 wt .-%, in particular from 5 to 15 wt .-%.
  • the proportion of the corticosteroid is preferably in the range of 0.01 to 10 wt .-%, in particular from 0.01 to 5 wt .-%.
  • These dermal dosage forms can be used in particular for the treatment of allergic skin diseases or allergic symptoms of the skin.
  • the invention includes nasal administration dosage forms containing dexpanthenol in combination with a corticosteroid.
  • Preferred dosage forms are ointments, sprays, aerosols, solutions and suspensions.
  • Preferred corticosteroids are hydrocortisone, beclomethasone 17,21-dipropionate and dexamethasone.
  • the dexpanthenol content is preferably in the range of 0.5 to 20 wt .-%, in particular from 5 to 15 wt .-%.
  • the proportion of the corticosteroid is preferably in the range of 0.01 to 10 wt .-%, in particular from 0.01 to 5 wt .-%.
  • the invention further extends to the use of a combination of active substances as defined above for the treatment of allergic symptoms of the skin, mucous membranes (in particular mucous membranes of the respiratory tract) or conjunctiva, and to the use of such an active ingredient combination for the manufacture of a medicament for the treatment of said allergic symptoms.
  • treatment includes preventive (prophylactic) treatment.
  • the allergic symptoms mentioned above are in particular those which occur in the following allergic diseases: atopic eczema, psoriasis, contact dermatitis, skin allergies, contact dermatitis, photoallergic dermatitis, allergic urticaria, allergic rhinitis (eg seasonal allergic rhinitis, perennial allergic Rhinitis), allergic rhinoconjunctivitis, allergic conjunctivitis, allergic sinusitis, allergic laryngeal edema, allergic alveolitis, allergic bronchitis, allergic edema, allergic rosacea, insect bites, drug allergy, drug rash.
  • allergic diseases atopic eczema, psoriasis, contact dermatitis, skin allergies, contact dermatitis, photoallergic dermatitis, allergic urticaria, allergic rhinitis (eg seasonal allergic rhinitis, perennial allergic Rhinitis), allergic rhinoconjunctivitis, allergic conjunctivitis, allergic sinusitis,
  • the aforementioned allergic symptoms include in particular the following: itching; Redness; erythema; eczema; Scaling of the skin; Crusting; Oozing the skin; Dry skin;
  • Inflammatory conditions of a mucous membrane especially the nasal mucosa; Burning in the nasopharynx, coughing, coughing; Sore throat, scratching, dryness in the throat;
  • the invention further encompasses a method for the therapeutic treatment of a person having one or more allergic symptoms on the skin, mucous membranes (especially mucous membranes of the skin)
  • Such a therapeutic method of the invention comprises administering a fixed one
  • Active substance combination in a therapeutically effective dose. If necessary, the administration of the drug combination is repeated at appropriate intervals to achieve the desired therapeutic effect.
  • the administration of the drug combination is preferably carried out by means of a solid, semi-solid, liquid or gaseous dosage form, as mentioned above.
  • the active ingredient combination, or a drug containing such a combination is generally applied topically, ie to those areas of the skin or mucous membrane affected by allergic symptoms.
  • the drug or drug combination is applied to the skin, to a mucous membrane, orally, intranasally, intratracheally, intrabronchially or intraocularly.
  • the particular suitable therapeutic dose depends on the nature of the active ingredients contained in the respective drug combination and the nature of the symptoms to be treated, and can be determined in a manner known to those skilled in the art.
  • the medicaments according to the invention may contain the active substances mentioned in the usual dosages. Due to the mentioned synergistic effect, the dosage of each active ingredient of the active ingredient combination contained in the medicaments according to the invention can be chosen lower than the dosage which is customary for a single preparation of the respective active ingredient.
  • the active compound combinations and medicaments according to the invention can be used not only in the field of human medicine but also in the field of veterinary medicine for the treatment of allergic symptoms of the skin or mucous membrane.
  • Example 1 Gel or Cream 2% by weight Bamipin
  • the gel or the cream is used for the treatment of allergic skin diseases, in particular of itchy skin diseases (eg urticaria).
  • the gel or cream is applied once or several times daily to the affected skin and massaged into the skin.
  • Example 2 Gel or cream 0.04% by weight of clemastine fumarate 5% by weight of dexpanthenol Excipients: carbomer, propylene glycol, polyol fatty acid ester.
  • the gel or the cream is used for the treatment of allergic skin diseases, in particular of itchy skin diseases.
  • the application is carried out as in Example 1.
  • Example 3 Cream 1.5% by weight chlorphenoxamine-HCl
  • Macrogol fatty acid ester Macrogol fatty acid ester.
  • the cream is used for the treatment of allergic skin diseases, in particular itchy skin diseases.
  • the application is carried out as in Example 1.
  • Excipients purified water, benzalkonium chloride, disodium EDTA.
  • the spray volume is 0.14 ml, corresponding to a single dose of 0.14 mg azelastine HCl per spray.
  • the nasal spray is used to treat allergic rhinitis.
  • one spray is injected into each nostril 1 to 3 times a day.
  • Example 5 Nasal spray (dosing spray) or solution 3.1% by weight of cromolyn sodium, disodium salt 5% by weight of dexpanthenol
  • Excipients purified water, benzalkonium chloride, disodium EDTA.
  • the spray volume is 0.09 ml, corresponding to a single dose of 2.8 mg cromolyn sodium per spray. If the chosen spray volume is 0.14 ml (as in Example 4), the concentration of active compound is optionally adjusted accordingly (2 wt .-%) to obtain the specified single dose of 2.8 mg cromolyn sodium per spray.
  • the nasal spray is used to treat allergic rhinitis.
  • one spray is injected into each nostril 1 to 5 times a day.
  • Example 6 cream or ointment for dermal application 0.5% by weight hydrocortisone
  • Cream white vaseline, isopropyl myristate, sorbitan monolaurate, propylene glycol, disodium
  • EDTA purified water.
  • Ointment white vaseline, purified water, propylene glycol, liquid paraffin, wool wax.
  • the cream or ointment is used for the treatment of allergic skin diseases (eg eczema, in particular contact dermatitis, atopic dermatitis, dermatitis, urticaria, skin dermatoses).
  • allergic skin diseases eg eczema, in particular contact dermatitis, atopic dermatitis, dermatitis, urticaria, skin dermatoses.
  • the cream or ointment is applied once or several times daily to the affected areas of the skin and rubbed in lightly.
  • Example 7 Solution for dermal application 1% by weight of hydrocortisone 10% by weight of dexpanthenol Excipients: purified water, isopropyl alcohol, preservative (methyl 4-hydroxybenzoate, propyl 4-hydroxybenzoate). Use and application: as in example 6.
  • Example 8 Suspension for dermal or nasal application 0.05% by weight of beclomethasone 17.21-dipropionate 5% by weight of dexpanthenol
  • Excipients purified water, benzalkonium chloride, anhydrous glucose, phenylethyl alcohol, polysorbate 80.
  • the suspension described above can also be formulated as a pump spray, for example for use as a nasal spray.
  • the suspension or spray is used for the prevention or treatment of allergic rhinitis.
  • one spray (0.09 ml) is sprayed into each nostril 2 to 5 times daily.
  • the dosing aerosol is used to treat allergic dermatitis or allergic dermatitis.
  • the aerosol is sprayed 2 to more times daily on the affected skin.
  • the nose ointment is used to treat allergic rhinitis.
  • an approximately pea-sized amount is introduced into each nostril and distributed by massaging from the outside.
  • Example 11 Nasal spray (dosing spray) or solution 3.5% by weight of dexpanthenol
  • the nasal spray is used for the treatment of allergic rhinitis and / or allergic rhinitis and is contemporaneous or delayed with other preparations containing at least one anti-allergic drug from the group of antihistamines, corticosteroids, synthetic mast cell degranulation inhibitors and / or leukotriene receptor anatagonists to apply.
  • one spray is sprayed into each nostril 1 to 5 times a day.
  • Example 11 The effect of a dexpanthenol nasal spray from Example 11 containing 3.5% dexpanthenol was tested on five patients suffering from diagnosed hay fever (grass pollinosis).
  • the observed symptoms such as runny or stuffy nose, sneezing, watery eyes, red and inflamed skin in and around the nose were classified as moderate to severe (depending on the time interval to taking the medication).
  • Example 11 Patients were encouraged to use the dexpanthenol nasal spray of Example 11 in situations in which they were exposed to high doses of an allergen (e.g., when crossing a field of flowering grasses) in addition to their ingested antiallergic medication. About two to three applications were reported.
  • an allergen e.g., when crossing a field of flowering grasses
  • dexpanthenol moisturizes the epidermis and mucosa, reducing side effects such as dryness of the nose or nosebleeds, which often occur during the application of antiallergic drugs or antihistamines, and thus improves it

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Abstract

L'invention concerne des combinaisons contenant au moins un principe actif du groupe contenant des acides de pantothène ou des dérivés d'acide de pantothène, en particulier du dexpanthenol, et au moins un principe actif anti-allergique, pour traiter les symptomes allergiques de la peau ou des muqueuses, des médicaments les contenant et leur procédé de fabrication.
PCT/EP2008/004567 2007-06-08 2008-06-07 Médicaments contenant une combinaison de principes actifs pour traiter les symptomes allergiques Ceased WO2008148573A2 (fr)

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Application Number Priority Date Filing Date Title
RU2009148577/15A RU2472499C2 (ru) 2007-06-08 2008-06-07 Лекарственное средство, включающее комбинацию активных веществ, содержащую пантотеновую кислоту или ее производные, для лечения аллергических симптомов
EP08773373A EP2164481A2 (fr) 2007-06-08 2008-06-07 Medicament comprenant une combinaison de principes actifs contenant de l'acide pantothenique ou des derives de celui-ci pour traiter les symptomes allergiques
BRPI0812750-6A2A BRPI0812750A2 (pt) 2007-06-08 2008-06-07 Medicamento compreendendo uma combinação de substância ativa para tratamento de sintomas de alergia

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EP07011305 2007-06-08
EP07011305.5 2007-06-08

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JP2010260808A (ja) * 2009-05-01 2010-11-18 Ikeda Mohando:Kk 肌状態改善用経口医薬組成物
WO2018015593A1 (fr) * 2016-07-07 2018-01-25 Diater Laboratorio De Diagnóstico Y Aplicaciones Terapéuticas, S.A. Compositions d'acide cromoglicique pour le traitement de la dermatite
CN111388673A (zh) * 2020-03-22 2020-07-10 华中科技大学同济医学院附属协和医院 一种抗过敏外用凝胶膜及其制备方法
US11224619B2 (en) * 2012-04-16 2022-01-18 Zemtsov Enterprises, Llc Formulations and methods for treatment of inflammatory skin diseases
US20220040203A1 (en) * 2014-08-08 2022-02-10 Shenzhen Hightide Biopharmaceutical, Ltd. Liquid formulation compositions, medicament delivery devices, and methods of preparation and use thereof
EP4566595A1 (fr) * 2023-12-07 2025-06-11 Bernhard Roth Preparation combinee pour le traitement de la rhinosinusite aigue et chronique

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RU2605617C1 (ru) * 2015-06-25 2016-12-27 государственное автономное научное учреждение "Институт стратегических исследований Республики Башкортостан " Композиция для назального средства
RU2646494C1 (ru) * 2017-07-05 2018-03-05 Общество с ограниченной ответственностью "НАТУРА СИБЕРИКА" (сокращенно ООО "НАТУРА СИБЕРИКА") Косметическая композиция против воспалений на коже для использования в составе косметических средств
UA122811C2 (uk) 2018-08-10 2021-01-06 Наталія Миколаївна Тихонівська Фармацевтична композиція

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US20040247686A1 (en) * 2003-04-04 2004-12-09 Boehringer Ingelheim International Gmbh Pharmaceutical compositions comprising epinastine for the treatment of skin diseases
JP5021155B2 (ja) * 2003-08-01 2012-09-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング エピナスチンと１種以上のさらなる抗−ｈ１−ヒスタミン類との組合せを含む皮膚疾患治療用製薬組成物

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JP2010260808A (ja) * 2009-05-01 2010-11-18 Ikeda Mohando:Kk 肌状態改善用経口医薬組成物
US11224619B2 (en) * 2012-04-16 2022-01-18 Zemtsov Enterprises, Llc Formulations and methods for treatment of inflammatory skin diseases
US20220040203A1 (en) * 2014-08-08 2022-02-10 Shenzhen Hightide Biopharmaceutical, Ltd. Liquid formulation compositions, medicament delivery devices, and methods of preparation and use thereof
US11559531B2 (en) * 2014-08-08 2023-01-24 Shenzhen Hightide Biopharmaceutical, Ltd. Liquid formulation compositions, medicament delivery devices, and methods of preparation and use thereof
WO2018015593A1 (fr) * 2016-07-07 2018-01-25 Diater Laboratorio De Diagnóstico Y Aplicaciones Terapéuticas, S.A. Compositions d'acide cromoglicique pour le traitement de la dermatite
CN109715153A (zh) * 2016-07-07 2019-05-03 迪亚特实验室诊断和治疗应用公司 用于治疗皮炎的包含色甘酸的组合物
RU2754006C2 (ru) * 2016-07-07 2021-08-25 Нутра Эссеншиал Отк, С.Л. Композиции, содержащие кромоглициевую кислоту, для лечения дерматита
CN111388673A (zh) * 2020-03-22 2020-07-10 华中科技大学同济医学院附属协和医院 一种抗过敏外用凝胶膜及其制备方法
EP4566595A1 (fr) * 2023-12-07 2025-06-11 Bernhard Roth Preparation combinee pour le traitement de la rhinosinusite aigue et chronique
WO2025119815A1 (fr) * 2023-12-07 2025-06-12 Bernhard Roth Préparation combinée pour le traitement de rhinosinusite aiguë et chronique et/ou de rhinite allergique

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RU2472499C2 (ru) 2013-01-20
RU2009148577A (ru) 2011-07-20
EP2164481A2 (fr) 2010-03-24
WO2008148573A3 (fr) 2009-05-07
BRPI0812750A2 (pt) 2014-12-23

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