Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1996-10-31
1998-09-29
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424435, 424443, 424430, 5147723, A61F 1300
Patent
active
058143300
DESCRIPTION:
BRIEF SUMMARY
CROSS REFERENCE TO RELATED APPLICATIONS
This application is based upon PCT Application Ser. No. PCT/EP 95/01760, filed May 10, 1995, which claims priority from European Patent Application Ser. No. 94.201.402.8, filed on May 18, 1994.
The development of an efficacious and readily manageable composition for vaginal use requires a satisfactory adhesion of the composition to the mucous membranes of the vagina in order to prevent the excretion of the product. A vaginal composition, therefore, should preferably show adequate mucoadhesive properties. The gels, foams, creams, suppositories and tablets that are presently used in the treatment of vaginal afflictions break down very rapidly after insertion into the vaginal cavity and have insufficient bioadherence to the vaginal walls. Hence, an unpleasant leakage is often experienced after administration and the effectivity of these products is limited. The present invention solves the problem by furnishing a mucoadhesive emulsion which comprises between 10% and 70% by weight of a cyclodextrin.
In particular, the present invention is concerned with the use of a cyclodextrin or a derivative thereof as a mucoadhesive in an emulsion or aqueous solution, said cyclodextrin or derivative thereof being used in an amount from 10% to 70% by weight based on the total weight of the composition. The subject mucoadhesive compositions may be applied to the mucous membranes of, for example, the nose, mouth and in particular of the vagina. Preferably, the composition comprises a drug such as, for example, an antibacterial, an antiviral, an anticonceptive or, in particular, an antifungal. Antifungals that may be included in the subject compositions are, for example, miconazole, clotrimazole, ketoconazole, terconazole, econazole, butoconazole, fluconazole, and, preferably, itraconazole.
A further aspect of the invention relates to mucoadhesive emulsions comprising itraconazole and a cyclodextrin or a derivative thereof in an amount between 10% and 70% by weight based on the total weight of the composition. Optionally, the subject compositions may comprise, apart from the cyclodextrin, further constituents having mucoadhesive properties.
Itraconazole is a broadspectrum antifungal compound and is disclosed in U.S. Pat. No. 4,267,179. In addition to their favourable mucoadhesive properties, the itraconazole compositions of the present invention show a further advantage in that cure rates in vaginal afflictions are higher and relapse rates are lower when compared to commercially available, antifungal compositions. Moreover, the present itraconazole compositions have an excellent physicochemical stability.
Itraconazole is the generic name of oxolan-4-yl!methoxy!phenyl!-1-piperazinyl!phenyl!-2,4dihydro-2-(1-methylpro pyl)-3H-1,2,4-triazol-3-one. The term "itraconazole" as used herein comprises the free base form, the pharmaceutically acceptable addition salts, the stereochemically isomeric forms thereof and the tautomeric forms thereof. The preferred itraconazole compound is the (.+-.)-(cis) form of the free base form.
The acid addition forms may be obtained by reaction of the base form with an appropriate acid. Appropriate acids comprise, for example, inorganic acids such as hydrohalic acids, e.g. hydrochloric or hydrobromic acid; sulfuric acid; nitric acid; phosphoric acid and the like; or organic acids such as, for example, acetic, propanoic, hydroxyacetic, 2-hydroxypropanoic, 2-oxopropanoic, ethanedioic, propanedioic, butanedioic, (Z)-butenedioic, (E)-butenedioic, 2-hydroxybutanedioic, 2,3-dihydroxybutanedioic, 2-hydroxy-1,2,3-propanetricarboxylic, methanesulfonic, ethanesulfonic, benzenesulfonic, 4-methylbenzenesulfonic, cyclohexanesulfamic, 2-hydroxybenzoic, 4-amino-2-hydroxybenzoic and the like acids. The term addition salt as used hereinabove also comprises the solvates. Said solvates are meant to be included within the scope of the present invention. Examples of such solvates are, e.g. the hydrates, alcoholates and the like.
The formation of an addition salt of the drug may be ad
REFERENCES:
patent: 5055303 (1991-10-01), Riley, Jr.
patent: 5324718 (1994-06-01), Loftsson
patent: 5472704 (1995-12-01), Santus
Fran.cedilla.ois Marc Karel Jozef
Putteman Peter
Snoeckx Eric Carolus Leonarda
Ciambrone Coletti Ellen
Faulkner D.
Janssen Pharmaceutica N.V.
Page Thurman K.
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