Other

Cellegy Pharmaceuticals Inc.

University of California

Dermatologic Research Corporation

Carl R Thornfeldt

Peter Michael Elias

Stephen Grayson

Kenneth R Feingold

Walter M Holleran

Robert E Thornfeldt

This invention provides compositions and methods for treatment of skin and mucous membranes suffering from a follicular dermatosis. The compositions include one or more pyridine-thiols and tautomers with attached metallic moieties. Administration of the compounds to aging skin and mucous membranes in topical formulations, either as the only active ingredient or in combination with other known active ingredients to treat a follicular dermatosis. Additional compositions for treating follicular dermatosis contain one or more sulfides and oxides of these same metallic ions, either alone or in combination with other molecules. Topical formulations containing both a pyridine-thiol and tautomers with attached metallic moiety and a metallic sulfide and/or metallic oxide effectively treat skin and mucous membranes suffering from a follicular dermatosis.

Pyridine-thiols for treatment of a follicular dermatosis

A method for disrupting epithelial barrier function in a host in need of the topical administration of a physiologically active substance which comprises applying to the epithelium of the host, barrier-disrupting amount of at least one agent selected from the group consisting of an inhibitor of ceramide synthesis, inhibitor of acylceramide synthesis, inhibitor of glucosylceramide synthesis, and inhibitor of sphingomyelin synthesis, an inhibitor of fatty acid synthesis, an inhibitor of cholesterol synthesis, a degradation enzyme of ceramides, acylceramide, glucosylceramides, sphingomyelin, an inhibitor of phospholipid, glycosphingolipid, including glucosylceramide, acylceramide or sphingomyelin degradation, and both inhibitors and stimulators of metabolic enzymes of free fatty acids, ceramide, and cholesterol, as well as a topical composition useful therefore are disclosed.

Method and compositions for disrupting the epithelial barrier function

This invention provides compositions and methods for preventing and reversing the signs and symptoms of intrinsic and photo aging. The compositions include one or more pyridine-thiols and tautomers with attached metallic moieties. Administration of the compounds to aging skin and mucous membranes in topical formulations, either as the only active ingredient or in combination with other known active ingredients, prevents and reverses aging symptoms. Additional compositions for preventing and reversing aging contain one or more sulfides and oxides of these same metallic ions, either alone or in combination with other molecules known or suspected to exhibit age reversing properties. Topical formulations containing both a pyridine-thiol and tautomers with attached metallic moiety and a metallic sulfide and/or metallic oxide effectively prevent and reverse the signs and symptoms of mucocutaneous aging.

Pyridine-thiols reverse mucocutaneous aging

The permeation of a therapeutic agent through the epithelium by topical administration is enhanced by the further topical administration of a stearylamine, transvaccenic acid or a combination of a stearylamine and transvaccenic acid.

Methods for enhancing permeation of a topically administered

A method for enhancing penetration of a therapeutic or prophylactic agent in a host in need of the topical administration thereof which comprises applying to the epithelium of the host, an effective amount of one or more penetration enhancing epithelial sterols and the therapeutic or prophylactic agent.

Methods for inducing phase separation of epithelial lipid bilayers

The epidermal permeability barrier to systemically and/or topically active agents or compositions designed for topical administration is enhanced to an unexpected degree by certain combinations of known penetration enhancing excipients. One group of combinations comprise a glycol and an alcohol at a weight ratio within the range of 1:0.1 to 1:10 with one or more further additives, selected from the excipient groups of branched-chain esters of fatty acids, surfactants, and membrane fluidizers. Another group of combinations comprise an alcohol of four or more carbon atoms and one or more further additives selected from the excipient groups of glycols and surfactants.

Potent penetration enhancers

A method for enhancing penetration of a therapeutic or prophylactic agent in a host in need of the topical administration thereof which comprises applying to the epithelium of the host, the agent and an effective amount of one or more penetration enhancing epithelial proton pump inhibitors.

Penetration enhancing compositions and methods of their use

Lipids for epidermal moisturization and repair of barrier function

The topical administration of therapeutic agents to a variety of disease conditions, both cutaneous and systemic, is enhanced by combining the therapeutic agents with dicarboxylic acids or analogs of such acids, which include mono- and dimercapto derivatives, salts, esters, amides and anhydrides. Preferred dicarboxylic acids are azelaic and dodecanedioic acids and their monoglyceride and sucrose salts. Preferred therapeutic agents are antiinflammatory compounds, antihistamine compounds, antineoplastic compounds, vitamin D and retinoid agents. Specific examples of some of these compounds are 5-fluorouracil, methotrexate, bleomycin, carmustine and nitrogen mustard. The acids and analogs of this invention enhance the penetration capabilities of the therapeutic agents and are thus effective in promoting the therapeutic effect of these agents inside diseased cells, particularly for diseases such as inflammatory skin diseases and premalignant and non-melanoma malignant skin tumors.

Administration of skin medications by use of dicarboxylic acids and

Noninfectious inflammatory and hyperpigmentation skin diseases, thermal injuries and premalignant skin tumors induced by radiation or virus, in both humans and animals, are treated with topical formulations of an ester or amide of a monocarboxylic acid, the acid moiety of which is 9 to 18 carbon atoms.

Treatment of skin diseases and tumors with esters and amides of

Hemorrhoids and viral-induced skin tumors such as warts and molluscum contagiosum are successfully treated with topical administration of artemisinin, dihydroartemisinin, its semisynthetic derivatives and its synthetic analogs.

Treatment of viral tumors and hemorrhoids with artemisinin and

Certain compounds having sesquiterpene structures, when combined with monocarboxylic fatty acids, esters or amides, have efficacy in the treatment of papulosquamous and eczematous diseases. Prime examples of the sesquiterpene compounds are artemisinin and analogs, and prime examples of the monocarboxylic fatty acid compounds are lauric acid, monolaurin and lauryl-N,N-dimethylamide.

Methods for treatment of papulosquamous and eczematous diseases

This invention relates to a new topical pharmaceutical composition for the treatment of pruritis, especially psychogenic and senile types, that contains esters and amides of 5 to 19 carbon atom length monocarboxylic acids. These esters and amides are formulated alone or with other known topical antipruritic agents, such as amine and 'Caine' anesthetics, alcohols, ketones, antihistamines, corticosteroids, counterirritants, and any combination of these.

Treatment of pruritis with esters and amides

Psoriasis, ultraviolet light induced skin conditions and tumors are successfully treated with topical or oral administration of artemisinin, dihydroartemisinin, its semisynthetic derivatives and its synthetic analogs. Viral tumors/diseases, hemorrhoids, and bullous skin diseases are also successfully treated with these topical compositions.

Treatment of skin diseases with artemisinin and derivatives

Teething and colic are alleviated in infants and toddlers by the administration of a combination of an antihistamine and a benzodiazepine having sedative hypnotic activity. An exemplary antihistamine is hydroxyzine pamoate, and an exemplary benzodiazepine is diazepam.

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Ontario, OR, United States of America

Carl R Thornfeldt