Macrochem Corporation

The Kendall Company

Bristol-myers Company

Other

Colgate Palmolive Company

Boston University

Westwood Pharmaceuticals, Inc.

Carlos M Samour

Julius A Vida

Scott F Krauser

Mildred C Richards

Robert J Gyurik

Stefanos Daskalakis

Samuel J Thomas

Solomon R Eisenberg

James R Marshall

Earl G Jackson

Louie E Davidson

Lawrence G Raisz

A nail lacquer for the treatment or prevention of fungal infections, such as, onychomycosis, includes fungicidally effective amount of ciclopirox, econazole, or other antifungal agent in a compatible film-forming lacquer vehicle which includes a water-insoluble film-forming polymer; pentadecalactone, or similar cyclic lactone compound or derivative thereof, and volatile solvent. The pentadecalactone functions as a plasticizer for the film-forming polymer and as a penetration enhancer for the antifungal agent. The composition, when applied to the nails provides a hard, clear, water-resistant film containing the antifungal agent. The compositions are used for the treatment of onychomycosis.

Antifungal nail lacquer and method using same

A nail lacquer effective for the treatment or prevention of fungal infections, such as, onychomycosis, includes fungicidally effective amount of ciclopirox, econazole, or other antifungal agent in a clear, stable, film-forming lacquer vehicle which includes a water-insoluble film-forming polymer; 2-n-nonyl-1,3-dioxolane or similar penetration enhancer; and volatile solvent. A plasticizer for the film-forming polymer which is also compatible with the other components may be included although the preferred penetration enhancers may also function as plasticizer. The composition, when applied to the nails provides a hard, clear, water-resistant film containing the antifungal agent. The film is resistant to multiple washings and is effective in the treatment of onychomycosis.

Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.

Non-steroidal antiinflammtory drug formulations for topical application

Topical alcoholic or aqueous alcoholic gels containing testosterone, progesterone, estradiol or other hormones have enhanced penetration through skin by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound.

Hormone replacement therapy drug formulations for topical application to

A composition for the topical transdermal administration to the penis is based on prostaglandin E.sub.1. The composition is non-irritating and effective for relieving erectile impotence or other penile erectile dysfunction. A penetration enhancing effective amount of a dioxolane, dioxane, or acetal skin penetration enhancing compound in a pharmaceutically acceptable aqueous alcoholic carrier is used to facilitate the penetration of the prostaglandin E.sub.1 active ingredient through the skin. Phentolamine or prazosin may be used in combination with prostaglandin E.sub.1.

Composition and method for treating penile erectile dysfunction

Lipophilic and amphiphilic or hydrophilic film-forming polymer

A mixture of lipophilic and amphiphilic/hydrophilic film-forming polymers of the formula (I)

Cationic film-forming polymer compositions, and use thereof in topical

The combination of minoxidil and 2-n-nonyl-1,3-dioxolane is effective in promoting hair growth when applied once daily.

Method for treating hair loss

New and improved method for the transdermal administration of agents is provided utilizing iontophoresis in conjunction with a water-insoluble, stratum corneum-lipid modifier. The lipid modifier may be used prior to iontophoresis or simultaneously therewith. The lipid modifier may be selected from a wide variety of moieties of the general formula R--X where R is a C.sub.5 to C.sub.28 alkyl or unsaturated alkyl and X is a member of the following: 1,3-dioxane; 1,3-dioxolane; lactam; morpholine; --COOH; --OH; --COOR'; --C--N(R').sub.2 ; cyclo ethylene and propylene carbonates; --CONH.sub.2 ; --(CH.sub.2 --CH.sub.2 O).sub.n H; ##STR1## acetals, and hemiacetals; and wherein R' is lower alkyl (e.g., C.sub.1 to C.sub.3) and n is an integer of from 1 to 20. Optionally there may be present a polar, water-soluble chemical compound from the group of alcohols, glycols, lactams, dioxolanes, esters, ureas, morpholine and the like. Compositions and articles useful in the processes of the present invention are also provided.

Process for transport of agents across the skin and compositions and

Malignancy-induced hypercalcemia is treated with thionapthene-2-carboxylic acid (TNCA) and the pharmaceutically acceptable salts thereof. The treatment is also effective in tumor bearing hosts even before there is significant abnormal serum calcium levels. There is no 'escape' from the hypocalcemic effects of these compounds as with e.g., calcitonin. The useful dosage in humans for TNCA itself ranges from about 1 to about 60 mg/kg/day preferably from about 2 to about 30 mg/kg/day and more preferably from about 5 to about 20 mg/kg/day (20 mg is approximately 0.106 mmol) Orally administered TNCA or salts thereof, is a much desired and obviously clinically advantageous mode of administering compounds to control or ameliorate hypercalcemia.

Method for treating hypercalcemia using salts of TNCA

Lysine and arginine salts of thionaphthene-2-carboxylic acid (TNCA) are disclosed. These compounds are useful as treatments for osteoporosis and exhibit an increased water solubility.

Water soluble salts of thionaphthene-2-carboxylic acid

A transdermal medication device for applying medication on the skin of the user comprising upper and lower layers having cooperating filaments for detachably securing the upper layer to the lower layer. The lower layer has an opening therethrough, the upper layer carrying a medication reservoir which seats in the opening. In one form of the invention, the device is a patch attached by pressure-sensitive adhesive to the skin. In another form of the invention, the lower layer is a band for attaching the device about the chest, waist, arm or leg of the user.

Transdermal medicator

Novel 1,3-dioxolanes (1,3-dioxyacyclopentanes) are provided along with new 1,3-dioxolanes (1,3-dioxacyclopentanes) compositions which are useful in enhancing the absorption of therapeutic agents through the skin of humans and animals. The method for enhancing skin penetration of therapeutic agents using 1,3-dioxacycloalkanes is also described. The preferred compounds are 1,3-dioxolanes (1,3-dioxacyclopentanes) and 1,3-dioxanes (1,3-dioxacyclohexanes). The preferred compounds have the formula: ##STR1## wherein R, R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently selected from hydrogen and C.sub.1 to C.sub.18 aliphatic groups, preferably alkyl, alkenyl, and the halo, hydroxy, carboxy, carboxamide and carboalkoxy substituted forms thereof, with at least one of said R's an alkyl or alkenyl group of C.sub.4 to C.sub.18 and n=0 or 1; the total number of carbon atoms in all of said R groups being no more than 40, and preferably less than 20 and not more than 1 thereof containing 18 or more carbon atoms.

Percutaneous absorption enhancers, compositions containing same and

Various derivatives of barbituric acid and of diphenylhydantoin are described in which alkoxymethyl or benzyloxymethyl groups are attached to the nitrogen atoms of the rings. Therapeutic compositions containing these compounds and their use as anti-convulsant agents are described.

Growing community of inventors

Wellesley, MA, United States of America

Carlos M Samour