ANHYDROUS ANTIPERSPIRANT COMPOSITION

FIELD OF INVENTION

This invention relateLS to a composition particularly suitable for treating localized hyperhidrosis.

BACKGROUND OF THE INVENTION

Control of excessive perspiration by use of a topical formulation has long been a medical and social goal. Excessive sweating accounts for intertrigo, infection, dermatitis, and friction blisters of wet soles. It also results in disability for typing and writing due to dripping palms, being handicapped in sporting events from facial sweat, and having a compromised grip on baseball bats, tennis racquets, and basketballs. On the social side, hyperhidrosis induces the embarrassment of wet armpit clothing, gustatory sweating and auriculotemporal facial sweating (Frey's syndrome), and varied patches of nevoid localized sweating. All intertriginous areas, including fat folds and toe-webs, are susceptible to harm by unevaporated trapped sweat which induces maceration and leads to secondary bacterial and fungal infections. Add to this the cost of dry cleaning clothing and shoe replacement. Total localized control of sweating by topical means has thus been a long term medical objective.

The first commercial antiperspirant was introduced approximately 100 years ago. It was an aqueous-alcoholic solution of aluminum chloride hexahydrate with an effectiveness now estimated to be 60-70%. Through the century, the effectiveness of commercial antiperspirants has dropped to the 30-55% range due to the industry replacing aluminum chloride hexahydrate with weaker, more alkaline, less irritating salts of aluminum. Indeed, today the FDA approves the label "antiperspirant" for any product that reduces axillary sweating by 20% in 50% of users — and no product can be labeled "stops sweating" (Laden K., Ed., Antiperspirants and Deodorants 2 ^nd Edition, 1999).

Numerous commercial over-the-counter and prescription products are useful for controlling excessive sweating in localized areas such as the axilla. Nearly all

depend on the well-known antiperspirant action of aluminum chloride hydrate and its cognate derivatives, including the fellow metallic antiperspirant zirconium salts.

SUMMARY OF THE INVENTION The present invention provides an effective alternative antiperspirant that contains no aluminum or zirconium salts. This invention controls hyperhidrosis topically by the application of a unique and safe chemical - calcium sulfate hemihydrate - in an anhydrous system.

DESCRIPTION OF INVENTION

The present invention embodies the hither-to unrecognized antiperspirant effect of topical calcium sulfate hemihydrate in an anhydrous system.

Calcium sulfate hemihydrate, CaSO4-l/2 H2O or (CaSO4)2-H2O, which has a formula weight of 145.15, is a white compound. It has the unique property of reacting with sweat, i.e. water, to form a hard crystalline film of the dihydrate of calcium sulfate in an exothermic reaction. This focal reaction specifically occludes the sweat pores, thereby counteracting hyperhidrosis. The formulations of calcium sulfate hemihydrate are sensitive to water, and hence must be anhydrous and protected from excessive atmospheric water vapor.

Calcium sulfate hemihydrate is available commercially as a fine white hygroscopic powder kept in closed containers. In an illustrative embodiment of the invention, this antiperspirant agent is applied directly as a powder or from a compacted stick. Alternately, it is applied as an impalpable powder from 5 to 25 micron incorporated into an anhydrous carrier vehicle. The formulation preferably should be dispensed in a sealed container or applicator, but other means of dispensing and application are within the spirit and scope of the invention.

The calcium sulfate hemihydrate may be applied directly as a powder from a powder container or an aerosol unit with appropriate protective shield to guard against inhalation. Alternatively, it may be made into a stick applicator, consisting of

compacted powder with or without an excipient to prevent crumbling. The stick is preferably oval, measuring, for example, 1.5 inches by 0.75 inches. It may be dispensed in a standard plastic holder with a knurled screw at the base for advancement.

In another embodiment of the invention, the calcium sulfate hemihydrate is incorporated by trituration into any of a number of anhydrous vehicles. The carrier vehicle is anhydrous castor oil from which trace water has been eliminated by the addition of molecular sieve 3 A, either in powder or granular form.

Other satisfactory vehicles include anhydrous ethyl alcohol, dehydrated castor oil (Castung R 103 G-H) or safflower oil. Glycerol, petroleum and aqueous agents are not satisfactory. The calcium sulfate hemihydrate is preferably triturated into a paste, cream, or suspension, wherein the ratio of antiperspirant agent to vehicle is 1 :1 on a weight/volume basis, although it can be varied from a ratio as high as 1.5:1 or as low as 1:10. Calcium sulfate hemihydrate is insoluble in all common solvents. The only solubilizer is tetrahydrofuran, a compound too toxic for human use.

In the manufacture of the invention a dry atmosphere is preferable since calcium sulfate hemihydrate is hygroscopic and thereby converted to inactive calcium sulfate dihydrate.

The compacted stick can be molded by appropriate compression machinery. A powder processor (Micronizer R. Jet Mill Sturdevant, Hanover, MA) may be used to grind the active ingredient to a particle size of 3 to 35 micron, ideally about 5 micron. The powder is added in a homogenizer to the selected vehicle, all operations being carried out in ambient dry air or water-free nitrogen gas. As desired, pigments, fragrance, and necessary modifiers, as for example cyclomethicones, may be added.

The product may be packaged in an applicator appropriate for a cream, paste, gel, suspension, or stick. When the formulation is liquid the standard roll-on unit is satisfactory. The pure stick formulation has the advantage of simplicity and ease of use.

In a further embodiment of the invention, emulsifϊers, structurants or a combination thereof are added to the composition to form a cream or gel.

The anhydrous antiperspirant composition of the invention may be applied topically to the axillae, intertriginous areas, forehead, palms, and soles in amounts covering the skin site in question.

The compositions act specifically on the sweat pore when applied to dry skin. The are activated by sweat.

Formulation Example I

Calcium sulfate hemihydrate 30.0 grams 5 micron powder

Castor Oil USP 30 ml

Formulation Example II

Calcium sulfate hemihydrate 30 grams Ethyl alcohol, absolute 30 ml

Dispense in Roll On and shake before use

Formulation Example III Calcium sulfate hemihydrate 30 grams

Dehydrated Castor Oil 30 ml

Formulation Example IV Calcium sulfate hemihydrate Compressed in stick mold shape. Active powder released by friction of application.

While the invention has been described by illustrative embodiments, additional advantages and modifications will occur to those skilled in the art. Therefore,

the invention in its broader aspects is not limited to specific details shown and described herein. Modifications, for example, to the relative concentrations and types of components may be made without departing from the spirit and scope of the invention. Accordingly, it is intended that the invention not be limited to the specific illustrative embodiments, but be interpreted within the full spirit and scope of the appended claims and their equivalents.