Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1995-09-14
1997-07-15
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514772, 514943, A61K 706
Patent
active
056483945
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/US93/05068 filed May 27, 1993.
BACKGROUND OF THE INVENTION
This invention relates to a new topical composition for inhibiting mammalian hair growth. It also relates to a method of inhibiting hair growth by applying a topical composition according to this invention to the skin.
In U.S. Pat. No. 4,720,489 it is disclosed that the topical application of a composition comprising an ornithine decarboxylase ("ODC") inhibitor will inhibit hair growth, including beard hair growth. A particularly advantageous ODC inhibitor for use in this application is 2-(difluoromethyl)-2,5-diaminopentanoic acid, also identified as .alpha.-(difluoromethyl)ornithine ("DFMO"). This patent demonstrates the effectiveness of ODC inhibitors for inhibiting hair growth by measuring changes in flank organ hair mass in adult male hamsters treated with ethanol solutions of such compounds. The patent also generally proposes the possible incorporation of ODC inhibitors in cosmetic formulations such as skin lotions and creams, but the effectiveness of such proposed formulations and their stability and aesthetic attributes are unknown. Since DFMO is a highly ionic material, it would tend to destabilize emulsion systems and would be difficult to formulate in such systems, particularly at higher dosage levels necessary to achieve maximum efficacy.
In U.S. Pat. No. 5,095,007, U.S. Pat. No. 5,096,911, and U.S. Pat. No. 5,132,293, additional hair growth inhibitors are disclosed which are completely unrelated to the aforementioned ODC inhibitors. However, each of these patents discloses a water-ethanol vehicle for delivering the active compound. The vehicle comprises 68% water, 16% ethanol, 5% propylene glycol, 5% dipropylene glycol, 4% benzyl alcohol, and 2% propylene carbonate. This vehicle is not aesthetically pleasing or easy to use since it is very runny and feels wet and tacky. Moreover, the efficacy of the active material in this vehicle may not be optimum even though the vehicle contains two known penetration enhancers, namely benzyl alcohol and propylene carbonate.
It is an object of the present invention to provide a topical composition for inhibiting hair growth which is stable, highly efficacious and aesthetically pleasing.
SUMMARY OF THE INVENTION
The present invention embraces a topical composition for inhibiting mammalian hair growth, particularly human beard hair growth (including hirsutism), comprising a water-soluble, hair-growth-inhibiting agent dispersed in an oil-in-water emulsion in the form of a lotion or cream. The invention also embraces a method of inhibiting mammalian hair growth by applying an effective amount of the above composition to the skin. The invention further embraces a topical composition for delivering a water-soluble, pharmacological agent to the skin.
DETAILED DESCRIPTION OF THE INVENTION
The hair growth inhibiting agent which is utilized in the composition and method of the present invention may be any water-soluble, hair-growth-inhibiting agent, particularly any highly ionic, water-soluble, hair-growth-inhibiting agent. Such active agents may be selected from any of the classes of agents described in the aforementioned U.S. patents, namely U.S. Pat. No. 4,720,489, U.S. Pat. No. 5,095,007, U.S. Pat. No. 5,096,911, and U.S. Pat. No. 5,132,293, provided such agents are water soluble. In a preferred embodiment, the hair growth inhibiting agent is 2-(difluoromethyl)-2,5-diaminopentanoic acid, which is also identified as .alpha.-(difluoromethyl)ornithine, hereinafter abbreviated "DFMO".
The topical composition of the present invention comprises about 1 to 20 parts by weight, preferably 5 to 15 parts, of the aforedescribed water-soluble, hair-growth-inhibiting agent, particularly DFMO, dispersed in 99 to 80 parts by weight, preferably 95 to 85 parts, of a vehicle comprising an oil-in-water emulsion of the formula (the last two ingredients being optional):
______________________________________ Ingredient Wt. Percent Ex. I Ex. II
______________________________________
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Ahluwalia Gurpreet S.
Amery Geoffrey Wilfred
Boxall Brian Alfred
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