Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from palmaceae
Reexamination Certificate
2000-05-03
2002-03-19
Weber, Jon P. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from palmaceae
C424S074000, C424S070100, C424S725000
Reexamination Certificate
active
06358541
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to an improved preparation and method for treating androgenetic alopecia; and more particularly to a preparation comprising an active extract of saw palmetto berries and a compound which exhibits low irritability and enhances penetration of the extract into hair follicular pores.
2. Description of the Prior Art
Human hair undergoes a normal growth cycle, known as the pilar cycle where each hair grows continuously for about 2 to 4 years, stops growing for 2 to 4 months, and then falls out. In its place, healthy new hair begins to grow, thereby restarting the cycle. Androgen receptors located in the hair follicle and sebaceous gland sensitize hair follicles to androgens. There is evidence that the pilar cycle of hair follicles on the scalp respond to higher levels of androgens by displaying shortened growth phases, and by displaying a greater fraction of increasingly thinner and shorter hairs.
Saw palmetto (serenoa repens) is a small berry-bearing palm native to the southeast United States. Saw palmetto berry extract (“SPBE”) has been shown to block 5-alpha reductase, the enzyme that converts the hormone testosterone into dihydrotestosterone (“DHT”), the major androgen implicated in changes in the pilar cycle. This enzyme also blocks the binding of DHT to androgen receptors. Thus, in treating the balding scalp, SPBE may act by blocking the formation of DHT, by inhibiting binding of DHT to the androgen receptors, or both. The use of SPBE in reducing hair loss is well known and has been cited for example in “The Green Pharmacy”, pp. 78-79, Rodale Press, Emmaus, Penn., 1996.
In U.S. Pat. No. 5,972,345, SPBE has been combined with the extracts of African Pygeum and stinging nettle to produce a formulation for administration to the scalp for the treatment of male pattern hair loss. Stinging nettle extract is a known rubefacient that may open the follicle entrance by producing irritation.
In U.S. Pat. No. 5,750,108, SPBE is administered to the scalp as the third step in a procedure comprising lengthy, sequential preparatory treatments, first with tea tree oil, and then with an acidic solution of chlorine dioxide. The purpose of these preparatory treatments is to remove sebum from the follicle entrance and improve the effectiveness of the SBPE. However, chlorine dioxide is an irritant and an extremely hazardous material. The Occupational Safety and Health Administration of the U.S. Department of Labor, in a list published by Government Institutes, Inc. Rockville, Md., 1990, shows a Permissible Exposure Level (PEL) for chlorine dioxide vapor as 0.1 ppm. To understand this level of toxicity, it should be noted that elemental chlorine that has been used as a war gas, has a PEL that is five fold greater than that of chlorine dioxide.
SPBE has also been disclosed in U.S. Pat. Nos. 5,624,673, 5,653,983, and 5663,160 as an optional minor ingredient in topical formulations.
Other known topical formulations for treatment of hair loss are minoxodil, and a combination of minoxodil with tretinoin. The efficacy of minoxidil is limited as only a relatively small percentage of patients using it develope mild to moderate regrowth of hair. Further, Pharmacia and Upjohn, manufacturers of ROGAINE® minoxodil solution, warn that the most common side effect of minoxodil is itching and skin irritation of the treated area of the scalp. Tretinoin may also act as an irritant as indicated by the publication “Topical Tretinoin in Acne Therapy”, by G.F. Webster,
Journal of the American Academy of Dermatology
, S38-S43, (1998).
A need exists for an SPBE formulation and method of preventing hair loss/promoting hair growth that exploits the merits of SPBE without requiring lengthy and hazardous pretreatment of the scalp. Especially needed is an SPBE formulation that offers enhanced effectiveness without causing scalp irritation.
SUMMARY OF THE INVENTION
The invention provides an improved preparation and a method for treating androgenetic alopecia. The preparation comprises an extract of saw palmetto berries containing phytosterols and a non-irritating compound to enhance the penetration of the extract into the follicles. More specifically, the improved low irritability topical preparation comprises saw palmetto berry extract containing phytosterols and one or more penetration enhancing constituents selected from the group consisting of adapalene, tretinoin gel microsponges, tretinoin and polyolprepolymer-2, retinaldehyde, tazarotene, salicylic acid, azelaic acid, and glycolic acid. Preferably the penetration enhancing constituents consist of one member selected from the group consisting of adapalene, tretinoin and polyolprepolymer-2, and tretinoin gel microsponges, and another member selected from the group consisting of salicylic acid and glycolic acid.
In another embodiment, the improved low irritability topical preparation comprises an active saw palmetto berry extract containing phytosterols, polyolprepolymer-2 and one or more penetration enhancing constituents selected from the group consisting of adapalene, tretinoin, retinaldehyde, tazarotene, salicylic acid, azelaic acid, and glycolic acid. Preferably the penetration enhancing constituents consist of one member selected from the group consisting of adapalene and tretinoin and another member selected from the group consisting of salicylic acid and glycolic acid.
Most preferably, in both of the above embodiments, the penetration enhancing constituents are adapalene and glycolic acid.
The preparations of the invention may include a vehicle suitable for topical application to the scalp in the form of a liquid, a gel, a foam, a styling hair tonic, a styling mousse, a styling hair spray, a pad dampened with a liquid, or any other means suitable for application to the scalp.
The method for the treatment of androgenetic alopecia comprises applying to the scalp a low irritability preparation comprising saw palmetto berry extract containing phytosterols, and one or more penetration enhancing constituents selected from the group consisting of adapalene, tretinoin gel microsponges, retinaldehyde, tazarotene, salicylic acid, azelaic acid, and glycolic acid. In another embodiment, the method for the treatment of androgenetic alopecia comprises applying to the scalp a low irritability preparation comprising saw palmetto berry extract containing phytosterols, polyolprepolymer-2 and one or more penetration enhancing constituents selected from the group consisting of adapalene, tretinoin, retinaldehyde, tazarotene, salicylic acid, azelaic acid, and glycolic acid.
DETAILED DESCRIPTION OF THE INVENTION
The present invention provides low irritability formulations of SPBE offering enhanced effectiveness in reducing hair loss by their greater ability to penetrate the pores of the scalp. In addition, there is provided by the invention a method for reducing hair loss by application to the scalp of a preparation comprised of the improved formulations.
The pilar cycle in humans is measured in years, typically two to four years. Consequently, a topical preparation to be effective in reducing hair loss or promoting hair growth must be used for extended periods of time. It is evident that a preparation or a method that causes irritation of the scalp often cannot be used for the time essential to be effective.
The SPBE constituent of the preparation of the invention may be obtained from a number of commercial sources. Satisfactory non-irritating SPBEs include Permixon® from P.F. Medicaments, Paris, France, SPBE from McZand Herbal Inc., Santa Monica, Calif., and others.
In a preferred embodiment of the preparation of the present invention, the SPBE constituent is the alcohol soluble material sold by Saw Palmetto Harvesting Company, Frostproof Fla. This SPBE is non-irritating when applied to the scalp. Typically, it has the following major components and concentrations:
Phytosterols
capesterol
about 0.01 to about 0.1 wt.wt. %
beta-sitosterol
about 0.1 to about 0.4 wt. %
stimasterol
about 0.01 to about 0.1 wt. %
To
Goodman David S.
Patten Patricia
Pearlman Robert I.
Riker, Danzig, Scherer, Hyland & Perretti LLP
Weber Jon P.
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