Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
1999-02-18
2001-07-17
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S714000
Reexamination Certificate
active
06262117
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to a method and composition for treating acne vulgaris.
BACKGROUND OF THE ART
Acne vulgaris is an inflammatory disease of the sebaceous glands characterized by an eruption of the skin, often pustular in nature but not suppurative. Acne is a common affliction of the adolescent and affects a small but significant percentage of the adult population. Acne involvement results in unsightly lesions, particularly on the face, and in some cases results in severe scarring.
Various topical agents are utilized in the treatment of acne and these include sulfur, resorcinol, salicylic acid, benzoyl peroxide, retinoids and topical antibiotics. An effective anti-acne agent (or composition) must exhibit the following activities:
(a) a sebostatic activity so as to inhibit hyperseborrhea;
(b) a keratolytic and comedolytic activity so as to avoid hyperkeratosis of the follices and to permit removal of comedos;
(c) a bacteriostatic activity so as to inhibit the activity of Propionibacterium acnes.
Nevertheless, acne vulgaris is seldom cured and only can be contained with difficulty.
The antibiotic clindamycin has been used, topically, to treat acne vulgaris. (See U.S. Pat. No. 3,969,516, to Stoughton.) Various references discuss the use of vehicle formulations to enhance the efficacy of topically-applied clindamycin. (See U.S. Pat. Nos. 3,932,653; 3,989,816; 3,991,203; 4,132,781; 4,671,956; 4,746,675; 4,789,667; 4,803,228 and 4,882,359.) Clindamycin salts, clindamycin derivatives, and various dosage forms of clindamycin have also been discussed as a treatment for acne vulgaris. (See U.S. Pat. Nos. 3,849,396; 4,621,075 and 4,916,118.) Finally, combinations of clindamycin and other compounds active for the treatment of acne vulgaris are disclosed in U.S. Pat. Nos. 4,323,558; 4,505,896; 4,607,101; 4,906,617; 4,942,031 and 4,018,918.
Benzoyl peroxide has been suggested for treating acne vulgaris. (See U.S. Pat. No. 4,387,107.) For many years, benzoyl peroxide has been proven to be a particularly powerful keratolytic and anti-seborrhic agent, as well as being endowed with antibacterial properties. Topical benzoyl peroxide compositions, including a vehicle to enhance the efficacy thereof, are known (See U.S. Pat. No. 4,411,893). Topical compositions of benzoyl peroxide combination with antibiotics are also known. (See U.S. Pat. Nos. 4,407,794; 4,692,329 and 4,387,107)
Peroxides, other than benzoyl peroxide, have been suggested for treatment of acne vulgaris, alone, or in combination with other compounds useful in treating acne vulgaris. (See U.S. Pat. Nos. 4,607,101 and 4,906,617.) These peroxides are suggested as having certain advantages, e.g. stability over benzoyl peroxide. U.S. Pat. No. 4,671,956 identifies the problem of benzoyl peroxide decomposing coingredients in topical formulations to thereby cause itching upon application. It is suggested that this problem may be solved by including a sunscreen in the topical formulation to retard this decomposition effect of benzoyl peroxide.
Azelaic acid has been used topically and systemically to treat acne. See, for example, U.S. Pat. No. 4,386,104 to Nazzo-Pavarro.
In view of the above, it is apparent that there is a great deal of interest in utilizing topical compositions for the treatment of acne vulgaris, such compositions utilizing as an active ingredient clindamycin or benzoyl peroxide or azelaic acid, alone, or in combination with other active ingredients for the treatment of acne vulgaris.
Therefore, one object of the instant invention is to provide a method of treating acne vulgaris with topical compositions including benzoyl peroxide and azelaic acid.
It is another object of the invention to provide a method of treatment of acne vulgaris by topical application of compositions of benzoyl peroxide in a gel form and azelaic acid in a cream form.
It is another object of this invention to provide compositions for the topical treatment of acne vulgaris.
Another object of the invention is to provide topical compositions of benzoyl peroxide and azelaic acid that may be used for treating acne vulgaris.
Other objects and advantages of the instant invention will become apparent from a careful reading of the specification below.
SUMMARY OF THE INVENTION
The present invention provides a method for treating acne vulgaris by topically applying a composition of benzoyl peroxide and azelaic acid, serially, in a therapeutically-effective amount. The azelaic acid or its pharmaceutically acceptable salts or prodrugs (e.g. azelaic acid, sodium salt or lower alkyl ester), may be applied in an amount sufficient to provide from about 0.1 to about 30 percent, and preferably from about 0.5 to about 25 percent, by weight, e.g. about 20 percent azelaic acid. Benzoyl peroxide, which has keratolytic and antiseborrheic properties, may be present in an amount sufficient to provide from about 0.1 to about 30 percent, and preferably from about 2.5 to about 10 percent, by weight, benzoyl peroxide. The benzoyl peroxide may more preferably be used as hydrous benzoyl peroxide and may be suspended preferably in the form of microparticles. The above described topical composition may be in the form of a solution, gel, ointment, cream, a liquid suspension or emulsion or a stick base.
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Allergan Sales Inc.
Baran Robert J.
Jarvis William R. A.
Kim Vickie
O'Donohue Cynthia H.
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