Title:  Method for diminishing wrinkles and fine lines of the skin by the topical application of .DELTA.5-androstene-3.beta.-ol-7, 17 dione and metabolizable precursors thereof

United States Patent:  6,399,084

Assignee:  Humanetics Corporation (Chanhassen, MN)

Filed:  March 5, 2001

Wrinkles and fine lines occurring on human skin can be diminished by the administration of .DELTA.5-androstene-3.beta.-ol-7,17 dione and metabolizable precursors thereof, such as .DELTA.5-androstene-3.beta.-acetoxy-7,17 dione, to the skin.

DETAILED DESCRIPTION OF THE INVENTION INCLUDING A BEST MODE

Wrinkles and fine lines occurring on human skin can be diminished by the administration of .DELTA.5-androstene-3.beta.-ol-7,17 dione and metabolizable precursors thereof, such as .DELTA.5-androstene-3.beta.-acetoxy-7,17 dione, to the skin.

The Compound

The steroid .DELTA.5-androstene-3.beta.-ol-7,17 dione is a derivative of dehydroepiandrosterone (DHEA) which does not appreciably stimulate, increase or otherwise enhance the production of sex hormones. The steroid is commercially available from a number of sources including Steraloids, Inc. of Wilton, N.H. A number of procedures are available for synthesizing .DELTA.5-androstene-3.beta.-ol-7,17 dione from DHEA, with one such procedure described in U.S. Pat. No. 5,296,481.

Precursors of .DELTA.5-androstene-3.beta.-ol-7,17 dione may also be usefully employed to diminish wrinkles and fine lines occurring on human skin. Such precursors are readily metabolized in vivo to the active .DELTA.5-androstene-3.beta.-ol-7,17 dione. One example of such a metabolizable precursor is the commercially available .DELTA.5-androstene-3.beta.-acetyl-7,17 dione. The 3.beta.-acetyl group is hydrolyzed in vivo by esterases located in the blood and various tissue to produce the active .DELTA.5-androstene-3.beta.-ol-7, 17 dione, and is believed to be less susceptible to oxidation during the manufacturing process than the hydroxy group found on the active .DELTA.5-androstene-3.beta.-ol-7,17 dione. The steroid is commercially available from Humanetics Corporation of Chanhassen, Minn. under the trademark "7-KETO."

Other metabolizable precursors include .DELTA.5-androstene-3.beta., 17.beta.-diol-7-one, .DELTA.5-androstene-3.beta., 7.alpha.-diol-17-one, .DELTA.5-androstene-3.beta., 7.beta.-diol-17-one and the corresponding acetyl esters of these steroids.

Administration

The steroid can be conveniently administered by incorporating the steroid into a lipophilic carrier to form a cream, lotion, ointment, gel, pomade, or balm (hereinafter collectively referenced as composition) and topically applying the composition to the area in need of a diminishment in wrinkles and fine lines.

The composition may be applied over the entire body or selected areas. Areas of particular interest, which can benefit from the anti-wrinkling effect of the steroid include the hands and face.

The composition can include from about 0.2 to 20-wt % steroid, preferably about 0.5 to 10-wt %, steroid. A concentration of less than about 0.2 wt % steroid tends to require the application of an uncomfortably large amount of the composition to achieve the desired diminishment in wrinkles and fine lines while a concentration of greater than about 20-wt % steroid tends to increase the cost of the composition without a corresponding increase in the extent or duration of the dimishiment in wrinkles or fine lines.

The composition can contain those adjuvants or additives which are commonly included in such compositions, such as hydrophilic or lipophilic gelling agents, preservatives, antioxidants, solvents, fragrances, fillers, screening agents, and colorants. The amounts of these various adjuvants or additives are those conventionally used in the cosmetics and dermatological fields, which are commonly from about 0.01 to about 20-wt % of the composition.

The composition can be beneficially employed by topically applying the steroid to the skin on a daily basis, such as after bathing or just prior to bedtime.

Claim 1 of 9 Claims

We claim:

1. A method of diminishing wrinkles and fine lines in human skin comprising administering an effective amount of a compound selected from .DELTA.5-androstene-3.beta.-ol-7,17-dione, .DELTA.5-androstene-3.beta., 17.beta.-diol-7-one, .DELTA.5-androstene-3.beta., 7.alpha.-diol-17-one, .DELTA.5-androstene-3.beta., 7.beta.-diol-17-one and corresponding acetyl esters thereof to human skin in need of a diminishment in wrinkles and fine lines.

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