Antiperspirant product and method

Details Antiperspirant product and method Antiperspirant product and method

1999-09-14

2001-06-26

Dodson, Shelley A. (Department: 1616)

Drug, bio-affecting and body treating compositions

Anti-perspirants or perspiration deodorants

C424S066000, C424S067000, C424S068000, C424S400000, C424S401000

Reexamination Certificate

active

06251376

ABSTRACT:

This invention relates to antiperspirant compositions and to methods of improving the efficiency of antiperspirant compositions, and to cosmetic methods of inhibiting perspiration on the skin.
Cosmetic antiperspirant compositions are known, and typically comprise topically acceptable compositions containing a metal salt, such as an aluminium and/or zirconium salt, in combination with a cosmetically suitable vehicle. Such cosmetic antiperspirant products may be available in a variety of product forms, for example as sticks, roll-on lotions, aerosols and pump spray formulations to name a few.
Whilst such compositions provide a degree of perspiration inhibition, it has long been desirable to improve the efficacy of such topical compositions in order that a user may experience fewer wetness events. Further, if the efficacy of such products can be improved, it may be possible to devise products in which the concentration of the metal salt providing antiperspirant efficacy can generally be reduced, but whilst still providing products of equal or even higher efficacy. This could lead to such products being cheaper, easier to formulate (by virtue of the reduced amount of antiperspirant active used), or generally having improved sensory properties.
We have found that it may be possible to enhance the efficacy of known antiperspirant materials in topical compositions, such as contain actives, such as but not limited to aluminium and zirconium salts, by the addition to, or use with, the topical composition of a composition which raises the pH of sweat in the eccrine gland.
Thus, according to a first aspect, there is provided an antiperspirant product for application to the human skin, comprising an antiperspirant active for topical application and an effective amount of a compound which inhibits the acidification mechanism in the eccrine gland to elevate the pH of sweat.
Herein, the antiperspirant product can comprise the antiperspirant active and the compound which inhibits the acidification mechanism in the eccrine gland in a single composition for topical application or, alternatively, the product can comprise separate means for the administration of the aforementioned components. When the components are administered via separate means, they can be supplied in a pack, together with instructions for their administration. In using such a product, the components can be applied consecutively, or, for greater convenience, concurrently. In a preferred embodiment, both components are applied topically.
According to a further aspect of the invention, there is provided a cosmetic method of elevating the pH of sweat in the eccrine gland comprising topically applying thereto an effective amount of a compound which raises the pH of sweat in the gland.
According to a further aspect of the invention, there is provided a cosmetic method of preventing perspiration of the human body, comprising topically applying to the body a composition comprising an antiperspirant active, and also applying a compound which elevates the pH of sweat in the eccrine gland. For greater convenience, the two components involved in the method may both be topically-applied from a single composition.
Thus, according to a further aspect of the invention, there is provided an antiperspirant composition for topical application to the human skin, comprising an antiperspirant active, and an effective amount of a compound which elevates the pH of sweat in the eccrine gland.
In order to generate the elevation of sweat pH in an eccrine gland, we have found that this can be achieved by the inhibition of bicarbonate reabsorption in the eccrine gland, and as such the invention also comprises compositions and methods which comprise and utilize compounds which are topically applied and which inhibit the reabsorption of bicarbonate in the eccrine gland.
Bicarbonate reabsorption is a known transport mechanism, which operates in the eccrine gland. This is more fully described in “Biology of sweat glands and their disorders. I. Normal sweat gland functions” by Sato, Hang, Saga & Sato, Journal of American Academy of Dermatology, pp 537-563, Volume 20, No 14, April 1989. Without wishing to be bound by theory as to how the invention may work, it is suspected that by disrupting this reabsorption mechanism in the cell lumen, the pH of secreted sweat can be caused to raise by somewhere in the region of (but not limited to) 0.5-1 pH units. Such an elevation of pH in sweat prior to its arrival at the skin surface has been found to provide for the enhancement of efficacy of antiperspirant actives that gel better at pH values higher than those of unmodified sweat in the eccrine duct. Examples include (but are not limited to) aluminium, aluminium/zirconium, and zirconium salts, in topically applied compositions.
It is thus a preferred aspect of the methods and products of the invention that the compound which is capable of elevating the pH of sweat in the eccrine gland is a compound which inhibits the bicarbonate reabsorption mechanism.
In a further preferred aspect, the compound which inhibits bicarbonate reabsorption may be a carbonic anhydrase inhibitor. Suitable and preferred carbonic anhydrase inhibitors include acetazolamide, and especially ethyl tosylamide. Such compounds can be added to topical antiperspirant compositions to provide compositions which may have enhanced antiperspirant efficacy over other known compositions.
We have also found that the invention is particularly efficacious on areas of the human skin that excrete sweat having a naturally low pH; in particular, the skin of the lower back, the feet, the forehead, and the back of the neck.
The compound which is capable of elevating the pH of sweat in the eccrine gland when applied in conjunction with a topical antiperspirant composition will preferably elevate the pH of sweat by at least 0.05, more preferably by at least 0.1, even more preferably by at least 0.2 pH units. Conveniently the pH of sweat will not be elevated by more than 1.5 pH units, more preferably by not more than 1.0 pH units.
Antiperspirant active materials which may have their efficacy enhanced by the methods and products according to the invention are those that gel better at pH values higher than those of unmodified sweat in the eccrine duct, for example aluminium, aluminium/zirconium, and zirconium salts. Particular examples are: aluminium chlorohydrate, activated aluminium chlorohydrate, zirconium aluminium chlorohydrate, zirconium aluminium glycinate, and activated zirconium aluminium glycinate.
The invention is capable of being utilized with any suitable antiperspirant composition form, including (but not limited to) sticks, roll-on lotions, aerosols, and pump spray formulations. The antiperspirant active in such compositions is present at a level of 0.5 to 60%, particularly 5 to 30 or 40%, and especially from 10 to 30 or 35% by weight.
Acetazolamide (N-[5-sulfamoyl-1,3,4-thiadiazol-2-yl] acetamide) is a known compound, and is commercially available as Diamox powder from Wyeth Research UK Ltd. It has been clinically used previously as a diuretic, to ameliorate high altitude sickness, and to treat glaucoma and various forms of epilepsy. It has been found that the introduction of acetazolamide into eccrine glands leads to the elevation in the pH of sweat from that gland, and has also lead to the increase in efficacy of a conventional antiperspirant composition topically applied to those glands.
A further suitable compound suitable for use in conjunction with the topical antiperspirant compositions is Sibercizer C6 (N-ethyl-O and P-toluenesulfonamide), available from Merck. Other suitable compounds may include Dorzolamide (4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-,7,7-dioxide,(4S,6S)- (9Cl)) and Sezolamide (4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 5,6-dihydro-4-[(2-methylpropyl)amino]-,7,7-dioxide, (S)-), together with cosmetically acceptable and effective salts and analogues of all of the above mentioned specific compounds. A preferred

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