Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1990-05-14
1992-09-01
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424 65, 424 68, A61K 732, A61K 738
Patent
active
051437180
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to an antiperspirant composition as well as a method for controlling perspiration without the disadvantages often associated with such methods.
BACKGROUND OF THE INVENTION
It is a well known fact that AlCl.sub.3 is a most effective antiperspirant salt (Holtze E., Kligman A.: "Mechanism of antiperspirant aluminium salts." J. Soc. Cosmet. Chem. 30, 279 (1979), and Shelley B., Hurley H.J.: "Studies on topical antiperspirant control of axillary hyperhydrosis." Acta Dermatoven. Stockh. 55, 241 (1975)). Most of the comercially available antiperspirant compositions contain AlCl.sub.3 as the active component, e.g. dissolved in a suitable solvent. AlCl.sub.3 exerts its antiperspirant activity by reacting with water to form aluminium hydroxychloride which acts as an astringent and thereby reduces the sweat output of the sweat glands. However, the disadvantage of using AlCl.sub.3 is that the reaction with water to form aluminium hydroxychloride also generates hydrogen chloride or hydrochloric acid as a side product which may cause local skin irritation because of the high acidity; in most clinical studies, 20-50% of the members of the test groups indicated that irritation occurred, and about 10% reported severe irritation (soreness). Also, clothes in contact with the application area may be damaged, and both of these adverse effects can be ascribed to the formation of hydrochloric acid on the skin and in the sweat ducts.
Also, the antiperspirant activity of AlCl.sub.3 is furthermore believed to be partly due to the aluminium hydroxychloride forming a perspiration-blocking "cast" of a polymeric gel precipitate in the sweat ducts. However, the acidity generated in sweat which reacts with AlCl.sub.3 will impair the efficiency of the AlCl.sub.3 -containing composition since AlCl.sub.3 is not capable of forming the gel precipitate when the water with which it reacts has a pH of less than 5; among other things this means that the AlCl.sub.3 composition is not effective when used during sweating.
In the known art, several attempts have been made to prevent the development of acid which causes skin irritation and damaging of clothes. Thus, European Patent No. 70517 describes a two-part kit comprising an AlCl.sub.3 -containing composition and a basic buffer composition, the basic composition being applied subsequent to the AlCl.sub.3 -containing composition but after having allowed the AlCl.sub.3 -containing composition to work for a certain specified period of time. However, as will be self-evident, such a two-stage application sequence is not very practical in actual use since most users would much prefer to have the antiperspirant treatment conducted in a single application.
From the above it is clear that there is a need for an antiperspirant composition which, while still having the advantages conferred by AlCl.sub.3, does not have the consequent disadvantages and which at the same time is simple to use.
SUMMARY OF THE INVENTION
The above described disadvantages in the known art are avoided in the antiperspirant composition of the invention which comprises AlCl.sub.3 and one or more aluminium salts of one or more acids dissolved and/or dispersed in a suitable carrier, the acid or acids having no pK value in aqueous solution lower than 2.5 and being present in an amount capable of substantially neutralising the amount of hydrogen chloride formed by the hydrolysis of the amount of AlCl.sub.3 present.
The idea behind the invention is to exploit the high acidity of hydrogen chloride by allowing the hydrogen chloride to react with a salt of the weaker acid with no pK value below 2.5, the weaker acid then, according to well known principles, being liberated from the salt by the stronger hydrochloric acid to give the free weaker acid and a chloride instead. The fact that an aluminium salt of the weaker acid is used has the advantage of resulting in the formation of a further amount of aluminium hydroxychloride, thereby resulting in a further antiperspirant effect. On t
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Remington's Pharmaceutical Sciences Treatise, Mack Publishing Co., 17th Ed., 1985, pp. 777-778.
Holze et al., "Mechanism of Antiperspirant Action of Aluminum Salts", J. Soc. Cosmet. Chem 30, 279-295 (Sep./Oct., 1979).
Shelley et al., "Studies on Topical Antiperspirant Control of Axillary Hyperhidrosis" Acta Dermatonvener (Stockholm) 55: 241-260, 1975.
Colucci D.
Page Thurman K.
Riemann Trading ApS
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