Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1985-07-11
1990-06-05
Schenkman, Leonard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514691, 514703, 514725, 514859, A61K 3107, A61K 31215
Patent
active
049314670
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a drug composition for treating or preventing acne by oral administration.
Until relatively recently, no large differences had been noted in the qualitative composition of the surface cutaneous lipids secreted by the skin of acne patients and individuals not suffering from acne.
By using thin layer chromatography, it has been possible to study the presence of lipid oxides in the cutaneous lipid secretions supplied by the sebaceous glands and inside an open or closed comedo. Thus, in an instance of thin layer chromatography of the surface cutaneous lipids, elution gave a succession of spots corresponding, respectively, to a polymerized and oxidized squalene, cholesterol, fatty acids, triglycerides, two other different oxidation states of squalene, waxes and unoxidized squalene, the latter being present in the secretion in the proportion of 10 to 15% by weight. The three substances which correspond to oxidized squalene are three different substances; that eluted in the first place has undergone, relative to squalene, a polymerization as a result of the presence of oxygen: this oxidized squalene is a very polar gum-polymer having an oxygen content of 25 to 28% by weight.
There have been carried out statistical measurements which have made it possible to verify that there is a strong correlation between the extent to which a skin is affected by acne and the presence of oxidized lipids of sebaceous and/or epidermal origin, and oxidized squalene in particular, in the layers of the said skin. This observation already appeared in a publication "Free Communications 289, FC 16-4 D, Article No. 386, Ayako Yamamoto", which reported the 16th Dermatological Congress in May 1982, and stated as a conclusion that normal human skin appeared to possess a factor which plays a role in the inhibition of the permeation of lipid oxides inside the epidermis, and that irritation of the skin and cytotoxicity by squalene oxides take place not only according to the level of lipid oxides but also depending on the chemical structure thereof. Furthermore, the studies of K. MOTOYOSHI, reported in the journal "British Journal of Dermatology", (1983) 109, 191-198, have demonstrated that the presence of oxidized lipids, and squalene oxides in particular, in the follicular infundibulum is highly comedogenic.
Thus, oxidized lipids, which prove to be cytotoxic and comedogenic for cutaneous tissue, can be considered to be largely responsible for the pathogenesis of acne. Moreover, it is known from the studies of O. H. MILLS, M. PORTE and A. M. KLIGMAN, "British Journal of Dermatology" (1978) 98, 145, that UV-A radiation increases the capacity of human sebum and squalene to produce comedos; it has hence been suggested that this radiation could increase the levels of lipid oxides, these oxides irritating the epithelium in the follicular infundibulum and hence increasing the formation of comedos.
In parallel with the studies thus performed by the specialists in basic research in the therapeutic field, specialist beauticians have, for their part, carried out experiments which have led to the following observations:
comedos appear to result from irritation caused by certain agents such as squalene oxides: thus, it has been possible to note the formation of comedos on a rabbit's ear which has received squalene oxide by topical application.
carotenoids are natural agents used in the cosmetics field for protecting the cutaneous tissue against peroxidation phenomena and photosensitisation phenomena and, as a general rule, phenomena of irritation by chemical means or by irradiation. Thus, apart from their function of coloring the skin for the purpose of tanning, illustrated in particular by French Patent No. 2,384,500, which describes a formulation for gelatin capsules based on .beta.-carotene, and by French Patent No. 2,430,765, which describes a product consisting of pure carotene in a carrier, carotenoids are known, as a general rule, for their function of protecting against sunburn. Thus, French Patent Application No.
REFERENCES:
Chemical Abstracts 67: 72388p (Fegeler et al.), 1967.
Merck Index, 9th ed; 1926, pp. 1852-1855.
Bague Arlette
Saint-Leger Didier
"L'Oreal"
Schenkman Leonard
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