Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Patent
1994-09-28
1997-06-10
Kishore, Gollamudi S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
424 63, 424 64, 424 701, 424 707, 514844, 514845, 514846, 514847, 514880, 514881, 514944, A61K 700, A61K 7025, A61K 7032, A61K 706
Patent
active
056373040
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The invention relates to the topical use of deacylated glycerophospholipids and of the physiologically acceptable salts thereof.
Particularly, the invention relates to the use of deacylated glycerophospholipids named L-.alpha.-glycerylphosphorylcholine, L-.alpha.-glycerylphosphorylethanolamine, L-.alpha.-cglycerylphosphorylserine, L-.alpha.-cglycerylphosphoryl-D-myo-inositol, respectively.
These compounds, in the present invention, can be used alone or in mixtures thereof.
BACKGROUND OF THE INVENTION
The deacylated glycerophospholipids are mainly obtained by the semisynthetic route, for example those preferred in the present invention are obtained by selective deacylation of the natural phospholipids extracted from soy.
Glycerophospholipids are compounds widely occurring in nature, where they exert important biological functions, for example they are the main lipid components of cell phospholipids.
Their administration by the oral and parenteral routes, for example as diet supplements or as medicaments, proved to be useful in the prevention of the involution processes of the cell membranes, since they can play an important role on the biochemical lesions occurring on the membrane phospholipids.
SUMMARY OF THE INVENTION
Now it has surprisingly been found that the deacylated glycerophospholipids of the present invention can be adsorbed by the topical route, if suitably formulated, and this is a valuable alternative to the exogenous supply to the skin cells.
Deacylated glycerophospholipids, mainly those preferred in the present invention, have interesting properties which can suitably be exploited also in the cosmetic field.
The use of the glycerophospholipids is based on the fact that these compounds can be considered both as basic substances (for the formulation of excipients) and as specializing functional substances.
As basic substances, they can be used, for example, to give wetting, antidehydrating, plasticizing, co-solvent and co preservative properties.
As specializing functional substances, they can be used, for instance, as moisturizers, emollients, elasticizers, restitutives and the like.
These compounds can usefully be applied also to the hair cosmetic, for example as antistatics, restitutives, voluminizing agents and the like.
The used concentrations of the deacylated glycerophospholipids in the present invention can vary within wide ranges, according to the envisaged uses and the kind of the prepared formulation; for example they can be used in a range from 0.01% up to 50% by weight. preferably from 0.1% to 10%.
The deacylated phospholipids have a very low systemic toxicity as well as a particularly low topical toxicity, as evidenced by the tests carried out in the animal, hereinafter described.
Cutaneous sensitization
350-450 g guinea pigs, depilated on the back, were used.
50 mg of the product were applied on the left side of the depilated area every other day for 15 days. 30-35 days from the beginning of the treatment, 50 mg of the product were applied on the right side of the back, and the observations were recorded during 24 hours.
No cutaneous reactions were observed during the treatment and in the final phase of antigenic induction.
Eye Irritation
The eye tolerance was determined on New Zealand rabbits.
0.1 ml of a 1% solution of the product were instilled into the conjunctival sac of the right eye of the rabbit, whereas 0.1 ml of saline solution were instilled into the left eye.
The eyes were carefully checked for a time of 24 hours, recording any anomalies.
Immediately after the administration of the product and of the saline solution, an abundant lachrymation was observed. Subsequently conjunctiva, iris and cornea remained normal during the whole observation time.
Cutaneous Irritation
350-450 g guinea pigs were used, which were depilated on the back by means of a razor.
4 Product doses, corresponding to 50 mg-100 mg-200 mg-300 mg, were applied, then observation started, which lasted 24 hours at least.
No cutaneous irritations were observed at the various p
REFERENCES:
patent: 4424234 (1984-01-01), Alderson
patent: 5089269 (1992-02-01), Noda
patent: 5208031 (1993-05-01), Kelly
patent: 5315023 (1994-05-01), De Ferra
Flarer S.A. Pharmaceutical Fine Chemicals
Kishore Gollamudi S.
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