GB2078111A - Composition for treating the hair, based on stigmasterol and purified lyophilised amniotic liquid - Google Patents

Abstract

A composition to combat hair loss and to promote its growth contains, in solution in alcohol of alcoholic strength >/=98 DEG , (i) stigmasterol in the pure form or in the form of an unsaponifiable material derived from wheatgerm oil or soya oil, and (ii) lyophilised amniotic liquid purified by solubilisation with alcohol. s

Description

SPECIFICATION Composition for treating the hair, based on stigmasterol and purified lyophilised amniotic liquid The present invention relates to a cosmetic composition for treating the hair, especially for reducing hair loss and for promoting hair growth.

It is well known that the problem of hair loss, especially in men, is a relatively common phenomenon, in particular at a certain time of life; it results from a variety of causes, which are still not fully understood, but the genotype without any doubt plays a considerable part. Nevertheless, hair loss can also be caused by certain other factors. Furthermore, poor functioning of the sebaceous glands can also lead to seborrheic alopecia, which can result in baldness.

In order to overcome excessive hair loss as far as possible and also to promote its growth, numerous so-called "tonic" compositions based on a variety of active compounds have been proposed.

Such compositions for treating the hair must essentially possess the following characteristics: 1. a slightly irritant action for promoting blood circulation in the region of the dermal papillae, 2. the presence of vitamins or sulphur-containing amino acids for improving the biosynthesis of the keratin, and 3. the presence of antiseborrheic agents or certain medicaments for controlling the seborrhea and other scalp phenomena which can interfere with the growth or regrowth of the hair.

Certain phenols, such as resorcinol and P-naphthol, may be mentioned, in particular, amongst the various active compounds used in hair compositions. Also, certain natural extracts, such as quinine, cade oil, capsicum and pylocarpine, as well as certain derivatives of sulphur-containing aminoacids, such as derivatives of cysteine or cysteamine, have been recommended.

Finally, it is important to mention the use of lyophilised amniotic liquid originating from a ruminant animal, preferably from cattle, at a certain stage of the gestation which is more than 60 days but less than 90 days. This type of composition has been described in US specification No 3 733 402 (French Patents Nos 985458 and 22 503) and has proved particularly effective especially in the case of seborrheic alopecia.

The present invention is in the same cosmetic field and relates to a composition which makes it possible to influence the pylogenetic phenomena by inhibiting hair loss and by promoting its growth.

In other words, it is not part of the aim of the present invention to treat subjects already affected with baldness, but, quite on the contrary, to treat those showing certain premonitary symptoms, so as to arrest the process or at least slowdown its effects.

The present invention provides a hair composition in the form of a lotion for combating hair loss and for promoting its growth, this composition containing, in solution in alcohol of alcoholic strength 98 , (i) stigmasterol in the pure form or in the form of an unsaponifiable material derived from wheatgerm oil or soya oil, and (ii) lyophilised amniotic liquid purified by solubilisation with alcohol.

By an "alcoholic strength of at least 98"" is meant that the "alcohol" contains at least 98% by volume of alcohol i.e. the water contant is at most 2% by volume.

The experiments which have been carried out using a composition of this invention have made it possible to show its excellent activity, initially on Wistar rats, and then, by way of confirmation, on men.

The growth of the fur on Wistar rats can be followed daily by a simple and direct method.

For each experiment, male Wistar rats, all born on the same day, are divided up into cages each containing five rats, and are individually characterised by a picric acid mark. Four cages, that is to say twenty animals, constitute a series. At the start of the experiment, the surface of the back of each animal is shaved over about 20 cm2 using an electric shaver.

The first daily topical application of 0.5 ml of the composition to be tested in the case of the treated series, and of distailled water in the case of the control series, is started three days later.

The treatment is continued for three weeks and a clinical notation system makes it possible to follow the individual progress of the fur and to assess the effectiveness of the treatment. The second clinical reading makes it possible, in particular, to select, from each series, the five animals on which the regrowth starts to be visible.

These animals then receive an oxidation dye on the treated zone. The daily topical applications are continued and a tuft of hairs is removed each day.

These hairs are then examined with the aid of a micrometer magnifying glass with 1/10 mm graduations, so as to measure the distance between the lower end of the root and the point where the colouration begins. The measurement is carried out each day on 10 hairs from each animal.

By this method, it is possible to determine, by comparing the treated animals with the control animals, the variation in the average growth index.

The various results found by this method will be given below.

Stigmasterol or 3 - () - hydroxy - 24 - ethyl A5 22 cholestadiene (C29K48O; molecular weight 412) is, together with sitosterol, one of the phytosterols, these being high molecular weight alcohols present in numerous plants.

Stigmasterol in the form of the monohydrate has a melting point of 1700C.

Stigmasterol can be obtained either by synthesis or, more commonly, from the mixture of phytosterols from certain plants which are particularly rich in this substance, such as wheatgerm and soya.

The preparation of the unsaponifiable materials derived from wheatgerm oil and soya oil which can be used in the compositions according to the invention is known and it has been possible to determine their composition with precision, according to their origin; thus, the unsaponifiable material derived from wheatgerm oil contains from 9 to 13% of stigmasterol.

Unsaponifiable materials derived from wheatgerm oil or soya oil and having a stigmasterol content which is greater than or equal to 9% are preferably used in the compositions of this invention.

The concentration of stigmasterol in the compositions according to the invention is generally from 0.1 to 0.5% by weight, relative to the total weight of the composition.

The other active ingredient of the compositions according to the invention is lyophilised amniotic liquid which has been purified beforehand by solubilisation with alcohol.

As indicated above, it has already been recommended to use lyophilised amniotic liquid for treating the hair, but, in that case, the amniotic liquid was essentially used in the form of an aqueous solution in which it was soluble.

In order to obtain a fraction of amniotic liquid which is soluble in alcohol, the lyophilised amniotic liquid obtained, typically in accordance with the technique described in U.S. Patent No. 3,733,402 is treated with an alcohol, preferably ethanol, and this makes it possible to solubilise about 50% thereof.

Checks carried out especially by chromatography on Sephadex LH20 have made it possible to show that only the various active fractions of the lyophilised amniotic liquid are present in the alcoholic solution.

A purification of this type by solubilisation has made it possible to improve, on the one hand, the activity and, on the other hand, the penetration by removing inhibiting substances such as high molecular weight proteins.

The removal of inactive substances furthermore makes it possible to avoid certain reactions of an immunological nature.

In view of the fact that, according to the invention, the vehicle of the hair composition is alcohol, that is to say ethanol or isopropanol, but preferably ethanol, it is not necessary to isolate the purified product, it being possible for the alcoholic solution resulting from the purification process to be employed direct.

In this case, the amount of alcoholic solution used is typically such that the hair composition according to the invention contains from 0.3 to 2% and preferably from 0.4 to 0.6% by weight of purified amniotic liquid.

The hair compositions according to the invention can also contain various other ingredients and especially a perfume, a colouring substance capable of dyeing the composition, a resin or a hair or scalp treating agent.

The compositions according to the invention have been shown to possess excellent stability with time, both from the bacteriological point of view and from the point of view of its original activity.

The results obtained on the growth of the fur on Wistar rats after the third week of treatment, in accordance with the technique described above, are summarised below.

Product Concentration Vehicle Variation in the average growth index, relative to the control (in %) Pure stig- Absolute masterol 0.2 ethanol +46 (I) Unsaponifiable material derived from wheatgerm oil, 2 Absolute +39 containing ethanol 10% of stig masterol (I') Purifed Absolute amniotic 0.5 ethanol +47 liquid (11) (I) + (11) (1) 0.2 Absolute (II) 0.5 ethanol +56 The results observed that, by using stigmasterol in association with purified amniotic liquid, a very substantial improvement is obtained from the point of view of the hair growth, compared with the improvement observed when these substances are used by themselves.

The present invention also provides a process for treating the hair in order to reduce hair loss and to promote its growth, which consists in applying a suf ficient amount of the composition according to the invention, as described above, and in massaging the scalp.

In general, 8 to 60 cm3 of the composition is sufficient to impregnate the whole of the scalp and the hair.

The treatment should preferably be applied daily for an extended period of, say, 1 to 3 months, it then being possible for the applications to be less frequent.

According to a preferred form of treatment according to the invention, the composition is diluted, at the time of use, with water or an aqueous soltuion containing a treating product such ascysteine derivative, in particular S - carboxymethylcysteine, or collagen, and is then applied to the scalp. Certain irritation phenomena on subjects who are particu larly sensitive to pure alcohol can thus be avoided.

The following Examples further illustrate the present invention.

EXAMPLE 1: A composition for treating the hair in order to arrest hair loss and to promote its growth is prepared according to the invention by mixing the following ingredients: Pure stigmasterol 0.2 9 Perfume ........................................ 0.1 g Purified amniotic liquid (0.5% strength solution in absolute ethanol) q s p ..... 100 g When applied, by rubbing, on a subject with copious hair loss, this composition (30 cm3) made it possible to arrest the loss after a daily treatment lasting 2 months. Furthermore, a very marked improvement in the hair growth was noted, compared with that observed before the start of the treatment.

EXAMPLE2 Pure stigmasterol .................................. 0.3 g Perfume ........................................ 0.05 g Vinyl acetate/crotonic acid copolymer (90/10) ........................................ 0.3 g Purified amniotic liquid (0.4% strength solution in absolute ethanol)q.s.p 100 .................................... 100 g 25 cm3 of the above composition are diluted with 20 cm3 of water containing a treating product (0.2% of S - carboxymethylcysteine). A daily treatment lasting about 3 months gave remarkable results on various subjects with copious hair loss, the daily loss after the treatment being on average the same as that for normal subjects.

Comparable results were obtained with the aid of the following composition, with or without dilution with an aqueous solution.

EXAMPLE3 Pure stigmasterol .................................. 0.5 g Quaternary vinylpyrrolidone copolymer sold underthe name Gafquat734 0.6 g Perfume ........................................ 0.1 g Dyestuff (sufficient for dyeing the composition) Purified amniotic liquid (0.5% strength solution in absolute ethanol) q s p .................. 100 g EXAMPLE 4 Pure stigmasterol .................................. 0.4 g Perfume ........................................ 0.08 g Dyestuff (sufficient for dyeing the composition) Camphor ........................................ 0.05 g Purified amniotic liquid (0.4% strength solution in absolute ethanol)q s p 100 ..................................... 100 g Before being applied to the hair, the above composition (20 cm3) is diluted with 20 cm3 of water. A daily treatment lasting 2 months on a subject with copious hair loss gave excellent results, the daily loss then corresponding to that for a normal subject.

EXAMPLE 5 Unsaponifiable material derived from wheatgerm oil containing 10% of stigmasterol ........................................ 2 g Perfume ........................................ 0.1 g Purified amniotic liquid (0.5% strength solution in absolute ethanol) q s p 100 ....................................... 100 g Similar results were obtained.

Claims (12)

1. A composition suitable for application to the hair or scalp which comprises, in solution in alcohol of alcoholic strength at least 98 , (i) stigmasterol either alone or as present in an unsaponifiable material derived from wheatgerm oil or soya oil, and (ii) lyophilised amniotic liquid which has been purified by solubilisation with alcohol.

2. A composition according to claim 1 in which the said unsaponifiable material derived from wheatgerm oil has a stigmasterol content of at least 9% by weight.

3. A composition according to claim 1 or 2 in which the concentration of stigmasterol is 0.1 to 0.5% by weight, relative to the total weight of the composition.

4. A composition according to any of claims 1 to 3 in which the alcohol is ethanol or isopropanol.

5. A composition according to any one of the preceding claims in which the lyophilised amniotic liquid originates from a ruminant animal and has been removed after 60 days but less than 90 days of gestation.

6. A composition according to any one of the preceding claims which contains from 0.3 to 2 6% by weight of the purified amniotic liquid.

7. A composition according to claim 6 which con tails from 0.4 to 0.6% by weight of the purified amniotic liquid.

8. A composition according to any one of the preceding claims which contains at least one of a perfume, a colouring substance for dyeing the composition, a resin ora hair or scalp treating agent.

9. A composition according to claim 1 substantially as described in any one of the Examples.

10. Process for treating the hair in order to reduce hair loss and to promote its growth which comprises applying a composition as claimed in any one of the preceding claims thereto and massaging the scalp.

11. Process according to claim 10 in which the composition is diluted with water or an aqueous solution containing a treating product, before it is applied to the scalp.

12. Process according to claim 10 substantially as hereinbefore described.