GB2081580A - Sapindus trifoliatus extracts - Google Patents

Abstract

A topical medicament for the promotion of hair growth comprises an extract from the pericarp of the fruit of Sapindus trifoliatus L. This extract is obtained by air-drying the pericarp of the fruit of Sapindus trifoliatus L., grinding the dried pericarp and soaking the ground pericarp in a polar solvent such as 70% aqueous propan-2-ol and fitering the resulting solution. The extract has been found to contain galactose, fructose, oleic palmitic, linolenic and stearic acids; stigmasterol, beta -sitosterol, camposterol and cholesterol.

Description

SPECIFICATION A medicament for the promotion of hair growth and a process for preparing same The present invention relates to a topical medicament which maybe used to alleviate the problems of hair loss, dandruff and associated skin diseases.

According to the present invention there is provided a topical medicament for the promotion of hair growth and alleviation of dandruff comprising an extract from the pericarp of the fruit of Sapindus trifoliatus L.

Preferably the extract comprises a polar solvent soluble fraction containing galactose, fructose, oleic, palmitic, linolenic and stearic acids, stigmasterol, psitosterol, camposterol and cholesterol.

Advantageously the polar solvent is 70% aqueous propan-2-ol.

A process for preparing the medicament according to the invention comprises air-drying the pericarp of the fruit of Sapindus trifoliatus L., grinding the dried pericarp, soaking the ground pericarp in a polar solvent to form a solution of extract in solvent and filtering the solution.

Preferably the filtrate is stored in the dark until use.

Preferably the dried pericarp is soaked for a period of 24 hours in 70% aqueous propan-2-ol.

A series of tests were carried out on severe dandruff and excessive hair loss sufferers by ten trichologists in England and Scotland.

Medicaments made up of extracts from Sapindus trifoliatus L. were provided in 100 ml nozzled P.V.C.

bottles for direct application, twice daily, to the hair partings on the scalp. No prenor post-application hair wash or massages were carried out.

The extracts were obtained from the fruit of Sapindus trffollatus L. by air drying of the pericarp of the fruit, grinding the dried pericarp and soaking the ground pericarp for 24 hours in 70% propan-2-ol.

The resulting solution was then filtered and the filtrate was stored in the dark prior to use.

Table 1 below illustrates the results of the tests on 70 volunteers, all of whom were suffering from severe dandruff with or without excessive hair loss.

Male and female patients with Pityriasis Simplex (A), Pityriasis Steatoides (B) and Seborrhoeic Dermititis (C) were included. In view of the fact that the medicament has a drying effect on the scalp, patients with Pityriasis Sicca were excluded.

An ancillary double-blind test using 20 volunteers indicated that 20% noted an improvement in dandruff symptoms with the placebo of solvent only (70% propan-2-ol).

Responses were graded according to the following key.

Grading of Dandruff Lesion Pityriasis Simplex -A Pityriasis Steatoides - B Seborrhoeic Dermatitis - C Grading of Response at the end of 4 weeks Dandruff - Worse O No effect + Patient notes improvement, but not observer ++ Slight improvement +++ Significant improvement ++++ Eliminated HafrLoss - Worse O No effect + Doubtful improvement ++ Slight improvement +++ Significant improvement ++++ Hair loss normalized Table 1.

No. of Duration Dandruff Excessive hair loss volunteers Age Sex (years) Type Result Duration Result 1 36 M 10 B ++++ 1 ++++ 2 49 M 13 C ++++ 0.5 +++ 3 41 M 11 B +++ 4 4 27 M 5 C ++ 5 5 47 M 15 C ++ 6 53 M 15 B + 7 34 F 10 C ++++ 8 42 F 12 C ++++ 2 ++++ 9 47 M 5 B ++++ 1 ++++ 10 29 M 2 C ++++ 11 40 M 4 C ++++ 12 22 M 7 C ++++ 13 39 M 3 B ++++ 14 38 M 2 C ++++ 15 20 M 2 B ++++ 16 23 F 4 C ++++ Table 1 contd.

17 75 F 10 C +++ 18 27 M 8 C ++++ 19 22 M 4 C ++ 20 60 F 10 C ++ 5 ++++ 21 29 M 2 B ++++ 22 48 F 10 C ++++ 2 +++ 23 45 F 6 C ++++ 6 ++++ 24 38 F 8 C ++++ 3 +++ 25 60 F 12 C ++++ 1 ++++ 26 54 M 8 C ++++ 0.5 +++ 27 50 M 10 B ++++ 2 ++++ 28 42 M 4 C +++ 29 18 F 1 B ++++ 2 +++ 30 61 F 10 B + 1 +++ 31 68 F 15 C +++ 32 16 F 1 C ++++ 4 ++++ 33 18 M 2 C +++ 1 +++ 34 25 F 3 B +++ 1 +++ 35 78 F 20 B + 1 0 36 52 F 8 A + 2 0 37 77 F 20 B 0 38 60 F 14 C O 39 33 F 3 A ++++ 40 44 F 6 A +++ 41 38 F 8 A +++ 3 ++++ 42 61 F 10 B O 43 17 F 1 C O 44 16 M 1 B ++++ 45 18 F 2 C ++++ 46 21 F 4 C ++++ 47 23 F 5 C +++ 48 37 F 8 C ++++ 49 77 F 20 C ++++ 4 ++++ 50 66 F 18 C ++++ 2 ++++ 51 73 F 20 C O 52 69 F 25 C ++++ 1 +++ 53 58 F 10 C ++++ 1 +++ 54 58 F 10 C ++++ 1 +++ 55 56 M 15 B ++++ 1 +++ 56 43 M 10 B O 57 41 M 8 C ++++ 58 68 F 20 C +++ 59 42 M 10 C ++ 60 28 M 6 C +++ 4 0 61 34 M 6 C ++ 2 0 62 36 F 4 C ++ 1 0 63 40 F 8 C ++ 2 - 64 32 F 7 C ++ 1 - 65 48 F 8 C +++ 2 +++ 66 60 M 10 A +++ 3 +++ 67 28 M 4 A +++ 1 +++ 68 39 F 5 B +++ 69 42 F 10 B ++ 70 28 M 4 B +++ The results of these preliminary tests suggested a significant improvement in the symptoms of both males and females following treatment for 4 weeks.

These observations provided a basis for investigating the effects of extracts on an experimental animal, the normal, outbred mouse. Abundant hair growth was noted in treated female mice whereas this response was not evident in male animals.

Extracts were prepared as before by soaking ground, air-dried pericarp of Sapindus trifollatus L.

fruit for 24 hours in 70% propan-2-ol; the solution was then filtered and stored in the dark. In all experiments the treatment consisted of daily applications of extract and control solutions to shaved patches of skin chosen symmetrically on either side of the dorsal midline of each mouse. Treatment was continued for periods of from 4 to 5 weeks on animals of known ages. The animals were then killed and samples of the skin from the treated areas were taken for detailed histology. In some instances, the skin samples were sectioned in two directions, parallel and at right angles to the midline. At least 10 sections were picked out at 240 zm intervals from the ribbon of serial sections available for each skin sample.

In one test, 9 animals were treated with the extract and another 9 with solvent only. The two groups were formed by allocating to each an equal number of animals from each one of two litters. In another test 21 animals were treated with extract on one side of the back and with solvent on the other side.

A consistent difference between all treated and control samples was noted when the results were grouped by the sex of the animals. The stage of hair cycle at the start of treatment was not known except that there could be no difference between sibs. At the end of treatment the stage is seen in the histological sections.

In female mice, the samples treated with extract showed abundant hair growth, with hair reaching all through the subcutaneous adipose tissue even where the corresponding solvent-treated animal or solvent-treated side was in the resting stage (telogen) of the hair growth cycle (Dry, 1926) (Fig. 1).

The extract appeared to have a localised influence on the progress of the hair development cycle, and favoured retention of hair in its fully grown ('anagen') stage. Alternatively, the extract may have shortened the telogen stage and thus brought forward the next hair cycle, but this is unlikely in view of the fact that intermediary stages were not evident.

Only further work, involving skin sampling at the start of treatment and at several intervals thereafter could provide a final decision between the two alternatives.

In male animals, on the other hand, there were no significant histological differences between extract and solvent-treated zones.

Related studies were carried out on the chemical composition of the extract and source material.

Samples were derivatised with bis-trimethylsilyl (trifluoro) acetamide and analysed by combined gas chromatography-mass spectrometry (Hillman et al, 1975). Positive identifications were made of galactose and fructose, and the fatty acid oleic, palmitic, linolenic and stearic acids as well as the sterols stigmasterol, sitosterol, campesterol and cholesterol. No other steroids could be detected even when using selective ion detection mass fragmentography (Young etal, 1977).

The differential response noted between female and male mice cannot be attibuted, therefore, to the presence in the extract of significant quantities of steroidal oestrogens, although some plant species are known to synthesis these compounds (Young et al, 1977, 1978) and related substances (Guens, 1978).

None of the compounds indentified in the extract has been reported to modify hair growth and further studies on the active compoments of the extract are merited. Moreover, in contrast to the experiments on mice, there was no evidence from the clinical trials on humans to suggest that hair growth was different in males and females treated with extract. Comparisons between animal experiments and the human are in any case inappropriate because baldness in man is not connected to hair growth cycles.

Claims (6)

1. A topical medicament for the promotion of hair growth and alleviation of dandruff comprising an extract from the pericarp of the fruit of Sapindus trifoliatus L.

2. A medicament according to claim 1 wherein the extract comprises a polar solvent soluble fraction containing galactose, fructose; oleic, palmitic, linolenic and stearic acids; stigmasterol, Rsitosterol, camposterol and cholesterol.

3. A medicament according to claim 1 or claim 2 wherein the solvent is propan-2-ol.

4. A process for preparing the medicament claimed in claim 1 comprising air-drying the pericarp of the fruit of Sapindus trifoliatus L., grinding the dried pericarp soaking the ground pericarp in a polar solvent to form a solution of extract in solvent and filtering the solution.

5. A process according to claim 4 wherein the filtrate is stored in the dark until use.

6. A process according to claim 4 or 5 wherein the dried pericarp is soaked for a period of 24 hours in 70% aqueous propan-2-ol.