ALLYL ISOTHIOCYANATE AND USE THEREOF TO INHIBIT HAIR LOSS

Abstract: Allyl isothiocyanate is useful to inhibit human hair loss.

Description: Title: ALLYL ISOTHIOCYANATE AND USE THEREOF TO INHIBIT HAIR LOSS This application is concerned with pharmaceutical compositions allyl isothiocyanate (AITC) , and the use of such compositions of AITC itself to inhibit hair loss from the human scalp. Allyl isothiocyanate is a known compound. It may be prepared by reaction between allyl iodide and potassium thiocyanate as described by Duliere J. Pharm. Belg. 2 j _ 981 (1920). It has now been discovered that topical application of AITC to the human scalp, preferably in a pharmaceutically acceptable carrier will assist in the prevention of hair loss. The AITC may be applied, generally by massage, in any of a variety of compositions including liquids, and viscous bases such as creams, lotions, emollients, and other compositions generally employed for topical application. Useful compositions will contain from about 0.01% to 5%, preferably 0.1% to 2% by weight based on the total weight of the composition of the active ingredient. One particularly convenient procedure, is to prepare a shampoo composition containing an effective amount of the active ingredient, and to utilize the shampoo for daily washing of the hair and scalp. For the purposes of this description, shampoos may be considered as pharmaceutical compositions. SUBSTITUTE SHEET AITC may be used in dilute solution in water, but because of its low solubility in this carrier it will be generally employed in liquid compositions which are mixtures of water and a water miscible alkanol such as methyl, ethyl, propyl or isopropyl alcohol. For creams and lotions, AITC may be compounded with vaseline, petrolatum, hydrocarbon waxes, vegetable oils such as safflower, almond or peanut oil, or other inert, pharmaceutically acceptable carriers. The compositions may contain other active ingredients such as antiseptics, germicides or anti-dandruff compounds. It has been found that direct application of AITC to the human scalp assists in the prevention of hair loss as determined by measuring newly grown hair length, diameter and cuticle by light microscopy. In one study used to determine the effectiveness of AITC, the compound was used in a 1:1 water isopropyl alcohol solution at a concentration of 0.01% by weight. It was administered to 35 different human subjects with a hair loss problem. It was found that 20 of the 35 subjects showed definite improvement. There were no toxic manifestations from the use of the AITC even after the sixty day study. The following non-limiting examples are given by way of illustration only. EXAMPLE I A liquid composition useful for inhibiting hair, loss is prepared by dissolving 0.5 ml. or AITC in 100 ml. of 70% ethanol-water. EXAMPLE II An ointment composition of the invention is prepared by thoroughly mixing the following ingredients: SUBSTITUTE SHEET AITC 10 mg. WHITE PETROLATUM 510 mg. WATER 400 mg. METHYL PARABEN 1.0 mg. PROPYL PARABEN 0.02 mg. MINERAL OIL 50 mg. EXAMPLE III Twenty-seven patients, ten male and seventeen female, ages 17-77 with hair loss were evaluated for reduction in hair loss using allyl isothiocyanate in 2:1 ethanol-water at a concentration of 1.5% by weight. Procedure: A small amount was applied to scalp nightly and gently massaged. Results: Evaluations were made by the patient and examiner and rates as: 0 - no change, 1+ - less hair loss, 2+ - much less hair loss and 3+ - no further hair loss. 1) Ten subjects (8 female, 2 male) used the mixture for one month. Of these, 6 were 0, 3 were 1+ and 1 was 3+. 2) Five subjects (3 female, 2 male) used the mixture for two months. Of these, 3 were 0, 1 was 1+ and 1 was 3+. 3) Four subjects (1 female, 3 male) used the mixture for three months. Of these 1 was 0, 1 was 2+ and 2 were 3+. 4) One subject (female) used the mixture for four months. This patient was 2+. 5) Three subjects (1 female, 2 male) used the mixture for five months. 1 was 2+ and 2 were 3+. 6) Four subjects (3 female, 1 male) used the mixture for six months. Of these, 1 was 0, 1 was 2+ and 2 were 3+. SUBSTITUTE SHEET No adverse reactions were observed. One patient complained of "stinging". Summary: 1 ) Fifteen patients used the mixture for 1-2 months. Of these, 9 were 0, 4 were 1+ and 2 were 3+. 2) Twelve patients used the mixture for 3-6 months. Of these, 2 had no change (0), 4 had moderate reduction in hair loss (2+) and 6 had no further hair loss (3+). The results are summarized in the following table-. TABLE FEMALE Duration of Use (Months) One Tvo Three Four Five Six Age Result Age Result Age Result Age Result Age Result Age Result 77 1+ 70 1+ 36 0 58 2+ 70 3 41 0 33 0 50 3+ 70 3+ 45 0 32 0 70 2+ 40 1+ 40 0 65 0 50 0 63 3+ MALE 31 0 35 0 28 3+ 34 3+ 49 3+ 50 1+ 17 0 33 2+ 25 2+ 33 3+ SUBSTITUTE SHEET

Claims: WHAT IS CLAIMED IS: 1. A pharmaceutical composition for the inhibition of hair loss from the human scalp which comprises from 0.01% to 5% by weight of allyl isothiocyanate together with a pharmaceutically acceptable carrier in ointment form. 2. A composition of Claim 1 containing from 0.1% to 2% by weight of allyl isothiocyanate. 3. A composition of Claim 1 wherein the pharmaceutical carrier is an aqueous liquid. 4. A composition of Claim 1 wherein the pharmaceutical carrier is a viscous base. 5. A method of inhibiting hair loss from the human scalp which comprises topical application of an amount of allyl isothiocyanate which is effective for that purpose. 6. A method of Claim 5 wherein the allyl isothiocyanate is applied in a liquid composition containing from 0.01% to 5% by weight based on the weight of the composition of allyl isothiocyanate. 7. A method of Claim 5 wherein the allyl isothiocyanate is applied in a viscous base containing from 0.01% to 5% by weight based on the weight of the composition of allyl isothiocyanate. 8. A method of Claim 5 wherein the allyl isothiocyanate is applied in a viscous base containing from 0.1% to 2% by weight based on the weight of the composition of allyl isothiocyanate. SUBSTITUTE SHEET

Inventors: DARKO LASZLO L, DARKO, LASZLO, L.
Applicants: FARMACON INC, FARMACON, INC.
Application year: 1986
Main classification: A61K31
IPC codes: A61K8, A61K31, A61Q5, A61Q7