Treatment of hair loss

Abstract: The invention concerns the use of a compound selected from the group consisting of dicarboxylic acids having 7 to 13 carbon atoms, mercapto derivatives thereof and salts thereof for the manufacture of a medicament for the topical treatment of skin suffering from inflammatory or hormone hair loss.

Description: BACKGROUND AND SUMMARY OF THE INVENTION This invention relates to the use of dicarboxylic acids having 7 to 13 carbon atoms for the manufacture of a medicament for treatment of hair loss resulting from inflammation or hormonal anomalies. In particular, this invention is directed toward conditions involving inflammation or hormonal involution of hair follicles including such dermatoses as alopecia areata and male pattern baldness. The present invention resides in the discovery that certain dicarboxylic acids are effective in the treatment of these conditions, and represents a departure from the types of skin conditions on which such acids have previously been disclosed as effective. U.S. Patents Nos. 4,292,326 (Nazarro-Porro, September 29, 1981) and 4,386,104 (Nazarro-Porro, May 31, 1983) disclose the use of dicarboxylic acids in the treatment of acne and melanocytic hyperpigmentary dermatoses. Acne is a sebaceous gland abnormality with inflammatory papules, pustules, and cysts and noninflammatory comedos. It afflicts teenagers and young adults. Melanocytic hyperpigmentary disorders are noninflammatory conditions involving an excess of melanin formation in the skin. The producing cells may be benign, premalignant, or malignant. Hair loss results from a variety of diseases including inflammatory conditions like alopecia areata and hormone hypersensitivity like male pattern baldness. In general, the invention applies to alopecias resulting from inflammatory disease states or from hormonal abnormalities. DETAILED DESCRIPTION OF THE INVENTION The dicarboxylic acids of the present invention are those having 7 to 13 carbon atoms, inclusive. Preferred such acids are saturated aliphatic acids, particularly straight-chain species. Those having 8-10 carbon atoms are the most preferred. Examples include azelaic (1,9-nonanedioic) acid, suberic (1,8-octanedioic) acid, sebacic (1,10-decanedioic) acid, and pimelic (1,7-heptanedioic) acid. The invention also extends to mercapto derivatives of such acids, including mono- and dimercapto derivatives, as well as salts such as, for example, sodium. The compounds are generally applied in dermatological formulations. These include any of the various known mixtures and combinations which may be applied topically and which will permit even spreading of the active ingredient over the affected area. Examples include creams, lotions, solutions, ointments and unguents. The concentration of the dicarboxylic acid in the formulation is not critical and may vary over a wide range. The acid concentration may indeed range as high as the upper limit of dissolvability in any given formulation. In most cases, however, best results are achieved within a range of 2% to 40% by weight, preferably from 15% to 20% by weight. The formulation may contain additional ingredients on an optional basis, including both those which are biologically active and those which are biologically inactive. Keratolytic agents are particularly useful in some cases as added active ingredients. Examples are salicylic acid, sulfur and retinoid derivatives. Optional concentrations will vary among keratolytic agents. Salicylic acid, for example, is preferably used at 0.5% to 5.0%, while sulfur is preferably used at 2.0% to 10.0%. Appropriate concentration ranges for any particular keratolytic agent will be apparent to those skilled in the art. Examples of inactive ingredients are wetting agents, surfactants, emollients, and solvents. The term "therapeutically effective amount" is used herein to denote any amount which will cause a substantial improvement in a disease condition (such as a subsidence of a lesion, for example) when applied to the affected area repeatedly over a period of time. The amount will vary with the condition being treated, the stage of advancement of the condition, and the type and concentration of formulation applied. Appropriate amounts in any given instance will be readily apparent to those skilled in the art or capable of determination by routine experimentation. The compositions are generally applied in topical manner to the affected area, i.e., localized application to the skin region where the inflammation or abnormality is manifest. The following examples are offered for illustrative purposes. EXAMPLE 1 - FORMULATION Formulation A: One pound of Cetaphil cream and 90 grams of azelaic acid were heated separately until each was liquified (approximately two hours). Cetaphil cream is a commercially available nonprescription mixture of water, ethyl alcohol, propylene alcohol, sodium lauryl sulfate, stearyl alcohol, methylparaben, propylparaben and butylparaben obtainable from Owen Laboratories, San Antonio, Texas. Once the cream and acid were liquified, the acid was slowly beat into the cream to form a smooth homogeneous cream. EXAMPLE 2 - APPLICATION Individual patients suffering from male pattern baldness and alopecia areata used Formulation A for 12 weeks three times daily. Spotty terminal hair growth developed. The new growth occurred in the region of most recent hair loss.

Claims: Use of a compound selected from the group consisting of dicarboxylic acids having 7 to 13 carbon atoms, mercapto derivatives thereof and salts thereof for the manufacture of a medicament for the topical treatment of skin suffering from inflammatory or hormone hair loss. Use in accordance with claim 1 in which said dicarboxylic acids are straight-chain. Use in accordance with claim 1 in which said dicarboxylic acids are straight-chain and contain 8 to 10 carbon atoms. Use in accordance with claim 1 in which said compound is a straight-chain dicarboxylic acid having 8 to 10 carbon atoms. Use in accordance with claim 1 in which said compound is selected from the group consisting of azelaic acid, mercapto derivatives thereof and salts thereof. Use in accordance with claim 1 in which said compound is azelaic acid. Use in accordance with claim 1 in which said compound is in the form of a dermatological formulation of which said compound comprises from 2 % to 40 % by weight. Use in accordance with claim 1 in which said compound is in the form of a dermatological formulation of which said compound comprises from 15 % to 20 % by weight. Use in accordance with claim 1 in which said compound is in a form selected from the group consisting of a cream, an unguent, an ointment and a solution. Use in accordance with claim 1 in which said compound is in the form of a dermatological formulation further comprising a therapeutically effective amount of a keratolytic agent. Use in accordance with claim 1 in which said compound is in the form of a dermatological formulation of which said compound comprises from 15 % to 20 % by weight and which further comprises a keratolytic agent. Use of a compound selected from the group consisting of straight-chain dicarboxylic acids having 7 to 13 carbon atoms, mercapto derivatives thereof and salts thereof for the manufacture of a dermatological formulation containing from 2 % to 40 % by weight of said compound for the topical treatment of skin suffering from hair loss from inflammatory or hormonal disease conditions. Use of azelaic acid for the manufacture of a dermatological formulation containing from 15 % to 20 % by weight of said compound for the topical treatment of skin suffering hair loss resulting from inflammatory or hormonal anomalies.

Inventors: THORNFELDT CARL RICHARD, THORNFELDT, CARL RICHARD
Applicants: CELLEGY PHARMA INC, CELLEGY PHARMACEUTICALS, INC.
Application year: 1987
Main classification: A61K7
IPC codes: A61Q19, A61K31, A61K8, A61Q7