Rapamycin-containing pharmaceutical composition

Abstract

A method of producing a rapamycin-containing composition for treating skin disease, which comprises the steps of dissolving rapamycin in an ethanol-containing solvent, adding a gelling and / or thickening agent to the resulting rapamycin-containing solution, and adjusting the pH of the resulting rapamycin-containing composition to 5.5 to 6.1 with triethanolamine or tris(hydroxymethyl)aminomethane (TRIS) is provided. A method of inhibiting degradation of rapamycin in a rapamycin-containing composition for treating skin diseases, wherein the method comprises the step of adjusting the pH of the composition to 5.5 to 6.1 with triethanolamine or tris(hydroxymethyl)aminomethane is also provided. A rapamycin-containing composition for treating skin diseases comprising (i) rapamycin, (ii) carboxylic acid-containing aqueous polymer, and (iii) at least one pH adjuster selected from triethanolamine and tri(hydroxymethyl)aminomethane, having a pH of 5.5 to 6.1 is also provided. The carboxylic acid-containing polymer may be carboxy vinyl polymer (carbomer), carboxymethyl cellulose or carboxyethyl cellulose. The skin disease may be dermatitis, contact dermatitis, psoriasis, atopic dermatitis, seborrheic dermatitis, nummular eczema, vitiligo, keloids, autosensitised dermatitis, stasis dermatitis, sebaceous deficiency eczema, skin tumours of tuberous sclerosis, and skin tumours of Recklinghausen’s disease. Preferred topical gels comprise rapamycin, carboxy vinyl polymer (carbomer), ethanol, water and either triethanolamine or tris(hydroxymethyl)aminomethane.

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