FORMULATION BASE COMPRISING A POLYOXYETHYLENE/POLYOXYPROPYLENE BLOCK COPOLYMER, ETHANOL AND WATER, OPTIONALLY PHOSPHOLIPIDS AND WATER SOLUBLE EXCIPIENTS; FOR USE IN NANOSUSPENSIONS

摘要

Pharmaceutical compsn. for intravenous admin. of staurosporin deriv. (A) with low solubility in water comprises (A); a polyoxyethylene-polyoxypropylene block copolymer (B); ethanol and water as transport materials; and opt. a phospholipid of formula (I) or its salts, and/or other adjuvants. R1 = 10-20C acyl, R2 = H or 10-20C acyl, R3 = H, 2-trimethylamino-1-ethyl, 2-amino-1-ethyl, 1-4C alkyl, 1-5C alkyl substd. by carboxy, 2-5C hydroxyalkyl (opt. substd. by carboxy), 2-5C alkyl (substd. by carboxy and amino), inositol or glyceryl. Also claimed is the prepn. of the compsn. by mixing all the components to form a homogenous dispersion; and (1) adding more water and opt. adjuvants, filtering, and opt. dialysing to give a clear soln.; or (2) filtering, opt. dialysing, drying the dispersion (opt. with addn. of adjuvants) and reconstitution of the dry prepn. to an injectable dispersion. Also claimed is a nanosuspension contg. (A).