LACTONE STABLE FORMULATION OF CAMPTOTHECIN OR 7-ETHYL CAMPTOTHECIN.

摘要

Camptothecin (CPT) and 7-ethyl camptothecin (ECPT), are poorly soluble in water. Because of their poor water-solubility, they have not been directly administered by parenteral or oral routes in human patients for the purpose of inhibiting the growth of tumors. The invention provides a pharmaceutically acceptable formulation in the form of an acidic solution or suspension comprising (1) CPT or ECPT, preponderantly in the desired lactone form (1a') (wherein R is hydrogen or ethyl) and (2) dimethylisosorbide or dimethylacetamide.