Stabilized and lyophilized formulation of anthracycline compounds

摘要

The present invention provides a lyophilized amrubicin formulation and a process thereof. In the process, the concentration of the aqueous solution before lyophilization is controlled to about 7.5 mg(potency)/mL or more. Thus, the formulation decreases the production of desaccharified compound and is stable to storage for a long period. The formulation is useful as a cancer chemotherapeutic agent.

主权项

1. A process for preparing a lyophilized amrubicin formulation comprising the following Steps (1) to (3):
(1) preparing an aqueous solution comprising (a) amrubicin or a pharmaceutically acceptable salt thereof and (b) L-cysteine or a salt thereof wherein the concentration of amrubicin or a pharmaceutically acceptable salt thereof is in the range of 7.5 mg(potency)/mL to 30 mg(potency)/HmL, (2) sterilizing the aqueous solution of Step (1) by filtration, and (3) lyophilizing the aqueous solution obtained in Step (2).