Slow released anticancer medicine preparation with both amrubicin and its synergist

Abstract

The slow released anticancer medicine injection containing both amrubicin and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent carboxymethyl cellulose, etc. and with viscosity of 100-3000 cp at 25 deg.c. The effective anticancer component is amrubicin, idarubicin, etc and / or antimetabolite composition selected from carmofur, tegafur, zalcitabine, etc. The slow releasing supplementary material is selected from EVAc, sebacic acid copolymer, lactic acid polymer, etc. The slow released microsphere may be also prepared into slow released implanting agent set around or inside the tumor to strengthen the chemotherapy or radiotherapy effect.

Description

(1) Technical field

[0001] The invention relates to an anticancer drug sustained-release agent loaded with amrubicin and its synergist, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing amrubicin and / or its synergist, mainly slow-release injections and slow-release implants. (2) Background technology

[0002] As a new anticancer drug, amrubicin ((+)-(7S, 9S)-9-acetyl-9-amino-7-[(2-deoxy-β-D-erythro-pyranpental (sugar)oxyl]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-tetracenedione) showed obvious therapeutic effect on solid cancer. However, in the rabbit chronic toxicity experimental model, the cardiotoxicity (Invest.New Drug, 15,219-225 (1997)) shown by anthracycline compounds such as amrubicin and doxorubicin has greatly limit its clinical application. In addition, many anthracyclines exert their antitumor effects through their metabolites. For example, amrubicin is easily reduced ...