Sustained-release injection containing nitrosourea drugs

Abstract

The invention provides a sustained-release injection containing nitrosourea drug (galamustine), which contains sustained-release microspheres and solvents. The sustained-release microspheres each comprise an anticancer-active component selected from nitrosourea drugs (such as nimustine and carmustine) and / or topoisomerase inhibitors, and a sustained-release agent. The solvents are common solvents or special solvents containing suspending agent. The viscosity of the suspending agent ranges from 100cp to 3000cp (at a temperature ranging from 20 DEG C to 30 DEG C). The suspending agent is selected from sodium carboxymethylcellulose and the like. The sustained-release agent is selected from p(LAEG-EOP) or p(DAPG-EOP) or other polyphosphate ester copolymers, or copolymer or blend of polyphosphate ester and PLA, polifeprosan, PLGA or poly(erucidic acid dipolymer-sebacic acid). The topoisomerase inhibitor is selected from camptothecin, hydroxycamptothecine, topotecan, lartotecan, irinotecan, etoposide or teniposide. The anticancer composition is also available in the dosage form of sustained-release implant, can retain the effective drug concentration for more than 60 days after intratumoral or local injection or implantation, can obviously reduce the systemic reaction to the drug, and can selectively enhance the curative effect of non-operative treatments such as radiotherapy and chemotherapy.

Description

(1) Technical field

[0001] The invention relates to a slow-release injection containing nitrosourea drugs and topoase inhibitors and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology

[0002] As a class of commonly used chemotherapeutic drugs, nitrosourea drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs.

[0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "Intratumoral placement of camptothecin plus systemic camptothecin in the treatment of brain tumors in rats" "Journ...