替莫唑胺局部缓释制剂的研究进展  

Advances in Locally Sustained Release Formulations of Temozolomide

作　　者：张晶晶[1] 王永峰[2] 王国成[2] 杨海龙[2] 范立君[1] 

机构地区：[1]天士力控股集团有限公司研究院专利部,天津300402 [2]天士力控股集团有限公司研究院化学所,天津300402

出　　处：《生物技术进展》2014年第4期263-267,共5页Current Biotechnology

摘　　要：近年来,为更有效地发挥替莫唑胺对神经胶质瘤的治疗活性,局部、缓释给药成为替莫唑胺的研究热点。本文简述了几种研发中的替莫唑胺的局部缓释新制剂,其中替莫唑胺-聚酸酐缓释微球(TMZ-pCPP:SA)由于聚酸酐表面溶蚀等特性,具有良好的缓释特性,鼠颅内植入试验显示,比口服替莫唑胺具有更好的治疗效果,因此替莫唑胺-聚酸酐缓释微球作为颅内缓释制剂具有极为光明的前景。In order to overcome the toxicity and side effects of systemic administration of temozolomide,locally sustained release administration of temozolomide has become the hot research topics in recent years. This paper reviewed a number of newly locally and sustained release fomulations of temozolomide. Among them,temozolomide-polyanhydrid（TMZ-pCPP：SA）,for its character of surface erosion,has the favourable sustained release property. The intracranial implantation test of rats indicated that TMZpCPP：SA had better treatment effects,less toxicity and side effects than oral administration of temozolomide. Thus,TMZ-pCPP：SA as an intracranial sustained release formulation has a bright future.

关 键 词：替莫唑胺 缓释 局部 颅内 聚酸酐 

分 类 号：R943[医药卫生—药剂学]