生物技术进展 ›› 2014, Vol. 4 ›› Issue (4): 263-267.DOI: 10.3969/j.issn.2095-2341.2014.04.06

• 进展评述 • 上一篇    下一篇

替莫唑胺局部缓释制剂的研究进展

张晶晶1,王永峰2,王国成2,杨海龙2,范立君1   

  1. 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
  • 收稿日期:2014-04-18 出版日期:2014-07-25 发布日期:2014-06-24
  • 作者简介:张晶晶,高级工程师,硕士,主要从事知识产权调研与专利维护研究。E-mail:essal@126.com

Advances in Locally Sustained Release Formulations of Temozolomide

ZHANG Jing-jing, WANG Yong-feng, WANG Guo-cheng, YANG Hai-long, FAN Li-jun   

  1. 1.Department of Patent, Tianjin Tasly Group Ltd., Tianjin 300402, China;
    2.Department of Chemical Pharmaceutical, Tianjin Tasly Group Ltd., Tianjin 300402, China
  • Received:2014-04-18 Online:2014-07-25 Published:2014-06-24

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。

关键词: 替莫唑胺, 缓释, 局部, 颅内, 聚酸酐

Abstract: 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 TMZ-pCPP: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.

Key words: temozolomide, sunstained release, locally, intracranial, polyanhydrid