紫杉醇新型制剂及临床研究进展  

Advances in clinical research of new formulation of paclitaxel

作　　者：徐佳茗 夏学军[1] 刘玉玲[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所,“药物传输技术及新型制剂”北京市重点实验室,北京100050

出　　处：《实用药物与临床》2016年第4期510-517,共8页Practical Pharmacy and Clinical Remedies

摘　　要：紫杉醇是一种临床应用广泛的广谱抗肿瘤药物,其独特的阻碍微管蛋白解聚的作用机制使其对多种实体瘤具有良好的疗效。但由于紫杉醇的水溶性极低,早期上市的传统制剂采用了高浓度的聚氧乙烯蓖麻油（Cremophor EL）作为增溶剂,后者易引发一系列过敏反应,用药前需进行脱敏处理,严重限制了紫杉醇的临床使用,同时给患者带来极大的痛苦。不含Cremophor EL的紫杉醇新制剂的开发多年来持续受到国内外的广泛关注,其中成功上市的有紫杉醇脂质体（力扑素~）、注射用白蛋白结合型紫杉醇（Abraxane~）和紫杉醇聚合物胶束Genexol~-PM,进入Ⅰ~Ⅲ期临床研究的有脂质体LEP-ETU、阳离子脂质体EndoTAG~-1、胶束化纳米粒NK105和新型口服制剂DHP107。本文对上述新型制剂的特点及临床研究进展进行回顾和综述。Objective Paclitaxel is a widely used broad spectrum antitumor drug in clinical treatment.Its specific mechanism of anti-cancer,which is inhibiting depolymerization of microtubules,makes it efficient in various solid tumors.However,Cremophor EL has always been used as solubilizer in the market because of the poor aqueous solubility of paclitaxel.Premedication to prevent a series of side effects caused by Cremophor EL is necessary,which has severely restricted the use of paclitaxel and brought patients great suffering.Recently,various new formulations of paclitaxel without Cremophor EL have been developed and have been given widespread attention at home and abroad for years.Among them,liposomal paclitaxel formulation（Lipusu~）and albumin-bound paclitaxel（Abraxane~）have already been on the market,meanwhile,other formulations,such as paclitaxel encapsulated in liposomes（LEP-ETU）,cationic liposomes（EndoTAG~-1）,polymeric micelles（Genexol~-PM）or micellar nanoparticles（NK105）and oral paclitaxel formulation（DHP107）,are being studied in Phase Ⅰto Phase Ⅲ.In this article,the characteristics and research advances of these formulations of paclitaxel are reviewed.

关 键 词：紫杉醇 脂质体 白蛋白结合型紫杉醇 阳离子脂质体 聚合物胶束 

分 类 号：R979.1[医药卫生—药品]