紫杉醇新型制剂及临床研究进展

发布时间：2018-05-14 23:34

  本文选题：紫杉醇 + 脂质体　； 参考：《实用药物与临床》2016年04期

【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~汶)、注射用白蛋白结合型紫杉醇(Abraxane~汶)和紫杉醇聚合物胶束Genexol~汶-PM,进入Ⅰ~Ⅲ期临床研究的有脂质体LEP-ETU、阳离子脂质体EndoTAG~汶-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。
[Abstract]:Paclitaxel is a widely used broad-spectrum antitumor drug. It has a good effect on many solid tumors due to its unique mechanism of blocking tubulin depolymerization. However, due to the extremely low water solubility of paclitaxel, the traditional formulations that were put on the market in the early stage used high concentration of polyoxyethylene castor oil (Cremophor ELL) as the solubilizing solvent, the latter could easily cause a series of allergic reactions and should be desensitized before medication. It severely limits the clinical use of paclitaxel and causes great pain to patients. The development of taxol new preparation without Cremophor El has been paid more and more attention at home and abroad for many years. Among them, paclitaxel liposomes (paclitaxel liposome, albumin bound paclitaxel Abraxane- Wen for injection) and paclitaxel polymer micelle Genexol-Wen-PMwere successfully listed. There were liposome LEP-ETU, cationic liposomes in stage 鈪，

本文编号：1889990