本文選題：紫杉醇 + 脂質(zhì)體��； 參考：《實用藥物與臨床》2016年04期

【摘要】：紫杉醇是一種臨床應(yīng)用廣泛的廣譜抗腫瘤藥物,其獨特的阻礙微管蛋白解聚的作用機制使其對多種實體瘤具有良好的療效。但由于紫杉醇的水溶性極低,早期上市的傳統(tǒng)制劑采用了高濃度的聚氧乙烯蓖麻油(Cremophor EL)作為增溶劑,后者易引發(fā)一系列過敏反應(yīng),用藥前需進行脫敏處理,嚴重限制了紫杉醇的臨床使用,同時給患者帶來極大的痛苦。不含Cremophor EL的紫杉醇新制劑的開發(fā)多年來持續(xù)受到國內(nèi)外的廣泛關(guān)注,其中成功上市的有紫杉醇脂質(zhì)體(力撲素~汶)、注射用白蛋白結(jié)合型紫杉醇(Abraxane~汶)和紫杉醇聚合物膠束Genexol~汶-PM,進入Ⅰ~Ⅲ期臨床研究的有脂質(zhì)體LEP-ETU、陽離子脂質(zhì)體EndoTAG~汶-1、膠束化納米粒NK105和新型口服制劑DHP107。本文對上述新型制劑的特點及臨床研究進展進行回顧和綜述。
[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，

本文編號：1889990