紫杉醇新剂型的开发及临床研究进展.pdfVIP

66 2007 1 5 1 ONCOLOGY PROGRESS, Jan 2007, Vol5, No1 张晓静 张 频# , 100021 综 紫杉醇广泛用于卵巢癌乳腺癌肺癌等多种肿瘤的治疗但由于其难溶于 述 水, 溶于聚氧乙烯蓖麻油 ( cremophor EL) 与无水乙醇混合溶媒中增加水溶性, 而 cre- mophor EL 在体内降解时释放组胺, 导致不同程度的过敏反应, 亦可引起神经细胞内颗粒 释放及脱髓鞘改变而加重紫杉醇的外周神经毒性为降低毒性, 提高其疗效, 近年来临 床上陆续开发了紫杉醇的新剂型, 其中不含聚氧乙烯蓖麻油注射紫杉醇白蛋白纳米混悬 液 (ABI- 007) 已在欧美上市, 具有不用抗过敏预处理疗效较好毒性较低等特点; 现正在国内进行临床研究我国研发的紫杉醇脂质体已开始在临床应用而紫杉醇的前体药 物 ( DHA- PTX) 和聚合物剂型 enexol- PM 及 xyotax 也正在临床前和临床~ 期研究 中, 显示了良好的前景本文就紫杉醇的作用机制, 不良反应及新制剂的开发和应用进 行回顾和综述 关键词 + 中图分类号 R73- 36 1 文献标识码 A A dvances in clin ical research and developm en t of new form of paclitaxel # Zhan X iaojin Zhan P in Can cerH osp ita,l CAM S PUMC, Beijin 100021, Ch ina Ab strac t Over the past tw o decades, paclitaxel has p layed a si n ificant role in the treatmen t of va- rious mali nancies. H ow ever, intravenous adm in istration of paclitaxel is h indered by poorw ater solubility of the dru . Currently, paclitaxel is dissolved in am ixture of ethanol and Cremophor EL, and this formu- lation is associated w ith si n ificant side effects, w hich are considered to be related to the pharm aceutical veh icle, includ in clinically relevant acute hypersensitivity reactions and peripheral neuropathy, etc. A l- ternative formu lations of paclitaxelw ere developed in order to m