紫杉醇新剂型研究现状

紫杉醇是近几年来被广泛应用于临床的新型广谱抗肿瘤药物,但由于其水溶性差,传统注射剂把紫杉醇溶于聚氧乙烯蓖麻油与无水乙醇混合溶媒中增加水溶性,但聚氧乙烯蓖麻油在体内会产生毒副作用。用普通载体或修饰和改性的载体载药可以显著增强紫杉醇的药效或降低毒副作用,也可对紫杉醇进行改性和结构修饰以增加其水溶性,降低紫杉醇的毒副作用。本文对紫杉醇的应用现状、不良反应和紫杉醇新剂型进行综述。

Advances in development of new dosage form of paclitaxel

In recent years,paclitaxel has played a significant role in the treatment of various malignancies.However,intravenous administration of paclitaxel was hindered by poor water solubility.Paclitaxel was dissolved in a mixture of ethanol and Cremophor EL,and this formu1ation was associated with significant side effects in vivo,The efficacy of paclitaxel could be significantly enhanced and the toxicity could be reduced by the common carrier or the modified and reshaping carrier.Also,the modified and the structural modification of paclitaxel could increase its water-soluble and reduce its toxicity.The application status,adverse effects and dosage form of paclitaxel was overviewed in this article.