肝动脉栓塞用原位植烷三醇液晶体外释放行为的研究  

In vitro Drug Release Characteristics of in situ Phytantriol Liquid Crystalline for Hepatical Arterial Embolization

作　　者：韩珂[1,2] 董怡萱[1] 王周华[1] 彭新生[1,3] 谭银合[1] 吴传斌[1] 

机构地区：[1]中山大学药学院,广州510006 [2]广州医学院第二附属医院,广州510260 [3]广东医学院药学院,广东东莞523808

出　　处：《中国药学杂志》2012年第3期213-217,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(81001643/H2806)

摘　　要：目的考察原位植烷三醇液晶的体外药物释放特点,评价其作为肝动脉介入治疗中化疗药物载体的可行性。方法以多西紫杉醇为模型药物,采用透析袋法考察处方组成、载药量、碘化油及释放条件对体外释放的影响,并考察此栓塞材料的弹性张力。结果原位植烷三醇液晶的体外释放行为符合Higuchi模型,摇床转速对释放无影响,但处方组成及载药量的改变均会引起药物释放速率的变化,且碘化油形成的外油相在一定程度上可缓解原位植烷三醇液晶的突释;另外,流变学结果显示,植烷三醇液晶可承受的最大压强为(3 070±2.135)Pa。结论原位植烷三醇液晶可缓释药物达30 d,抗压弹性较好,有望作为抗肿瘤药物载体应用于临床肝动脉介入治疗以取得局部化疗和物理栓塞的综合治疗效果。OBJECTIVE To investigate the in vitro drug release characteristics of in situ phytantriol liquid crystalline for hepati- eal arterial embolization. METHODS The release study was conducted using dialysis membrane tubing. The influences of initial compositions of in situ phytantriol liquid crystalline, drug loading, iodinated oil and rotation speed on dissolution behaviour were inves- tigated respectively using docetaxel as the model drug. Moreover, the elasticity of phytantriol liquid crystalline was investigated by rheo- logical measurement. RESULTS The in vitro release profile could be described by Higuchi model. No significant difference in drug release behaviour was observed under different rotation speed. Nevertheless, the drug release rate decreased with increasing drug load-ing and phytantriol content. Furthermore, iodinated oil was found to relive the burst effect to a certain extent. And the maximal pres- sure load of phytantriol liquid crystalline was （ 3 070 ±2. 135 ） Pa. CONCLUSION The in situ phytantriol liquid crystalline can sus- tainedly release drug for up to 30 d and has good elasticity, which suggests that the in situ phytantriol ]iquid crystalline can be hopefully applied in clinic for combination of embolization and chemotherapy.

关 键 词：植烷三醇 液晶 体外释放 多西紫杉醇 

分 类 号：R944[医药卫生—药剂学]