奥沙利铂-碘油乳剂制备比例的试验研究  

An Experimental Study of Mixture Ratio of Oxaliplatin-lipiodol Emulsion

作　　者：范芳[1] 郝明志[2] 林海澜[2] 杨琳[1] 王劲[1] 谢瑞祥[1] 

机构地区：[1]福建省肿瘤医院药理实验室,福州市350014 [2]福建省肿瘤医院介入治疗科,福州市350014

出　　处：《中国药房》2010年第41期3892-3894,共3页China Pharmacy

摘　　要：目的:研究肝动脉导管注射使用的奥沙利铂-碘油乳剂中溶媒(5%葡萄糖注射液)与碘油的较佳用量比例。方法:取50mg奥沙利铂分别溶解于0.5、1、2、2.5mL的5%葡萄糖注射液中,再分别与5mL的碘油混合后置于注射器中,用"单泵法"制备乳剂;采用普通显微镜观察乳滴分布情况,37℃观察油水分层情况,透析法进行体外释放试验,用高效液相色谱法测定透析液中奥沙利铂的浓度并计算累积释放度。结果:随着奥沙利铂-碘油乳剂中5%葡萄糖注射液比例的降低,乳滴分布趋向均匀,油水分层时间延长,缓释作用延长。二者比例为0.5∶5时,乳剂乳滴分布均匀,乳剂在放置时间超过24h时未见分层,释放慢,具有良好的物理化学稳定性。结论:奥沙利铂在葡萄糖注射液-碘油(0.5∶5)乳剂中具有稳定的物理化学性质和优良的缓释作用。OBJECTIVE：To study the optimal mixture ratio of 5% glucose injection to lipiodol in Oxaliplatin-lipiodol emulsion for hepatic artery catheter injection.METHODS：50 mg oxaliplatin were respectively dissolved in 0.5 mL,1 mL,2 mL,2.5 mL 5% glucose injection,mixed with 5 mL lipiodol and put in injector,then prepared emulsion by single pump method.Distribution of emulsion drops was observed with a regular microscope.The oil-water stratification was observed at 37 ℃.The in vitro release test was carried out by dialysis method.The concentrations of oxaliplatin in dialysate were measured by HPLC,then the accumulative release percentage was calculated.RESULTS：With the reduction of the ratio of 5% glucose injection in Oxaliplatin-lipiodol emulsion,the distribution of emulsion drops tended to uniformity,the time of oil-water stratification and release of oxaliplatin were postponed.When the ratio of glucose injection to lipiodol was 0.5：5,emulsion drops were evenly distributed,Oxaliplatin-lipiodol emulsion was set for more than 24 h while oil-water stratification hadn＇t been found;Oxaliplatin-lipiodol emulsion released slowly and had good chemicophysical stability.CONCLUSION：Oxaliplatin in glucose injection-lipiodol emulsion（0.5：5） has good chemicophysical stability and sustained-release effect.

关 键 词：奥沙利铂 碘油 5%葡萄糖注射液 乳剂 稳定性 高效液相色谱法 

分 类 号：R979.1[医药卫生—药品] R913[医药卫生—药学]