论文部分内容阅读
按正交设计筛选乳化热固化法制备顺铂白蛋白微球的最佳工艺，并对影响微球粒径大小和体外释药速率的诸多因素进行了研究。该微球粒径范围为５０．８～２５６μｍ。平均粒径为１４８．４６μｍ，药物含量为５１．１６％（Ｗ／Ｗ）。兔肝动脉栓塞后，与对照组相比铂的分布半衰期延长３３６％，消除半衰期延长１２３％，体内最高血浓仅为对照组的３０％。肝组织顺铂量显著增加（Ｐ＜０．０１），肾组织药物量明显降低（Ｐ＜０．０５），体内外相关性研究表明顺铂白蛋白微球体外累积溶出百分率与兔体内药物吸收分数呈显著相关（Ｐ＜０．０１）。
Orthogonal design was used to screen the optimum conditions for the preparation of cisplatin albumin microspheres by emulsification and thermosetting method. Many factors influencing microsphere size and in vitro release rate were also studied. The size of the microspheres is 50.8 ~ 256μm. The average particle size was 148.46 μm and the drug content was 51.16% (W / W). After hepatic artery embolization, the half-life of platinum was prolonged by 336% compared with the control group, the elimination half-life was prolonged by 123%, and the highest blood concentration in the body was only 30% of the control group. The amount of cisplatin in liver tissue was significantly increased (P <0.01), and the amount of drug in kidney tissue was significantly decreased (P <0.05). The correlation between in vitro and in vivo studies showed that the cumulative dissolution percentage of cisplatin albumin microspheres in vitro and the drug absorption in rabbits Scores were significantly correlated (P <0.01).