卡铂白蛋白微球的制备和体外性质  

Preparation of carboplatin-loaded albumin microsphere and its properties in vitro

作　　者：主皓 蒋雪涛[1,2,3] 徐风华 

机构地区：[1]总后医药管理局 [2]第二军医大学药学院药剂教研室 [3]解放军总医院药材处

出　　处：《中国药学杂志》1998年第2期91-94,共4页Chinese Pharmaceutical Journal

基　　金：总后卫生部"八五"医学科技攻关课题

摘　　要：目的：制备可生物降解的卡铂白蛋白微球。方法：以白蛋白为载体，用乳化直接加热固化法制备了卡铂白蛋白微球。结果：微球外观呈米黄色，平均粒径５８．２μｍ，药物含量（１１．２６±０．４８）％，包封率（８４．５±３．６）％。体外释放具有明显的突释效应，２ｈ后的药物释放符合零级动力学过程。其释放曲线方程为：Ｑ＝２１．９０＋８．５０ｔ（ｄ），ｒ＝０．９９５８，ｔ５０＝３ｄ。微球在４℃和３７℃贮存３个月，其外观、粒径及含药量均未见明显改变。结论：本法工艺简便，重现性好，所得微球稳定，药物包封率高，体外药物释放符合零级过程，具有较好的临床应用前景。OBJECTIVE: To prepare biodegradable albumin microspheres containing carboplatin. METHODS: Bovin serum albumin microspheres containing carboplatin were prepared by using emulsiondirect heat cross linking techniques. RESULTS: The microsphere was yellow, powdery, with a mean diameter of 58.2 μm. The microphere loaded (11.26±0.48)% carboplatin. The trapping efficiency was (84.5±3.6)%. The pattern of drug releasing from the microspheres in vitro fitted to zero order release plot, with an initial burst in the first 2 hours. The releasing rate can be expressed by the follow equation: Q=21.90+8.50 t (d), r=0.995 8. t50=3 d. Stored at 4 ℃ and 37 ℃ respectively for 3 months, the microspheres did not alter much in shape, size and drug content. CONCLUSIONS: This method is simple, reproducible, having high drug trapping efficiency. The microsphere obtained is stable and release drug at a consistant rate in vitro, leading to a prosperity in clinical use.

关 键 词：卡铂 白蛋白 微球 制备 抗肿瘤药物 

分 类 号：R979.1[医药卫生—药品] R944.9[医药卫生—药学]