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以牛血清白蛋白为囊材,采用喷雾干燥工艺将环丙沙星制成微球。以水溶液系统制备的白蛋白微球不含任何有机溶剂,外观呈圆球型,微球粒径在1~5 (m之间,符合干粉末肺部吸入给药的要求。以不同的环丙沙星/白蛋白比例(1:1、1:2及1:4)配制喷雾干燥样品,制得微球的载药量分别为46.93%、32.96% 和20.56% (n=3),药物的包封产率均在90% 以上。采用不同的粉末加热变性温度 (100~120 ℃) 和时间 (3~6~12 小时),对喷雾干燥制得的粉末白蛋白微球进行热变性处理,考察热变性后微球的体外释药情况,热变性程度越大,药物释放愈缓慢,说明可通过改变热变性条件调控微球中药物的释放。
With bovine serum albumin as the material of the capsule, the ciprofloxacin microspheres were made by spray drying process. Albumin microspheres prepared from aqueous solution system do not contain any organic solvents, the appearance of spherical, microspheres particle size between 1 ~ 5 (m, in line with the dry powder inhalation of lungs .Different cyclopropane The drug loadings of the prepared microspheres were 46.93%, 32.96% and 20.56% (n = 3), respectively, for the preparation of spray-dried samples with the ratios of shale / albumin (1: 1, 1: 2 and 1: 4) The encapsulation yield was over 90% .The powder albumin microspheres prepared by spray drying were heat denatured by using different heating temperature (100 ~ 120 ℃) and time (3 ~ 6 ~ 12 hours) The thermal denaturation microspheres in vitro release of the study, the greater the degree of thermal denaturation, the more slowly the drug release, indicating that by changing the conditions of heat denaturation control the release of drugs in the microspheres.