盐酸普萘洛尔微球剂的制备及其质量评价  

Preparation of BSA propranolol microspheres and its quality evaluation

作　　者：张奇志[1,2] 蒋新国[1,2] 杨程[1,2] 邱涤非 奚念朱[1,2] 

机构地区：[1]上海医科大学药学院生物药剂学研究室 [2]上海医科大学药学专业

出　　处：《中国药学杂志》1999年第5期308-310,共3页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金

摘　　要：目的：对盐酸普萘洛尔白蛋白微球的制备工艺进行考察，并评价其质量。方法：采用乳化－热固化法制备微球，并对其形态学、载药量、体外释药等性质进行了研究，同时用在体蟾蜍上腭模型评价了其鼻纤毛毒性。结果：微球形态圆整，大小较均匀，粒径１～１０μｍ，载药量４．０５％，２４ｈ累计释药达８５．５％。给予微球４ｈ后，蟾蜍上腭７０％纤毛活动剧烈，而溶液剂给药５ｍｉｎ，纤毛全部死亡。结论：微球剂的制备工艺对其质量有较大影响，制备良好的微球剂能有效降低盐酸普萘洛尔的鼻纤毛毒性。OBJECTIVE:To study the preparation of BSA propranolol hydrochloride microspheres (PRO AM) and evaluate its quality.METHODS:The microspheres were prepared by an emulsion heat stabilization technique.The morphology of PRO AM,the drug loading and the release characteristics in vitro were studied.The effects of microspheres on ciliary movement were evaluated in vitro with toad palate model.RESULTS:The microspheres were spherical with size of 1～10μm and drug loading of 4.05%.The drug release was observed up to 85.5% within 24h.While PRO AM was applied to the upper palate of toad for 4h,more than 70% ciliary moved lively,but all ciliary died 5min after applying PRO solution.CONCLUSION:The preparation of propranolol hydrochloride microspheres seems to decrease the ciliotoxicity of PRO.

关 键 词：盐酸普萘洛尔 白蛋白微球 鼻纤毛毒性 

分 类 号：R972.3[医药卫生—药品] R944.9[医药卫生—药学]