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盐酸普萘洛尔微球剂的制备及其质量评价
引用本文:张奇志,蒋新国,杨程.盐酸普萘洛尔微球剂的制备及其质量评价[J].中国药学杂志,1999,0(5):308-301.
作者姓名:张奇志  蒋新国  杨程
作者单位:上海医科大学药学院生物药剂学研究室,上海医科大学药学专业
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?

关 键 词:盐酸普萘洛尔  白蛋白微球  鼻纤毛毒性
收稿时间:1998-12-10;

Preparation of BSA propranolol microspheres and its quality evaluation
Zhang Qizhi.Preparation of BSA propranolol microspheres and its quality evaluation[J].Chinese Pharmaceutical Journal,1999,0(5):308-301.
Authors:Zhang Qizhi
Institution:(Zhang QZ),Jiang Xinguo(Jiang XG),Yang Cheng(Yang C),et a
Abstract: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.
Keywords:propranolol hydrochloride  albumin microspheres  ciliotoxicity
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