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.