黄芩苷缓释微囊的研制研究

Study on the Preparation of Baicalin Sustained-release Microcapsule

[目的]制备黄芩苷缓释微囊,设计并优化处方,初步制定该制剂的质量标准。[方法]采用复凝聚法,以明胶和阿拉伯胶为囊材,黄芩苷为囊心物,吐温-80为润湿剂制备缓释微囊。以包封率作为主要质量判定指标,通过单因素考察和正交试验优化处方工艺。借助显微镜和电镜观察微囊形态;采用紫外分光光度法进行含量测定;以水为溶出介质考察该制剂的体外溶出情况;。[结果]最优处方是明胶和阿拉伯胶浓度皆为13.3 mg/ml,反应温度为50℃,pH为3.90,材药比为5∶1。按该处方制得的微囊囊形圆整光滑,载药量较高。[结论]复凝聚法可成功制备出包封率较高的黄芩苷缓释微囊,且产品稳定性良好。该法可操作性强,重复性好,有一定的实用价值。

[Objective] To prepare sustained-release microcapsules of baicalin,design and optimize the prescription,and make initial quality standards of this preparation.[Method] A complex coacervation method was applied to prepare sustained-release microcapsules using gelatin and gum arabic as wall materials,baicalin capsule as core and Tween-80 as the wetting agent.Taking the encapsulation rate as main quality indicators,the preparation process of microcapsules was optimized by single factor experiment and orthogonal test.Microencapsulated form was observed using microscopy and electron microscopy;content was determined by ultraviolet spectrophotometry;the in vitro dissolution of preparation was investigated using water as dissolution medium.[Result] The optimum prescription process was： gelatin concentration of 13.3 mg/ml,gum arabic of 13.3 mg/ml,reaction temperature of 50 ℃,pH value of 3.90 and drug material ratio of 5∶1.The microcapsules of baicalin prepared under the above prescription were capsule-shaped and round smooth and of high drug loading.[Conclusion] The baicalin microcapsules with high encapsulation rate could be successfully prepared by complex coacervation method,and the product had good stability.This method was feasible,reproducible,and of some practical value.