达比加群酯自微乳分散片的制备及质量评价

发布时间：2018-06-17 12:28

本文选题：达比加群酯 + 自微乳　；参考：《中国新药杂志》2017年16期

【摘要】：目的:制备达比加群酯自微乳分散片并评价其质量。方法:筛选可在45 min内完全释药的固体吸附材料,以粉末直接压片法制备自微乳分散片,通过单因素实验优化处方,考察所得自微乳分散片的质量。结果:以MCC KG 802作为固体吸附材料,能有效吸附达比加群酯自微乳液并形成固体吸附混合物(Mix)。分散片处方组成为:25%Mix,25%崩解剂PVPP,适量由4%微粉硅胶与0.5%硬脂酸镁组成的润滑剂,其余为填充剂MCC 102。制得分散片的硬度、脆碎度、分散均匀性及崩解时间均符合要求。在纯化水中分散后形成的微乳粒径为200~230 nm,与达比加群酯液体自微乳液的粒径相当。结论:自微乳分散片能较好的保持液体自微乳系统的特性,有望提高达比加群酯生物利用度,扩展了自微乳系统的应用范围。
[Abstract]:Objective: to prepare self-microemulsion dispersible tablets of Darby and group ester and evaluate its quality. Methods: Self-microemulsion dispersible tablets were prepared by direct powder pressing method. The quality of self-microemulsion dispersible tablets was investigated by single factor experiment. Results: using MCC KG802 as the solid adsorption material, the self-microemulsion of Darby and group ester could be effectively adsorbed and the solid adsorption mixture could be formed. The formulation of dispersible tablets is composed of 25% disintegrating agent PVPP5, a lubricant composed of 4% silica gel and 0.5% magnesium stearate, and the rest as filler MCC102. The hardness, brittle degree, dispersion uniformity and disintegration time of the dispersible tablets all meet the requirements. The particle size of the microemulsion dispersed in purified water is 200 ~ 230nm, which is similar to that of Darby + group ester liquid self-microemulsion. Conclusion: the self-microemulsion dispersible tablets can maintain the properties of liquid self-microemulsion system, which is expected to improve the bioavailability of Darby and group ester, and expand the application range of self-microemulsion system.
【作者单位】：上海市浦东新区周浦医院药剂科;中国药科大学药剂学教研室;江苏恒瑞医药股份有限公司;
【基金】：浦东新区科技发展基金资助项目(PKJ2015-Y41) 国家自然基金资助项目(81402878)
【分类号】：R943

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