| 王秀敏,叶佳丽,徐煜彬,石森林,夏哲林.大黄白芨散有效组份口服结肠定位微丸的制备及其体外释药性能评价[J].浙江中西医结合杂志,2024,34(9): |
| 大黄白芨散有效组份口服结肠定位微丸的制备及其体外释药性能评价 |
| Comparative Study on in Vitro Release Performance and Quality Evaluation of Rhein Colon Targeted Pellets |
| 投稿时间：2024-03-10 修订日期：2024-08-09 |
| DOI： |
| 中文关键词: 大黄酸 白芨多糖 结肠定位微丸 质量评价 释药性能 |
| 英文关键词:Rhein Bletilla striata polysaccharide Colon positioning pellets Quality evaluation Drug release performance |
| 基金项目:浙江省中医药科技计划项目(2023ZF195),台州市科技计划项目(22ywb36) |
|
| 摘要点击次数: 811 |
| 全文下载次数: 0 |
| 中文摘要: |
| 目的:制备大黄白芨散有效组份口服结肠定位微丸，并对其体外释药性能和制剂学性质进行评价。方法:采用液相层积法制备大黄酸丸芯，以释药性能（结肠定位性能等）为评价指标，对大黄白芨散有效组份口服结肠定位微丸的包衣处方进行筛选，并进行验证性试验。同时通过释药方程拟合和f2相似因子法，以及含量测定、外观性状、粉体学表征等方法，对大黄白芨散有效组份口服结肠定位微丸体外释药性能和制剂学性质进行评价，并比较了2种不同制备工艺的结肠定位微丸的体外释放性能。结果:根据体外释药性能结果，最终确定以白芨多糖为酶触型包衣材料，包衣增重为25%，以德国罗姆公司的Eudragit S100:Eudragit L100=9:1为膜控材料，增塑剂柠檬酸三乙酯的用量为15%，抗粘剂滑石粉的用量为20%，95%乙醇为溶剂，包衣增重为25%。该大黄酸结肠靶向包衣微丸在人工胃液、小肠液中大黄酸的累积泄漏率＜15%，在人工结肠液中累积释放率达90%以上。验证试验3批次微丸f2相似因子均＞50，一致性较好，且释放机制符合Ritger-Peppas模型，并相对挤出滚圆法制备的大黄酸结肠定位微丸在结肠段释放相对更迅速。结论:筛选确定了大黄白芨散有效组份口服结肠定位微丸的制备工艺，且其具有良好体外结肠定位性能、释放相对迅速且质量稳定的特点。 |
| 英文摘要: |
| ABSTRACT：Objective：Preparation of oral colon localized pellets of effective components of dahuang baiji powder and evaluation of their in vitro drug release performance and formulation properties.Methods: Preparation of rhein pill core by liquid phase layered method,Evaluation indicators include drug release performance (colon localization performance, etc.),Screening and conducting confirmatory experiments on the coating prescription of effective components of Dahuang Baiji powder oral colon-specific pellets. At the same time, the in vitro drug release performance and formulation properties of oral colon localized pellets of effective components of dahuang baiji powder were evaluated through drug release equation fitting and f2 similarity factor method, as well as content determination, appearance characteristics, and powder characterization methods,And compared the in vitro release performance of colon targeted microspheres prepared by two different processes. Results:Based on the results of in vitro drug release performance, it was ultimately determined that bai ji polysaccharide was used as an enzyme triggered coating material, with a coating weight gain of 25%,Using Eudragit S100: Eudragit L100=9:1 from german company rom as the membrane control material, the dosage of plasticizer triethyl citrate is 15%, the dosage of anti adhesive talc powder is 20%, 95% ethanol is the solvent, and the coating weight gain is 25%.The cumulative leakage rate of rhein in the colon targeted coated microspheres in artificial gastric and intestinal fluids is less than 15%, and the cumulative release rate in artificial colon fluid is over 90%.The similarity factor of f2 in all three batches of microspheres in the validation experiment is greater than 50, with good consistency, and the release mechanism conforms to the ritger peppas model. Compared with the rhein colon-specific microspheres prepared by extrusion and rolling method, the release of rhein colon-specific microspheres is relatively faster in the colon segment. Conclusion:Screening and determining the preparation process of effective components of Dahuang Baiji powder for oral colon targeted pellets, And it has the characteristics of good in vitro colon localization performance, relatively rapid release, and stable quality. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|
