| 白术黄连微丸结肠靶向胶囊的制备及体外释放研究 |
| 投稿时间：2020-08-13 修订日期：2021-01-13 点此下载全文 |
| 引用本文：唐晓萌,骆锦前,汪五清,顾永卫,刘继勇.白术黄连微丸结肠靶向胶囊的制备及体外释放研究[J].药学实践杂志,2021,39(1):29~34 |
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| 基金项目:上海市科委生物医药领域科技支撑项目（18401931500），上海市卫生局中医药科研基金项目（2012L073A） |
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| 中文摘要:目的 将中药“白术黄连方”制备成以胃溶微丸和肠溶微丸为基础的结肠靶向胶囊，优化其处方组成和制备工艺，考察其体外释放特性。方法 采用单因素实验和正交实验法优化微丸的处方组成和工艺参数。用挤出-滚圆技术制备素丸，流化床底喷方式进行包衣，考察隔离衣增重、肠溶衣中聚合物比例、增塑剂用量和包衣增重对肠溶微丸释放行为的影响，并对其释药行为进行模型拟合。结果 最终确定胃溶微丸的处方为：载药量50%，交联聚维酮(PVPP)5%，微晶纤维(MCC)：乳糖=2∶1，润湿剂40%；工艺参数为：挤出速度20 Hz，滚圆速度500 r/min，滚圆时间5 min。肠溶微丸的处方为：载药量27%，PVPP 5%，MCC：乳糖=5∶2，润湿剂30%，粘合剂20%；工艺参数为：挤出速度20 Hz，滚圆速度700 r/min，滚圆时间7 min；肠溶衣处方为：EUDRAGIT® L30D-55：EUDRAGIT® FS30D=1∶2，增塑剂用量10%，包衣增重15%。肠溶微丸的体外释放时间达24 h，其释放行为符合Higuchi模型。结论 成功制备了白术黄连微丸结肠靶向胶囊，肠溶微丸表现出缓释和结肠靶向的特性。 |
| 中文关键词:结肠靶向 挤出-滚圆技术 流化床包衣 体外释放 |
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| Preparation and in-vitro drug release of Baizhu Huanglian pellets containing colon-targeting capsules |
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| Abstract:Objective Colon-targeting capsules based on gastric pellets and enteric pellets were prepared from Baizhu Huanglian prescription. The formulation composition and preparation process were optimized and the in-vitro release characteristics were investigated.Methods Optimum formulation composition and process parameters of Baizhu Huanglian pellets were screened out by single factor experiment and orthogonal design. The pellets core were prepared by extrusion-spheronization technique and coated in the fluid bed using bottom spray coating technique. To investigate the effect of coating level of the isolation layer, the proportion of polymer, the amount of plasticizer and weight gain of enteric coating on the release behavior of the enteric pellets. The pellets release behavior was fitted by model as well.Results The prescription of gastric pellets was drug loading 50%, PVPP 5%, MCC to lactose 1∶2 and wetting agent 40%. The process parameters were extrusion frequency 20 Hz, rounding speed 500 r/min and rounding time 5 min. The prescription of enteric pellets was drug loading 27%, PVPP 5%, MCC to lactose 5∶2, wetting agent 30% and adhesive 20%. The process parameters were extrusion frequency 20 Hz, rounding speed 700 r/min and rounding time 7 min. For enteric coating layer, the coating mixture of EUDRAGIT®L30D-55 to EUDRAGIT® FS30D was 1∶2. The amount of plasticizer was 10%. The increased weight of coating layer was 15%. The release time of enteric pellets in-vitro was up to 24 hours. The release behavior of the pellets conforms to the Higuchi model.Conclusion The colon targeting capsule of Baizhu Huanglian pellets were successfully prepared and showed the characteristics of sustained release and colon targeting. |
| keywords:colon-targeting extrusion-spheronization technique fluid bed coating in-vitro drug release |
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