姜黄素缓释微丸的制备工艺及处方优化

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目的研究姜黄素缓释微丸的制备工艺和最优处方,并对体外释药机制进行探讨。方法利用挤出滚圆法制备姜素丸芯,单因素考察和正交设计筛选最优处方,并对最优处方进行包衣。通过体外释药实验探讨释药机制。结果采用挤出滚圆法制备的姜黄素缓释微丸外观圆整。筛选的最优处方姜黄素、卡波姆、乙基纤维素、硬脂酸、微晶纤维素的比例为5∶6∶5∶3∶50。包衣干燥的最佳工艺因素为60℃,24 h。包衣处方为100 g水分散体滑石粉用量为1 g,增塑剂PEG6000为2 g,包衣增重为10%。结论通过挤出滚圆方法制备的姜黄素丸芯外观圆整,收率高。缓释微丸12 h释药量达90.54%,释放曲线符合Weibull方程。 Objective To study the preparation process of curcumin sustained-release pellets and the optimal prescription, and to explore the mechanism of drug release in vitro. Methods Ginger pellets were prepared by extrusion spheronization method, single factor test and orthogonal design were used to screen the optimal prescription, and the optimal prescription was coated. Drug release mechanism was explored by in vitro drug release experiment. Results The curcumin sustained-release pellets prepared by extrusion-spheronization method showed a round appearance. The optimal prescription of curcumin, carbomer, ethyl cellulose, stearic acid and microcrystalline cellulose was 5: 6: 5: 3: 50. The optimum drying process is 60 ℃, 24 h. The coating formulation was 100 g aqueous dispersion of talc at 1 g, plasticizer PEG6000 at 2 g, and coating weight gain at 10%. Conclusion The curcumin pellets prepared by extrusion spheronization have round appearance and high yield. The release of sustained-release pellets in 12 h was 90.54%, and the release curve accorded with Weibull equation.
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