目的 采用干法压制包衣法制备黄芩苷结肠靶向片。方法 根据单因素考察结果,以结肠靶向片的释药时滞和8 h累积释放度为指标,采用Box-Behnken响应面法对结肠靶向片的包衣处方进行优化。通过体外释放研究,优选包衣处方并评价其结肠靶向性。通过DDSolver软件进行释药模型拟合。结果 确定最佳的包衣处方为包衣增重110 mg,微晶纤维素和乳糖比例1∶2,瓜尔胶和填充剂比例1∶1,制备的包衣片释药时滞约6.5 h,在人工胃液和小肠液中均无释放,8 h累积释放度可达90%。黄芩苷结肠靶向片的体外释放度拟合度顺序为Logistic模型>Korsmeyer-Peppas模型>Higuch模型,Logistic模型的拟优合度(Rsqr_adj)为0.999 9,拟合度(AIC)为10.974 2,因此该结肠靶向片的释药机制为S型的溶蚀过程。结论 按Box-Behnken响应面法优选处方制备的黄芩苷压制包衣结肠靶向片,符合结肠靶向制剂的释药标准。
Abstract
OBJECTIVE To prepare baicalin colon-targeted tablets by dry pressing coating method. METHODS According to the results of single factor investigation, the coating formulation of colon-targeted tablets was optimized by Box-Behnken design-response surface methodology, with the release delay and 8 h cumulative release as indexes. Through in vitro release study, the coating formulation was optimized and its colon targeting was evaluated. The drug release model was fitted by DDSolver software. RESULTS The optimal coating formulation was as follows: the coating weight was 110 mg, the ratio of microcrystalline cellulose to lactose was 1:2, and the ratio of guar gum to filler was 1∶1. The drug release delay was about 6.5 h, and there was no release in artificial gastric and small intestine juice, and the cumulative release rate of 8 h was up to 90%. The fitting order of baicalin colon-targeted tablet in vitro release was Logistic model >Korsmeyer-Peppas model >Higuch model. The Rsqr_adj of Logistic model was 0.999 9, and the AIC of Logistic model was 10.9742. Therefore, the drug release mechanism of this colon targeted tablet was an S-type dissolution process. CONCLUSION The baicalin compression-coated colon-targeted tablets prepared according to the optimized formulation by Box-Behnken design-response surface methodology meet the drug release standards of colon-targeting preparations.
关键词
黄芩苷 /
结肠靶向片 /
Box-Behnken设计 /
干法压制包衣 /
累积释放度
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Key words
baicalin /
colon-targeted tablet /
Box-Behnken design /
dry pressing coating /
cumulative release
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中图分类号：
R944
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参考文献
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脚注
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基金
江西省杰出青年基金项目资助(20224ACB216019)
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