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目的:优选贯叶连翘提取物凝胶骨架缓释片的处方并考察其体外释药机制。方法:以贯叶连翘提取物中金丝桃素在不同时间点的累积释药率为综合评价指标,采用正交试验考察乳糖和MCC质量比、骨架材料及HPMC用量对处方工艺的影响。利用体外释放度试验考察缓释片的释药机制。结果:优选的处方工艺为HPMC K15M用量30%,MCC用量6.4%,乳糖用量12.6%,硬脂酸镁用量1%。贯叶连翘提取物凝胶骨架缓释片在2 h释药率15%~30%,6 h释药率40%~75%,12 h释药率>85%,释药行为符合Ritger-Peppas方程,释药过程为药物扩散和骨架溶蚀的协同作用。结论:优选的处方工艺合理、简单。制备的缓释片体外释药缓慢、平稳,药物释放机制符合释放动力学模型。
OBJECTIVE: To optimize the formulation of gel matrix sustained-release tablets of Hypericum perforatum and investigate its mechanism of drug release in vitro. Methods: The cumulative release rate of hypericin from Hypericum perforatum at different time points was taken as the comprehensive evaluation index. The effects of lactose and MCC mass ratio, matrix material and HPMC dosage on the prescription process were investigated by orthogonal test. In vitro release test was used to investigate the release mechanism of sustained-release tablets. Results: The optimal prescription was HPMC K15M 30%, MCC 6.4%, lactose 12.6% and magnesium stearate 1%. Hypericum perforatum extract gel matrix sustained-release tablets in 2 h release rate of 15% to 30%, 6 h release rate of 40% to 75%, 12 h release rate of> 85%, release behavior in line with Ritger-Peppas equation , Drug release process for the synergy of drug diffusion and skeleton erosion. Conclusion: The preferred prescription process is reasonable and simple. The sustained-release tablets prepared in vitro release slow, smooth, drug release mechanism in line with the release kinetic model.