[关键词]
[摘要]
目的 制备马钱子碱固体脂质纳米粒(SLN)及其冻干粉,进一步制备成马钱子碱固体脂质纳米粒凝胶骨架缓释片(SLN-HMST),并探讨体外释药影响因素及释药机制。方法 在单因素考察的基础上设计正交试验优化马钱子碱SLN-HMST处方。分别采用零级模型、一级模型和Higuchi模型对马钱子碱SLN-HMST体外释药模型进行拟合,采用Ritger-Pappas模型探讨缓释片释药机制。结果 优化后的马钱子碱SLN-HMST体外释放行为符合一级释药模型,释药方程为ln(1-Mt/M∞)=-0.212 1 t+0.106 4(r=0.992 3),12 h内累积释放度为91.48%,具有明显的缓释特征,释药机制为扩散和溶蚀共存。结论 制备的马钱子碱SLN-HMST,工艺重复性较好,在12 h内具有良好的体外缓释作用。
[Key word]
[Abstract]
Objective To prepare brucine solid lipid nanoparticles (SLN) and its lyophilized powder, and then hydrogel matrix sustained-release tablets (HMST) of brucine SLN (SLN-HMST) were prepared. The factors that may influence drug release in vitro and release mechanism were also investigated in present study. Methods Based on single factor test, orthogonal test was designed to gain the optimum prescription. Zero-order, First-order and Higuchi models were used for the model fitting of drug release. Ritger-Pappas models were employed to study release mechanism of brucine SLN-HMST. Results Brucine SLN-HMST was better agreed with First-order kinetics model. The equation was ln(1-Mt/M∞)=-0.212 1 t + 0.106 4 (r=0.992 3). The cumulative release could achieve 91.48% in 12 h. The sustained release features were obviously. The drug release from the tablets was controlled by diffusion and degradation of the matrix. Conclusion The prepared brucine SLN-HMST can deliver drug continually for 12 h with good reproducibility.
[中图分类号]
[基金项目]
国家科技重大专项(2018ZX09201009-002-009)