目的 制备白藜芦醇固体脂质纳米粒缓释凝胶骨架片,并对其释药影响因素及释药模型进行探讨。方法 采用薄膜超声分散法制备白藜芦醇固体脂质纳米粒,进一步分散于凝胶骨架片辅料中制备缓释凝胶骨架片。通过单因素考察填充剂种类、PEG种类、HPMC种类和HPMC K15用量对释药行为的影响,并采用正交试验得出最佳处方。采用零级、一级、Higuchi及Ritger-Pappas方程,对白藜芦醇固体脂质纳米缓释凝胶骨架片的药物释放进行拟合。结果 白藜芦醇固体脂质纳米缓释凝胶骨架片体外释放行为符合零级释药模型,释药方程为M_t/M_∞=0.078 7 t+0.003 6(r=0.998 0)。释药机制为骨架溶蚀机制。结论 白藜芦醇固体脂质纳米缓释凝胶骨架片处方合理,制备工艺可行,在12 h内具有良好的体外缓释作用。

Objective To prepare hydrogel matrix sustained-release tablets of resveratrol solid lipid nanoparticles, and the factors that might influence drug release and in vitro release models were also investigated in present study. Methods The resveratrol-solid lipid nanoparticles (Res-SLN) were prepared by thin-film ultrasonic dispersion method, and then the hydrogel matrix was prepared by dispersed in excipients of hydrogel matrix sustained-release tablets. Single factor analysis was used to study the effects of varieties of adhesives, PEG, HPMC, and the amounts of HPMC K15 on drug release. Then the orthogonal design was used to gain the optimum formulation. Zero-order, first-order, Higuchi, and Ritger-Pappas models were used for the model fitting of drug release. Results Hydrogel matrix sustained-release tablet of Res-SLN was better accorded with Zero-order kinetics model. The equation was M_t/M_∞ = 0.078 7 t + 0.003 6 (r = 0.998 0). In vitro release behavior was in line with Ritger-Peppas equation, and the drug release from the tablets was controlled by degradation of the matrix. Conclusion Prescription of hydrogel matrix sustained-release tablet of Res-SLN is reasonable; The preparation technology is feasible and exhibits perfect sustained-release characteristics in vitro in 12 h.

河南省科技发展计划项目(144300510019)