白杨素固体脂质纳米粒水凝胶骨架缓释片的制备

目的制备白杨素固体脂质纳米粒水凝胶骨架缓释片。方法乳化超声-低温固化法制备固体脂质纳米粒后进一步制成冻干粉,再以HPMC 15KM为缓释材料制备水凝胶骨架缓释片。在单因素试验基础上,以HPMC 15KM用量、PEG400与PEG4000比例、PEG用量、硬脂酸镁用量为影响因素,累积释放度为评价指标,正交试验优化处方,再进行释药模型拟合。结果最优处方为HPMC K15 M用量50 mg,PEG 400与PEG 4000比例2∶1,PEG用量30 mg,硬脂酸镁用量0.5%,12 h内累积释放度为93.19%。水凝胶骨架缓释片体外释放符合一级方程(r=0.994 1),释药机制为骨架溶蚀与扩散并存。结论该方法简便可靠,可用于制备具有明显体外缓释特征的白杨素固体脂质纳米粒水凝胶骨架缓释片。

Preparation of hydrogel matrix sustained-release tablets of chrysin solid lipid nanoparticles

AIM To prepare the hydrogel matrix sustained-release tablets of chrysin solid lipid nanoparticles.METHODS The solid lipid nanoparticles were prepared by emulsification ultrasound-low temperature solidification method and then further prepared into freeze-dried powder, after which hydrogel matrix sustained-release tablets were prepared with HPMC 15 KM as a sustained-release material. With HPMC 15 KM consumption, PEG400-PEG4000 ratio, PEG consumption and magnesium stearate consumption as influencing factors, and accumulative release rate as an evaluation index, the formulation was optimized by orthogonal test, then the model fitting of drug release was performed.RESULTS The optimal formulation was determined to be 50 mg for HPMC 15 KM consumption, 2∶1 for PEG400-PEG4000 ratio, 30 mg for PEG consumption, and 0.5% for magnesium stearate consumption, the accumulative release rate within 12 h was 93.19%. The in vitro release of hydrogel matrix sustained-release tablets accorded with first-order equation(r=0.994 1), whose drug release mechanism was the coexistence of matrix corrosion and diffusion.CONCLUSION This simple and reliable method can be used for the preparation of hydrogel matrix sustained-release tablets of chrysin solid lipid nanoparticles with obvious in vitro sustained-release characteristics.