去甲斑蝥素缓释片的处方优化及其体外释药特性研究

目的:优化去甲斑蝥素缓释片制备处方及考察其释药特性。方法:以羟丙基甲基纤维素(HPMC)为骨架材料制备去甲斑蝥素亲水凝胶缓释骨架片;以HPMC用量(A)、乳糖用量(B)、乙醇浓度(C)、乙醇用量(D)为因素,以体外释放度综合评分值为指标筛选缓释片的最佳处方并考察其累积释药率。结果:缓释片的最佳处方为A12g、B1.5g、C90%、D10mL;所制缓释片2、6、12h的累积释药率分别为(30.63±1.03)%、(51.70±1.51)%、(89.25±1.04)%,药物释放机制为扩散和骨架溶蚀的协同作用。结论:优化处方制备的去甲斑蝥素缓释片可以达到预期缓释效果。

Preparation and Drug Release Characteristics in Vitro of Norcantharidin Sustained - release Tablet

OBJECTIVE： To optimize the formulation of norcantharidin sustained - release tablet and investigate its in vitro release characteristics. METHODS： The tablet was prepared by using hydroxy-propyl methyl cellulose （HPMC） as the matrix material. The formulation of the tablet was optimized with the amount of HPMC （A）, the amount of lactose （B）, the concentration of ethanol （C） and the amount of ethanol （D） as factors and with the comprehensive scores of the in vitro release rate as index. Meanwhile, the in vitro release characteristics of the optimized tablets were investigated. RESULTS： The optimal formulation of the tablet was as follows： A = 12 g, B = 1.5 g, C = 90%, D = 10 mL. At 2, 6 and 12 h the cumulative release rates of the tablet reached （30.63±1.03） %, （51.70±1.51） % and （89.25±1.04）%, respectively. The mechanism for the drug release was the joint action of diffusion and bulk erosion. CONCLUSION： The optimized norcantharidin sustained- release tablet is up to the expected sustained-release efficacy.