苦参碱凝胶剂的制备及体外释药特性考察

Preparation and in vitro Release of Matrine Gels

目的:优选苦参碱凝胶剂的处方工艺并考察其体外释药特性。方法:采用HPLC测定苦参碱含量,流动相乙腈-0.02 mol·L-1磷酸二氢钾溶液(6∶94),检测波长210 nm。利用动态透析法测定苦参碱凝胶剂体外释放率,以1,5,10 h累计释放率的综合评分为指标,通过正交试验考察卡波姆-940用量、苦参碱用量、氮酮用量及凝胶pH对处方工艺的影响。结果:优选的处方工艺为卡波姆-940、苦参碱和氮酮用量分别为1.0,2.0,0.5 g,pH调节至6.8;苦参碱凝胶剂在1,5,10 h内的体外累计释放率分别为(10.17±0.35)%,(74.90±0.70)%,(94.53±0.74)%。结论:优选的处方工艺稳定可行,制备的苦参碱凝胶剂具有缓释特性。

Objective： To optimize formulation process of matrine gels and evaluate its in vitro release characteristics. Method： The content of matrine was measured by HPLC, mobile phase of acetonitrile-0. 02 mol.L^-1 potassium dihydrogen phosphate solution （6： 94） , detection wavelength 210 nm. Dynamic dialysis method was adopted to determine in vitro release rate of matrine gels, taking composite score of cumulative release rates at 1, 5, 10 h as index, orthogonal test was applied to optimize formulation process with amounts of carbomer-940, matrine and azone, gels pH as factors. Result： Optimized formulation process of matrine gels was obtained, dosages of carbomer-940, matrine and azone were 1.0, 2.0, 0.5 g, respectively; Gels pH was adjusted to 6.8 eventually. In vitro cumulative release rate at 1, 5, 10 h were （ 10. 17± 0.35 ） % , （74.90 ± 0.70） % and （94.53 ±0.74）%, respectively. Conclusion： This optimized process was simple and feasible, these prepared matrine gels had sustained release properties.