香连丸中生物碱类成分的溶出行为及影响因素分析

Dissolution Behavior and Influencing Factors Analysis of Alkaloids in Xianglian Pills

摘要:

目的: 建立香连丸中生物碱类成分的溶出度测定方法,揭示其体外溶出行为及影响因素. 方法: 采用HPLC测定盐酸小檗碱、盐酸巴马汀含量,流动相乙腈-磷酸二氢钾缓冲液(30 :70),检测波长350 nm.通过小杯法检测香连丸中盐酸小檗碱、盐酸巴马汀在不同溶出介质pH和体积、搅拌桨转速条件下的溶出曲线.运用Origin Pro 8.0软件对溶出曲线进行威布尔分布(Weibull)模型拟合,计算 T₅₀(溶出50%所用时间)和 T_d(溶出63.2%所需时间)等溶出度参数. 结果: 盐酸小檗碱、盐酸巴马汀的溶出曲线均可采用Weibull方程成功拟合.2种成分在pH 1.0介质中溶出快而完全,且随pH升高,溶出减慢且溶出率降低,当pH 6.8,7.8时,2种成分的累积溶出率均<50%.随搅拌桨转速增加,2种成分的 T₅₀和 T_d均略有降低;溶出介质体积在100~250 mL时,2种成分的 T₅₀和 T_d均无明显差异.在相同溶出条件下,盐酸巴马汀的 T₅₀和 T_d均小于盐酸小檗碱. 结论: 溶出介质pH对香连丸中生物碱类成分溶出有显著影响,搅拌桨转速对溶出速率有一定影响,介质体积则无明显影响.盐酸巴马汀的溶出略快于盐酸小檗碱.

Abstract:

Objective: To establish determination method for in vitro dissolution of alkaloids in Xianglian pills,reveal its in vitro dissloution behavior and influence factors. Method: HPLC was used to determine contents of berberine hydrochloride and palmatine hydrochloride with mobile phase of acetonitrile-potassium dihydrogen phosphate buffer (30 : 70) and detection wavelength at 350 nm.Small cup method was used to determine and draw dissloution curves of berberine hydrochloride and palmatine hydrochloride in Xianglian pills under different pH and volume of dissolution medium,rotation speed of stirring paddle.Origin Pro 8.0 was used to fit dissolution curves with Weibull distribution model and calculate dissolution parameters of T₅₀ (the time for dissolution 50%) and T_d (the time for dissolution 63.2%). Result: Dissloution curves of berberine hydrochloride and palmatine hydrochloride all fitted successfully with Weibull equation.These two components dissoved quickly and completely in dissolution medium with pH of 1.0,with increasing of pH of dissolution medium,both dissolution speed and rate decreased.When pH were 6.8 and 7.8,cumulative dissolution rate of these two components was less than 50%.With increasing of stirring speed, T₅₀ and T_dof these two components slightly decreased.In volume range of 100-250 mL,both T₅₀ and T_d of these two components had not significant difference.Under the same conditions, T₅₀ and T_d of palmatine hydrochloride were less than these two parameters of berberine hydrochloride. Conclusion: Dissolution medium pH has significant influence on dissloution of alkaloids in Xianglian pills,rotation speed of stirring paddle has a certain effect on dissolution speed,but dissolution medium volume almost has no effect.Dissloution of palmatine hydrochloride is slightly quicker than berberine hydrochloride.