香连丸中内酯类成分的溶出行为及影响因素分析

Dissolution Behavior of Lactones in Xianglian Wan and Its Influencing Factors

目的:建立香连丸中内酯类成分的溶出度测定方法,揭示其体外溶出行为及关键影响因素。方法:采用小杯法,利用HPLC测定香连丸中木香烃内酯、去氢木香内酯在不同p H,搅拌桨转速和聚山梨酯-80质量分数条件下的溶出量,计算累积溶出率,绘制溶出曲线。采用软件Origin Pro 8.0对溶出曲线进行模型拟合,计算溶出参数。结果:在各种p H介质及转速条件下,香连丸中木香烃内酯、去氢木香内酯的6 h累积溶出率均<50%;当介质中聚山梨酯-80质量分数>0.3%时,2种成分的4 h累积溶出率均>90%,说明已溶出完全,且随着聚山梨酯-80质量分数的升高,2种成分的T50(溶出50%所用时间)和Td(溶出63.2%所需时间)均明显缩短,溶出速率加快。结论:香连丸中内酯类成分的体外溶出不完全,介质中表面活性剂质量分数对其溶出有较为显著的影响。

Objective： To establish a determination method for in vitro dissolution of lactones in Xianglian Wan, and reveal its dissloution behavior and key influencing factors. Method： Small cup method and HPLC were used to determine dissolution quantity of costunolide and dehydrocostuslactone from Xianglian Wan under different pH, rotational speed of stirring paddle and tween-80 concentration, cumulative dissolution rate was calculated and dissloution curves were drawn. Origin Pro 8.0 was used to fit dissolution curves with model and calculate dissolution parameters. Result： Under all pH dissolvents and rotational speeds of stirring paddle, cumulative dissolution rate of costunolide and dehydrocostuslactone in 6 hours were less than 50%. When tween-80 concentration exceeding 0.3% , cumulative dissolution rate of these two components in 4 hours both exceeded 90%. With increasing of tween-80 concentration, both T50 （the time for dissolution 50% ） and Td （the time for dissolution 63.2% ） of these two components obviously became shorter, their dissolution speeds became quicker. Conclusion ： In vitro dissolution of lactones in Xianglian Wan are not completely, the concentration of surfactant in dissolution medium has significant influence on dissolution of lactones in Xianglian Wan.