复方丹参黏附微丸与普通微丸中隐丹参酮与丹参酮ⅡA体外溶出对比研究

Comparative study on dissolution in vitro of cryptotanshinone and tanshinone IIA in Fufang Danshen Adhesive Pellets and Ordinary Pellets

关键词:  复方丹参制剂  黏附制剂  体外溶出

Key words:  Fufang Danshen Preparation  adhesive preparation  dissolution in vitro

摘要:

[目的]建立复方丹参微丸中脂溶性成分隐丹参酮与丹参酮ⅡA含量测定方法，并对比不同工艺制备的3种复方丹参微丸（冰片包合复方丹参黏附微丸、冰片不包合复方丹参黏附微丸、普通微丸）中隐丹参酮与丹参酮ⅡA体外溶出度的差异。[方法]采用高效液相色谱（HPLC）法测定3种复方丹参微丸中隐丹参酮与丹参酮ⅡA的含量，计算溶出度，并绘制溶出度曲线，采用相似因子对比不同微丸中这两种成分的体外溶出差异性。[结果]丹参类的脂溶性成分累积溶出度均较低。其中，两种黏附微丸隐丹参酮溶出行为较为相似，24 h的累积溶出度均在40%左右，普通微丸中隐丹参酮的溶出行为与黏附微丸具有明显的差异性，其累积溶出度为64.05%。两种黏附微丸的隐丹参酮溶出更符合Higuchi方程，普通微丸更符合Peppas模型，n<0.43，均符合Fickian扩散。3种制剂中丹参酮ⅡA的溶出过程均较缓慢，3个制剂的溶出行为比较相似，累积溶出曲线接近重合，3种制剂的累积溶出度基本一致，均在40%左右。3种微丸更符合Higuchi方程，同样属于Fickian扩散。[结论]黏附微丸具有一定的缓释效果，丹参类脂溶性成分中，由于溶出度的限制，体外溶出实验评价隐丹参酮缓释效果更为明显。

Abstract:

[Objective] To establish a method for the determination of cryptotanshinone and tanshinone ⅡA in Fufang Danshen Pellets,and compare the dissolution in vitro of them in three kinds of Fufang Danshen Pellets prepared by different techniques (borneol included Fufang Danshen Adhesive Pellets,borneol excluded Fufang Danshen Adhesive Pellets,and Fufang Danshen Pellets).[Methods] The contents of cryptotanshinone and tanshinone ⅡA in three formulations were determined by HPLC. Dissolution was calculated and the dissolution curve was plotted. Similar factors were used to compare differences ofthe dissolution in vitro in three kinds of pellets.[Results] The cumulative dissolution of cryptotanshinone and tanshinone ⅡA was low. The dissolution behaviors of cryptotanshinone in two adhesive pellets were similar,the cumulative dissolution rate of 24 h was about 40%.The dissolution behavior of cryptotanshinone in normal pellets was significantly different from that of adhesive pellets,and its cumulative dissolution was 64.05%.The dissolution of cryptotanshinones in two adhesivet pellets was more in line with the Higuchi equation and the Peppas model normal pellets,n<0.43,which are consistent with Fickian diffusion. The dissolution behavior of tanshinone ⅡA in the three preparations was similar,and the cumulative dissolution curve was close to coincidence. The cumulative dissolution of tanshinone ⅡA were all about 40%. The dissolution were more in line with the Higuchi equation,consistent with Fickian diffusion,too.[Conclsion] Adhesive pellets have a certain sustained release effect. Among the fat-soluble components of Salvia,dissolution experiments in vitro showed that the sustained release effect of cryptotanshinone was more obvious,due to the limitation of dissolution.