儿黄缓释双层栓的体外释药特性研究

In vitro release characteristics of Double-layered Erhuang Sustained-release Suppository

目的建立儿黄缓释双层栓(儿茶、黄连、白及、明矾)体外释放度的测定方法。方法黄连乙醇提取液入双层栓外层中,儿茶、白及水提取液和明矾入内层,HPLC以小檗碱和儿茶素为指标分别测定黄连生物碱(小檗碱、巴马汀、表小檗碱、和黄连碱)和儿茶多酚(儿茶素和表儿茶素)累计释放量,并对数据进行方程拟合。结果在500 mL 0.1 mol/L HCl溶液为释放介质,微孔滤膜为包裹材料和转篮转速100 r/min时,黄连生物碱在4 h内累积释放100%;儿茶多酚在12 h内释放完全。各成分体外释药行为均符合零级方程,且无明显突释现象。结论儿黄缓释双层栓能避免配伍生成沉淀而影响制剂的成型性,建立的释放度测定方法简单易行,重复性好。

AIM To establish the dissolution method of Double-layered Erhuang Sustained-release Suppository （ Catechu, Coptidis Rhizoma , Bletillae Rhizoma and Alumen） （EHSRS） and to evaluate its in vitro release char- acteristics. METHODS The outer layer of the suppository contained an alcoholic extract of Coptidis Rhizoma and the inner layer held the rest of the herbs. Berberine and catechinic acid were the markers for the determination of the cumulative releasing quantity of both coptidis alkaloids （berberine, palmatine, epiberberine, and eoptisine） and cateehu polyphenol （catechinic acid and epicateehin）. Obtained data of the dissolution profiles were fitted. RESULTS With hydrochloric acid solution （500 mL 0. 1 mol/L） as release medium, millipore filter as packing material at rotation rate of 100 rpm, eoptidis alkaloids and eatechu polyphenol gained their 100% cumulative re- leased quantity at 4 h and in 12h, respectively. Both dissolution profiles fitted to Zero-order equation without burst release. CONCLUSION The double-layered design can avoid the insolubility of preparation due to interaction among the herbs. The established method is simnle and feasible_