中文摘要：

【目的】建立中药XJ复方（由制草乌、当归、地龙、乳香、没药等组成）全粉末缓释片混悬液的取样方法及其体外释放度的评价方法。【方法】取样采用注射器冲混悬液的方法,使其粉末均匀分布于混悬液中取得均匀的样品;释放度评价采用浆法,以水为溶出介质,100 r/min,以高效液相色谱法测定累积溶出百分率,绘制XJ的累积溶出曲线,并进行样品的释放度评价。【结果】以10 m L注射器冲混悬液5次并于液面以下2/3位置作为最佳取样方法;在溶出2、4、8 h取出片剂后的0~15 min,峰1、峰2、峰3的释放基本符合Ritger-Peppas释放模型;体外释放溶蚀为主,溶散的粉末、颗粒释放约15min,取出粉末前即片剂总释放2~6 h符合零级方程,除去溶散的粉末后片剂溶蚀释放符合Higuchi方程。片剂溶出8 h累计溶出百分率达97.47%。【结论】全粉末XJ复方缓释片的释放属于溶蚀—溶散过程,实现了均衡释放,建立的方法可用于XJ体外释放度的评价。

英文摘要：

Objective To establish a method for sampling suspension of XJ Compound whole powder sustainedrelease tablets and for assaying its release rate in vitro. Methods The homogeneous sample with the powder being evenly distributed in the suspension was achieved by injector suction and irrigation method. With water as dissolvent, slurry method was performed at 100 r/min, and then high performance liquid chromatography was used for the detection of the cumulative dissolution percentage. We drew the XJ cumulative dissolution curve based on the obtained data, and then evaluated the release rate. Results The optimal sampling method was rinsing the suspension 5 times with 10 m L syringe and sampling at 2/3 below the liquid level. The release of peak 1,peak 2,and peak 3 during 0-15 min after the tablets were dissolving for 2,4,8 h fit the Ritger-Peppas release model. The release in vitro was in dissolution mode, and the release time for the powder and granules was about 15 min. The total release rate for the tablets within 2-6 h before the powder was taken out conformed to zero equation, and the tablet dissolution release rate after removing dissolved loose powder was accorded with Higuchi equation. The cumulative dissolution percentage reached to 97.47% after the tablets dissolved for 8 h. Conclusion The release of whole powder XJ compound sustained-release tablets was in dissolution-diffusion process, and the process can ensure a balanced release. The established method can be applied for the evaluation of the in-vitro release of XJ tablets.