马来酸曲美布汀缓释片体外释放特征与体内J＇b~H关性研究

目的考察马来酸曲美布汀缓释片体外药物释放特征与体内外相关性。方法分别采用①水、②0．1mol／L盐酸、③0．01mol／L盐酸等三种溶剂作为释放介质，考察释放介质对释放度的影响。用Wagner—Nelson方程法计算马来酸曲美布汀缓释片在健康男性受试者体内吸收百分数，并与相应时间体外累积释放度线性回归，进行体内外相关性考察。结果马来酸曲美布汀缓释片在不同释放介质中的释放度一致，均符合零级动力学。将体内累积吸收百分数y与相应时间在0．01mol／L盐酸释放介质中的体外释放百分数X进行线性回归（n=7），回归方程为Y=1．0093x一0．3329，r：0．9600（P=0．000601〈0．001），表明具有良好的体内外相关性，呈A级相关。结论马来酸曲美布汀缓释片的释放度不受三种释放介质影响，释药恒速。体外释放累积百分数与体内吸收百分数呈A级相关。

Drug release characteristics in vitro and in vivo correlations study of trimebutine maleate sustained- release tablets

Objective To study the drug release characteristics in vitro and the correlation between the dissolution in vitro and the absorption in vivo of Trimebutine Maleate Sustained - Release Tablets. Methods Three kinds of release media were used respectively to study the effect of difference kinds of release media on the drug release characteristic of Trimebutine Maleate Sustained - Release Tablets. And for the release media of 0. 01 moL/L HCI. The in vivo absorption percents in healthy male volunteers were calculated by Wagner - Nelson method. The correlation between the dissolution in vitro and the absorption in vivo was studied. Results The drug release profiles in different media with various release media were similar. The linear regressive equation established between the absorption percent in vivo and the dissolution percent in vitro of Trimebutine Maleate Sustained - Release Tablets was y = 1. 0093x - 0. 3329, r = 0. 9600 （ P = 0. 000601 〈0. 001 ）. Conclusion The various release media had no effect on the drug release. The drug release in vitro was of zero -grade dynamics. There was a significant correlation between the absorption in vivo and the drug re- lease in vitro of Trimebutine Maleate Sustained- Release Tablets.