吲哚美辛肠溶滴丸在比格犬体内的药动学研究

Pharmacokinetics of Indometacin Enteric-coated Dropping Pills in Beagle Dogs

目的:对吲哚美辛(IDM)肠溶滴丸的药动学进行考察。方法:以比格犬为实验动物,以市售IDM肠溶片为对照,对同剂量IDM肠溶滴丸单剂量给药的药动学进行研究,用SPSS 21.0软件进行模型拟合及参数计算,并进行生物等效性评价。结果:IDM肠溶滴丸及肠溶片均符合一室模型,C_(max)、T_(max)、AUC_(0-∞)、Tlag等差异均有统计学意义(P<0.05),C_(max)及AUC_(0~∞)均显著升高,T_(max)及Tlag均显著缩短,肠溶滴丸的相对生物利用度为(121.0±7.7)%。结论:IDM肠溶滴丸相对于肠溶片而言,吸收显著增加,起效明显加快,值得进一步研发。

Objective： To study the pharmacokinetics of indometacin （IDM） enteric-coated dropping pills. Methods ： Beagle dogs were used as the experimental animals and the marketed IDM enteric-coated tablets were applied as the control, the pharmacokinetics of IDM enteric-coated dropping pills was studied after a single oral administration. DAS software was used for the model fit and parameter calculation, and the bioequivalenee was also evaluated. Results： Both IDM enteric-coated dropping pills and tablets were fitted a onecompartment model. Compared with those of IDM enteric-coated tablets, the Cmax, Tmax, AUC0-∞ and Tlag of IDM enteric-coated dropping pills all showed notable differences （ P 〈 0.05 ）, and the former two increased significantly, and the latter two were shortened significantly. The relative bioavailability of the dropping pills was （121.0 ± 7.7）%. Conclusion： Compared with IDM enteric-coated tablets, IDM enteric-coated dropping pills are with significantly enhanced absorption and shortened lag time, which is worthy of further studies and development.