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目的 研究家犬口服替硝唑结肠定位肠溶片的药代动力学特征。方法 实验家犬随机分成两组 ,分别服用受试制剂和参比制剂 ,采用RP HPLC法测定血浆和肠道中药物浓度。结果 受试制剂和参比制剂的Tmax分别为 (6 3±1 2 )h和 (2 4± 1 1)h ,Cmax分别为 (46 2 3± 8 93 )mg·L-1和 (5 8 0 8± 14 65 )mg·L-1,用梯形法计算所得的AUC0 -t分别为 (42 3 2 1± 93 0 8)mg·h·L-1和 (45 8 2 2±112 0 7)mg·h·L-1。与参比制剂相比 ,受试制剂的相对生物利用度为 92 9%± 6 6%。家犬服用替硝唑结肠定位肠溶片 6 5h后结肠中替硝唑的量较多 ,而小肠中则几乎未检测到替硝唑。结论 家犬服用替硝唑结肠定位肠溶片后药物吸收出现明显的滞后 ,替硝唑结肠定位肠溶片在胃和小肠中稳定 ,几乎不释放出药物 ,而在结肠处释放出大量药物 ,具有良好的结肠定位释放效果
Objective To study the pharmacokinetics of oral tinidazole colonic enteric-coated tablets in domestic dogs. Methods Experimental dogs were randomly divided into two groups, taking the test preparation and the reference preparation respectively, and the RP HPLC method was used to determine the concentration of the drug in the plasma and intestine. Results The Tmax of test and reference preparations were (6 3 ± 1 2) h and (24 ± 1 1) h, respectively, and the C max were (46 2 3 ± 8 93) mg · L -1 and (58 0 8 ± 14 65) mg · L-1, and the AUC0-t calculated by the trapezoidal method was (42 3 2 1 ± 93 0 8) mg · h · L -1 and (45 8 2 ± 112 7 ) mg · h · L-1. The relative bioavailability of the tested formulations was 92 9% ± 6 6% compared to the reference formulation. Tinidazolidin colon colonization enteric coated tablets 6 5h colon tinnitine more, but little tinnitus was detected in the small intestine. Conclusion The oral administration of tinidazole colonic enteric-coated tablets showed significant lag in drug absorption. Tinidazole colon-stabilized enteric-coated tablets were stable in the stomach and small intestine, almost no drug was released, and a large amount of drug was released in the colon, Good colon release effect