Laboratory of Veterinary Pharmacology, College of Veterinary Medicine, South China Agricultural University, Guangzhou 510642, PR China.
Res Vet Sci. 2012 Dec;93(3):1380-6. doi: 10.1016/j.rvsc.2012.02.015. Epub 2012 Mar 28.
Pharmacokinetics of mequindox (MEQ) and its metabolites were determined in rats after intravenous (i.v.) and oral (p.o.) administration of MEQ at a single dose of 10 mg kg(-1) bodyweight. After both administrations, MEQ and five of its metabolites were quantified, except M4, whereas M1 and M2 were the predominant ones. The areas under the concentration-time curves (h ng mL(-1)) of MEQ, M1, M2, M3, M5 and M10 after i.v. administration were 7559±495, 6354±2761, 5586±2337, 1034±160, 2370±791 and 1813±622, respectively, whereas after p.o. administration, remained as 2809±40, 4361±3544, 4351±1046, 1444±814, 3864±305 and 1213±569, respectively. The elimination half-lives (h) of these compounds after i.v. administration were 3.48±0.80, 4.20±0.76, 6.25±2.41, 4.77±1.54, 4.69±1.62 and 16.89±5.15, respectively, and were 3.21±0.40, 3.66±1.06, 4.20±1.03, 8.91±5.99, 4.20±2.02 and 20.84±10.85 after p.o. administration, respectively. After p.o. administration, the bioavailability of MEQ was 37.16%. The results showed that MEQ was extensively metabolized in rats and rapidly absorbed after p.o. administration.
给鼠单剂量 10mg/kg 静脉(i.v.)和口服(p.o.)给予马兜铃酸美喹多星(MEQ)后，测定 MEQ 及其代谢物的药代动力学。两种给药途径后，除 M4 外，均定量检测到 MEQ 和其 5 种代谢物，其中 M1 和 M2 为主要代谢物。i.v.给药后 MEQ、M1、M2、M3、M5 和 M10 的浓度-时间曲线下面积(h·ng·mL-1)分别为 7559±495、6354±2761、5586±2337、1034±160、2370±791 和 1813±622，而 p.o.给药后分别为 2809±40、4361±3544、4351±1046、1444±814、3864±305 和 1213±569。i.v.给药后这些化合物的消除半衰期(h)分别为 3.48±0.80、4.20±0.76、6.25±2.41、4.77±1.54、4.69±1.62 和 16.89±5.15，而 p.o.给药后分别为 3.21±0.40、3.66±1.06、4.20±1.03、8.91±5.99、4.20±2.02 和 20.84±10.85。p.o.给药后 MEQ 的生物利用度为 37.16%。结果表明，MEQ 在大鼠体内广泛代谢，p.o.给药后迅速吸收。
