美喹多司在大鼠静脉注射和口服给药后的药代动力学及其代谢物。
Pharmacokinetics of mequindox and its metabolites in rats after intravenous and oral administration.
机构信息
Laboratory of Veterinary Pharmacology, College of Veterinary Medicine, South China Agricultural University, Guangzhou 510642, PR China.
出版信息
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。
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