Beermann D, Schaefer H G, Wargenau M, Heibel B, Sturm Y, Kuhlmann J
Institutes of Clinical Pharmacology, Pharma Research Centre, Bayer AG, Wuppertal, FRG.
Eur J Clin Pharmacol. 1992;42(3):307-12. doi: 10.1007/BF00266353.
The pharmacokinetics of BAY w 8199, the active metabolite of the prodrug repirinast (BAY u 2372), has been investigated after oral administration of 150, 300 and 450 mg repirinast to twelve healthy male Caucasians. Plasma BAY w 8199 concentrations were very variable between subjects. The mean peak level (geom.mean; 1s-range) was 0.14 (0.08-0.25), 0.19 (0.13-0.29) and 0.24 (0.14-0.42) mg/l after the 150, 300 and 450 mg doses, respectively. Peak levels were reached 0.5-2.5 h after drug intake. Terminal half-lives were calculated as 5.9 h (150 mg), 8.0 h (300 mg) and 9.8 h (450 mg). The dose proportionality of the plasma profiles of BAY w 8199 and of its excretion in urine was demonstrated by testing several parameters. About 7.4% of each dose (calculated as BAY w 8199) was excreted in urine over 36 h. The renal clearance of about 27 l/h suggests that BAY w8199 is excreted by tubular secretion in addition to glomerular filtration.
对12名健康的白人男性口服150、300和450毫克瑞吡司特（BAY u 2372）后，研究了其活性代谢产物BAY w 8199的药代动力学。受试者之间血浆中BAY w 8199的浓度差异很大。150、300和450毫克剂量后，平均峰值水平（几何平均值；1个标准差范围）分别为0.14（0.08 - 0.25）、0.19（0.13 - 0.29）和0.24（0.14 - 0.42）毫克/升。服药后0.5 - 2.5小时达到峰值水平。终末半衰期经计算分别为5.9小时（150毫克）、8.0小时（300毫克）和9.8小时（450毫克）。通过测试几个参数证明了BAY w 8199血浆曲线及其尿排泄的剂量比例关系。在36小时内，各剂量（以BAY w 8199计算）约7.4%经尿液排出。约27升/小时的肾清除率表明，除肾小球滤过外，BAY w 8199还通过肾小管分泌排泄。
