Lin C, Lim J, Radwanski E, Marco A, Affrime M
Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.
Antimicrob Agents Chemother. 1995 Feb;39(2):359-61. doi: 10.1128/AAC.39.2.359.
The pharmacokinetics and dose proportionality of ceftibuten were evaluated in healthy male volunteers receiving single oral doses of 200, 400, and 800 mg of ceftibuten. The drug was absorbed with similar times to the maximum concentration of drug in plasma for all three doses. Concentrations of ceftibuten in plasma increased with increasing dose. Analysis of variance was carried out on the dose-adjusted values for the maximum concentration of drug in plasma and the area under the plasma concentration-time curve; the results indicated that the concentrations in plasma after the 200- and 400-mg doses were dose proportional, and after the 800-mg of dose they were less than dose proportional. The elimination half-life from plasma ranged from 2.0 to 2.3 h and was independent of dose. The total excretion of unchanged ceftibuten in urine accounted for 53 to 68% of the dose, and the renal clearance was estimated to be 53 to 61 ml/min after all doses. The amount of ceftibuten-trans, the major in vitro and in vivo conversion product of ceftibuten, was low in both plasma and urine.
在接受单次口服200毫克、400毫克和800毫克头孢布烯的健康男性志愿者中评估了头孢布烯的药代动力学和剂量比例关系。对于所有三种剂量，药物吸收至血浆中药物最大浓度的时间相似。血浆中头孢布烯的浓度随剂量增加而升高。对血浆中药物最大浓度和血浆浓度-时间曲线下面积的剂量校正值进行方差分析；结果表明，200毫克和400毫克剂量后的血浆浓度呈剂量比例关系，而800毫克剂量后则低于剂量比例关系。血浆消除半衰期为2.0至2.3小时，且与剂量无关。尿液中未变化的头孢布烯总排泄量占剂量的53%至68%，所有剂量后的肾脏清除率估计为53至61毫升/分钟。头孢布烯反式体（头孢布烯主要的体外和体内转化产物）在血浆和尿液中的含量均较低。
