Khoo K C, Szuna A J, Colburn W A, Aogaichi K, Morganroth J, Brazzell R K
J Clin Pharmacol. 1984 Jul;24(7):283-8. doi: 10.1002/j.1552-4604.1984.tb01834.x.
The pharmacokinetics of cibenzoline were evaluated in four young healthy volunteers who received ascending oral doses of 65, 97.5, 130, 162.5, 195, 227.5, and 260 mg separated by one week. Cibenzoline plasma concentrations exhibited an apparent biexponential decline following oral absorption. Maximum plasma concentrations and area under the plasma concentration-time curve increased in proportion to the dose. The mean elimination half-life among subjects was independent of dose and ranged from 7.3 to 8.7 hours. Oral clearance ranged from 380 to 575 ml/min and was also independent of dose. A single pharmacokinetic equation was used to adequately describe the plasma concentration data over the entire range of doses for each subject, indicating dose-proportional and linear pharmacokinetics.
对4名年轻健康志愿者进行了西苯唑啉的药代动力学评估，他们口服递增剂量的西苯唑啉，剂量分别为65、97.5、130、162.5、195、227.5和260 mg，每次服药间隔1周。口服吸收后，西苯唑啉的血浆浓度呈现明显的双指数下降。血浆最大浓度和血浆浓度-时间曲线下面积与剂量成正比增加。受试者的平均消除半衰期与剂量无关，范围为7.3至8.7小时。口服清除率范围为380至575 ml/min，也与剂量无关。使用单一药代动力学方程足以描述每个受试者在整个剂量范围内的血浆浓度数据，表明其药代动力学呈剂量比例和线性关系。
