Shoaib Muhammad Harris, Shaikh Dilnawaz, Yousuf Rabia Ismail, Naqvi Baqir S, Hashmi Khursheed
Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi.
Pak J Pharm Sci. 2008 Oct;21(4):400-6.
To observe and discuss the difference in the pharmacokinetics of cephradine in Pakistani population with the reported data of other ethnic origins. A Single group pharmacokinetic study was conducted having six healthy male volunteers of 20-24 years of age. Blood samples were collected at appropriate times up to 7 hours. Plasma concentrations of cephradine was determined by HPLC technique and pharmacokinetic parameters were determined by both compartmental and noncompartmental methods using Kinetica ver 4.4.1 and Winnonlin ver 5.01. Peak plasma concentration was 11.49+/-1.73 microg/ ml achieved at 0.76+/-0.12 hr, after the administration of 250 mg cephradine to fasting volunteers. Area under the serum concentration-time curve was found to be 16.4+/-1.71 g.hr/ ml. Absorption, distribution, disposition and elimination half lives were calculated as 0.183 +/- 0.038 hr, 0.248 +/- 0.143 hr, 2.126 +/- 0.341 hr and 0.441+/-0.193 hr respectively where as the volume of central compartment and total body clearance were found to be 9.65+/-3.78 L and 15.4+/-1.89 L/hr. The plasma concentration time curves showed the absorption rate constant was 3.968 +/- 0.05 hr(-1), disposition rate constant was 0.333+/-0.05 hr(-1), distribution rate constant was 3.64+/-2.18 hr(-1) and elimination rate constant was 1.738+/-0.468 hr(-1). The value of micro-constants i.e. K(12) (central to peripheral compartment) and K(21) (peripheral to central compartment) were found to be 1.529+/- 1.499 hr(-1) and 0.704 +/- 0.44 hr(-1) respectively, where as MRT and AUMC were calculated as 2.04+/-0.09 hr and 35.92+/-1.86 hr(2) microg/ ml. The findings showed that the results of Pakistani subjects are slightly different when compared with the reported data of other ethnic origin.
观察并探讨头孢拉定在巴基斯坦人群中的药代动力学与其他种族来源的报告数据之间的差异。进行了一项单组药代动力学研究，招募了6名年龄在20 - 24岁的健康男性志愿者。在长达7小时的适当时间采集血样。采用高效液相色谱（HPLC）技术测定头孢拉定的血浆浓度，并使用Kinetica ver 4.4.1和Winnonlin ver 5.01通过房室和非房室方法测定药代动力学参数。对空腹志愿者给予250 mg头孢拉定后，在0.76±0.12小时达到血浆峰浓度11.49±1.73 μg/ml。血清浓度 - 时间曲线下面积为16.4±1.71 μg·hr/ml。吸收、分布、处置和消除半衰期分别计算为0.183±0.038小时、0.248±0.143小时、2.126±0.341小时和0.441±0.193小时，而中央室容积和全身清除率分别为9.65±3.78 L和15.4±1.89 L/hr。血浆浓度 - 时间曲线显示吸收速率常数为3.968±0.05 hr⁻¹，处置速率常数为0.333±0.05 hr⁻¹，分布速率常数为3.64±2.18 hr⁻¹，消除速率常数为1.738±0.468 hr⁻¹。微观常数即K(12)（中央室到外周室）和K(21)（外周室到中央室）的值分别为1.529±1.499 hr⁻¹和0.704±0.44 hr⁻¹，而平均滞留时间（MRT）和一阶矩曲线下面积（AUMC）计算为2.04±0.09小时和35.92±1.86小时²·μg/ml。研究结果表明，与其他种族来源的报告数据相比，巴基斯坦受试者的结果略有不同。
