Department of Pharmacy, Shenyang Northern Hospital, Shenyang, China.
J Clin Pharm Ther. 2010 Apr;35(2):231-7. doi: 10.1111/j.1365-2710.2009.01097.x.
The purpose of the present study was to investigate and compare the influence of ethnicity (including Han, Mongolian, Korean, Hui and Uygur) and gender on the pharmacokinetics of fluconazole in healthy adult volunteers after administration of 200-mg fluconazole tablet.
Ten healthy subjects (five males and five females) of each ethnicity were recruited and given a single 200-mg dose of fluconazole in tablet form. Blood samples were obtained before dosing and at various predetermined time points after administration up to 96 h. Drug levels were measured by high-performance liquid chromatography. The blood concentration-time profiles were analyzed using a non-compartmental approach to estimate the absorption parameters (AUC((0-96)), C(max) and t(max)), the distribution parameter (V(d)) and the disposition parameters (t(1/2) and CL).
Ethnicity did not affect the parameter estimates, but gender did. However, the gender differences in pharmacokinetic parameter could be accounted for by differences in weight. There was a high linear correlation between weight and ln C(max), ln AUC (ln means natural logarithmic transformation), V(d) and CL.
Ethnicity (Chinese Han, Mongolian, Korean, Hui and Uygur) influences the pharmacokinetics of fluconazole tablet. However, there were statistically significant gender differences in AUC, C(max), V(d) and CL. But these could be accounted for by weight differences. If fluconazole dose-adjustment is deemed necessary, this can be done on a weight basis rather than gender basis.
本研究旨在探讨和比较种族（包括汉族、蒙古族、朝鲜族、回族和维吾尔族）和性别对健康成年志愿者服用 200mg 氟康唑片后氟康唑药代动力学的影响。
招募了 10 名健康受试者（每种族 5 名男性和 5 名女性），给予单剂量 200mg 氟康唑片。在给药前和给药后至 96 小时的各个预定时间点采集血样。采用高效液相色谱法测定药物浓度。采用非房室模型分析血药浓度-时间曲线，估算吸收参数（AUC（0-96）、Cmax 和 tmax）、分布参数（Vd）和处置参数（t1/2 和 CL）。
种族不影响参数估计值，但性别有影响。然而，药代动力学参数的性别差异可以通过体重差异来解释。体重与 lnCmax、lnAUC（ln 表示自然对数转换）、Vd 和 CL 之间存在高度线性相关。
种族（汉族、蒙古族、朝鲜族、回族和维吾尔族）影响氟康唑片的药代动力学。然而，AUC、Cmax、Vd 和 CL 方面存在统计学显著的性别差异。但这些可以通过体重差异来解释。如果认为需要调整氟康唑剂量，可以根据体重而不是性别进行调整。
