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目的:１９名健康志愿者随机交叉给予伊曲康唑胶囊（试验药和对照药），进行人体相对生物利用度研究。方法：固相萃取方法用于血清中伊曲康唑的浓缩和纯化，用ＨＰＬＣ测定伊曲康唑的血药浓度，并进行药代动力学计算。结果：对测试获得的受试者血药浓度－时间数据用３Ｐ９７进行拟合，受试者的血药浓度－时间曲线符台二室模型，所获得的药代动力学参数如下：对照药： Ｃｍａｘ为１５３．９± ７８．２μｇ· Ｌ－１， Ｔｍａｘ为 ４．８±１．６ ｈ， Ｔ１／２（β）为 ２０．２ ±５．６ ｈ， Ａ ＵＣ为 ２２７２．６１± ８９４· ７μｇ· ｈ· Ｌ－１；试验药： Ｃｍａｘ为 １４７． ８ ± ７１． ３μｇ· Ｌ－１， Ｔｍａｘ＝５．１±１．４ｈ， Ｔ１／２（β）＝２１．８± ４．８ｈ， Ａ ＵＣ＝ ２３１８．８± ９０１．８μｇ· ｈ· Ｌ－１．试验药的相对生物利用度值为 Ｆ＝ １．０６± ０．３。结论：经１—２ａ置信区间检验、方差分析显示两种药物具有生物等效性。试验中没有受试者出现药物不良反应。
PURPOSE: Nineteen healthy volunteers were randomly assigned to receive itraconazole capsules (test and control) for relative bioavailability in humans. Methods: The solid phase extraction method was used for the concentration and purification of itraconazole in serum. The plasma concentration of itraconazole was determined by HPLC and its pharmacokinetics were calculated. Results: The plasma concentration-time data of the test subjects were fitted with 3P97. The blood concentration-time curve of the subjects was in accordance with the two-compartment model. The pharmacokinetic parameters obtained were as follows: Control drug: Cmax was 153.9 ± 78.2 μg · L-1, Tmax was 4.8 ± 1.6 h, T1 / 2 (β) was 20.2 ± 5.6 h, A UC was 2272.61 ± 894 · 7μg · h · L-1; test drug: Cmax 147. 8 ± 71. 3μg · L-1, Tmax = 5.1 ± 1.4h, T1 / 2 (β) = 21.8 ± 4.8h and AUC = 2318.8 ± 901.8μg · h · L-1. The relative bioavailability of the test drug was F = 1.06 ± 0.3. CONCLUSION: Variance analysis showed that the two drugs were bioequivalent after 1-2 years of confidence interval test. No adverse drug reactions occurred in the trial.