酮康唑胶囊人体生物利用度研究

Pharmacokinetics and relative bioavailability of ketoconazole capsule in human

目的：研究酮康唑胶囊在正常人体内的药代动力学与相对生物利用度。方法：采用高效液相色谱法测定８名志愿者随机交叉ｐｏ４００ｍｇ酮康唑胶囊和里素劳片后的血药浓度，计算两者的药代动力学参数与相对生物利用度。结果：国产酮康唑胶囊和片剂的药时曲线符合ｐｏ吸收二房室模型。ｔｍａｘ分别为（１．７３±０．５２）ｈ和（１．８１±０．４３）ｈ；ｃｍａｘ分别为（７．８３±３．０１）μｇ·ｍｌ－１和（７．８８±２．８８）μｇ·ｍｌ－１；ＡＵＣ分别为（５８．４８±２０．２２）μｇ·ｈ·ｍｌ－１和（５９．７３±２１．０７）μｇ·ｈ·ｍｌ－１；ｔ１／２β分别为（６．９７±０．５１）ｈ和（６．８８±０．４６）ｈ。经配对ｔ检验，各药代动力学参数无显著性差异（Ｐ＞０．０５）。结论：国产酮康唑胶囊相对于片剂的生物利用度为（９８．３６±７．８４）％，结果提示酮康唑胶囊和片剂具有生物等效性。

OBJECTIVE :To study the pharmackinetics and relative bioavailability of ketoconazole capsule in 8 healthy volunteers. METHODS: The ketoconazole concentrations in serum were determined by HPLC method following a single oral does of ketoconazole capsule and ketoconazole tablet respectively in an open randomized crossover way. RESULTS: The concentrationtime curves of the two products were fitted to a two compartment model with oral absorption.The tmax of the capsule and tablet were (1.730.52)h and (1.870.43)h,cmax were (7.833.01)gml-1 and (7.882.88)gml-1,AUC were (58.4820.22)ghml-1 and (59.7321.07)ghml-1,t1/2 were (1.970.51)h and (1.880.46)h respectively.There was no significant difference between the two products on and of the following pharmacokinetic parameters:tmax cmax AUC and t1/2(P>0.05). CONCLUSION:BZThe relative bioavailability was (98.367.84)% of ketoconazole capsule.It showed that the two fornulations were bioequivalent.