酮康唑胶囊人体生物利用度研究

 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po 400mg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?t_max分别为(1.73±0.52)h和(1.81±0.43)h;c_max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;t_1/2β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?

Pharmacokinetics and relative bioavailability of ketoconazole capsule in human

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.