国产氟康唑片在人体生物利用度研究

RELATIVE BIOAVAILABILITY OF THE FLUCONAZOLE TABLET

本文采用反相高效液相色谱法测定血清中氟康唑的浓度，并对８名健康志愿者随机交叉口服２００ｍｇ国产氟康唑片剂和进口胶囊的生物利用度进行了研究，结果表明：国产氟康唑片剂和进口胶囊的药─时曲线均符合口服吸收二室模型，Ｔｐｅａｋ为１．７２±０．４８ｈ和１．５７±０．４２ｈ，Ｃｍａｘ分别为４．１６±０．４４ｍｇ·Ｌ－１和４．２１±０．３５ｍｇ·Ｌ－１，ＡＵＣ为１７９．１±２６．５ｍｇ·ｈ·Ｌ－１和１８３．２±２６．１ｍｇ·ｈ·Ｌ－１，０～９６ｈ尿药累积排泄率为８８．２±４．１％和８６．９±３．６％。经配对Ｔ检验，各药代动力学参数无显著性差异（Ｐ＞０．０５），国产氟康唑片剂相对进口氟康唑胶囊的生物利用度为９８．０５±９．０３％。结果提示氟康唑国产片剂和进口胶囊具有生物等效性。

In this study, the concentrations of unchanged fluconazole in serum have been determined by using high-performance liquid chromatography. A single oral 200mg of the domestic product tablet or the imported product capsule was given to 8 healthy male volunteers in a randomized cross-over study. It was found that the serum concentration-time curves of the two preparations were fitted to a two-compartment model with oral absorption. Tpeak of the domestic fluconazole tablet and the imported fluconazole capsule were 1.72±0.49 h and 1.57±0.42 h. Cmax were 4. 16±0.44 mg·L-1 and 4.21±0.35 mg·L-1,AUC were 179.1±26.5 mg·h·L-1 and 183± 26.1 mg·h·L-1, respectively. There were no statistically significant difference for fluconazole between the domestic product tablet and the imported product capsule on any of the following pharmacokinetic parameters Tpeak,Cmax and AUC (P>0.05). The relative bioavailability of the domestic fluconazole to the imported was 98.05±9.03%. These results suggested that the two preparations are bioequivalent.