国产苯扎贝特片人体相对生物利用度的研究

Relative Bioavailability of Bezafibrate Tablet in Healthy Volunteers

观察２０名男性健康志愿者随机交叉口服单剂量２００ｍｇ国产和进口苯扎贝特片后血药浓度变化，进行药代动力学和相对生物利用度研究；方法：用反相高效液相色谱测定苯孔贝特血药浓度，用３Ｐ８７药代动力学程序计算有关药代动力学参数，其主要药代动力学参数经三因素方差分析；结果：国产和进口苯扎贝特片的血药浓度一时间曲线均符合口服吸收一室模型，主要药代动力学参数Ｔｍａｘ分别为２．３８±０．８９ｈ和２．１６ ± ０．７９ ｈ， Ｃｍａｘ分别为６．２２ ±１．３０ｍｇ·Ｌ－１和６．５７ ±１．２３ ｍｇ·Ｌ－１， Ｔ１／２分别为１．６７±０．４３ｈ和１．４９ ± ０．３５ｈ，Ａ ＵＣ０－１２分别为２０．３２±３．９８ ｍｇ·ｈ·Ｌ－１和１９．８０±３．６５ｍｇ·ｈ·Ｌ－１；两种制剂的主要药代动力学参数均无显著性差异（Ｐ＞０．０５）；结论：以进口片为标准参比制剂，国产片的相对生物利用度为１０２．６ ± ８．３％，双单侧ｔ检验结果提示，两种制剂生物等效。

OBJECTIVE: The pharmacokinetic profiles and the bioavailability of domestic tablets of bezafibrate were studied in 20 healthy volunteers. METHODS. A single oral dose of 200mg bezafibrate domestic or imported tablet was given to each volunteer according to a crossover design. The concentrations in plasma were measured by HPLC. RESULTS. The results showed that the plasma concentration-time curves of the domestic and imported products were fitted to one-compartment model. The main pharmacokinetic parameters of bezafibrate were:AUC0 - 12 20.32 ±3.98 mg·L-1 and 19.80 ± 3.65 mg·h· L-1, Tmax 2.38 ± 0.89 h and 2.16 ± 0.79 h, Cmax 6.22 ± 1.30 mg·L-1 and 6.57 ± 1.23 mg·L-1; T1/2 1.67 ± 0.43h and 1.49 ± 0.35h for domestic and imported tablet respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between domestic and imported tablets (P>0.05). CONCLUSION: The relative bioavailability of two products was 102.6 ± 8.3 %. The results showed that both formulations were bioequivalent.