吉非罗齐胶囊剂的相对生物利用度

RELATIVE BIOAVAILABILITY OF GEMFIBROZIL CAPSULE

8名健康受试者口服两种吉非罗齐胶囊剂后,血清样品经提取、甲酯化,以气相色谱法测定吉非罗齐的含量。其血药浓度-时间过程符合一房室模型。国产制剂的药代动力学参数分别为:k_a=2.97±2.84h^(-1),k=0.761±0.215h^(-1),t_(max)=1.42±0.83h,C_(max)=21.68±6.50mg/l,t_0=0.65±0.52h,V/F=0.122±0.040l,AUC=61.4±14.0mg·h/l。国外制剂的药代动力学参数分别为:k_a=3.26±2.94h^(-1),k=0.712±0.266h^(-1),t_(max)=1.26±0.54h,C_(max)=18.56±7.46mg/l,t_0=0.33±0.43h,V/F=0.153±0.045l,AUC=53.74±10.57mg·h/l。两者相对生物利用度F=1.14。4名受试者3次服药的峰浓度与谷浓度同单剂量给药的药代动力学参数结果的拟合值较为一致。

After oral administration of two kinds of gemfibrozil capsules in 8 healthy volunteers,the drug was extracted from the serum samples, then methylated and determined by gas chromatographyOne compartment model was fitted to the concentration-time profiles. Pharmacokinetic parameters forproduct A (Wuxi 7th pharmaceutical factory) werc k_α=2.97±2.84 h^(-1), k=0.761±0.215 h^(-1), t_(max)=1.42±0.83 h, C_(max)=21.68±6.5 mg/l, t_0=0.65±0.52 h, V/F=0.122±0.040 l and AUC=61.4±14.0mg·h^(-1) respectively; for the product B (PARKE-DAVIS Company) were ka=3.26±2.94 h^(-1), k=0.712±0.266 h^(-1), t_(max)=1.26±0.54 h, C_(max)=18.56±7.46 mg/l, t_0=0.33±0.43 h. V/F=0.153±0.045 l.AUC=53.74±10.57 mg·h^(-1). Relative bioavailability of product A was 1.14 compared with product B.4 of volunteers were subjected to administrated the drug 3 times daily (τ=6 h, X_0=300 mg), C_(max)and C_(min)were determined, which were very close to the simulated values.