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目的通过18名健康志愿者,研究利巴韦林分散片的药动学和生物等效性。方法HPLC(C18,150 mm×4.6 mm,5μm,紫外检测器,波长215 nm)测定血浆中提取的药物,流动相为0.01 mol.L-1磷酸二氢铵和磷酸,流速1.5 mL.min-1。18名健康志愿者单次口服利巴韦林分散片或利巴韦林普通片600 mg,采用随机自身交叉试验方法,测定药动学参数和相对生物利用度。结果标准曲线线性范围0.05~1.60 mg.L-1,最低检测限0.05 mg.L-1。利巴韦林质量浓度为0.1、0.41、.6 mg.L-1时平均回收率分别为102.5%、101.7%和101.9%,日内RSD、日间RSD分别为(3.9±1.4)%和(3.1±2.4)%,药-时曲线显示两制剂符合二室模型。利巴韦林分散片和普通片的主要药动学参数如下:t1/2β(28.36±3.12)和(28.71±2.95)h,tmax(1.24±0.33)和(1.28±0.31)h,ρmax(0.651±0.127)和(0.654±0.081)mg.L-1,AUC0→72 h(13.22±2.28)和(13.23±2.09)mg.h.L-1,两剂型主要药动学参数差异无显著性意义(P>0.05);利巴韦林分散片相对生物利用度为(100.65±13.85)%。结论利巴韦林分散片与普通片生物等效。
Objective To study the pharmacokinetics and bioequivalence of ribavirin dispersible tablets in 18 healthy volunteers. Methods HPLC (C18, 150 mm × 4.6 mm, 5 μm, UV detector, wavelength 215 nm) was used to determine the drug in plasma. The mobile phase consisted of 0.01 mol·L -1 ammonium dihydrogen phosphate and phosphoric acid at a flow rate of 1.5 mL · min- 1.18 healthy volunteers oral administration of ribavirin dispersible tablets or ribavirin tablets 600 mg randomized to their own cross-test method to determine the pharmacokinetic parameters and relative bioavailability. Results The linear range of standard curve was 0.05 ~ 1.60 mg.L-1, the lowest limit of detection was 0.05 mg.L-1. The average recoveries of Ribavirin at the concentrations of 0.1,0.41 and .6 mg.L-1 were 102.5%, 101.7% and 101.9%, respectively. The intra-day RSD and daytime RSD were (3.9 ± 1.4)% and ± 2.4)%, the drug-time curve shows that the two formulations meet the two-compartment model. The main pharmacokinetic parameters of ribavirin dispersible tablets and ordinary tablets were as follows: t1 / 2β (28.36 ± 3.12) and (28.71 ± 2.95) h, tmax (1.24 ± 0.33) and (1.28 ± 0.31) h, ± 0.127) and (0.654 ± 0.081) mg.L-1, AUC0 → 72 h (13.22 ± 2.28) and (13.23 ± 2.09) mg.hL-1, respectively. There was no significant difference in the main pharmacokinetic parameters > 0.05). The relative bioavailability of ribavirin dispersible tablets was (100.65 ± 13.85)%. Conclusion Ribavirin dispersible tablets are bioequivalent to common tablets.