利巴韦林片在人体的药物动力学和生物等效性研究

Pharmacokinetics and bioequivalence of ribavirin tablets in healthy volunteers

目的研究利巴韦林片在健康人体内的药物动力学，并对2种制剂的生物等效性进行判定。方法采用液质联用（LC-MS／MS）法测定血浆中利巴韦林浓度并计算其主要药动学参数。结果受试制剂和参比制剂中利巴韦林的主要药动学参数如下：tmax分别为（1．35±0．38）、（1．30±0．50）h；Cmax分别为（674．8±227．7）、（693．94±223．3）ng·mL-1，t1／2分别为（25．6±6．0）、（26．6±5．3）h；AUC0-1分别为（8606．2±2132．0）、（8452．0±1978．8）ng·h·mL-1，AUC0-∞分别为（9903．3±2494．1）、（9632．1±2404．2）ng·h·mL-1，相对生物利用度为（102．2±9．5）％。结论2种利巴韦林制剂具有生物等效性。

Objective To determine the pharmacokinetics and bioequivalence between 2 ribavirin tablets in healthy vol-unteers. Methods A single oral dose of 2 ribavirin tablets was given to 18 healthy volunteers in a randomized 2-period crossover study. The concentrations of ribavirin in the plasma were determined by the liquid chromatography tandem mass spectrometry （LC-MS/MS） method. The plasma concentratio-time curves were plotted and the main pharmacokinetic parameters were calculated. Results The main pharmacokinetic parameters of test and reference tablets in the plasma were as follows： tmax was （1.35 ± 0.38） and （1.33 ±0.50） h, Cmax was （674.8±227. 7） and （693.9± 223.3） ng-mL-1; t1/2was （25. 6±6.0） and （26.6±5.3） h, AUC0-1,was （8 606.2 ± 2 132.0） and （8 452.0± 1 978. 8） ng ·h · mL- 1 ; AUC0- ∞was （9 903.3 ± 2 494.1） and （9 632.1 ± 2 404.2） ng · h · mL-1 , respectively. The relative bioavailabitity of the tested drug was （ 102.2 ± 9.5） %. Conclusion The 2 ribavirin formulations are bioequivalent in healthy volunteers.