三种利巴韦林的药动学和相对生物利用度

目的: 测定利巴韦林血药浓度及其在健康人体内的相对生物利用度和药动学。方法: 18 名男性健康受试者, 单剂三交叉口服两种利巴韦林被试制剂和标准参比制剂各 600 mg 后, 采用 HPLC 法测定不同时间血浆中的药物浓度, 数据经3P97 软件处理计算药代动力学参数。结果: 三者药-时曲线均符合一房室模型, 标准参比制剂和两种被试制剂峰浓度(C max) 分别为 0.76 ±0.37、0.72 ±0.22 和 0.75 ±0.40 mg°L^-1, 达峰时间(T_max) 分别 2.07±0.89、1.67±0.49 和 1.86±0.41 h, 消除半衰期(T_1/2ke) 分别为22±3、24±4 和 22 ±4 h, $AUC^{t}_{0}$ 分别为 12 ±4、14±4和12±4 mg°h°L^-1, $AUC^{∞}_{0}$ 别为 16±5、18±5 和 15±5 mg°h°L^-1。两种被试制剂的相对生物利用度分别为(112 ±21) %和(100 ±18) %。结论: 两种被试制剂与标准参比制剂具有生物等效性。

Pharmacokinetics and relative bioavailability of ribavirin in Chinese healthy volunteers

AIM: To study the pharmacokinetics and bioavailability of ribavirin in 18 young healthy volunteers.METHODS: The ribavirin concentrations in plasma were determined by HPLC after a single oral dose of the stan-dard formulation and the tested formulation which were re-spectively given to 18 volunteers in randomized cross-over test. RESULTS: The concentration-time curves of three formulations fitted to one-compartment open model. The C max were 0.76 ±0.37, 0.72 ±0.22 and 0.76 ±0.40 mg°L^-1;T_max were 2.07±0.89, 1.67±0.49 and 1.86 ±0.41 h;T_1/2ke was 22 ±3, 24 ±4 and 22 ±4 h; $AUC^{t}_{0}$ were 12±4, 14 ±4 and 12 ±4 mg°h°L^-1;and $AUC^{∞}_{0}$ were 16±5, 18±5 and 15±5 mg°h°L^-1 in a standard formulation and two tested formulations, respec-tively. The pharmacokinetic parameters showed no signifi-cant difference among three formulations (P>0.05). The relative bioavailability of two tested formulations was (112 ±21) % and (100 ±18) %.CONCLUSION: The two tested formulations are bioequivalent with refer-enced formulation.