中国临床药学杂志

目的:评价单剂量口服国产和进口伊贝沙坦片的人体药动学特性和生物等效性。方法:采用随机、开放、交叉的试验设计,20名健康受试者随机口服单剂量的国产和进口伊贝沙坦片150 mg,采用HPLC-荧光检测法测定受试者血浆中的伊贝沙坦浓度。c_max,t_max采用实测值,梯形法计算AUC,双单侧t检验及置信区间法进行生物等效性检验。结果:国产和进口伊贝沙坦片的AUC_0→t分别为(6534.69±1448.77),(6430.47±1384.13)mg·h·mL^-1;c_max为(1284.16±420.68),(1294.50±466.71)ng·mL^-1;t_max分别为(1.60±0.35),(1.53±0.47)h;T_1/2为(13.62±1.19),(13.33±1.26)h。经统计学处理,上述各项主要药动学参数间差别均无显著性意义(P>0.05)。国产伊贝沙坦的相对生物利用度为(101.98±5.32)%,生物等效性检验表明伊贝沙坦国产品与进口品具有生物等效性。结论:国产和进口伊贝沙坦片具有生物等效性。

AIM: To evaluate the pharmacokinetic characteristic and bioequivalence of domestic and imported irbesartan tablets. METHODS: The plasma concentration in healthy volunteers was determined by an validated HPLC-fluorescence method. A randomized, open, crossover study of 20 healthy Chinese volunteers was conducted with single o-ral dose of 150 mg irbesartan. The concentrations of irbesartan in plasma were assessed with non-compartment model to obtain the pharmacokinetic parameters. The relative bioavailability of domestic irbesartan tablet versus imported was calculated. RESULTS: The HPLC assay was sensitive, specific, accurate, and precise. The pharmacokinetic parameters for domestic and imported irbesartan were as follows: AUCo→1(6 534.69± 1 448.77) and (6 430.47 ± 1 384.13) ng· h·mL·-1, tmax( 1.60±0.35) and (1.53±0.47) h, cmax(1284.16 ± 420.68) and (1 294.50 ± 466.71) ng·ml-1, T1/2(13.62± 1.19) and (13.33±1.26) h, respectively. There were no significant differences (P > 0.05) in AUCo→t, tmax, cmax and T1/2 between 2 preparations by analysis of variance according to crossover design. The relative bioavailability of domestic irbesartan tablet was (101.98± 5.32)% compared with imported. No adverse drug reactions were observed during this study. CONCLUSION: The study shows that the domestic and imported irbesartan tablets were bioequivalent.