伊贝沙坦胶囊生物等效性的评价研究

Experimental evaluation of the bioequivalence of irbesartan capsules

目的 评价伊贝沙坦两种制剂是否生物等效。方法 男性健康受试者 2 4名 ,随机分成两组 ,交叉口服试验品与参比制剂各 3 0 0mg ,在一定时间点取静脉血分离血浆 ,以HPLC法测定血药浓度 ,各受试者服药后的血药浓度经时数据以BECS软件处理得到主要药代动力学参数 ,Cmax、AUC0 tn,AUC0 inf经对数转换地行双单侧t检验分析 ,Tmax经Wilcoxon铁和检验 ,判断两制剂的等效性。结果 试验品与参比制剂的T1 2 分别为 ( 14 3± 6 3 )h及 ( 14 4± 4 9)h ,Tmax分别为 ( 2 0 8±0 5 8)h及 ( 2 12± 0 61)h ,Cmax分别为 ( 2 3 70 7± 83 4 5 )ng ml及 ( 2 193 2± 60 8 3 )ng ml,AUC0 tn分别为 ( 15 460± 70 0 7)ng·ml- 1 ·h- 1 与 ( 14 75 8± 43 95 )ng·ml- 1 ·h- 1 ,AUC0 inf分别为 ( 170 5 1± 710 5 )ng·ml- 1 ·h- 1 与 ( 1663 4± 472 4)ng·ml- 1 ·h- 1 。经统计分析试验药品与参比制剂的Cmax,AUC0 tn,AUC0 inf均在规定范围内。Tmax 无显著性差异 ,试验品的相对生物利用度为( 10 4 0 8± 2 6 85 ) % (以AUC0 Tn计算得出 )和 ( 10 2 2 5± 2 4 80 ) (以AUC0 inf计算得出 )。结论 两制剂生物等效。

Objective To evaluate the bioequivalence of two irbesartan preparations. Methods A total of 24 healthy male volunteers, divided randomly into two groups, were administered with two preparations of irbesartan respectively in an open randomized cross-over test. A single oral dose of the test and control preparations was 300 mg. Venous blood of the subjects was collected for separation of blood plasma. Irbesartan concentration in the plasma was determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters of irbesartan were obtained by using BECS software. Results Parameters of the test and control preparations were obtained. T 1/2 : (14.3±6.3) h vs (14.4±4.9) h; T max : (2.08±0.58) h vs (2.12±0.61) h; C max : (2370.7±834.5) ng/ml vs (2 193.2±608.3) ng/ml; AUC 0-tn : (15 460±7 007) ng·ml -1 ·h -1 vs (14 758±4 395) ng·ml -1 ·h -1 ; AUC 0-inf : (1 7051±7 105) ng·ml -1 ·h -1 vs (16 634±4 724) ng·ml -1 ·h -1 . The results of statistical analysis showed that there was no significant difference between C max , AUC 0-tn , and T max of irbesartan. Conclusion The two preparations are bioequivalent.