2种进口索他洛尔片在中国健康人体内的生物等效性研究  

Bioequivalence of Sotalol Tablets in Healthy Subjects by HPLC-FLU

作　　者：闫小华[1] 李东 周凡[1] 张宏久[1] 张毕奎[3] 许蕴[4] 马经野[4] 邓小敏[1] 张璇[1] 

机构地区：[1]广东省深圳市康宁医院,广东深圳518020 [2]暨南大学第二临床医学院.广东省深圳市人民医院,广东深圳518020 [3]中南大学湘雅三医院,湖南长沙410011 [4]广东省深圳市第二人民医院,广东深圳518035

出　　处：《中国药业》2008年第13期9-11,共3页China Pharmaceuticals

摘　　要：目的评价2种进口索他洛尔片剂在中国健康人体内的生物等效性。方法采用高效液相色谱-荧光检测法,测定12名中国健康志愿者交叉口服受试和参比索他洛尔片160mg后的血药浓度经时过程。由DAS2.0药学与统计程序处理计算药代动力学参数及生物等效性评价。结果最佳房室模型为二室模型(Wi=1),受试制剂和参比制剂的峰质量浓度分别为(1.214±0.279)μg/mL和(1.29±0.262)μg/mL,消除半衰期分别为(8.891±4.906)h和(8.780±3.034)h,达峰时间分别为(3.583±0.669)h和(3.042±0.753)h,药-时曲线下面积(AUC)分别为(16.221±3.098)μg·h/mL和(15.932±2.675)μg·h/mL,以AUC0→t计算的受试制剂的平均相对生物利用度为(108.0±0.146)%。结论两制剂生物等效。Objective To determine sotalol in human plasma for evaluating the relative bioavailability in healthy volunteers. Methods A randomized cross-over design was performed in 12 healthy volunteers. In the two study periods,a single 160 mg dose of each tablet was administered to each volunteer. The plasma concentrations of sotalol were determined by HPLC- FLU.The compartment model was fitted by F-test and AIC method and the pharmacokinetic parameters and bioequivalence were calculated by DAS 2.0 program. Results The pharmacokinetics was best fitted to a two-compartment model （Wi = 1）. The main pharmacokinetics parameters of t1/2, t Cmax and AUC were （8.891 ± 4. 906）h, （3. 583 ± 0. 669）h, （1.214 ± 0. 279） μg/mL and （16.221± 3. 098）μg · h/mL for the test tablet; （8.780 ± 3. 034）h, （3. 042 ± 0. 753） h, （1.29 ± 0. 262） μg/mL and （ 15. 932 ± 2. 675） μg · h/mL for the reference tablet. The relative bioavalability of the test was （108.0±0. 146）%.The results of variance analysis and two one-sided t-test showed that there was no significant difference between the two formulations in the AUC and C Conclusion The two formulations were bioequivalent.

关 键 词：索他洛尔 生物等效性 片剂 

分 类 号：R969.1[医药卫生—药理学] R972.2[医药卫生—药学]