摘要
目的比较2种进口比索洛尔片剂在健康人体的药动学及生物等效性。方法24例健康男性受试者随机交叉口服比索洛尔受试制剂和参比制剂5mg后,采用液相色谱-串联质谱(LC-MS/MS)法测定血浆中比索洛尔的浓度,经DAS2.0软件计算药动学参数,用方差分析和双单侧t检验评价2种制剂的生物等效性。结果健康受试者口服比索洛尔受试制剂和参比制剂5mg后,血浆中比索洛尔的ρmax、tmax、AUC(0~t)、AUC(0~∞)和t1/2分别为(18±s3)和(18.0±2.9)μg·L-1;(2.2±1.2)和(2.5±1.6)h;(266±48)和(263±39)μg·h·L-1;(276±50)和(274±39)μg·h·L-1;(9.0±1.3)和(9.2±1.0)h。以AUC(0~t)计算,受试制剂的相对生物利用度平均为100.3%,2种制剂各主要药动学参数经双单侧t检验及90%置信区间法检验,差异无显著意义(P>0.05)。结论2种比索洛尔片剂在体内具有生物等效性。
AIM To evaluate the pharmacokinetics and bioequivalence of two imported bisoprolol tablets in healthy volunteers. METHODS Twenty-four healthy male volunteers were cross alternative randomly administered a single dose of 5 mg of test and reference tablets. The bisoprolol concentrations in plasma were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) , and the pharmacokinetic parameters and bioequivalence of the tablets were analyzed through DAS 2.0 software. RESULTS After taking 5 mg of single dose of bisoprolol, the pharmacokinetic parameters of test and reference tabletsin plasma were asfollows: pmax (18 + s 3) vs (18.0 ± 2.9) μg'L^-1; tmax(2.2 ± 1.2) vs (2.5 ± 1.6) h; AUC(o-t) (266 ± 48) vs (263 ±39) μg·h·L^-1; AUC(0-∞) (276 ± 50) vs (274 ± 39) μg·h·L^-1; t1/2(9.0 ± 1.3) vs (9.2 ±1.0) h. The relative bioavailability of the test formulation was 100.3%. There were no significant differences in pmax tmax,AU C (o-t), and AUC(o-∞) between the two preparations (P 〉 0.05). CONCLUSION The test tablets are bioequivalent to the reference tablets through clinical research.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2009年第7期513-517,共5页
Chinese Journal of New Drugs and Clinical Remedies
基金
上海市科委科研计划项目(08411966700)
关键词
比索洛尔
色谱法
高压液相
光谱法
质量
电喷雾电离
药动学
生物等效性
bisoprolol
chromatography,high pressure liquid
spectrometry,mass,electrospray,ionization
pharmacokinetics
bioequivalence