药品评价
藥品評價
약품평개
DRUG REEVALUATION
2014年
6期
21-24,34
,共5页
雷力力%方芳%太史靖华%荆洪英%杨楠
雷力力%方芳%太史靖華%荊洪英%楊楠
뢰력력%방방%태사정화%형홍영%양남
比索洛尔%CYP3A4*1G%基因多态性%药动学
比索洛爾%CYP3A4*1G%基因多態性%藥動學
비색락이%CYP3A4*1G%기인다태성%약동학
Bisoprolol%CYP3A4*1G%Genetic Polymorphism%Pharmacokinetic
目的:研究C Y P3A4*1G基因多态性对健康志愿者体内比索洛尔药动学的影响。方法:采用聚合酶链式反应-限制性片段长度多态性(PCR-RFLP)方法分析CYP3A4*1G基因型。24名健康志愿者分为CC、CT、TT三组;受试者单剂量口服5mg富马酸比索洛尔片后,采用高效液相色谱法测定血药浓度,用3P97程序的一房室模型作药动学参数估算。结果:CC、CT、TT三种基因型受试者之间主要药动学参数t1/2,Cmax及AUC0-32分别为(7.79±1.57)、(7.49±0.77)、(7.88±1.21)h;(37.23±4.00)、(38.33±8.94)、(39.51±6.55)μ g/L;(386.42±91.49),(375.53±84.51),(406.24±87.24)μ g·h/L,通过t检验,三种基因型受试者之间的主要药动学参数差异没有显著性(P>0.05)。结论:比索洛尔药动学在个体间的差异与CYP3A4*1G基因型没有相关性。
目的:研究C Y P3A4*1G基因多態性對健康誌願者體內比索洛爾藥動學的影響。方法:採用聚閤酶鏈式反應-限製性片段長度多態性(PCR-RFLP)方法分析CYP3A4*1G基因型。24名健康誌願者分為CC、CT、TT三組;受試者單劑量口服5mg富馬痠比索洛爾片後,採用高效液相色譜法測定血藥濃度,用3P97程序的一房室模型作藥動學參數估算。結果:CC、CT、TT三種基因型受試者之間主要藥動學參數t1/2,Cmax及AUC0-32分彆為(7.79±1.57)、(7.49±0.77)、(7.88±1.21)h;(37.23±4.00)、(38.33±8.94)、(39.51±6.55)μ g/L;(386.42±91.49),(375.53±84.51),(406.24±87.24)μ g·h/L,通過t檢驗,三種基因型受試者之間的主要藥動學參數差異沒有顯著性(P>0.05)。結論:比索洛爾藥動學在箇體間的差異與CYP3A4*1G基因型沒有相關性。
목적:연구C Y P3A4*1G기인다태성대건강지원자체내비색락이약동학적영향。방법:채용취합매련식반응-한제성편단장도다태성(PCR-RFLP)방법분석CYP3A4*1G기인형。24명건강지원자분위CC、CT、TT삼조;수시자단제량구복5mg부마산비색락이편후,채용고효액상색보법측정혈약농도,용3P97정서적일방실모형작약동학삼수고산。결과:CC、CT、TT삼충기인형수시자지간주요약동학삼수t1/2,Cmax급AUC0-32분별위(7.79±1.57)、(7.49±0.77)、(7.88±1.21)h;(37.23±4.00)、(38.33±8.94)、(39.51±6.55)μ g/L;(386.42±91.49),(375.53±84.51),(406.24±87.24)μ g·h/L,통과t검험,삼충기인형수시자지간적주요약동학삼수차이몰유현저성(P>0.05)。결론:비색락이약동학재개체간적차이여CYP3A4*1G기인형몰유상관성。
Objective:To find the effect of different CYP3A4*1G genotypes on pharmacokinetics of bisoprolol's in healthy volunteers. Methods: CYP3A4*1G genotypes were determined by real-time PCR. 24 healthy people were divided into three different genotype groups of CC, CT and TT(n=8) in the research. All of them were administered with bisoprolol fumarate tablet as a single dosage of 5mg. Plasma concentrations of bisoprolol were measured by HPLC. Results: The main pharmacokinetic parameters of CC, CT and TT were as follows:t1/2(7.79±1.57)、(7.49±0.77)、(7.88±1.21)h,Cmax (37.23±4.00)、(38.33±8.94)、(39.51±6.55)μg/L and AUC0-32 (386.42±91.49), (375.53±84.51), (406.24±87.24)μg·h/L. There was no significant differences among the three genotypes by T test(P>0.05). Conclusion:The individual differences of bisoprolol's pharmacokinetics has no relationship with CYP3A4*1G genotypes.