5-单硝基异山梨醇酯血浆浓度的CGC-ECD检测及健康志愿者的药代动力学研究  

Determination of plasma level of isosorbide-5-mononitrate and its pharmacokinetics in healthy volunteers by capillary gas chromatography with electron-capture detection

作　　者：刘新宇[1] 吴芳[1] 陈连剑[1] 许香广[1] 陈小江[2] 

机构地区：[1]广东医学院附属福田医院,广东深圳518033 [2]广东医学院附属医院,广东湛江524001

出　　处：《广东医学院学报》2001年第4期243-244,共2页Journal of Guangdong Medical College

摘　　要：目的 :研究单剂量口服 5-单硝基异山梨醇酯 (5- ISMN)缓释小丸的人体药代动力学和相对生物利用度。方法 :1 2名男性健康志愿者随机交叉单剂量口服 40 mg5- ISMN国产缓释小丸和进口缓释小丸 ,采用 CGC- ECD测定体内 5- ISMN的血药浓度。结果 :缓释小丸呈一级吸收的二房室开放模型 ,国产受试药品和进口参比药品的 Cmax分别为 (62 1 .83± 77.48)μg/ L和 (61 9.83± 73.50 )μg/ L,tmax分别为 (5.0± 0 .6) h和 (5.2± 0 .9) h,MRT分别为 (1 2 .67± 1 .1 0 ) h和 (1 2 .88± 1 .2 6) h,t1 / 2 分别为 (7.83± 1 .2 1 ) h和 (7.75± 1 .1 0 ) h,AUC0 - 36 分别为 (682 4 .4± 61 8.9) μg· h/ L和 (6790 .4± 60 5.7) μg· h/ L。结论 :以 AUC0 - 36 数值表征的国产缓释小丸的相对生物利用度为 (1 0 0 .63± 5.86) % ;选择 tmax、Cmax和 AUC0 - 36 进行三因素方差分析与双单侧 t检验 ,结果表明国产缓释小丸和进口缓释小丸具有生物等效性。Objective: To study the pharmacokinetics and relative bioavailability of isosorbide 5 mononitrate (5 ISMN) sustained release pellets in healthy volunteers Methods: A capillary gas chromatography with electron capture detection(CGC ECD) method was established for determination of plasma level of 5 ISMN after single oral dose of 40 mg domestic and imported 5 ISMN sustained release pellets in a randomized crossover design of 12 healthy men Results: The pharmacokinetic course of plasma level of 5 ISMN conformed to a two compartment open model The main pharmacokinetic parameters after single oral dose of 40 mg domestic and imported sustained release pellets were as follows:C max being(621 83±77 48) μg/L and (619 83±73 50) μg/L,t max (5 0±0 6) h and (5 2±0 9) h,MRT (12 67±1 10) h and (12 88±1 26) h,t 1/2 (7 83±1 21) h and (7 75±1 10) h,and AUC 0 36 (6824 4±618 9) μg·h/L and (6790 4±605 7) μg·h/L,respectively Conclusion: The relative bioavailability of domestic 5 ISMN sustained release pellets was (100 63±5 86)% The results of statistical analysis for t max ,C max and AUC 0 36 showed that domestic and imported sustained release pellets were bioequivalent

关 键 词：5-单硝基异山梨醇酯 缓释小丸 药代动力学 相对生物利用度 毛细管气相色谱电子捕获检测法 

分 类 号：R97[医药卫生—药品]