5-单硝酸异山梨酯缓释片的生物利用度研究  

Study on Relative Bioavailability of SlowRelease Isosorbide5Mononitrate Tablet

作　　者：杨丽莉[1] 袁倚盛[1] 赵飞浪[1] 

机构地区：[1]南京军区南京总医院仪器分析室

出　　处：《中国药科大学学报》1998年第1期39-41,共3页Journal of China Pharmaceutical University

摘　　要：对５－单硝酸异山梨酯缓释片（ＳＲ）和普通片（ＩＲ）进行人体生物利用度比较，１０名健康男性志愿者随机交叉口服单剂量两种剂型后，利用气相色谱测得血药浓度。ＳＲ和ＩＲ的ＡＵＣ分别为３４３７．２±５６８．８ｎｇ／ｍｌ·ｈ和３８１０．８±８２２．７ｎｇ／ｍｌ·ｈ，ＭＲＴ分别为１５．７±１．０ｈ和９．４±１．５ｈ。ＳＲ的相对生物利用度为（９１．４±９．８）％。１０名受试者多剂量服用５－单硝酸异山梨酯ＳＲ和ＩＲ后，稳态时Ｃｍｉｎ分别为１６６．５±４７．９ｎｇ／ｍｌ和２３２．０±５５．０ｎｇ／ｍｌ，Ｃｍａｘ分别为６５０．１±１１８．５ｎｇ／ｍｌ和６２５．８±１２６．８ｎｇ／ｍｌ，两种制剂血药浓度的波动系数ＦＩ分别为１．１８±０．１８和０．９２±０．１６。经配对ｔ检验，两种制剂具有生物等效性。The pharmacokinetics and relative bioavailability of slowrelease isosorbide5mononitrate tablets(SR) were investigated at oral dose of 60 mg in 10 healthy volunteers. Drug concentrations in plasma were assayed by gas chromatography. The peak concentration(C max ) of 5ISMN SR was 480.4±85.5 ng/ml, and the areas under the drug concentration curves(AUC) was 3437.2±568.8 ng/ml·h. The relative bioavailability of 5ISMN SR was 91.4%±9.8%. After multiple dosing, the mean steady state C min values were 232.0±55.0 ng/ml and 166.5±47.9 ng/ml, and the mean C max values were 625.8±126.8 ng/ml and 650.1±118.5 ng/ml for immediate tablets(IR) and SR, respectively. The fluctuation indexes(FI) for the two formulation were 0.92±0.16 and 1.18±0.18, respectively. The results showed that the two formulations were bioequivalent.

关 键 词：5-单硝酸异山梨酯 缓释制剂 生物利用度 气相色谱法 

分 类 号：R972[医药卫生—药品] R969.1[医药卫生—药学]