摘要
１０名健康男性志愿者交叉口服单剂量国产５－单硝酸异山梨醇酯缓释片４０ｍｇ及进口５－单硝酸异山梨醇酯普通片（２０ｍｇ）２片，用ＧＣ－ＥＣＤ法测定血浆中５－单硝酸异山梨醇酯浓度，进行缓释片剂的药代动力学及生物利用度研究。实验结果表明：两种制剂的血药浓度－时间曲线均符合一房室模型。国产及进口制剂的体内药代动力学主要参数分别为：Ｃｍａｘ为４３８．８２±７９．５８和７３２．１０±１６６．４６μｇ·Ｌ－１；Ｔｐｅａｋ为５．２０±１．１４和０．８８±１．４３ｈ；Ｔ１／２为７．４１±０．７６和７．２２±０．６２ｈ；ＡＵＣ０→∞为５８６６．９０±９６１．３７和５９８５．７０±９５７．７０μｇ·ｈ·Ｌ－１；ＭＲＴ为１２．２９±０．８５和９．８５±０．９１ｈ。国产缓释片的平均相对生物利用度为９６．９８±１４．７７％。经统计学分析，两种制剂的ＡＵＣ无显著性差异，而Ｃｍａｘ和Ｔｐｅａｋ有显著性差异。结果说明５－单硝酸异山梨醇酯缓释片的缓释效果非常明显，与进口普通片相比，Ｃｍａｘ下降，Ｔｐｅａｋ延后。
In a randomized crossover study, single dose of isosorbide-5-mononitrate imported (conventional) tablet 40 mg (20 mg×2) or domestic (sustained release) tablet 40 mg was given to 10 healthy male volunteers. Plasma concentration was determined with GC-ECD method. The primary pharmacokinetics show: Cmax: 438.820±79.58, 732.10±166.46 μg·L-1; Tpeak: 5.20±1.14, 0.88±1.43 h ; T1/2: 7.41±0.76,7.22±0.62 h; Ke: 0.09±0.01, 0.10±0.01 h-1; AUC0→∞: 5866.90±961.37, 5985.70±957.70 μg·h·L-1; MRT: 12.29±0.85, 9.85±0.91 h in domestic and imported tablets, respectively. The concentration versus time curve after oral administration conformed to a one-compartment model with a first order absorption. The relative bioavailability of domestically sustained release tablet of IS-5-MN was 96.98±14.77%. There are no significant differences between the two products in AUC0→∞ obtained from the studies (P>0.05).
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1999年第2期126-128,148,共4页
The Chinese Journal of Clinical Pharmacology
关键词
IS-5-MN
相对生物利用度
硝酸酯类
心绞痛
isosorbide-5-mononitrate (IS-5-MN)
relative bioavailability
pharmacokinetics
sustained release tablets
