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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，可减少药物不良反应的发生
Ten healthy male volunteers were given a single oral dose of 40 mg of isosorbide-5-mononitrate sustained-release tablets and 2 of isosorbide mononitrate-normal tablets (20 mg), and the plasma concentrations of 5 - isosorbide mononitrate concentration, the sustained release tablets pharmacokinetics and bioavailability studies. The experimental results show that the plasma concentration-time curves of the two preparations conform to the one-compartment model. The main pharmacokinetic parameters of domestic and imported preparations were as follows: Cmax was 438.82 ± 79.58 and 732.10 ± 166.46μg · L-1; Tpeak was 5.20 ± 1.14 and 0.88 ± 1.43 h; T1 / 2 was 7.41 ± 0.76 and 7.22 ± 0.62 h; AUC0 → ∞ 5866.90 ± 961.37 and 5985.70 ± 957.70 μg · h · L -1 ; MRTs were 12.29 ± 0.85 and 9.85 ± 0.91 h. The average relative bioavailability of domestic sustained-release tablets was 96.98 ± 14.77%. The statistical analysis showed no significant difference in AUC between the two preparations, but Cmax and Tpeak were significantly different. The results showed that the sustained-release effect of isosorbide 5-mononitrate sustained-release tablets is very obvious, compared with the imported common tablets, Cmax decreased, Tpeak delayed, can reduce the occurrence of adverse drug reactions