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目的：对口服３种５－单硝异山梨醇酯（ＩＳ－５－ＭＮ）缓释制剂—长效异乐定（参比制剂）、德脉宁和莫诺美地（受试制剂）的药代动力学和生物利用度进行对比。方法：１２名男性志愿者分为３组，分别口服受试制剂和参比制剂，抽取给药前至给药后３６小时的血样本。采用气相色谱检测法测定ＩＳ－５－ＭＮ的血药浓度。结果：３种制剂平均在口服后５．０～５．８小时达到血药峰浓度５４３．３～６１７．２ｎｇ／ｍｌ，药—时曲线下面积（ＡＵＣ０～ｔ）的平均值分别为：８４０６．５±１５４８．４ｈｎｇ／ｍｌ（长效异乐定５０ｍｇ）、８０７６．４±１８４３．９ｈｎｇ／ｍｌ（德脉宁４０ｍｇ）和８７６３．４±１５４６．４ｈｎｇ／ｍｌ（莫诺美地５０ｍｇ）。德脉宁和莫诺美地的相对生物利用度分别为１２１．４％和１０５．４％。结论：经统计学分析显示，长效异乐定和莫诺美地具有生物等效性，德脉宁与长效异乐定不等效。
OBJECTIVE: To investigate the effects of oral administration of 5-nitro-isosorbide-5-mononitrate (IS-5-MN) sustained-release preparations - Pharmacokinetics and bioavailability were compared. Methods: Twelve male volunteers were divided into three groups, each of which was orally administered with a test preparation and a reference preparation, and a blood sample taken before administration to 36 hours after the administration was taken. Plasma concentrations of IS-5-MN were determined by gas chromatography. Results: The average peak plasma concentrations of 543.3 ~ 617.2 ng / ml of all three preparations reached from 5.0 to 5.8 hours after oral administration. The mean area under the drug-time curve (AUC0 ~ t) was 8406 .5 ± 1548.4 hng / ml (Long-Term Dosage 50 mg), 8076.4 ± 1843.9 ng / ml (Dermaining 40 mg) and 8763.4 ± 1546.4 ng / ml (Monomastat 50 mg). The relative bioavailability of Demaining and Monomaly was 121.4% and 105.4% respectively. Conclusion: The statistical analysis shows that the long-acting isolimidine and Monodome have bioequivalence, and the combination of longmanglin is not equivalent.