摘要
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 determine both the pharmacokinetic parameters and the relative bioavailability of three sustained release isosorbide 5 mononitrate preparations(IS 5 MN),the reference preparation Elantan long(EL),and two test preparation IS 5 mono retardratiopharm 40(IMR) and Mono MACK(MM)after single oral administration. Methods:The test and the reference preparations were examined in 12 health male volunteers according to a randomized cross over design,blood samples were withdrawn before and up to 36 hours after administration.The plasma concentrations of those preparations of IS 5 MN were determined by gas chromatography method. Results:The peak plasma level of three preparations of IS 5 MN was 543.3～617.2 ng/ml 5.0 to 5.8 hours after administration;The mean values of the areas under the curves (AUC 0～t ) were 8 406.5±1 548.4 h·ng/ml(EL 50 mg),8 076.4±1 843.9 h·ng/ml(IMR 40 mg) and 8 763.4±1 546.4 h·ng/ml(MM 50 mg),respectively.The relative bioavailability of IMR revealed 121.4%(IMR/EL) and that of MM 105 4%(MM/EL). Conclusion:The results showed that there is bioequivalence between MM and EL,but non bioequivalence between IMR and EL.
出处
《中国循环杂志》
CSCD
北大核心
1998年第5期290-292,共3页
Chinese Circulation Journal
关键词
单硝异山梨醇酯
缓释剂
药代动力学
生物利用度
Isosorbide 5 mononitrate
Pharmacokinetics
Bioavailability
Gas chromatography
