进口与国产5-单硝酸异山梨酯缓释胶囊在中国健康人体的生物等效性  

Bioequivalence of domestic and imported 5-isosorbide mononitrate sustained release capsules in Chinese healthy male subjects

作　　者：曲恒燕[1] 高洪志[1] 李媛媛[1] 郝光涛[1] 刘泽源[1] 

机构地区：[1]军事医学科学院附属医院临床药理室,北京100071

出　　处：《中国临床药理学杂志》2013年第7期512-514,518,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价进口与国产5-单硝酸异山梨酯缓释胶囊在健康中国男性受试者体内的生物等效性。方法单中心开放性单剂量双周期随机交叉设计,24位健康中国男性受试者随机分为2组,单次口服5-单硝酸异山梨酯缓释胶囊试验或参比药物50 mg,用HPLC-MS/MS法测定血浆中5-单硝酸异山梨酯浓度,用WinNonlin 5.2.1软件计算药代动力学参数。结果试验与参比药物的主要药代动力学参数:t1/2分别为(6.16±0.61),(6.29±0.50)h;Cmax分别为(473.13±107.54),(423.42±81.70)mg·L-1;tmax分别为(3.22±2.90),(2.51±2.56)h;AUC0-t分别为(6905.83±1135.22),(6495.00±1034.65)mg·h·L-1;AUC0-∞分别为(7088.75±1200.35),(6678.33±1086.71)mg·h·L-1。Cmax、AUC0-t、AUC0-∞的90%置信区间分别为102.86%～120.07%,100.54%～112.50%,100.32%～112.31%。结论进口与国产胶囊具有生物等效性。Objective To evaluate the bioequivalence of domestic and imported 5-isosorbide mononitrate sustained-release capsules in Chinese healthy male subjects.Methods A single oral dose of 50 mg domestic or imported 5-isosorbide mononitrate sustained-release capsules were given to 24 subjects according to a single center,open label,randomized 2-way crossover design.The plasma concentrations of 5 isosorbide mononitrate were determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated and bioequivalence was compared by WinNonlin 5.2.1 program.Results The main pharmacokinetic parameters of exported and domestic 5-isosorbide mononitrate were as follow： t1/2 were（6.16 ± 0.61）,（6.29 ± 0.50） h;Cmax were（473.13 ± 107.54）,（423.42 ± 81.70） mg.L-1;tmax were（3.22 ± 2.90）,（2.51 ± 2.56） h;AUC0-t were（6905.83 ± 1135.22）,（6495.00 ± 1034.65） mg.h.L-1;AUC0-∞ were（7088.75 ± 1200.35）,（6678.33 ± 1086.71） mg.h.L-1.The 90% confidential interval of Cmax,AUC0-t and AUC0-∞ of tested formulation were 102.86% 120.07%,100.54%-112.50% and 100.32%-112.31%.Conclusion The two formulations were bioequivalent.

关 键 词：5-单硝酸异山梨酯缓释胶囊 HPLC-MS MS 生物等效性 

分 类 号：R972.3[医药卫生—药品] R969.1[医药卫生—药学]