中国临床药理学与治疗学2013，Vol.18Issue(5)：527-531,5.
空腹或餐后服用国产伊曲康唑胶囊的人体生物等效性研究
Study on bioequivalence of domestic Itraconazole capsules before or after diet
摘要
Abstract
AIM:To study the bioequivalence of domestic Itraconazole capsules in healthy Chinese volunteers before diet or after diet respectively.METHODS:There were two randomized,open-label,two-period clinical studies,and 24 healthy Chinese male volunteers were enrolled in each study.All the volunteers in each study had taken a single dose of 200 mg Itraconazole test capsules and 200 mg of its reference.The plasma Itraconazole concentration were determined by HPLC-MS/MS.The major harmacokinetic parameters were calculated,the bioequivalence of Itraconazole test capsule and its reference before diet as well as after diet were evaluated respectively.RESULTS:The pharmacokinetic parameters before diet were as follows:Cmax were (124±79) and (124±86) μg/L;tmax were (2.9 ± 0.8) and (2.5 ± 0.9) h; AUC0-t were (1320 ± 826) and (1348 ± 1095)μg · h · L-1 ; AUC0-∞ were (1420 ± 902) and (1444 ± 1148) μg · h · L-1 ; AUC0-t/AUC0-∞were (93.0±4.9)％ and (92.3±5.1)％;t1/2were (17.7±4.7) and (18.1±2.8) h.The relative bioavailability of the test capsule was (106.5± 35.4) ％.The pharmacokinetic parameters after diet were as follows:Cmax were (202±107) and (218±109) μg/L;tmax were(4.2±0.8)and (3.9±0.8) h;AUC0-t were(2494±1163)and(2657± 1424) μg· h· L-1; AUC0-∞ were (2705±1290) and (2870±1578) μg· h· L-1;AUC0-t/AUC0-∞ were (92.3±5.2)％/(93.6±4.1)％;t1/2 were (19.3±5.5) and (18.0±5.1)h.The relative bioavailability of the test capsule was (100.5 ± 33.1) ％.CONCLUSION:The Itraconazole test capsule and its reference were bioequivalent both when administrated before diet and after diet.The Cmax and AUC were both significant higher when administrated after diet,so it is better to dose after diet for Itraconazolecapsule in order to gain a higher bioavailability and an increased effect.关键词
伊曲康唑/生物等效性/HPLC-MS/MSKey words
Itraconazole/ Bioequivalence/HPLC-MS/MS分类
医药卫生引用本文复制引用
黄洁,阳国平,项玉霞,杨柳,谭鸿毅,杨双..空腹或餐后服用国产伊曲康唑胶囊的人体生物等效性研究[J].中国临床药理学与治疗学,2013,18(5):527-531,5.基金项目
重大疾病新药临床评价研究综合技术平台建设(2012ZX09303014-001) （2012ZX09303014-001）
国家"重大新药创制"科技重大专项 （）
