3种伊曲康唑胶囊的人体相对生物利用度  

Relative bioavailability of three itraconazole capsules in healthy volunteers

作　　者：陈钧[1] 江文明[1] 高小玲[1] 蒋新国[1] 

机构地区：[1]复旦大学药学院药剂学教研室,上海200032

出　　处：《中国临床药学杂志》2004年第1期19-21,共3页Chinese Journal of Clinical Pharmacy

摘　　要：目的 :比较 3种市售伊曲康唑胶囊的生物等效性 ,为临床合理用药提供参考。方法 :15名健康男性受试者 ,随机分为3组 ,采用 3制剂、3周期的拉丁方设计 ,单剂量口服 2 0 0mg伊曲康唑后 ,采用HPLC法测定血浆药物浓度。cmax,tmax采用实测值 ,AUC用梯形法计算 ,并用双单侧t检验评价 3种制剂之间的生物等效性。结果 :口服制剂A ,B和参比制剂后的cmax分别为(197± 92 ) ,(2 16± 76 ) ,(2 72± 10 9) μg·L-1;tmax分别为 (4 17± 1 2 5 ) ,(4 2 7± 1 16 ) ,(4 0 0± 1 0 7)h ;T1/2 为 (2 5 2± 4 9) ,(2 4 6±5 5 ) ,(2 4 9± 3 9)h ;AUC0→ 72h分别为 (32 31± 1195 ) ,(30 38± 980 ) ,(4 2 97± 12 99) μg·h·L-1。制剂A ,B相对参比制剂的生物利用度分别为 (75 2 1± 9 18) %和 (71 72± 14 2 1) %。结论 :制剂A ,B与参比制剂的AUC ,cmax,均有显著性差异 (P <0 0 5 ) ;双单侧t检验结果显示A 。AIM: To evaluate relative bioavailability of 3 itraconazole capsules in healthy volunteers. METHODS: Fifteen healthy adult male volunteers participated in this 3 periods, 3 sequences crossover study. The volunteers were randomly assigned to 3 treatment groups and were administered with a single oral dose of 200 mg itraconazole capsule (test or reference drug) in each stage. Plasma was separated and the concentration of itraconazole in human plasma was determined by HPLC using fluorescence detector after liquid-liquid extraction. The values of c max and t maxwere directly measured, and AUC was calculated by linear trapezoid method, while the bioequivalence of the 3 products were compared by two one-side t-test. RESULTS: The c max,t max,AUC 0→72h of test drug A, test drug B and reference drug were ( 197±92), (216±76) and (272±109) μg·L -1; (4.17±1.25), (4.27±1.16) and (4.00±1.07) h; (3 231±1 195),(3 038±980) and (4 297±1 299) μg·h·L -1, respectively. The relative bioavailability of test A and test B as compared with reference drug were (75.21±9.18)% and (71.72±14.21)%, respectively. CONCLUSION: The pharmacokinetic parameters (AUC, c max) showed significant difference between test and reference formulations according to ANOVA analysis. The test and reference drugs are not bioequivalence after two one-side t-test.

关 键 词：伊曲康唑胶囊 人体 生物利用度 高效液相色谱 生物等效性 

分 类 号：R96[医药卫生—药理学]