格列吡嗪片在健康志愿者体内的生物等效性评价  

Assessment of bioavailability and pharmacokinetics of glipizide in healthy volun teers

作　　者：文爱东[1] 赵磊[1] 张三奇[1] 杨志福[1] 蒋永培[1] 

机构地区：[1]第四军医大学西京医院,陕西西安710032

出　　处：《中国医院药学杂志》2001年第9期515-517,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的：比较两种格列吡嗪片剂在健康志愿者体内的药动学及 生物等效性。方法： 12例男性健康志愿受试者，采用标准两周期交叉设计自身对照试验法，单剂量口服进口和国 产格列吡嗪片10 mg，以高效液相色谱法测定血浆中格列吡嗪的经时浓度，以双单侧t检 验统计法比较两种格列吡嗪片之间的差异。结果：两种格列吡嗪片在健康志愿者体内的药-时曲线均符合一级吸收的单室模型，国产格列吡嗪 片主要的药动学参数Tmax 、Cmax和AUC(0-17)分 别为：(2.6±0.5) h ，(609.7±112.9) ng·ml-1和(4499.8 ±969.0) ng·h-1·ml-1；进口 格列吡嗪片主要的药动学参数Tmax 、Cmax和AUC(0-17)分别为 ：(2.6±0.5) h, (568.8±1 01.9) ng·ml-1和(4108.3±724.9) ng·h·ml-1。两种格列吡嗪 片主要药动学参数间均无 统计学差异（P＞0.05），国产格列吡嗪片相对生物利用度F为（109.5± 4.5）%。结论：两种格列吡嗪片在健康志愿者体内具有相同的生物效应，可确保临床用药的安全有效。：OBJECTIVE To compare the pharmacokinetic parameters and relative bioav ailability of glipizide tablets (domestic and imported). METHODS An open, randomize d, two-period crossover study with a one-week washout interval was conducted in 12 male healthy volunteers. Concentrations of glipizide in plasma were assayed by HPLC after a single oral dose of 10 mg imported glipizide or domestic gl ipizide. The main pharmacokinetics parameters (AUC, C max and T max) were analyzed by two one-sided test. RESULTS The concentration-time curve after medication conformed to a 1-compartment ope n model with a first order absorption. T max, C max and AUC(0-17) of domestic product were (2.6±0.5) h ，(609.7 ±112.9) ng·ml-1 and (4499.8±969.0) ng·h-1·ml- 1· T max, C max and AUC(0-17) of imported product wer e (2.6±0.5) h, (568.8±101.9) ng·ml-1 and (4108.3± 724.9) ng·h·ml-1 respectively. CONCLUSIONS The relative bioavailability of domestic product to impor ted product was（109.5±4.5）% .The results showed that the two formulat ions were bioequivalent.

关 键 词：格列吡嗪 药动学 生物等效性 高效液相色谱法 降血糖药 

分 类 号：R977.15[医药卫生—药品] R969.1[医药卫生—药学]