格列吡嗪缓释胶囊及其生物利用度的研究  

Studies on Glipizide Sustained-Release Capsules and Their Bioavailability

作　　者：戈文兰[1] 王广基[2] 高凌中国药科大学药物代谢和药动学研究中心 何海燕[1] 郭建兰[1] 

机构地区：[1]江苏省药物研究所,南京210009 [2]中国药科大学药物代谢和药动学研究中心,南京210009

出　　处：《中国药科大学学报》2000年第5期371-374,共4页Journal of China Pharmaceutical University

摘　　要：研制了格列吡嗪缓释胶囊 (SRC) ,释放曲线与国外同类缓释片 (ESRT)基本一致。 10名健康志愿受试者交叉口服SRC和美吡达 (普通片 ,CT)后 ,进行了药物动力学和相对生物利用度的研究。单剂量口服 5mg ,SRC和CT的AUC分别为 5 189.33± 6 2 1.10ng·h/ml和 5 198.5 2± 881.73ng·h/ml,MRT分别为 11.97±2 .30h和 7.46± 0 .82h ,Cmax分别为 5 0 7.34± 114.0 2ng/ml和 834.5± 92 .8ng/ml;Tmax分别为 4.4± 1.3h和2 .0± 0 .4h ,SRC的相对生物利用度为 (99.8± 10 ) %。多剂量口服SRC(每日 1次 ,每次 10mg)和CT(每日 2次 ,每次 5mg)研究 ,Cmin分别为 6 8.1± 38.9ng/ml和 5 8.4± 44 .8ng/ml,Cmax分别为 5 6 5 .9± 10 4.6ng/ml和5 5 8.5± 181.3ng/ml,波动系数FI分别为 1.5 7± 0 .2 5和 1.6 4± 0 .4。表明日服一次SRC与日服 2次CT生物等效。Glipizide(GLP) sustained-release capsules(SRC) were prepared for reducing the administration times and making convenience to the patients. The studies showed that the release curve of SRC \%in vitro\% was almost similar to that of the Glucotrol XL (ESRT). The pharmacokinetics and relative bioavailability (F) of SRC and conventional tablets (CT) were investigated in 10 healthy male volunteers. The results of single dose test indicated that F of SRC was (99.8±10)%. AUC of SRC and CT were 5189.33±621.10 ng·h/ml and 5198.52±881.73 ng·h/ml. C max of SRC and CT were 507.34±114.02 ng/ml and 834.5±92.8 ng/ml, respectively. T max of SRC and CT were 4.4±1.3 h and 2.0±0.4 h. The C max and T max for the SRC and CT were significantly different while the AUC for the two preparations was equal. After multiple doses, C min of SRC and CT were 68.1±38.9 ng/ml and 58.4±44.8 ng/ml. C max of SRC and CT were 565.9±104.6 ng/ml and 558.5±181.3 ng/ml. FI of SRC and CT were 1.57±0.25 and 1.64±0.14, respectively. The results showed that the two preparations were bioequivalent.

关 键 词：格列吡嗪 缓释胶囊 相对生物利用度 降血糖药 

分 类 号：R96[医药卫生—药理学]