摘要
目的:研究诺氟沙星胃漂浮缓释片与普通片在犬体内的药动学特点及生物利用度。方法:将6只家犬随机分成2组,采用2种制剂双周期随机交叉自身对照实验设计方案,分别灌服400mg诺氟沙星胃漂浮缓释片(1片)或普通片(4片),于服药前和服药后0.5、1、2、3、4、6、8、10、13、16、24h分别取股静脉血,采用反相高效液相色谱法测定犬体内的血药浓度,用3p97药动学程序拟合,计算药动学参数并评价生物等效性。结果:诺氟沙星普通片和胃漂浮缓释片的Cmax分别为(3.51±0.57)、(2.51±0.55)μg.mL-1,tmax分别为(1.79±0.65)、(3.72±0.48)h,AUC0～24分别为(21.10±3.14)、(21.31±4.32)μg.h.mL-1,平均滞留时间分别为(5.68±0.51)、(7.71±0.67)h,胃漂浮缓释片相对生物利用度为103.5%。结论:诺氟沙星胃漂浮缓释片与普通片相比平均滞留时间延长,缓释效果更好,且2种制剂具有生物等效性。
OBJECTIVE： To study the pharmacokinetics and bioavailability of norfloxacin intragastric floating sustained - release tablets（NIFST） vs. its conventional tablets in dogs. METHODS： By a randomized crossover self-control design, 6 healthy dogs were randomly assigned to receive 400 mg NIFST （1 tablet） or its conventional tablets （4 tablets） . Femoral venous blood samples were taken at 0.5, 1, 2, 3, 4, 6, 8, 10, 13, 16 and 24 h respectively after oral medication. The concentration of norfloxacin in plasma was determined by RP- HPLC and fitted using 3p97 pharmacokinetic program. The main pharmacokinetic parameters were computed and the relative bioavailability of the NIFST was evaluated. RESULTS： The pharmacokinetic parameters of the conventional tablets vs. NIFST were as follows： Cmax： （3.51± 0.57） vs. （2.51± 0.55）ug·mL^-1; tmax： （1.79±0.65） vs. （3.72±0.48） h; AUC0-24： （21.10±3.14） vs. （21.31±4.32） ug·h·mL^-1; MRT： （5.68 ± 0.51） vs. （7.71 ±0.67） h. The relative bioavailability of NIFST was 103.5 %. CONCLUSION ： As compared with the conventional tablets, the NIFST had longer MRT and remarkable sustained release characteristics. The two kinds of tablets were proved to be bioequivalent.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第16期1216-1217,共2页
China Pharmacy
关键词
诺氟沙星
胃漂浮缓释片
普通片
犬
药动学
生物利用度
Norfloxacin
Intragastric floating sustained- release tablets
Common tablets
Dogs
Pharmacokinetics
Bioavailability
