酮洛芬脉冲控释片在家犬体内的药动学及生物利用度研究  

Pharmacokinetics and Bioavailability of Pulse Controlled-release Tablets of Ketoprofen in Dogs

作　　者：徐艳丽[1] 刘天富 张晓莉[3] 刘兰娣[3] 郎轶咏[3] 

机构地区：[1]哈尔滨医科大学附属第四医院药学部,哈尔滨市150001 [2]哈尔滨泰华药业股份有限公司,哈尔滨市150302 [3]解放军第202医院药学部,沈阳市110003

出　　处：《中国药房》2009年第7期506-508,共3页China Pharmacy

摘　　要：目的:考察酮洛芬脉冲控释片在家犬体内的药动学及生物利用度。方法:将6只犬随机均分为2组,分别口服受试制剂酮洛芬脉冲控释片和参比制剂酮洛芬肠溶胶囊150mg,1周后2组交叉试验。给药后不同时间点取样,采用高效液相色谱法测定血样中酮洛芬浓度并计算药动学参数及比较体内、外相关性。结果:受试制剂与参比制剂的tmax分别为(5.00±0.41)、(3.75±0.00)h;Cmax分别为(15.40±1.94)、(20.73±1.72)μg·mL-1,AUC0～t分别为(101.33±17.49)、(93.21±25.03)μg.h.mL-1,受试制剂相对生物利用度为108.71%,体外释药与体内吸收数据r=0.987,具有较好的相关性。结论:酮洛芬脉冲控释片与酮洛芬肠溶胶囊具有生物等效性。OBJECTIVE： To study the pharmacokinetics and bioavailability of pulse controlled - release tablets of ketoprofen（KRT） in dogs. METHODS： A total of 6 dogs were randomly assigned to receive KRT （trial group, n = 3） or KP enteric- coated capsules （control group, n = 3） 150 mg, then a crossover trial was conducted 1 week later. Plasma samples were taken at different time points and the plasma concentration of ketoprofen in dogs was determined by HPLC. The pharmacokinetie parameters of the two KP preparations were computed and the correlation between absorption percentage in vivo and release rate in vitro was compared. RESULTS： The pharmacokinetic parameters of KRT versus those of its control preparation were as follows： t ： （5.00±0.41） vs. （3.75±0.00） h; C ： （15.40±1.94） vs. （20.73±1.72）μg·mL^-1; AUC0-t （ 101.33 ± 17.49） vs. （93.21 ± 25.03）μg·mL^-1. The relative bioavailability of the trial preparation was 108.71%. The test preparation showed a good correlation （r = 0.987） between absorption percentage in vivo and release rate in vitro. CONCLUSIONS： The KRT and KP enteric coated capsules were bioequivalent.

关 键 词：酮洛芬脉冲控释片 犬 生物利用度 药动学 

分 类 号：R969.1[医药卫生—药理学] R965[医药卫生—药学]