复方烟酸缓释片与烟酸普通片在犬体内药代动力学的比较研究  

Pharmacokinetics comparison between compound nicotinic acid sustained-release tablets and nicotinic acid tablets in beagle dogs

作　　者：于华[1] 孙立新[1] 王婷婷[2] 孙峰[3] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]沈阳华泰药物研究有限公司,辽宁沈阳110015 [3]沈阳东陵药业股份有限公司,辽宁沈阳110161

出　　处：《西北药学杂志》2009年第3期201-204,共4页Northwest Pharmaceutical Journal

摘　　要：目的比较复方烟酸缓释片与烟酸普通片中烟酸及其代谢物烟尿酸在Beagle犬体内的药代动力学。方法6只Beagle犬采用随机交叉给药方案,单剂量口服500mg复方烟酸缓释片或烟酸普通片后,用RP-HPLC法同时测定Beagle犬血浆中烟酸及其主要代谢物烟尿酸的药物浓度,计算药动学参数和相对生物利用度。结果Beagle犬单剂量口服500mg复方烟酸缓释片和烟酸普通片后,烟酸主要药代动力学参数tmax分别为(2.17±0.61)h和(1.04±0.49)h,Cmax分别为(30.85±4.50)mg·mL-1和(68.05±20.48)mg·mL-1,t1/2分别为(0.69±0.43)h和(0.43±0.10)h,MRT分别为(2.12±0.62)h和(1.72±0.40)h,AUC0-12h分别为(62.17±21.13)mg·h·L-1和(138.67±44.86)mg·h·L-1;烟尿酸主要药代动力学参数tmax分别为(2.42±0.49)h和(1.50±0.45)h,Cmax分别为(0.76±0.34)mg·mL-1和(1.66±0.63)mg·mL-1,t1/2分别为(1.74±1.24)h和(1.64±1.03)h,MRT分别为(2.42±0.62)h和(1.79±0.38)h,AUC0-12h分别为(1.55±0.76)mg·h·L-1和(3.25±1.16)mg·h·L-1。结论单剂量口服复方烟酸缓释片,测得的Cmax、tmax和AUC与烟酸普通片均有显著性差异,受试缓释片的tmax长于参比普通片,Cmax低于参比普通片,说明受试缓释片无突释现象,有一定缓释效果。Objective To compare the pharmacokinetics of nicotinic acid and nicotinuric acid after oral administration of compound nicotinic acid sustained-release tablets and nicotinic acid tablets in beagle dogs. Methods A single oral dose of 500 mg compound nicotinic acid sustained-release tablets and nicotinuric acid tablets were administered to each dog according to an open randomized crossover design. Simultaneous determination of nicotinic acid and its metabolite,nicotinuric acid in beagle dog plasma was carried out by RP-HPLC. The pharmacokinetic parameters of compound nicotinic acid sustained-release tablets and nicotinuric acid tablets were calculated by DASver 1.0. Results The main pharmacokinetic parameters of nicotinic acid after oral adminstration of compound nicotinic acid sustained-release tablets and nicotinic acid tablets were as follows： tmax were（ 2.17 ± 0.61）h and （1.04±0.49） h, respectively, Cmax were （（30. 85±4.50）mg · L^-1 and （68.05±20.48）mg · L^-1 , respectively, t 1/2 were （0.69±0.43）h and （0.43± 0.10）h, respectively,MRT were （2.12±0.62）h and （1.72±0.40）h, respectively;AUC0-12h were（62. 17±21.13）mg · h · L^-1 and （138.67 ± 44.86）mg · h · L^-1, respectively. The main pharmacokinetic parameters of nicotininuric acid after oral administration of compound nicotinic acid sustained-release tablets and nicotinic acid tablets were as follows： t max were（ 2.42±0.49）h and （1.50±0.45）h, respectively, C max were （0. 76±0. 34）mg · L^-1 and （1.66±0.63）mg · L^-1 , respectively, t 1/2 were （1.74± 1.24）h and （1.64±1.03）h, respectively, MRT were （2.42±0.62）h and （1.79±0.38）h, respectively;AUC0-12 b were（1.55± 0.76）mg · h · L^-1 and （3.25±1.16）mg · h · L^-1 , respectively, mg · L^-1. Conclusions The t max of compound nicotinic acid sustained-release tablets was significantly longer than that of the conventional nicotinic acid tablets （ P 〈0.05 ）, and the C max was significantly lower than tha

关 键 词：烟酸 烟尿酸 缓释片 血药浓度 药代动力学 

分 类 号：R945[医药卫生—微生物与生化药学]