褪黑素缓释片与普通片在犬体内药动学研究

Study on Pharmacokinetics of the Sustained-release Tablets and Common Tablets of Melatonin in Beagle Dogs in Vivo

目的:比较褪黑素普通片与缓释片在Beagle犬体内药动学参数。方法:6只Beagle犬随机、交叉、单剂量灌服褪黑素缓释片6mg或普通片3mg后,采用高效液相色谱法测定其血药浓度;以3p97软件计算药动学参数。结果:普通片和缓释片犬体内药-时曲线符合二室模型,Cmax分别为(11.27±3.77)、(8.31±5.11)ng/ml,tmax分别为(0.50±0.18)h、(1.00±0.37)h,t1/2ke分别为(1.21±0.52)h、(3.27±0.89)h,AUC0～t分别为(25.23±7.71)、(38.03±16.45)(ng·h)/ml。结论:与普通片比较,缓释片吸收较慢,药物达峰时间更长,峰浓度更低,消除更慢,维持时间更长。

OBJECTIVE： To compare pharmacokinetic parameters of the common tablets and sustained - release melatonin tablets in beagle dogs in vivo. METHODS： The blood concentration of melatonin of 6 Beagle dogs was determined by HPLC and the pharmacokinetic parameters were calculated with 3p97 software after administered random crossover with single dose of sustained - release melatonin tablets 6mg or the common tablets 3 mg. RESULTS： The concentration - time curves of both the common tablets and sustained - release melatonin tablets were in conformity with two - compartment model, Cmax of common tablets and sustained- release tablets were （11.27± 3.77） ng/ml and （8.31± 5.11） ng/ml respectively, tmax of which were （0.50±0.18） h and （1.00±0.37） h respectively, t1/2ke of which were（1.21± 0.52） h and （3.27±0.89） h, AUC0-t of which were（25.23±7.71） （ng· h）/ml and（38.03± 16.45） （ng· h）/ml respectively. CONCLUSION： Compared with the common tablets, the sustained-release tablets showed slower absorption, longer peak time, lower peak concentration, slower elimination and longer duration.