褪黑素缓释片与普通片在犬体内药动学研究

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。

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

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 of6Beagle dogs was determined by HPLC and the pharmacokinetic parameters were calculated with3p97software after administered random crossover with single dose of sustained-release melatonin tablets6mg or the common tablets3mg.RESULTS:The concentration-time curves of both the common tablets and sustained-release melatonin tablets were in conformity with two-compartment model,C max of common tablets and sustained-release tablets were(11.27±3.77)ng/ml and(8.31±5.11)ng/ml respectively,t max of which were(0.50±0.18)h and(1.00±0.37)h respectively,t 1/2ke of which were(1.21±0.52)h and(3.27±0.89)h,AUC 0～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.