二氢杨梅素含片在实验兔体内的药物代谢动力学研究

Pharmacokinetics of dihydromyricetin buccal tablets in rabbits

目的研究2个不同剂量的二氢杨梅素含片在实验兔体内的药物代谢动力学。方法实验兔按500、1000 mg/只口腔给药后,HPLC-UV法测定血药浓度,采用DAS 3.0软件拟合药动学参数。结果 500、1000 mg/只剂量下的t1/2分别为:(3.37±2.51)h和(3.08±3.52)h;AUC0~t分别为:(329.76±174.48)μg·h·L^(-1)和(407.99±369.87)μg·h·L^(-1);AUC0~∞分别为:(471.04±305.25)μg·h·L^(-1)和(607.16±511.45)μg·h·L^(-1);Cmax分别为:(131.37±81.57)μg·L^(-1)和(113.45±82.01)μg·L^(-1);tmax分别为(2.67±1.21)h和(4.50±3.02)h。2个剂量组间的t1/2无明显差别,Cmax未见与剂量相关的差异。AUC、tmax随剂量的增加有增加的趋势,但AUC的增加与剂量增加不成比例关系,这可能与含片在动物口腔内给药后的崩解速度有关。结论本实验模拟人临床给药方式,对二氢杨梅素含片在实验兔体内的药动学过程进行了研究,为临床用药提供了一定的实验参考。

Objective To determine the pharmacokinetics of 2 doses of dihydromyricetin buccal tablets in rab- bits. Methods Two groups of rabbits were treated with dihydromyricetin buccal tablets （500 mg and 1000 mg）. The concentration of dihydromyricetin at different time was determined by HPLC-UV. Results The phar- macokinetic parameters t1/2, A UC0 - t,AUC0 -∞, Cmax and tmax of the 500, 1000 mg group were （3.37± 2.51） h and （3.08±3.52） h; （329.76± 174.48） μg · h · L - 1 and （407.99±369.87） μg · h ·L - t; （471.04±305.25） μg · h · L - 1 and （607.16±511.45） μg · h · L - 1; （131.37±81.57） μg · h · L - 1and （113.45±82.01） μg · h · L - 1 and （2.67 ± 1.21） h and （4.50 ± 3.02） h, respectively. There was no significant difference in tlj2, and dose related difference was not observed in Cmax. tmax increased with the dose. AUC also increased, but the increasing degree was disproportional with dose. These results might be related with the disintegration speed ofbuccal tablets after the administration. Conclusion This research studies the pharmacokinetics of dihydromyricetin buccal tablets in rabbits, and provides experimental reference for clinical practice.