反式和顺式二苯乙烯苷在大鼠体内的药代动力学比较研究

Comparison of pharmacokinetic parameters of trans- and cis-2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside on rats

关键词:  何首乌  反式二苯乙烯苷  顺式二苯乙烯苷  药代动力学  单次给药

Key words:  Polygonum multiflorum Thunb.  trans-2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside  cis-2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside  pharmacokinetics  single administration

摘要:

[目的] 比较何首乌中反式二苯乙烯苷和顺式二苯乙烯苷在大鼠体内的药代动力学差异。[方法] 分别单次灌胃给药（60mg/kg）反式二苯乙烯苷和顺式二苯乙烯苷后，测定大鼠给药后不同时间点的血浆中药物浓度，通过计算药代动力学参数，比较两者的体内药动学行为差异。[结果] 单次给药反式二苯乙烯苷和顺式二苯乙烯苷后，大鼠血浆中顺式二苯乙烯苷的半衰期（T_1/2）显著高于反式二苯乙烯苷（P<0.05），而反式二苯乙烯苷在大鼠体内的达峰浓度（C_max）和清除率（CLz/F）则显著高于顺式二苯乙烯苷（P<0.05）。[结论] 单次给予相同浓度的反式二苯乙烯苷和顺式二苯乙烯苷后，两者在大鼠体内的药代动力学行为存在明显差异。

Abstract:

[Objective] Comparison of the pharmacokinetic differences of trans-2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (trans-TSG) and cis-2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (cis-TSG) in Polygonum multiflorum Thunb. in rats.[Methods] After a single intragastric administration of 60 mg/kg of trans-TSG and cis-TSG,the drug concentrations in the plasma of rats were determined at different time points and the in vivo pharmacokinetic parameters were calculated.[Results] Significant differences were found in pharmacokinetic parameters. T_1/2 of cis-TSG was significantly higher than that of trans-TSG(P<0.05). However,CLz/F,and C_max of trans-TSG in the plasma were significantly higher than cis-TSG (P<0.05).[Conclusion] The pharmacokinetic behavior of trans-TSG and cis-TSG in rats was significantly different following a single intragastric administration of the same concentrations of them.