银杏叶总黄酮及其水解物静脉注射给药后在大鼠体内的药动学研究

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目的研究银杏叶提取物中黄酮类成分及其水解物大鼠尾iv给药后的药动学差异,同时研究内酯类成分对黄酮类成分药动学的影响。方法以高效液相色谱法测定血浆中槲皮素、山柰素和异鼠李素,用3p97软件进行药动学参数的计算。结果槲皮素药动学符合二房室模型,山柰素和异鼠李素的药动学符合非房室模型。银杏水解物中槲皮素的t1/2比银杏叶提取物中槲皮素的t1/2短,与水解物相比提取物的相对生物利用度低,水解物中异鼠李素的相对生物利用度高。结论银杏黄酮糖苷在大鼠体内转化为黄酮苷元的量较少,苷元的相对生物利用度较高;内酯对黄酮的代谢无明显影响。 Objective To study the pharmacokinetics differences of flavonoids and their hydrolyzates in the ginkgo biloba extract after iv administration, and to study the effects of lactones on the pharmacokinetics of flavonoids. Methods The contents of quercetin, kaempferol and isorhamnetin in plasma were determined by HPLC. The pharmacokinetic parameters were calculated by 3p97 software. Results The pharmacokinetics of quercetin was in accordance with the two-compartment model. The pharmacokinetics of kaempferol and isorhamnetin were in accordance with the non-compartmental model. The t 1/2 of quercetin in the ginkgo hydrolyzate was shorter than that of quercetin in the extract of Ginkgo biloba, and the relative bioavailability of the extract was lower than that of the hydrolyzate. The relative bioavailability of isorhamnetin in the hydrolyzate High utilization. Conclusions Ginkgo flavonoid glycosides are less converted to flavonol aglycone in rats and the relative bioavailability of aglycones is higher. Lactones have no obvious effect on the metabolism of flavonoids.
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