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Simultaneous Determination of Flavonols and Terpene Lactones in Beagle Dog Plasma by Ultra-Performance Liquid Chromatography-Tandem - Mass Spectrometry: 2. Application to Pharmacokinetic Studies on Ginkgo Leaf Extract
Lu, Yang; Li, Pengyue; Liu, Huimin; Du, Shouying; Cheng, Yanke; Wu, Huichao; Feng, Jiannan & Shao, Beibei
Abstract
Purpose: To evaluate the pharmacokinetics of the major compounds in Ginkgo leaf dosage
formulations (namely, Yikangning tablets, Ginaton tablets, Aoshi dropping pills and Yinxinke dispersible
tablets), commonly used in traditional Chinese medicine.
Methods: A randomized 4*4 crossover study with eight beagle dogs was carried out. Plasma samples
were collected following oral administration of four different preparations and the effective ingredients,
namely, kaempferol, quercetin, isorhamnetin, ginkgolides A, ginkgolides B, ginkgolides C and bilobalide
were detected by a validated ultra-performance liquid chromatography-tandem mass spectrometry
(UPLC-TMS). Then the pharmacokinetics of these target compounds, of different preparations were
studied.
Results: The adjusted pharmacokinetic data showed that the area under the concentration-time curve
from time-zero to the last measurable concentration (AUC0-t) of kaempferol, quercetin, isorhamnetin,
bilobalide, ginkgolides A, ginkgolides B, and ginkgolides C in plasma ranged from 124.37 ± 90.46 to
2261.87 ± 812.35, after administration of Yikangning; 142.28 ± 62.37 to 2529.46 ± 320.48 μg/L•h
following administration of Ginaton; 158.52 ± 55.48 to 1987.40 ± 766.21 μg/L•h after Aoshi
administration; 160.49 ± 104.66 to 2016.92 ± 1150.92 μg/L•h following Yinxinke administration. The
results also indicate that the flavonoids (especially quercetin) in dispersible tablets and dropping pills
hexhibited higher AUC than those in conventional tablets. There were no differences between Aoshi
(dropping pills) and Yinxinke (dispersible tablets) in terms of the bioavailability of the flavonoids, but the
dropping pill flavonoids showed lower tmax.
Conclusion: The results indicate that UPLC-TMS can used to simultaneously evaluate the plasma
pharmacokinetics of Ginko compounds in beagle dogs
Keywords
Ginkgo biloba; Beagle dog plasma; Kaempferol; Quercetin; Isorhamnetin; Ginkgolides A; Ginkgolides B; Ginkgolides C; Bilobalide; Pharmacokinetics; Bioavailability
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