Study of the pharmacokinetics of Ginkgolide J in rats by ultra-high-performance liquid chromatography tandem mass spectrometry.

BACKGROUND AND

OBJECTIVE

Ginkgolide J is an active ingredient extracted from Ginkgo biloba leaves and has potential therapeutic effects on Alzheimer's disease and rheumatoid arthritis. However, its pharmacokinetic behavior remains unclear. As the efficacy of an active ingredient in natural products is significantly affected by its pharmacokinetic characteristics, the pharmacokinetics of Ginkgolide J needs to be elucidated.

MATERIALS AND

METHODS

A rapid and sensitive quantitative method for Ginkgolide J using ultra-high-performance liquid chromatography-tandem mass spectrometry was established and validated. This method was then applied to pharmacokinetic studies in rats after oral and intravenous administration of a Ginkgolide J solution.

RESULTS

The linear range was 2-1000 ng/mL, with a correlation coefficient higher than 0.999. The specificity, precision, accuracy, stability, matrix effect, and recovery rate of this method met the analytical requirements. The pharmacokinetic results showed that the time to maximum plasma concentration (tmax) and half-life (t1/2) after oral administration of Ginkgolide J (10 mg/kg) were 1.50 h and 3.25 h, and t1/2 after intravenous administration (2 mg/kg) was 1.96 h, respectively. The absolute bioavailability of Ginkgolide J was 8.67%. Compared with intravenous medication, the oral bioavailability of Ginkgolide J is very low; therefore, the development of Ginkgolide J as an intravenous injection is more suitable for clinical applications.

CONCLUSION

In this study, we established a method for analyzing Ginkgolide J based on ultra-high-performance liquid chromatography tandem mass spectrometry and measured its pharmacokinetic behavior in rats. The results showed that the oral bioavailability of Ginkgolide J is very low, and intravenous administration may be necessary for drug development.