Journal of pharmaceutical and biomedical analysis
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J Pharm Biomed Anal · Mar 2012
Comparative StudyIn vivo microdialysis with LC-MS for analysis of spinosin and its interaction with cyclosporin A in rat brain, blood and bile.
Spinosin, a major bioactive herbal ingredient isolated from Semen Ziziphi Spinosae, plays an important role in sedation and hypnosis. However, the pharmacokinetic behavior of spinosin in special sites has not been reported. Microdialysis (MD) technique, as a continuous, realtime monitoring sampling technique, is very suitable for the evaluation of the disposition of diverse drugs. ⋯ The t(1/2) values of spinosin in blood, bile and brain also changed from 48.07 to 95.04 min, from 97.20 to 152.21 and from 42.18 to 73.83 min, respectively. These results demonstrated that the CsA decreased the efflux of spinosin through the inhibition of P-glycoprotein (P-gp) efflux transporter and it might be used as a group of P-gp substrate. Other transporters or pathways may also be involved in the metabolism of spinosin.