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Comparison alone or combined with P-gp inhibitors on spinosin absorption using single-pass intestinal perfusion

Hai-Ying Huang,De-En Han,Yan-Li Guo, Jian Li, Jin-Li Shi

Thiswork determined themechanisms of enhancing the oral bioavailability of Spinosin (SPI). The in situ perfusion method was used in rats to study the absorption mechanisms of SPI alone or combined with the P-gp inhibitors Verapamil (Ver) and cyclosporinA(CsA). The drug absorption rate constant(Ka) and apparent absorption coefficient (Peff) had little significant effect on duodenum, jejunum, ileum and colon at 40ug·mL- 1concentration of Spinosin(P>0.05), Compared with SPI group, SPI+Ver and SPI+ CsAgroups were increased significantly(P<0.05), Ver and CsA remarkably enhanced the effect of intestinal absorption of SPI on duodenum(P<0.05), The results of absorption in the intestines indicated that Efflux pump P-gpmight exert some effects on the absorption of SPI. In conclusion, these data indicate that P-gp inhibitors are an effective and promising delivery system to enhance the oral bioavailability of poorly water-soluble drugs.