Studies On The Absorption And Transport Of Trantlnterol In Vitro

In this study, I established Caco-2, MDCK-MDR1and MDCK cellmodel, evaluated these cell model for transmembrane resistance value, fluorescentyellow Permeance to prove that the cell model is available. Then use these three kindsof models studies transportion and absorption of trantinterol. Used for trantinterol(2-(4-amino-3-chloro-5-(trifluoromethyl) phenyl)-2-tert aminoethanols, trantinterol), Shenyang PharmaceuticalUniversity, Professor Cheng Maosheng based on the Mabuterol structuredeveloped a new type of β2agonists.1. Study the transport of trantinterol with Caco-2monolayer cell modelWe established Caco-2monolayer cell model, and verificated it through thecell growth curve determination, the Lucifer yellow transmembrane resistancevalue, proofed the Caco-2cell model in this laboratory can be applied to thetransport study of drugs.Caco-2cell model successfully established used for transportion study, andverapamil inhibition of the group as a negative control. The results show that theefflux ratio of trantintrol in the Caco-2cell model was1.08; negative control was1.11. There was no significant difference (P>0.05). After all trantintrol is not P-gpsubstrate.2. Transport of trantinterol in MDCK-MDR1cell monolayer modelWe established MDCK and MDCK-MDR1monolayer cell model, andverificated it through the cell growth curve determination, the Lucifer yellowtransmembrane resistance value, the TEER and the Rho123transportion. MDCKand MDCK-MDR1cell model were successfully established. Lucifer yellow apparentpermeability was less than5%. The efflux rate of Rho123was5.16, indicatingthat P-gp expression is high. The results show that MDCK and MDCK-MDR1cellconnected tightly, and highly expressed P-gp. After all MDCK and MDCK-MDR1cell model was successfully established, all the indexes required, can be used for thestudy of interaction of drugs with P-gp.Study the transportion of trantintrol in MDCK and MDCK-MDR1cell model. The results showed that: the efflux rate of trantinterol in MDCK-MDR1andMDCK cells are1.2and1.05, respectively. There is no significant difference, sotrantinterol is not a P-gp substrate.The effect of trantinerol on the transport of Rho123in MDCK-MDR1cell model,trantinterol significantly reduce the efflux ratio of Rho123(P <0.05). In thistable, trantinterol inhibits P-gp-mediated Rho123efflux, may be P-gp inhibitor.Interaction studies for trantinerol and ATPase (ATPase) on P-glycoprotein (P-gp),show that trantinterol inhibit P-gp achieved by inhibiting the ATPase activity of P-gp.