OBJECTIVE To study the transport characteristics of telmisartan in vitro. METHODS A human intestinal epithelial cell Caco-2 model in vitro was applied to study the transport characteristics of telmisartan. The effects of concentration, pH and P-glycoprotein(P-gp) inhibitors on the transport of telmisartan were investigated. RESULTS In the Caco-2 cells, the absorptive transport of TMS was pH dependent and the transport was enhanced at weakly acidic pH on the apical side. The comparison of apical to basolateral(AP-BL)and basolateral to apical(BL-AP)transports showed that efflux effects limited the oral absorption of TMS. In the presence of amioderone(10 μmol·L-1) and cyclosporin(10 μmol·L-1), potent inhibitors of P-gp, the Pratio decreased from 3.5 to 0.9 and 1.2,respectively(P<0.01). CONCLUSION The polarized efflux of TMS in Caco-2 cell is probably due to the presence of P-gp. The results initially explain the reasons for low and variable bioavailability of TMS, and provide a guidance for the rational treatment of hypertension.
SHEN Jie;JIO Zheng;LI Zhong-dong;SHI Xio-jin;TONG Ru-jing;ZHONG Ming-kng.
Transport Characteristics of Telmisartan in Human Intestinal Cell Line Caco-2 [J]. Chinese Pharmaceutical Journal, 2006, 41(21): 1624-1627
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