Add time:09/01/2019         Source:sciencedirect.com

The angiotensin-converting enzyme (ACE)-inhibitor Ceronapril (cas 111223-26-8) (SQ 29852) is shown to be a substrate of the intestinal dipeptide transporter. Uptake by Caco-2 cells, grown as confluent monolayers, follows a major saturable pathway (Km, 0.91 ± 0.11 mM; ∼90% at 1 mM) together with a minor passive component (kJ, 32.3 ± 6.6 ng (106 cells)−1 (20 min)−1. Uptake was inhibited by competition with dipeptides such as l-AIa-l-Pro (Ki, 2.96 mM) and l-Phe-Gly (Ki, 3.84 mM) but not by cephalosporins such as cephalexin. In contrast, transport was non-saturable, flux increased linearly with concentration and data were consistent with a passive transepithelial transport mechanism. Transport profiles showed a biphasic dependence upon time with an initial flux of 0.83 ± 0.02 ng insert−1 min−1 (k1) and a terminal value of 1.65 ± 0.08 ng insert−1 min−1 ((k2) at 100 μM. It is concluded that the basolateral efflux is retarded so that the passive paracellular transport controls the overall transepithelial transport characteristics in the Caco-2 model. Carrier-mediated uptake into intestinal enterocytres, followed by rate-limiting basolateral efflux, may explain the extended tmax in vivo following oral administration.

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