TABLE 2.
Grepafloxacin transport in EHBR intestinal tissue mounted in an Ussing chamber and inhibitory effects of P-gp and MRP2 modulatorsa
Rat strain and treatment | Permeability coefficient (μl/cm2/min)
|
Net secretion (μl/cm2/min) [(s-m) − (m-s)] | Secretory ratio [(s-m)/(m-s)] | |
---|---|---|---|---|
m-s | s-m | |||
SDR (control) | 0.759 ± 0.100 | 3.25 ± 0.48 | 2.49 ± 0.40 | 4.32 ± 0.36 |
EHBR | ||||
None | 0.652 ± 0.127 | 1.06 ± 0.17b | 0.404 ± 0.195b | 1.77 ± 0.37b |
Cyclosporine (10 μM) | 1.26 ± 0.28c | 1.34 ± 0.28 | 0.087 ± 0.108 | 1.11 ± 0.11c |
Probenecid (1 mM) | 1.12 ± 0.13c | 2.07 ± 0.33c | 0.951 ± 0.429 | 2.04 ± 0.59 |
Cyclosporine (10 μM) + probenecid (1 mM) | 1.68 ± 0.09c | 1.19 ± 0.14 | −0.485 ± 0.208c | 0.727 ± 0.123c |
The time course of grepafloxacin (10 μM) transport across the intestinal tissue was evaluated. The modulators were added to the donor solution. The experimental solution was adjusted to pH 7.4, and the temperature was maintained at 37°C.
Significantly different from the value for SDRs (control) by Student’s t test (P < 0.05).
Significantly different from the value for EHBRs by Student’s t test (P < 0.05).