Transport of gemifloxacin, a 4th generation quinolone antibiotic, in the Caco-2 and engineered MDCKII cells, and potential involvement of efflux transporters in the intestinal absorption of the drug
- Authors
- Jin, Hyo-Eon; Song, Boran; Kim, Sang-Bum; Shim, Won-Sik; Kim, Dae-Duk; Chong, Saeho; Chung, Suk-Jae; Shim, Chang-Koo
- Issue Date
- Apr-2013
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Gemifloxacin; bioavailability; BCRP; MRP2; P-gp
- Citation
- XENOBIOTICA, v.43, no.4, pp.355 - 367
- Journal Title
- XENOBIOTICA
- Volume
- 43
- Number
- 4
- Start Page
- 355
- End Page
- 367
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/14622
- DOI
- 10.3109/00498254.2012.720740
- ISSN
- 0049-8254
- Abstract
- 1. The oral (po) bioavailability of gemifloxacin mesylate in rats and its possible association with efflux transporters was investigated. 2. The apparent permeabilities (P-app) of gemifloxacin across the Caco-2 cell monolayer were 1.20 +/- 0.09 x 10(-5) cm/s for apical to basal (absorptive) transport, and 2.13 +/- 0.6 x 10(-5) cm/s for basal to apical (secretory) transport for a 5-500 mu M concentration range, suggesting the involvement of a carrier-mediated efflux in the secretory transport. 3. The secretory transport in Caco-2 cells was significantly decreased by MRP2 (MK571) and BCRP (Ko143) inhibitors. 4. The secretory transport was distinct in MDCKII/P-gp, MDCKII/MRP2 and MDCKII/BCRP cells, and the affinity was highest for MRP2, followed by BCRP and P-gp. The efflux was significantly decreased by verapamil and Ko143, but not significantly by MK571. 5. The comparative po bioavailability in rats was increased by the preadministration of Ko143 (four-fold), MK571 (two-fold) and verapamil (two-fold). 6. Efflux transporters appeared to significantly limit the bioavailability of gemifloxacin in rats, suggesting their possible contribution to the low bioavailability of the drug in the human (70%).
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