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
DC Field | Value | Language |
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dc.contributor.author | Jin, Hyo-Eon | - |
dc.contributor.author | Song, Boran | - |
dc.contributor.author | Kim, Sang-Bum | - |
dc.contributor.author | Shim, Won-Sik | - |
dc.contributor.author | Kim, Dae-Duk | - |
dc.contributor.author | Chong, Saeho | - |
dc.contributor.author | Chung, Suk-Jae | - |
dc.contributor.author | Shim, Chang-Koo | - |
dc.date.available | 2020-02-28T23:48:25Z | - |
dc.date.created | 2020-02-06 | - |
dc.date.issued | 2013-04 | - |
dc.identifier.issn | 0049-8254 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/14622 | - |
dc.description.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%). | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | TAYLOR & FRANCIS LTD | - |
dc.relation.isPartOf | XENOBIOTICA | - |
dc.subject | CANCER RESISTANCE PROTEIN | - |
dc.subject | P-GLYCOPROTEIN | - |
dc.subject | CLINICAL PHARMACOKINETICS | - |
dc.subject | IN-VITRO | - |
dc.subject | FUNCTIONAL-CHARACTERIZATION | - |
dc.subject | ORAL BIOAVAILABILITY | - |
dc.subject | TISSUE DISTRIBUTION | - |
dc.subject | RAT | - |
dc.subject | FLUOROQUINOLONE | - |
dc.subject | SECRETION | - |
dc.title | 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 | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000315636400005 | - |
dc.identifier.doi | 10.3109/00498254.2012.720740 | - |
dc.identifier.bibliographicCitation | XENOBIOTICA, v.43, no.4, pp.355 - 367 | - |
dc.identifier.scopusid | 2-s2.0-84879511957 | - |
dc.citation.endPage | 367 | - |
dc.citation.startPage | 355 | - |
dc.citation.title | XENOBIOTICA | - |
dc.citation.volume | 43 | - |
dc.citation.number | 4 | - |
dc.contributor.affiliatedAuthor | Shim, Won-Sik | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | Gemifloxacin | - |
dc.subject.keywordAuthor | bioavailability | - |
dc.subject.keywordAuthor | BCRP | - |
dc.subject.keywordAuthor | MRP2 | - |
dc.subject.keywordAuthor | P-gp | - |
dc.subject.keywordPlus | CANCER RESISTANCE PROTEIN | - |
dc.subject.keywordPlus | P-GLYCOPROTEIN | - |
dc.subject.keywordPlus | CLINICAL PHARMACOKINETICS | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | FUNCTIONAL-CHARACTERIZATION | - |
dc.subject.keywordPlus | ORAL BIOAVAILABILITY | - |
dc.subject.keywordPlus | TISSUE DISTRIBUTION | - |
dc.subject.keywordPlus | RAT | - |
dc.subject.keywordPlus | FLUOROQUINOLONE | - |
dc.subject.keywordPlus | SECRETION | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Toxicology | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Toxicology | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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