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Sotalol Permeability in Cultured-Cell, Rat Intestine, and PAMPA System
Liu, Wei1,2; Okochi, Hideaki2; Benet, Leslie Z.1,2; Zhai, Suo-Di1
关键词biopharmaceutics drug disposition classification system (BDDCS) MDCK cells permeability p-glycoprotein solute transporters
刊名PHARMACEUTICAL RESEARCH
2012-07-01
DOI10.1007/s11095-012-0699-3
29期:7页:1768-1774
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]P-GLYCOPROTEIN ; CLASSIFICATION ; MEMBRANE ; IMPACT ; DRUGS ; BCS
英文摘要

To clarify sotalol′s classification in the BCS versus BDDCS systems through cellular, rat everted sac and PAMPA permeability studies.

Studies were carried out in Madin Darby canine kidney (MDCK) and MDR1-transfected MDCK (MDCK-MDR1) cell lines, rat everted gut sacs and the Parallel Artificial Membrane Permeability Assay (PAMPA) system. Three-hour transport studies were conducted in MDCK cell lines (with apical pH changes) and MDCK-MDR1 cells (with and without the P-glycoprotein inhibitor GG918); male Sprague-Dawley rats (300 similar to 350 g) were used to prepare everted sacs. In the PAMPA studies, drug solutions at different pH′s were dosed in each well and incubated for 5 h. Samples were measured by LC-MS/MS, or liquid scintillation counting and apparent permeability (P-app) was calculated.

Sotalol showed low permeability in all of the cultured-cell lines, everted sacs and PAMPA systems. It might be a border line P-glycoprotein substrate. The PAMPA study showed that sotalol′s permeability increased with a higher apical pH, while much less change was found in MDCK cells.

The low permeability rate for sotalol correlates with its Class 3 BDDCS assignment and lack of in vivo metabolism.

语种英语
WOS记录号WOS:000305222000006
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被引频次:11[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/58861
专题北京大学第三临床医学院_药剂科
作者单位1.Peking Univ, Hosp 3, Dept Pharm, Beijing 100191, Peoples R China
2.Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94143 USA
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Liu, Wei,Okochi, Hideaki,Benet, Leslie Z.,et al. Sotalol Permeability in Cultured-Cell, Rat Intestine, and PAMPA System[J]. PHARMACEUTICAL RESEARCH,2012,29(7):1768-1774.
APA Liu, Wei,Okochi, Hideaki,Benet, Leslie Z.,&Zhai, Suo-Di.(2012).Sotalol Permeability in Cultured-Cell, Rat Intestine, and PAMPA System.PHARMACEUTICAL RESEARCH,29(7),1768-1774.
MLA Liu, Wei,et al."Sotalol Permeability in Cultured-Cell, Rat Intestine, and PAMPA System".PHARMACEUTICAL RESEARCH 29.7(2012):1768-1774.
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