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学科主题: 临床医学
题名:
Sotalol Permeability in Cultured-Cell, Rat Intestine, and PAMPA System
作者: 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
发表日期: 2012-07-01
DOI: 10.1007/s11095-012-0699-3
卷: 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
所属项目编号: RR031474
项目资助者: Chinese Scholarship Council ; NIH
WOS记录号: WOS:000305222000006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58861
Appears in Collections:北京大学第三临床医学院_药剂科_期刊论文

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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

Recommended Citation:
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.
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