Sotalol permeability in cultured-cell, rat intestine, and PAMPA system.

Pharmaceutical Research
Wei LiuSuo-Di Zhai

Abstract

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 (300~350 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.

References

Jul 1, 1976·Acta Pharmacologica Et Toxicologica·M AnttilaH Sundquist
Jul 1, 1990·Journal of Pharmaceutical Sciences·S YamashitaT Kimura
Oct 1, 1971·Journal of Pharmaceutical Sciences·R K Nayak, L Z Benet
Jan 6, 1999·Journal of Pharmaceutical Sciences·J D IrvineJ R Grove
Jun 23, 2004·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Axel AltHelga Oeser
Apr 14, 2006·Neoplasia : an International Journal for Oncology Research·Oliver ThewsMichael Gekle
May 5, 2006·Fundamental & Clinical Pharmacology·Iouri BachmakovMartin F Fromm
Jan 12, 2007·Clinical Pharmacology and Therapeutics·H GlaeserR B Kim
Jan 11, 2008·Pharmaceutical Research·Xiaoxi ChenPraveen V Balimane
Feb 1, 2008·Pharmaceutical Research·Leslie Z BenetLawrence X Yu
Dec 11, 2008·Journal of Pharmaceutical Sciences·Yukio KatoAkira Tsuji
Jan 10, 2009·Molecular Pharmaceutics·Mei-Ling Chen, Lawrence Yu
Apr 15, 2011·Pharmaceutical Research·Mei-Ling ChenLawrence X Yu
Jan 21, 2012·Advanced Drug Delivery Reviews·Fabio BroccatelliLeslie Z Benet

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Citations

Oct 9, 2012·Advanced Drug Delivery Reviews·Margarida EstudanteLeslie Z Benet
Jan 15, 2015·Biomedical Chromatography : BMC·Zhiping FengXianhua Zhang
Jun 21, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·F FranekB Steffansen
Aug 31, 2013·Integrative Biology : Quantitative Biosciences From Nano to Macro·Ann M FerrieYe Fang
Feb 18, 2017·Clinical Pharmacokinetics·Anton IvanyukThierry Buclin
Sep 6, 2012·Journal of Chemical Information and Modeling·Fabio Broccatelli

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