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Quantitative prediction of P-glycoprotein-mediated drug-drug interactions and intestinal absorption using humanized mice.

British journal of pharmacology

Miyake T, Tsutsui H, Haraya K, Tachibana T, Morimoto K, Takehara S, Ayabe M, Kobayashi K, Kazuki Y.
PMID: 34232502
Br J Pharmacol. 2021 Nov;178(21):4335-4351. doi: 10.1111/bph.15612. Epub 2021 Sep 06.

BACKGROUND AND PURPOSE: P-glycoprotein (P-gp) exhibits a broad substrate specificity and affects pharmacokinetics, especially intestinal absorption. However, prediction, in vivo, of P-gp-mediated drug-drug interaction (DDI) and non-linear absorption at the preclinical stage, is challenging. Here we evaluate the use...

Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, .

Frontiers in pharmacology

Kazi M, Al-Swairi M, Ahmad A, Raish M, Alanazi FK, Badran MM, Khan AA, Alanazi AM, Hussain MD.
PMID: 31118895
Front Pharmacol. 2019 May 02;10:459. doi: 10.3389/fphar.2019.00459. eCollection 2019.

OBJECTIVE: The aim of this study was to investigate the METHODS: Self-nanoemulsifying drug delivery systems of TAL were prepared using various oils, non-ionic surfactants and/or water-soluble co-solvents and assessed visually/by droplet size measurement. Equilibrium solubility of TAL in the...

Computer-Aided Selective Optimization of Side Activities of Talinolol.

ACS medicinal chemistry letters

Hiesinger K, Kramer JS, Achenbach J, Moser D, Weber J, Wittmann SK, Morisseau C, Angioni C, Geisslinger G, Kahnt AS, Kaiser A, Proschak A, Steinhilber D, Pogoryelov D, Wagner K, Hammock BD, Proschak E.
PMID: 31223445
ACS Med Chem Lett. 2019 May 29;10(6):899-903. doi: 10.1021/acsmedchemlett.9b00075. eCollection 2019 Jun 13.

Selective optimization of side activities is a valuable source of novel lead structures in drug discovery. In this study, a computer-aided approach was used to deorphanize the pleiotropic cholesterol-lowering effects of the beta-blocker talinolol, which result from the inhibition...

Showing 1 to 3 of 3 entries