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Critical Reviews™ in Therapeutic Drug Carrier Systems
Импакт фактор: 2.9 5-летний Импакт фактор: 3.72 SJR: 0.736 SNIP: 0.551 CiteScore™: 2.43

ISSN Печать: 0743-4863
ISSN Онлайн: 2162-660X

Выпуски:
Том 36, 2019 Том 35, 2018 Том 34, 2017 Том 33, 2016 Том 32, 2015 Том 31, 2014 Том 30, 2013 Том 29, 2012 Том 28, 2011 Том 27, 2010 Том 26, 2009 Том 25, 2008 Том 24, 2007 Том 23, 2006 Том 22, 2005 Том 21, 2004 Том 20, 2003 Том 19, 2002 Том 18, 2001 Том 17, 2000 Том 16, 1999 Том 15, 1998 Том 14, 1997 Том 13, 1996 Том 12, 1995

Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.v17.i2.10
28 pages

Oral Delivery of HIV-Protease Inhibitors

Lilian Y. Li
College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109-1065
Barbra H. Stewart
Parke-Davis/Warner-Lambert, Dept. of Pharmacokinetics, Dynamics, and Metabolism, 2800 Plymouth Rd., Ann Arbor, Michigan 48106-1047
David Fleisher
College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109-1065

Краткое описание

Strategies for optimizing the oral delivery of HIV-protease inhibitors draw from drug discovery efforts in molecular design, drug development tools in dosage formulation, and dosage regimen considerations in clinical medicine. This review outlines the evolution of these strategies for drugs that have been approved for human use, drug candidates still in development, and molecules that are no longer in development but from which valuable delivery information was obtained. Molecular design for obtaining desirable pharmacokinetics following oral administration primarily involved maximizing aqueous solubility and minimizing first-pass metabolism. Optimization of molecular design for oral drug delivery purposes is tempered by additional considerations for drug potency, toxicity, potential for interactions, and development of viral resistance. Strategies for improving oral bioavailability dirough dosage formulation use information from the effects of coadministered meals on drug plasma levels. Patient adherence to dosage regimens remains a major issue in assuring effective oral drug treatment and in preventing the development of resistance. Progress has been made in clinical studies where improved oral bioavailability and reductions in drug plasma level variability have been achieved with appropriate dosage regimen adjustment.


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