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Evaluation and prediction of drug permeation

Pagliara, Alessandra
Reist, Marianne
Geinoz, S.
Testa, Bernard
Published in Journal of Pharmacy and Pharmacology. 1999, vol. 51, no. 12, p. 1339-1357
Abstract A major challenge confronting the pharmaceutical scientist is to optimize the selective and efficient delivery of new active entities and drug candidates. Successful drug development requires not only optimization of specific and potent pharmacodynamic activity, but also efficient delivery to the target site. Following advances in rational drug design, combinatorial chemistry and high-throughput screening techniques, the number of newly discovered and promising active compounds has increased dramatically in recent years, often making delivery problems the rate-limiting step in drug research. To overcome these problems, a good knowledge of the pharmacokinetic barriers encountered by bioactive compounds is required. This review gives an overview of the properties of relevant physiological barriers and presents some important biological models for evaluation of drug permeation and transport. Physicochemical determinants in drug permeation and the relevance of quantitative and qualitative approaches to the prediction and evaluation of passive drug absorption are also discussed.
Keywords AnimalsBiological Transport/physiologyChemistry, PharmaceuticalHumansIntestinal Absorption/physiologyModels, BiologicalPharmaceutical Preparations/chemistry/*metabolism
PMID: 10678488
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PAGLIARA, Alessandra et al. Evaluation and prediction of drug permeation. In: Journal of Pharmacy and Pharmacology, 1999, vol. 51, n° 12, p. 1339-1357.

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Deposited on : 2010-08-06

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