Evaluation and Prediction of Drug Permeation

Autor: Alessandra Pagliara, Bernard Testa, Pierre-Alain Carrupt, Marianne Reist, Sandrine Geinoz
Rok vydání: 1999
Předmět:
Zdroj: Journal of Pharmacy and Pharmacology, Vol. 51, No 12 (1999) pp. 1339-1357
ISSN: 2042-7158
0022-3573
DOI: 10.1211/0022357991777164
Popis: 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.
Databáze: OpenAIRE