The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
The rise of PAMPA
Abstract
The parallel artificial membrane permeability assay (PAMPA), as a passive-permeability screen, is a possible low-cost alternative to cellular models for the earliest ADME primary screening of research compounds. Its popularity in the industry has risen rapidly. This review examines state-of-the-art PAMPA methods. The various covered topics include: different lipid formulations, the quantitative relationships between hexadecane, dioyleyoylphosphatidycholine and Double-Sink PAMPA measurements, the use of individual-well stirring, issues of ultraviolet sensitivity, timing strategies, reproducibility of measurements, the correct pH to perform the measurement to avoid aqueous boundary layer problems, the pKa(flux) method for determining intrinsic permeability coefficients and the cosolvent method for very insoluble molecules. Examples of the determination of permeability of very difficult molecules, but molecules that are well absorbed, are given. Carefully gathered evidence in support of the use of the Double-Sink PAMPA model is presented. The review concludes with a binning strategy to predict human intestinal absorption, based on the use of the sum of permeability coefficients, measured at gradient pH 5.0, 6.2 and 7.4. Opinions regarding the future of PAMPA are offered.
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Cites
Molecular properties that influence the oral bioavailability of drug candidates
Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., & Kopple, K. D. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020017n · Cited by 8,420
Amidon, G. L., Lennernäs, H., Shah, V. P., & Crison, J. R. (1995) · Pharmaceutical Research · doi:10.1023/a:1016212804288 · Cited by 5,430
Kansy, M., Senner, F., & Gubernator, K. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm970530e · Cited by 1,304
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Structure−Brain Exposure Relationships
Hitchcock, S. A., & Pennington, L. D. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm060642i · Cited by 698
Coexistence of passive and carrier-mediated processes in drug transport
Sugano, K., Kansy, M., Artursson, P., Avdeef, A., Bendels, S., Di, L., Ecker, G. F., Faller, B., Fischer, H., Gerebtzoff, G., et al. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3187 · Cited by 649
Self-citationWhen poor solubility becomes an issue: From early stage to proof of concept
Stegemann, S., Leveiller, F., Franchi, D., de Jong, H., & Lindén, H. (2007) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2007.05.110 · Cited by 567
PAMPA—critical factors for better predictions of absorption
Avdeef, A., Bendels, S., Di, L. I., Faller, B., Kansy, M., Sugano, K., & Yamauchi, Y. (2007) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21068 · Cited by 240
Self-citationDrug permeability profiling using cell-free permeation tools: overview and applications
Berben, P., Bauer-Brandl, A., Brandl, M., Faller, B., Flaten, G. E., Jacobsen, A.-C., Brouwers, J., & Augustijns, P. (2018) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2018.04.016 · Cited by 199
Metadata
- Authors
- Avdeef, A.
- Venue
- Expert Opinion on Drug Metabolism & Toxicology
- Publisher
- Informa Healthcare
- Published
- 2005-08
- Volume
- 1
- Issue
- 2
- Pages
- 325-342
- ISSN
- 1742-5255 (ISSN-L)
- 1744-7607
- OpenAlex
- W2104016565
- Cited by
- 222
- References
- 3
- FWCI
- 4.44
- Type
- journal article
- Language
- en
- Open access
- closed
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