Shapes of membrane permeability-lipophilicity curves: extension of theoretical models with an aqueous pore pathway.
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Summary
It is demonstrated that the well-known sigmoid permeability-lipophilicity relationship should be considered as a molecular weight-dependent set of sigmoidal relationships and shows that combined log D values and molecular weight are important determinants for membrane transport processes through, e.g. Caco-2 monolayers and the mucosal GI membranes.
- Type
- article
- Published
- 1998-10-01
- Cited by
- 49
- References
- 40
- OpenAlex
- https://openalex.org/W1986246787
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:4012031
Keywords
Lipophilicity, Membrane, Permeation, Chemistry, Aqueous solution
References
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- The Partition of Organic Compounds Between Higher Alcohols and Water.
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- Quantitative approach to biochemical structure-activity relationships
- Physicochemical and drug-delivery considerations for oral drug bioavailability
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Cited by
- PAMPA--a drug absorption in vitro model 7. Comparing rat in situ, Caco-2, and PAMPA permeability of fluoroquinolones.
- PAMPA--a drug absorption in vitro model 13. Chemical selectivity due to membrane hydrogen bonding: in combo comparisons of HDM-, DOPC-, and DS-PAMPA models.
- 6 A Practical Approach to Computational Models of the Blood-Brain Barrier
- Transfer of Small Molecules Across Membrane-Mimetic Interfaces
- Predicting oral absorption and bioavailability.
- From protein binding to pharmacokinetics: a novel approach to active drug absorption prediction
- Study of the lipophilicity of selenium species
- Modelling partitioning of sparingly soluble drugs in a two-phase liquid system.
- Transmission of p-anisic acid through nanofiltration and goat membranes
- Lipophilicity and Its Relationship with Passive Drug Permeation
- Prediction of intestinal permeability.
- Estimation of permeability by passive diffusion through Caco-2 cell monolayers using the drugs' lipophilicity and molecular weight.
- Prediction of oral drug absorption in humans by theoretical passive absorption model.
- Prediction of drug absorption using multivariate statistics.
- Novel membranes for simulating biological barrier transport
- Pharmacokinetics and metabolism in early drug discovery.
- Modeling the Release Kinetics of Poorly Water-Soluble Drug Molecules from Liposomal Nanocarriers
- Prediction of oral absorption in humans by experimental immobilized artificial membrane chromatography indices and physicochemical descriptors.
- An In Silico Transwell Device for the Study of Drug Transport and Drug–Drug Interactions
- A bioavailability score.
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