See also: Theories of general anaesthetic action and Passive transport
In medicinal chemistry, Drug Permeability is an empirical parameter that indicates how quickly a chemical entity or an active pharmaceutical ingredient crosses a biological membrane or another biological barrier to become bioavailable in the body. Drug permeability, together with drug aqueous solubility are the two parameters which defines the fate of the active ingredient after oral administration that ultimately defines its bioavailability.[1] When drug permeability is empirically measured in vitro, it is generally called apparent permeability (Papp) as its absolute value varies according to the method selected for its measurement. Papp is measured in vitro utilizing cellular based barriers such as the Caco-2[2] model or utilizing artificial biomimetic barriers, such as the Parallel Artificial Membrane Permeation Assay (PAMPA)[3] or the PermeaPad.[4] All these methods are built on an acceptor compartment (from 0.2 up to several mL according to the method uses) where the drug solution is placed, a biomimetic barrier and an acceptor compartment, where the drug concentration is quantified over time. By maintaining sink condition, a steady state is reached after a lag time (τ, Fig. 1) .
^Amidon, G. L.; Lennernäs, H.; Shah, V. P.; Crison, J. R. (March 1995). "A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability". Pharmaceutical Research. 12 (3): 413–420. doi:10.1023/a:1016212804288. hdl:2027.42/41443. ISSN 0724-8741. PMID 7617530. S2CID 21085622.
^Artursson, P.; Karlsson, J. (1991-03-29). "Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells". Biochemical and Biophysical Research Communications. 175 (3): 880–885. doi:10.1016/0006-291x(91)91647-u. ISSN 0006-291X. PMID 1673839.
^Kansy, M.; Senner, F.; Gubernator, K. (1998-03-26). "Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes". Journal of Medicinal Chemistry. 41 (7): 1007–1010. doi:10.1021/jm970530e. ISSN 0022-2623. PMID 9544199.
^di Cagno, Massimiliano; Bibi, Hanady A.; Bauer-Brandl, Annette (2015-06-20). "New biomimetic barrier Permeapad™ for efficient investigation of passive permeability of drugs". European Journal of Pharmaceutical Sciences. 73: 29–34. doi:10.1016/j.ejps.2015.03.019. ISSN 1879-0720. PMID 25840123.
its bioavailability. When drugpermeability is empirically measured in vitro, it is generally called apparent permeability (Papp) as its absolute value...
Drugpermeability Semipermeable membrane, a membrane which will allow certain molecules or ions to pass through it by diffusion Vascular permeability...
currently faces obstacles such as low drug retention time due to washing out with urine and issues with the low permeability of the bladder wall itself. Due...
folic acid. Reduced drug accumulation: by decreasing drugpermeability and/or increasing active efflux (pumping out) of the drugs across the cell surface...
either side, as well as the permeability of the membrane to each solute. Depending on the membrane and the solute, permeability may depend on solute size...
(2016). "Cell-based in vitro models for dermal permeability studies". Concepts and Models for DrugPermeability Studies. Elsevier. pp. 155–167. doi:10...
Vascular permeability, often in the form of capillary permeability or microvascular permeability, characterizes the capacity of a blood vessel wall to...
could potentially be improved with the use of mucoadhesive polymers. Drugpermeability through the cornea could be facilitated with addition of penetration...
affects the permeability of topical drugs. Another part of the skin is called the appendages, and it is known as the “shortcut” for topical drug delivery...
Classification System. This classifies drugs according to their solubility and permeability or absorption properties. Psychoactive drugs are substances that affect...
chemistry, parallel artificial membrane permeability assay (PAMPA) is a method which determines the permeability of substances from a donor compartment...
dictionary. Acid–base reaction Acidity function Dissociation (chemistry) Drugpermeability Inorganic nonaqueous solvent List of ions in pure water (aqueous chemistry)...
intestinal permeability. The solubility classification is based on a United States Pharmacopoeia (USP) aperture. The intestinal permeability classification...
OCLC 48553325. Sarmento, Bruno (30 September 2015). Concepts and Models for DrugPermeability Studies: Cell and Tissue based In Vitro Culture Models. Woodhead....
intestinal lumen. Selective permeability is mediated via two major routes: Transepithelial or transcellular permeability. This consists of specific transport...
preformed folic acid. Reduced drug accumulation: by decreasing drugpermeability or increasing active efflux (pumping out) of the drugs across the cell surface...
have varying degrees of oxygen permeability. For example, it has been shown that SCLs have limited oxygen permeability while silicon-based contact lenses...
neuroimmune response that, through several mechanisms, increases the permeability of the blood–brain barrier, thereby making the brain more susceptible...
coefficients are useful in estimating the distribution of drugs within the body. Hydrophobic drugs with high octanol-water partition coefficients are mainly...
intestinal permeability. For the Canadian legal classification, see Controlled Drugs and Substances Act For the UK legal classification, see Drugs controlled...
of many drugs with poor water solubility and/or membrane permeability. A wide variety of drug carrier systems have been developed and studied, each of...
a permeability barrier means that organisms were able to evolve detoxification systems that exploit the hydrophobicity common to membrane-permeable xenobiotics...
dynamics, especially for macromolecular drugs. This phenomenon is referred to as the "enhanced permeability and retention (EPR) effect" of macromolecules...
Juliano RL, Ling V (November 1976). "A surface glycoprotein modulating drugpermeability in Chinese hamster ovary cell mutants". Biochimica et Biophysica Acta...
An adverse drug reaction (ADR) is a harmful, unintended result caused by taking medication.: 1.1 Adverse Drug Reaction (ADR) ADRs may occur following...
function as antagonists. Histamine makes blood vessels more permeable (vascular permeability), causing fluid to escape from capillaries into tissues, which...
synthetic molecule with the ability to reduce capillary permeability in the body. In Switzerland the drug is sold by the pharmaceutical company OM Pharma under...
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