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Evidence-based approach to assess passive diffusion and carrier-mediated drug transport

Di, Li (author)
Artursson, Per (author)
Uppsala universitet,Institutionen för farmaci
Avdeef, Alex (author)
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Ecker, Gerhard F. (author)
Faller, Bernard (author)
Fischer, Holger (author)
Houston, J. Brian (author)
Kansy, Manfred (author)
Kerns, Edward H. (author)
Kraemer, Stefanie D. (author)
Lennernäs, Hans (author)
Uppsala universitet,Institutionen för farmaci
Sugano, Kiyohiko (author)
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 (creator_code:org_t)
Elsevier BV, 2012
2012
English.
In: Drug Discovery Today. - : Elsevier BV. - 1359-6446 .- 1878-5832. ; 17:15-16, s. 905-912
  • Research review (peer-reviewed)
Abstract Subject headings
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  • Evidence supporting the action of passive diffusion and carrier-mediated (CM) transport in drug bioavailability and disposition is discussed to refute the recently proposed theory that drug transport is CM-only and that new transporters will be discovered that possess transport characteristics ascribed to passive diffusion. Misconceptions and faulty speculations are addressed to provide reliable guidance on choosing appropriate tools for drug design and optimization.

Keyword

membrane permeation assay
central-nervous-system
pept1 knockout mice
neutral amino-acid
lipid-bilayers
p-glycoprotein
artificial membranes
hydrophilic pores
transient pores
caco-2 cells

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