1996
DOI: 10.1016/0024-3205(96)00224-x
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Estimation of oral drug absorption in man based on intestine permeability in rats

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Cited by 33 publications
(15 citation statements)
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“…Adult male Sprague-Dawley rats (380 to 450 g) were used in this study. The rat is an appropriate animal model to investigate the GI absorption of AMB following oral administration due to similarities in rat and human intestinal characteristics (i.e., anatomical, metabolic, and biochemical characteristics) (5,9,11,16). AMB levels in plasma and tissues were analyzed by high-pressure liquid chromatography (HPLC) as previously described (20)(21)(22).…”
mentioning
confidence: 99%
“…Adult male Sprague-Dawley rats (380 to 450 g) were used in this study. The rat is an appropriate animal model to investigate the GI absorption of AMB following oral administration due to similarities in rat and human intestinal characteristics (i.e., anatomical, metabolic, and biochemical characteristics) (5,9,11,16). AMB levels in plasma and tissues were analyzed by high-pressure liquid chromatography (HPLC) as previously described (20)(21)(22).…”
mentioning
confidence: 99%
“…Although it is possible and reasonable to use a cut off between high and low permeability in terms of fraction absorbed as defined by the BCS, a challenge is to find a suitable permeability measurement which has an adequate correlation to fraction absorbed, but is also simple to perform. Methods reported in the literature include those based on in silico drug properties such as log D and hydrogen bonding potential,31, 32 passive diffusion across an artificial membrane,33 in vitro permeability across cell lines,34–36 across excised human or animal tissue37, 38 and permeability as determined by in situ perfusion techniques 39. Simpler methods are preferred during the early phases of product development and for assessment of drug candidates, whereas in later development more complex measurements may be performed.…”
Section: Theoretical/backgroundmentioning
confidence: 99%
“…In aqueous or organic solution, AMP decomposed under exposure to light, and colored photolysis product was formed. The permeability through rat intestine mucosa determined in our laboratory was 9.3 × 10 −6 cm/s, and oral drug absorption in humans based on the intestinal permeability in rats could be less than 10% [7]. Use of AMP in most pharmaceutical preparations and some research experiments was thereby limited due to its low water solubility, low intestine permeability and degradation in solution.…”
Section: Introductionmentioning
confidence: 99%