• Corpus ID: 25689156

Pharmacokinetics of acarbose. Part I: Absorption, concentration in plasma, metabolism and excretion after single administration of [14C]acarbose to rats, dogs and man.

@article{Ahr1989PharmacokineticsOA,
  title={Pharmacokinetics of acarbose. Part I: Absorption, concentration in plasma, metabolism and excretion after single administration of [14C]acarbose to rats, dogs and man.},
  author={Hans Juergen Ahr and Michael Boberg and H. P. Krause and William Maul and F M{\"u}ller and H. J. Ploschke and H. Weber and Christian W{\"u}nsche},
  journal={Arzneimittel-Forschung},
  year={1989},
  volume={39 10},
  pages={
          1254-60
        }
}
The absorption, disposition, metabolism, and excretion of acarbose (O-4,6-dideoxy-4-[[(1S, 4R, 5S, 6S)-4,5,6-trihydroxy-3- (hydroxymethyl)-2- cyclohexen-1-yl]amino]-a-D-glucopyranosyl- (1----4)-O-a-D-glucopyranosyl- (1----4) -D-glucopyranose, Bay g 5421) have been studied following a single administration of the 14C-labelled compound to rats and dogs via different routes (intravenous, oral, intraduodenal) in the dose range of 2-200 mg.kg-1 as well as to man in a single oral dose of 200 mg… 
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58 Citations
Highly Influential Citations
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Background Citations
18
Methods Citations
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58 Citations

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From the calculation of the unbound fraction in plasma based on in vitro KD and Bmax, the dose-dependent increase in fu after oral administration is speculated to lead to a dose- dependent increase in total body clearance and a high area under the curve/dose at lower doses, such as 0.3 mg/kg in rats.
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Data from large-scale fermentation of acarbose using strains derived from Actinoplanes sp.
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