Estimating bioavailability

Van de Waterbeemd, H. Physicochemical approaches to drug absorption. In Drug Bioavailability Estimation of Solubility, Permeability, Absorption and Eioavailability (Methods and Principles in Medicinal Chemistry), Van der Waterbeemd, H., Lennernas, H Artursson, P. (eds.), Wiley-VCH, Weinheim, 2003, pp. 1-20. 

Figure 7.15 Kinetics of transport across a filter-immobilized artificial membrane (a) desipramine and (b) dihydromethysticin concentrations in acceptor well. [Reprinted from Avdeef, A., in van de Waterbeemd, H. Lennemas, H. Artursson, R (Eds.). Drug Bioavailability. Estimation of Solubility, Permeability, Absorption and Bioavailability. Wiley-VCH Weinheim, 2003 (in press), with permission from Wiley-VCH Verlag GmbH.]...

Drug Bioavailability Estimation of Solubility, Permeability, Absorption and Bioavailability. Edited by Han van de Waterbeemd. Hans Lennernas and Per Artursson Copyright 2003 WILEY-VCH Verlag GmbH Co. KGaA, Weinheim ISBN 3-527-30438-X... 

Karlsson, M. O., Bredberg, U., Bioavailability estimation by semi-simultaneous drug administration a Monte Carlo simulation study,... 

In vivo evaluation of the semi-simultaneous method for bioavailability estimation using controlled intravenous infusion as an... 

Fig. 19.9. G raphical oral bioavailability estimation map. (Reproduced with permission from Ref. [26] 2002 American Chemical Society.)...

Avdeef A (2002) Eligh-throughput measurement of permeability profiles. In Van de Waterbeemd H, Lennernas H, Arturrson P (Eds) Drug Bioavailability— Estimation of Solubility, Permeability and Absorption. Wiley-VCH, Weinheim, pp 46-70. 

Absorption - Although well absorbed orally, naltrexone is subject to significant first-pass metabolism with oral bioavailability estimates ranging from 5% to 40%. Following oral administration, naltrexone undergoes rapid and nearly complete absorption with approximately 96% of the dose absorbed from the Gl tract. Peak plasma levels of naltrexone and 6- -naltrexol occur within 1 hour of dosing. 

Comer, J.E.A. 2004. High-throughput measurements of log D and pK. In Drug bioavailability Estimation of solubility, permeability, absorption and bioavailability, eds. H. van de Waterbeemd, H. Lennernas, P. Artursson, R. Mannhold, H. Kubinyi, and G. Folkers, 21. Weinheim Wiley-Verlag. 

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