Results 221 to 230 of about 111,693 (253)
Some of the next articles are maybe not open access.
Xenobiotica, 2012
We previously reported that the accuracy of clearance (CL) prediction could be differentiated by permeability. CL was drastically under-predicted by in vitro metabolic intrinsic clearance (CL(int)) for compounds with low permeability (11 and >47 by metabolic CL(int), with and without applying a scaling factor of 4, respectively.
Liyue, Huang +6 more
openaire +2 more sources
We previously reported that the accuracy of clearance (CL) prediction could be differentiated by permeability. CL was drastically under-predicted by in vitro metabolic intrinsic clearance (CL(int)) for compounds with low permeability (11 and >47 by metabolic CL(int), with and without applying a scaling factor of 4, respectively.
Liyue, Huang +6 more
openaire +2 more sources
Biochemical Pharmacology, 1987
Pseudoracemic hexobarbital (HB), consisting of equal molar fractions of S (+) HB and deuterium-labeled R (-) HB, d3 R (-) HB, was administered orally to rats in a dose of 50 mg/kg. Concentrations of both enantiomers in blood were measured by an enantioselective mass fragmentographic assay.
van der Graaff, M +3 more
openaire +3 more sources
Pseudoracemic hexobarbital (HB), consisting of equal molar fractions of S (+) HB and deuterium-labeled R (-) HB, d3 R (-) HB, was administered orally to rats in a dose of 50 mg/kg. Concentrations of both enantiomers in blood were measured by an enantioselective mass fragmentographic assay.
van der Graaff, M +3 more
openaire +3 more sources
Drug Metabolism and Disposition, 2005
Due to the time-dependent loss of cytochrome P450 (P450)-mediated metabolism in freshly isolated hepatocytes, several types of culture systems have been developed to extend their lifespan. The aim of this study was to evaluate the ability of monolayer cultures of rat hepatocytes to determine the in vitro CL(int) compared with suspensions of freshly ...
Griffin, Sarah J., Houston, J. Brian
openaire +3 more sources
Due to the time-dependent loss of cytochrome P450 (P450)-mediated metabolism in freshly isolated hepatocytes, several types of culture systems have been developed to extend their lifespan. The aim of this study was to evaluate the ability of monolayer cultures of rat hepatocytes to determine the in vitro CL(int) compared with suspensions of freshly ...
Griffin, Sarah J., Houston, J. Brian
openaire +3 more sources
Drug Metabolism and Disposition, 2004
Freshly isolated hepatocytes are currently regarded as the most superior in vitro model for use in prediction studies, in particular to provide estimates of in vivo intrinsic clearance (CL(int)). However, due to their loss of viability within 4 h and a decrease in cytochrome P450-dependent metabolism upon culture, newer cellular models are being ...
Griffin, Sarah J., Houston, J. Brian
openaire +2 more sources
Freshly isolated hepatocytes are currently regarded as the most superior in vitro model for use in prediction studies, in particular to provide estimates of in vivo intrinsic clearance (CL(int)). However, due to their loss of viability within 4 h and a decrease in cytochrome P450-dependent metabolism upon culture, newer cellular models are being ...
Griffin, Sarah J., Houston, J. Brian
openaire +2 more sources
Xenobiotica, 2010
Intrinsic clearance (CL(int)) of seven probe cytochrome P450 substrates, across a wide range of clearance, was compared in microsomes and cryopreserved hepatocytes from the same four livers. Previous comparisons have shown system dependence, but using preparations from different donor livers.
Foster, Joanne A. +2 more
openaire +2 more sources
Intrinsic clearance (CL(int)) of seven probe cytochrome P450 substrates, across a wide range of clearance, was compared in microsomes and cryopreserved hepatocytes from the same four livers. Previous comparisons have shown system dependence, but using preparations from different donor livers.
Foster, Joanne A. +2 more
openaire +2 more sources
Journal of Pharmacokinetics and Biopharmaceutics, 1983
The influence of altered drug binding on the hepatic elimination of tolbutamide, a drug of low intrinsic clearance, and on the formation of its metabolite, hydroxytolbutamide, was examined under linear conditions at steady state in the isolated in situ single-pass perfused rat liver preparation, with perfusate flow fixed at 15 ml/min.
W L, Schary, M, Rowland
openaire +2 more sources
The influence of altered drug binding on the hepatic elimination of tolbutamide, a drug of low intrinsic clearance, and on the formation of its metabolite, hydroxytolbutamide, was examined under linear conditions at steady state in the isolated in situ single-pass perfused rat liver preparation, with perfusate flow fixed at 15 ml/min.
W L, Schary, M, Rowland
openaire +2 more sources
In Vitro-In Vivo Correlation for Intrinsic Clearance for Drugs Metabolized by Human Aldehyde Oxidase
Drug Metabolism and Disposition, 2010The ability to predict in vivo clearance from in vitro intrinsic clearance for compounds metabolized by aldehyde oxidase has not been demonstrated. To date, there is no established scaling method for predicting aldehyde oxidase-mediated clearance using in vitro or animal data.
Michael, Zientek +3 more
openaire +2 more sources
European Journal of Clinical Investigation, 1992
Abstract. Intrinsic hepatic clearance (K) of indocyanine green (ICG) is used as a quantitative measure of liver function. ICG is tightly bound to plasma proteins. The purpose of this study was to examine the effect of changes of plasma protein concentration on K. in anaesthetized pigs with intact hepatic circulation.
OTT P., KEIDING S., BASS L.
openaire +4 more sources
Abstract. Intrinsic hepatic clearance (K) of indocyanine green (ICG) is used as a quantitative measure of liver function. ICG is tightly bound to plasma proteins. The purpose of this study was to examine the effect of changes of plasma protein concentration on K. in anaesthetized pigs with intact hepatic circulation.
OTT P., KEIDING S., BASS L.
openaire +4 more sources
Xenobiotica, 2016
1. We compared direct scaling, regression model equation and the so-called "Poulin et al." methods to scale clearance (CL) from in vitro intrinsic clearance (CLint) measured in human hepatocytes using two sets of compounds. One reference set comprised of 20 compounds with known elimination pathways and one external evaluation set based on 17 compounds ...
Tetsuo, Yamagata +5 more
openaire +2 more sources
1. We compared direct scaling, regression model equation and the so-called "Poulin et al." methods to scale clearance (CL) from in vitro intrinsic clearance (CLint) measured in human hepatocytes using two sets of compounds. One reference set comprised of 20 compounds with known elimination pathways and one external evaluation set based on 17 compounds ...
Tetsuo, Yamagata +5 more
openaire +2 more sources
Journal of Pharmacokinetics and Biopharmaceutics, 1984
The influence of protein binding on the extraction ratio, and availability, of diazepam has been examined in the single-pass isolated perfused rat liver preparation. Binding of diazepam was varied by adjusting the concentration of albumin in the perfusate. In the absence of binding the extraction ratio of diazepam was high, 0.93-0.995.
M, Rowland +3 more
openaire +2 more sources
The influence of protein binding on the extraction ratio, and availability, of diazepam has been examined in the single-pass isolated perfused rat liver preparation. Binding of diazepam was varied by adjusting the concentration of albumin in the perfusate. In the absence of binding the extraction ratio of diazepam was high, 0.93-0.995.
M, Rowland +3 more
openaire +2 more sources