Results 211 to 220 of about 103,612 (260)

Comparison of intrinsic metabolic clearance in fresh and cryopreserved human hepatocytes

Xenobiotica, 2009
1. We compared the intrinsic clearance (CL(int)) of a number of substrates in suspensions of fresh and cryopreserved human hepatocytes from seven donors. 2. CL(int) values for a cocktail incubation of phenacetin, diclofenac, diazepam, bufuralol, midazolam, and hydroxycoumarin were 4.9 +/- 3.4, 18 +/- 7.2, 5.1 +/- 4.9, 6.3 +/- 3.3, 9.8 +/- 5.8 and 22 +/-
E, Floby, J, Johansson, J, Hoogstraate, N J, Hewitt, J, Hill, A-K, Sohlenius-Sternbeck   +5 more
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Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds

Xenobiotica, 2010
We compare three different approaches to scale clearance (CL) from human hepatocyte and microsome CL(int) (intrinsic CL) for 52 drug compounds. By using the well-stirred model with protein binding included only 11% and 30% of the compounds were predicted within 2-fold and the average absolute fold errors (AAFE) for the predictions were 5.9 and 4.1 for ...
A-K, Sohlenius-Sternbeck, L, Afzelius, P, Prusis, J, Neelissen, J, Hoogstraate, J, Johansson, E, Floby, A, Bengtsson, O, Gissberg, J, Sternbeck, C, Petersson   +10 more
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Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance

Journal of Pharmacological and Toxicological Methods, 2006
This study was conducted to compare and contrast published in vitro intrinsic clearance values reported for compounds from different laboratories and the predictivity of these data to project in vivo clearance.A total of 103 compounds were selected for investigation and an exhaustive literature search was conducted to identify in vitro intrinsic ...
Rakesh, Nagilla, Kelly A, Frank, Larry J, Jolivette, Keith W, Ward   +3 more
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Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds

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, April, Chen, John, Roberts, Brett, Janosky, Xuhai, Be, Loren, Berry, Min-Hwa Jasmine, Lin   +6 more
openaire   +2 more sources

DIRECT DETERMINATION OF UNBOUND INTRINSIC DRUG CLEARANCE IN THE MICROSOMAL STABILITY ASSAY

Drug Metabolism and Disposition, 2005
The microsomal stability assay is commonly used to rank compounds according to their metabolic stability. Determination of the unbound intrinsic clearance (CL(in,u)) is essential for the accurate comparison of compounds, since nonspecific binding to microsomes can lead to an underestimation of the microsomal clearance.
Claudio, Giuliano, Mark, Jairaj, Christian M, Zafiu, Ralph, Laufer   +3 more
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Scaling of antipyrine intrinsic clearance of unbound drug in 15 mammalian species

European Journal of Drug Metabolism and Pharmacokinetics, 1984
The intrinsic clearance of unbound drug (CLuint) for antipyrine in 15 mammalian species was characterized by an equation of the form, CLuint = theta 1 (body weight) theta 2 (brain weight) theta 3, where thetas are constants. Maximum lifespan potential in mammals can also be characterized by an equation of this form.
H, Boxenbaum, J B, Fertig
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Frequency Distribution of Bilirubin Intrinsic Clearance in Adult Male Sprague–Dawley Rats

Journal of Pharmaceutical Sciences, 1978
The intrinsic body clearance of bilirubin was determined in 48 adult male Sprague--Dawley rats that received an intravenous infusion of bilirubin. The intrinsic body clearance was calculated from the infusion rate, the steady-state plasma concentration of total (free and protein-bound) bilirubin, and the free fraction of bilirubin in plasma.
S, Oie, G, Levy
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A METHOD OF DETERMINING INTRINSIC HEPATIC CLEARANCE FROM THE FIRST‐PASS EFFECT

Clinical and Experimental Pharmacology and Physiology, 1980
SUMMARY1. The relation between systemic hepatic clearance, intrinsic hepatic clearance and hepatic blood flow is considered from the point of view of the sinusoidal perfusion (parallel tube) model of the liver.2. It is shown how intrinsic hepatic clearance may be calculated, for substrates eliminated in the liver and the kidney only, from data obtained
Bass L., Winkler K.
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Clearance of 5-hydroxytryptamine by rat lung and liver: the importance of relative perfusion and intrinsic clearance.

The Journal of Pharmacology and Experimental Therapeutics, 1980
Since it is replete with degradative enzymes, the liver is commonly viewed as the organ primarily responsible for clearing circulating substances which are eliminated by metabolism. However, the enzyme content of an organ is not the only determinant of clearance.
D A, Wiersma, R A, Roth
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A UNIFIED MODEL FOR PREDICTING HUMAN HEPATIC, METABOLIC CLEARANCE FROM IN VITRO INTRINSIC CLEARANCE DATA IN HEPATOCYTES AND MICROSOMES

Drug Metabolism and Disposition, 2005
The aim of this study was to evaluate a unified method for predicting human in vivo intrinsic clearance (CL(int, in vivo)) and hepatic clearance (CL(h)) from in vitro data in hepatocytes and microsomes by applying the unbound fraction in blood (fu(b)) and in vitro incubations (fu(inc)).
Robert J, Riley, D F, McGinnity, R P, Austin   +2 more
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