Intestinal human absorption

Human intestinal absorption of 5 (01JPS749) and 6 (01MI30) was predicted by using five Abraham descriptors and CaCo-2 monolayer, respectively. The effect of hydrophobicity and molecular mass on the accumulation of 10 fluoroquinolones, including 5, by Staphylococcus aureus were evaluated (01MI14). 

Zmuidinavicius D, Didziapetris R, Japertas P, Avdeef A and Petrauskas A. Classification structure-activity relations (C-SAR) in prediction of human intestinal absorption. J Pharm Sci 2003 92 621-33. 

For 31 passively transported dmgs, excellent sigmoidal relationships were found between human intestinal absorption and their H-bond acceptor and donor factors [65] ... 

C. N., Boutina, D., Beck, G., Sherbom, B., Cooper, J., Platts, J. A. Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with the Abraham descriptors. J. Pharm. Sci. 2001, 90, 749-784. 

Trospium chloride, a quaternary ammonium drug (Fig. 7.45), appears to be a substrate of P-gp, and it can be taken up by cells quicky [597]. The evidence for transmembrane diffusion appears substantial. The molecule is very soluble in water (>50 mg/mL), but not in lipids (9.2 pg/mL in mineral oil) the octanol-water log Kp is —1.22 [598]. The human intestinal absorption (HIA) is 11% the molecule is not metabolized. In cell intestinal patch uptake studies, trospium is absorbed from a... 

Caco-2 Models for Prediction of Human Intestinal Absorption (HIA)... 

Figure 7.64 Human intestinal absorption compared to Caco-2 permeabilities from several groups.

Figure 7.67 Human intestinal absorption compared to (a) pION s double-sink sum-P, PAMPA GIT model and (b) human jejunal permeabilities [56],...

Pontier, C. Pachot, J. Botham, R. Lefant, B. Amaud, R, HT29-MTX and Caco-2/TC7 monolayers as predictive models for human intestinal absorption Role of mucus layer, J. Pharm. Sci. 90, 1608-1619 (2001). 

Uptake and transport of the ACE-inhibitor ceronapril (SQ 29852) by monolayers of human intestinal absorptive (Caco-2) cells in vitro, Int. 

Walgren, R. A., Walls, T., The influence of plasma binding on absorption/exsorption in the Caco-2 model of human intestinal absorption, J. Pharm. Pharmacol. 1999, 52, 1037— 1040. 

J. W., and Muskal, S. M., Prediction of human intestinal absorption of drug compounds from molecular... 

Another set of compounds that have been collected and used for modeling human intestinal absorption is that of Wessel and co-workers [23]. This dataset consists... 

Agatonovic-Kustrin, S., Bereseord, R., Yusoe, A. P. M., Theoretically-derived molecular descriptors important in human intestinal absorption, J. Pharm. Biomed. Anal. 

Area under the time-concentration curve Adenocarcinoma cell line derived from human colon Percent human intestinal absorption... 

Yalkowsky SH, Johnson JL, Sanghvi T and Machatha SG (2006) A Rule of Unity for Human Intestinal Absorption. Pharm Res 23 pp 2475-2481. 

Zhao YH, Abraham MH, Le J, Hersey A, Luscombe CN, Beck G, Sherborne B, Cooper I (2003) Evaluation of rat intestinal absorption data and correlation with human intestinal absorption. Eur. J. Med. Chem. 38 233-243. 

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