Permeability intestinal

Infants are particularly sensitive to endosulfan due to their higher intestinal permeability and immature detoxification system. In a study of human breast milk conducted in the country of Kazakhstan in 1994, the concentration of various contaminants, including endosulfan, were determined (Lutter et al. 1998). 

Van de Waterbeemd, H. Intestinal permeability prediction from theory. In Oral Drug Absorption, Dressman, J. B., Lennemas, H. (eds.), Dekker, New York, 2000, pp. 31-49. 

Winiwarter, S., Ax, F., Lennemas, H., Hallberg, A., Pettersson, C., Karlen, A. Hydrogen bonding descriptors in the prediction of human in vivo intestinal permeability. J. Mol. Graph. Model. 2003, 21, 273-287... 

Wyatt, J., Vogelsang, H., Hiibl, W., Waldhoer, T. and Lochs, FI. (1993). Intestinal permeability and the prediction of relapse in Crohn s disease. Lancet 341, 1437-1439. 

Kynaston, J. A., Fleming, S. C., Laker, M. F. and Pearson, A. D. J., Simultaneous quantification of mannitol, 3-O-methyl glucose and lactulose in urine by HPLC with pulsed electrochemical detection, for use in studies of intestinal permeability, Clin. Chem., 39, 453, 1993. 

Artursson, P., Application of physicochemical properties of molecules to predict intestinal permeability, AAPS Workshop on Permeability Dehnitions and Regulatory Standards, Arlington, VA, Aug. 17-19, 1998. 

Dowty, M. E. Dietsch, C. R., Improved prediction of in vivo peroral absorption from in vitro intestinal permeability using an internal standard to control for intra- inter-rat variability, Pharm. Res. 14, 1792-1797 (1997). 

Steinbaugh, MD Taylor. Comparison of intestinal permeabilities in multiple in vitro and in situ models Relationship to absorption in humans. Pharm Res 12 693-699, 1995. 

Hu Ming, HI Mosberg, GL Amidon. Use of the peptide carrier system to improve the intestinal absorption of L-alpha-methyldopa Carrier kinetics, intestinal permeabilities, and in vitro hydrolysis of dipeptidyl derivatives of L-alpha-methyldopa. Pharm Res 6(1) 66—69, 1989. 

E Lipka, LX Yu, D Liu, JR Crison, GL Amidon. Evaluation of the intestinal permeability of (3-blocker drugs and their potential for oral controlled release. Proc Int Symp Controlled Release Bioact Mater 22 366-367, 1995. 

Mast cell-dependent alterations in smooth muscle contractility and intestinal permeability may also be important in expulsion of H. polygyms and T. spiralis. Increases in smooth muscle contractility (with associated... 

Van de Waterbeemd, H., Intestinal permeability prediction from theory, in Oral Drug Absorption. Dressman,... 

In conclusion, there are several drawbacks to the use of Caco-2 cells in studies of active drug transport. Despite these drawbacks, we note that a recent comprehensive study comparing various P-glycoprotein drug efflux assays in drug discovery came to the conclusion that the Caco-2 transport assay is the method of choice, since it displays a biased responsiveness towards compounds with low or moderate permeability - in other words, towards compounds whose intestinal permeability is most likely to be significantly affected by drug efflux mechanisms [101]. 

A. Sokolowski, R. Rai, W. Young, and B. Sjostrom. In vitro intestinal permeability of factor Xa inhibitors influence of chemical structure on passive transport and susceptibility to efflux, Pharm. Res. 2001, 38, 1735— 1741... 

Friedrichsen, G., P. Jakobsen, M. Taub, and M. Begtrup. Application of enzymatically stable dipeptides for enhancement of intestinal permeability. Synthesis and in vitro... 

Fine, K. D., C. A. Santa Ana, J. L. Porter, and J. S. Fordtran. Effect of changing intestinal flow rate on a measurement of intestinal permeability, Gastroenterology 1995, 108, 983-989... 

Fig. 5.2. Two-step process for evaluation of intestinal drug absorption. The first step represents the prediction of intestinal permeability (e.g., over Caco-2 monolayers) from in-silico models or from physico-chemical...

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