Download e-book for iPad: Pharmacology of Intestinal Permeation II by T. Z. Csáky (auth.), Tihamér Z. Csáky M.D. (eds.)

Pharmacology

By T. Z. Csáky (auth.), Tihamér Z. Csáky M.D. (eds.)

ISBN-10: 3642695086

ISBN-13: 9783642695087

ISBN-10: 3642695108

ISBN-13: 9783642695100

The gut, really the small bowel, represents a wide floor (in the grownup 2 human nearly two hundred m ) by which the physique is uncovered to its environ­ ment. A lively substrate alternate happens throughout this huge floor: meals and xenobiotics are absorbed from the lumen into the bloodstream or the lymph, and concurrently, an analogous forms of substrate cross again into the lumen. The luminal floor of the gut is covered with a "leaky" epithelium, hence the passage of the substrates, in both path, proceeds through either transcellular and intercellular routes. uncomplicated and carrier-mediated diffusion, lively delivery, pinocytosis, phagocytosis and persorption are all excited about this passage around the intestinal wall. The time period "intestinal permeation" refers back to the strategy of passage of varied ingredients around the intestine wall, both from the lumen into the blood or lymph, or within the other way. "Permeability" is the of the intestine which governs the speed of this advanced two-way passage. The pharmacologist's curiosity within the challenge of intestinal permeation is twofold: at the one hand, this technique determines the bioavailability of substances and contributes considerably to the pharmacokinetics and toxicokinetics of xeno­ biotics; however, the pharmacodynamic results of many medications are manifested in a signigicant alteration of the physiological means of intestinal permeation.

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It has been shown by ALBERT and REES (1955,1956) that a number of polyvalent cations, namely aluminum, bismuth, calcium, iron, magnesium, and zinc, form complexes with tetracycline which are much less soluble, therefore much less readily absorbed from the gut. Clinically, it has been demonstrated that the absorption of tetracyclines was reduced by the simultaneous administration of aluminum- or magnesium-containing antacids (WAISBREN and HUECKEL 1950; SEED and WILSON 1950; MICHEL et a1. 1950), by iron preparations (NEUVONEN and PENTTILA 1974), by foods containing high calcium, levels such as milk, buttermilk, and cottage cheese (NEUVONEN et a1.

As discussed in Sect. Z. s _ UiQl I ..... 01 S _. 2 3 'c 'E . 0 E 2 c Ql U C ~ o Ql 0. 0. « o .. g- 1 j Fig. 5. Interdependence ofthe absorption of salicylic acid and net water flux in the intestine of the rat (OCHSENFAHRTand WINNE 1974 b) the stomach. Consequently, the rate of gastric emptying may significantly modify the rate of absorption. In human subjects, in whom the rate of gastric emptying and the absorption of acetaminophen (paracetamol) was simultaneously monitored, a very close parallelism was found between the rates (PRESCOTT et al.

Adis, New York Neuvonen PJ, Elonen E (1980) Effect of activated charcoal on absorption and elimination of phenobarbitone, carbamazepine and phenylbutazone in man. Eur J Clin Pharmacol 17:51-57 Neuvonen PJ, Penttilii 0 (1974) Effect of oral ferrous sulphate on the half-life of doxycycline inman. Eur J Clin PharmacoI7:361-363 Neuvonen P, Mattila M, Gothoni G, Hackman R (1971) Interference of iron and milk with absorption of tetracycline. Scand J Clin Lab Invest [SuppI27] 116:76 Neuvonen PJ, Elfving SM, Elonen E (1978) Reduction of absorption of digoxin, phenytoin and aspirin by activated charcoal in man.

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Pharmacology of Intestinal Permeation II by T. Z. Csáky (auth.), Tihamér Z. Csáky M.D. (eds.)


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