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Drug Interactions with Diosmectite: a Study Using the Artificial Stomach–duodenum Model by N. Castela-Papin; S. Cai; J. Vatier; F. Keller; C.H. Souleau; R. Farinotti is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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Drug interactions with diosmectite, a gastric-protective drug, were studied in vitro using an artificial stomach-duodenum model. The behavior of neutral and ionisable drugs with pKa values ranging between 2 and 8 was monitored to determine the physicochemical characteristics of the interactions. The main neutral (digoxin) and acid (valproic acid) drug substances were moderately fixed by clay (<27%), in a pH-independent manner. Basic compounds with a pKa /=7 (ranitidine, pyrimethamine) were adsorbed by more than 81% by diosmectite in gastric and duodenal compartments. In the part of the model representing the distal duodenum, the potential site for drug absorption, only the active substances which remained positively charged (amphoteric and basic compounds) showed a large reduction (>/=80%) in their available free fraction. Ionisation of drug substances administered per os concomitantly with diosmectite plays a crucial role in these interactions.

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Author

N. Castela-Papin; S. Cai; J. Vatier; F. Keller; C.H. Souleau; R. Farinotti

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

1999

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)