Pharmacological inducement of the fed mode for enhanced drug...

A - Human Necessities – 61 – K

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A61K 47/42 (2006.01) A61K 9/00 (2006.01) A61K 9/20 (2006.01) A61K 9/24 (2006.01) A61K 9/50 (2006.01) A61K 47/00 (2006.01) A61K 47/02 (2006.01) A61K 47/12 (2006.01) A61K 47/14 (2006.01) A61K 47/18 (2006.01) A61K 47/22 (2006.01) A61K 47/26 (2006.01)

Patent

CA 2389236

Drugs intended for absorption in the stomach or upper intestinal tract are administered in oral drug delivery systems in conjunction with any of various substances that have been discovered to function as potent agents for inducing the fed mode. By inducing the onset of the fed mode, these agents cause the stomach to prolong its retention of the drug delivery system, which is either large enough to be retained in the stomach during the fed mode or swells or expands to such a size upon ingestion. The fed mode inducing agents include the following compounds and their salts: glycine and glycylglycine, xylitol and related sugar alcohols, sodium and other metal docusates, .szlig.- casomorphins, a-lipoic acid and similarly structured acids, 2,2-diaryl-4-(4'- aryl-4'-hydroxypiperidino)butyramides, arginine, Trp-Trp, alkylpyridinium halides, dihydroxybenzoic acids, and potent sweeteners such as aspartame, aspartic acid, acesulfame, and stevioside.

L'invention concerne des médicaments destinés à être absorbés dans l'estomac ou la partie supérieure du tractus intestinal, par le biais de systèmes d'administration orale, en combinaison avec différentes substances dont on a découvert qu'elles étaient de puissants agents déclencheurs du mode par ingestion. En déclenchant ce mode, lesdits agents conduisent l'estomac à prolonger la rétention du système d'administration des médicaments, lequel a une taille suffisamment importante pour une rétention dans l'estomac en mode par ingestion ou subit une expansion pour atteindre cette taille au moment de l'ingestion. Les agents déclencheurs du mode par ingestion comprennent les composés suivants et leurs sels: glycine et glycylglycine, xylitol et alcools de sucre connexes, sodium et autres docusates métalliques, .szlig.-casomorphines, acide a-lipoïque et acides à structure similaire, 2,2-diaryle-4-(4'-aryle-4'-hydroxypiperidino)butyramides, arginine, Trp-Trp, halogénures d'alkylpyridinium, acides dihydroxybenzoïques, et puissants édulcorants du type aspartame, acide aspartique, acésulfame, et stévioside.

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