Selective metabolic approach to increasing oral bioavailability of phenylephrine and other phenolic bioactivities

摘要

Presystemic metabolism in intestine of bioactives such as phenylephrine is avoided by administering a subject (human or animal) the bioactive (e.g., phenylephrine) in combination with one or more inhibitors of sulfation (e.g., sulfotransferase enzymes aka SULTs). This can also be enhanced be co-administering inhibitors of monoamine oxidases aka, MAOs, and uridine diphosphate glucoronysl transferases, aka UGTs. Preferably the inhibitors are GRAS compounds. The one or more inhibitor compounds inhibit the enzymes responsible for rapid presystemic metabolism, thus allowing the bioactives (e.g., phenylephrine) to be more readily absorbed intact into the circulatory system.

主权项

1. A method of orally administering phenylephrine to a subject in need thereof so as to enhance bioavailability of phenylephrine, comprising the step of orally administering to said subject phenylephrine in combination with one or more inhibitors of one or more sulfotransferase (SULTs) in an amount effective to enhance the bioavailability of phenylephrine, wherein said one or more inhibitors of SULTs comprises resveratrol, quercetin, vanillin, and propylparaben.