摘要:
A novel compound N-demethyl-sinomenine, a metabolite of the anti-arthritic alkaloid sinomenine, has been identified and characterized. The compound may be incorporated in a pharmaceutical composition and may be administered to patients for treatment of various disorders, such as rheumatoid arthritis. The novel compound has superior biological activity and water solubility as compared to sinomenine.
摘要:
A method for increasing bioavailability of an orally administered hydrophobic pharmaceutical compound, which comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with an essential oil or essential oil component in an amount sufficient to provide bioavailability of the compound in the presence of the essential oil or essential oil component greater than bioavailability of the compound in the absence of the essential oil or essential oil component, wherein the essential oil or essential oil component has an activity of at least 10% inhibition at a concentration 0.01 wt.% or less in an assay that measures reduced conversion of cyclosporine to hydroxylated products using an assay system containing 250 νg rat liver microsomes, 1 νM cyclosporine and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1 M sodium phosphate buffer, pH 7.4.
摘要:
A method for increasing bioavailability of an orally administered pharmaceutical compound comprises orally coadministering the pharmaceutical compound to a mammal in need of treatment with the compound and a gallic acid ester. Preferred gallic acid esters of the invention include octyl gallate, propyl gallate, lauryl gallate, and methyl gallate. Improved formulations of pharmaceutical compounds include the gallic acid ester to enhance the biovailability of the active ingredient of the pharmaceutical compound.
摘要:
A method for increasing bioavailability of an orally administered pharmaceutical compound comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with propyl gallate. Improved formulations of pharmaceutical compounds include propyl gallate to enhance the bioavailability of the active ingredient of the pharmaceutical compound.