| abstract |
Pharmaceutical presentations of phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are protected from binding to active ingredient in the stomach. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: (I) wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X 1 , X 2 , X 3 , X 4 , and X 5 are either all hydrogens or one or two of X 1 , X 2 , X 3 , X 4 , and X 5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R 1 is not methyl. A wide variety of enteric mechanisms may be utilized so as to provide release of the active ingredient essentially out of the environment of the stomach after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include enteric coated tablets, enteric coated capsules, capsules containing enteric coated beads. |