Oral formulations of mitochondrially-targeted antioxidants and their preparation and use

摘要

Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.

主权项

1. A pharmaceutical formulation comprising a compound of Formula I in oxidized and/or reduced form: wherein:
A is an antioxidant of Formula II: and/or reduced form thereof, wherein:
m comprises an integer from 1 to 3;Y is methyl; L is a linker group comprising a straight or branched hydrocarbon chain optionally substituted by one or more double or triple bond, or ether bond, or ester bond, or C—S, or S—S, or peptide bond; and which is optionally substituted by one or more substituents selected from alkyl, alkoxy, halogen, keto group, amino group;
n is an integer from 1 to 20; andB is a targeting group is:
a Skulachev ion Sk+Z−, wherein:
Sk is a lipophilic cation or a lipophilic metalloporphyrin; andZ is a pharmaceutically acceptable anion, the compound being in about 10% to about 100% of a liquid solvent selected from the group consisting of glycol and glycerol.