Oral formulations for the selective inhibition of thrombin comprising boronic acid species

摘要

A pharmaceutical formulation adapted for oral administration, whether directly or after combining with a liquid, and comprisinga) a first species selected from (a) boronic acids of formula (I), (b) boronate anions thereof, and (c) any equilibrium form of the aforegoing (e.g. an anhydride); and(b) a second species selected from the group consisting of pharmaceutically acceptable metal ions.;Formula (I) comprises specified peptidyl boronic acids having anti-thrombotic activity and the formulations are useful for the treatment of thrombosis. An exemplary boronic acid is Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)₂.