Combining Two Antitubercular Drugs, Clofazimine and 4-Aminosalicylic Acid, in Order to Improve Clofazimine Aqueous Solubility and 4-Aminosalicylic Acid Thermal Stability.

Four forms of a salt combining two antitubercular drugs, clofazimine and 4-aminosalicylic acid, are reported and the crystal structure of two of these forms are described. TG/DSC analysis of all four forms demonstrate an increase in the temperature at which degradation (upon decarboxylation) occurs in comparison to pure 4-aminosalicylic acid. Water solubility evaluation indicates a significant increase of the amount of clofazimine detected in water (10.