Xilobam: Effect of salt form on pharmaceutical properties

Abstract

In an effort to protect xilobam from the effects of high temperatures and high humidities without adversely affecting its dissolution from tablets, three arylsulfonic acid salts and the saccharin salt were prepared. All of the salts were determined to be more stable at 74% relative humidity and 70° than the free base.

In spite of the large differences between the effect of high humidity at a high temperature on the salts versus the free base, the dissolution of the most stable salt (1-napsylate) was essentially equivalent to the dissolution of the free base when both were prepared as formulated tablets.