Physical characterization of solid iopanoic acid forms.

Abstract

Three solid forms of iopanoic acid were characterized by X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, thermal microscopy, IR spectroscopy, and dissolution studies. X-ray analysis demonstrated that two solid forms were crystalline and that the third was amorphous. The amorphous form had been reported previously as crystalline. Enthalpies and entropies of transition were calculated using differential scanning calorimetry. A fourth form, a benzene solvate, also was isolated but proved to be too unstable at room temperature to permit conclusive characterization. The amorphous form demonstrated a 10-fold greater intrinsic dissolution rate than the commercially available form (Form I). Form II's intrinsic dissolution rate was 1.5 times greater than that of Form I. In powder dissolution studies, the peak solubilities of the different forms followed the same rank order as their intrinsic dissolution rates. Form II was relatively stable in aqueous saturated solutions, but the amorphous form was rapidly converted to Form I under similar conditions.