Characterization of ultrasound extrudated and cut citric acid/paracetamol blends

The purpose of the present work was to study the effect of ultrasound extrusion and cutting on the physical stability of a viscous and sticky supercooled melt containing (50/50, w/w, %) citric acid anhydrate and paracetamol. Samples were extrudated at temperatures of 50, 60, and 70°C using power levels of 0, 50, 100, and 150 W. Similarly, extrudates prepared at 60°C were cut at temperatures ranging from 25-60°C with an ultrasound knife in the range 0, 50, and 100 W. The characterization methods used were: high performance liquid chromatography, differential scanning calorimetry, Karl Fischer titration, X-ray powder diffraction, Fourier transform infrared microscopy, optical- and stereomicroscopy. There was no physical difference in extrudates or cut surfaces whether processed with or without ultrasound. During 1-year aging time in dry conditions, all the samples were observed to crystallize slowly and ultrasound processing did not enhance the crystallization. Ultrasound thus holds some promise for processing of viscous and sticky pharmaceuticals, provided the material is physically stable enough to withstand mechanical and thermal stress. Processing of sticky and viscous material would be difficult without ultrasound with the methods currently used in pharmaceutical industry. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:2140-2148, 2009