PURPOSE: The purpose of the article was to study melt sonocrystallization (MSC) for a drug forming a viscous melt when processed below its glass transition temperature. METHODS: A molten mass of drug was poured in a vessel containing deionized water, maintained at 40 degrees C using cryostatic bath, and sonicated for 1 min using probe ultrasonicator at an amplitude of 80% and a cycle of 0.8 per second. The product obtained after solidification of dispersed droplets was separated by filtration and dried at room temperature. MSC celecoxib was characterized by solubility determination, scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and stability study. RESULTS: The MSC technique was designed for celecoxib, which undergoes fast solidification. The particles obtained by MSC were porous, irregular in shape, and amorphous in nature. An increase in the apparent solubility was observed for the MSC particles. These amorphous particles also exhibited a higher stability in the amorphous state as compared with particles obtained by melt quenching. CONCLUSIONS: The reported MSC technique for celecoxib demonstrates advantages over other approaches and can be exploited in area of particle design for the amorphization of drugs.
PURPOSE: The purpose of the article was to study melt sonocrystallization (MSC) for a drug forming a viscous melt when processed below its glass transition temperature. METHODS: A molten mass of drug was poured in a vessel containing deionized water, maintained at 40 degrees C using cryostatic bath, and sonicated for 1 min using probe ultrasonicator at an amplitude of 80% and a cycle of 0.8 per second. The product obtained after solidification of dispersed droplets was separated by filtration and dried at room temperature. MSC celecoxib was characterized by solubility determination, scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and stability study. RESULTS: The MSC technique was designed for celecoxib, which undergoes fast solidification. The particles obtained by MSC were porous, irregular in shape, and amorphous in nature. An increase in the apparent solubility was observed for the MSC particles. These amorphous particles also exhibited a higher stability in the amorphous state as compared with particles obtained by melt quenching. CONCLUSIONS: The reported MSC technique for celecoxib demonstrates advantages over other approaches and can be exploited in area of particle design for the amorphization of drugs.
Authors: S K Paulson; M B Vaughn; S M Jessen; Y Lawal; C J Gresk; B Yan; T J Maziasz; C S Cook; A Karim Journal: J Pharmacol Exp Ther Date: 2001-05 Impact factor: 4.030