Main Article Content

Dissolution enhancement of ketoprofen using meltsonocrystallization technique


Nassim Belkacem
Mutaz Salem
Hatim Alkhatib
Chiraz Amrine

Abstract

Purpose: To investigate the effect of melt-sonocrystallization technique (MS) on the physicochemical
characteristics and dissolution of a poorly soluble drug (ketoprofen).
Methods: Ketoprofen was heated in paraffin oil bath at 97 °C and then poured into a beaker containing
25 mL deionized water at 25 oC and immediately treated using a probe ultrasonicator at different
ultrasonic times, and varying amplitudes at frequency of 20 KHz. Prepared suspensions were evaluated
for the effect of temperature and energy of production. Powders were characterized using differential
scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier
transform infra-red spectrophotometry (FTIR). The Heckle plot, Carr's compressibility index, and
Hausner's ratio were used to determine compressibility properties. Furthermore, the angle of slide was
used to evaluate flow characteristics.
Results: There was a significant reduction in particle size characteristics following meltsonocrystallization
(p < 0.05). The SEM micrographs revealed needle-shaped particles with smooth
surfaces. There was no significant difference in DSC thermograms with peaks ranging from 97.3 to 98.1
°C (p < 0.05). The FT-IR spectra showed two specific sharp and symmetrical peaks at (1654.5 cm-1)
and (1697.3 cm-1). Also, distinctive peaks of ketoprofen remained detectable in XRD patterns,
indicating that the substance had not undergone structural modification. The solubility increased by 15
%. There was no improvement in flowability or compressibility. Dissolution was greatly improved from
67 to 85 %.
Conclusion: Melt-sonocrystallization reduces particle size, solubility, and dissolution with no structural
modification to ketoprofen. In vivo investigation of drug bioavailability from the generated powders would
be required.


Journal Identifiers


eISSN: 1596-9827
print ISSN: 1596-5996