http://dx.doi.org/10.4314/tjpr.v12i3.7
Abstract
Purpose: To enhance the solubility and
dissolution characteristics of ketoprofen using various
crystallization techniques.
Methods:
Ketoprofen crystals were prepared by various
crystallization technique including spherical
agglomeration (SA), spray drying (SD), freeze drying
(FD) and super cooling (SC). The crystallization medium
used for all the techniques consisted of water and
chloroform. Residual solvents in the crystals were
determined and the crystals were characterized by DSC,
FT-IR, XRD and SEM. Both solubility and dissolution
behavior studies were carried out. The physical
stability of the crystals were also evaluated after
storage over a period of time.
Results:
Residual
IPA and chloroform in the crystals ranged from 4.10 -
5.70 and 1.84 - 2.57 ppm, respectively, which are well
below their toxic limits. The crystals obtained
exhibited lower crystallinity than the original drug.
The solubility of FD crystals in water increased almost
fivefold to 0.0926 mg/ml compared with that of the drug
(0.0172 mg/ml), while the dissolution rates of the
developed crystals were than that of the original
crystals. For example, FD crystals demonstrated the
highest dissolution (99.9 %) compared with original
crystals (64.3 %). In the stability test, the
dissolution profiles of the developed crystals remained
largely unchanged over the period of the stability
study.
Conclusion:
The re-crystallization techniques used in this study can
be applied to obtain modified ketoprofen for formulation
of tablets of the drug with improved drug dissolution.
Keywords: Crystallization,
Ketoprofen, Crystallinity, Dissolution, Stability.