Der Pharmacia Lettre
Abstract
Author(s): V.Rama Mohan Gupta, K Srikanth, B.Sree Giri Prasad, G.Naveen Kumar Reddy, B.Sudheer
Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using
acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively.The
agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction
(XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy
and DSC results indicated the absence of any interactions between drug and additives. XRD
studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly
improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug
per 100 mg crystals) was in the range of 93.9 Ã?â??Ã?± 2.3 and 97.3 Ã?â??Ã?± 1.3% (n = 3) with all
formulations. The aqueous solubility and dissolution rate of the drug from crystals was
significantly (p < 0.05) increased (nearly two times). The solubility and in vitro drug release
rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies
showed that the crystal posseses a good spherical shape with smooth and regular surface. Based
on these results, formulation prepared using 10% w/v PVP K 30 selected as optimized
formulation. In vivo studies carried out on human volunteers with optimized formulation and the
pharmacokinetic parameters were compared with marketed formulation. The celecoxib spherical
crystals have shown enhanced therapeutic activity than the marketed formulation.
