Acta Pharm. 57 (2007) 173-184

full paper

Original research paper

 

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

 

VENKADARI RAMMOHAN GUPTA1*, SRINIVAS MUTALIK2, MADHOBHAI M. PATEL3 and GIRISH K. JANI4

vrmgupta_05@yahoo.co.in

1Department of Pharmaceutics, N.E.T. Pharmacy College, Navodaya Nagar, Mantralayam Road, Raichur-584103, India

2 Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal-576104, India

3 Vice Chancellor, Hemachandracharya North Gujarat University, Patan, India

4 Department of Pharmaceutics, L. M. College of Pharmacy, Navrangpura, Ahmedabad, India

Accepted January 31, 2007

 

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 2.3 and 97.3 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 possesses a good spherical shape with smooth and regular surface.

 

Keywords: celecoxib, spherical crystallization, solubility, dissolution rate, micromeritic properties