Celecoxib-Cyclodextrin Systems: Characterization and Evaluation of In Vitro and In Vivo Advantage

• Published in: Drug development and industrial pharmacy 2005, Vol.31 (2), p.169-178
• Main Authors: Nagarsenker, M. S., Joshi, M. S.
• Format: Article
• Language: English
• Subjects: 2-Hydroxypropyl-beta-cyclodextrin; Administration, Oral; Animals; beta-Cyclodextrins - chemistry; Biological and medical sciences; Calorimetry, Differential Scanning; Celecoxib; Chemistry, Pharmaceutical; Cyclooxygenase Inhibitors - administration & dosage; Cyclooxygenase Inhibitors - pharmacokinetics; Cyclooxygenase Inhibitors - pharmacology; Excipients - chemistry; General pharmacology; Hydroxypropyl β cyclodextrin; In vitro dissolution studies; In vivo study; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Pyrazoles - administration & dosage; Pyrazoles - pharmacokinetics; Pyrazoles - pharmacology; Rats; Rats, Wistar; Solid dispersion; Solubility; Sulfonamides - administration & dosage; Sulfonamides - pharmacokinetics; Sulfonamides - pharmacology; Tablets
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1081/DDC-200047795

Solid dispersions of Celecoxib were prepared with hydroxypropyl β cyclodextrin by various methods such as physical mixture, cogrinding, kneading, and coevaporation. The dispersions were characterized by differential scanning calorimetry (DSC), X-ray diffraction patterns, infrared spectroscopy, and nuclear magnetic resonance studies. The DSC thermograms of the dispersions indicated potential of heat-induced interaction between Celecoxib and cyclodextrin that could influence in vitro drug dissolution. The dispersions exhibited faster rates of dissolution compared to that of Celecoxib. The kneaded dispersion with the fastest in vitro dissolution rate when compressed into tablets showed a better release profile compared to the tablets of pure Celecoxib. In vivo studies revealed that the kneaded dispersion provided for quicker response and was more effective in inhibiting rat paw edema as compared to Celecoxib alone, thus confirming the advantage of improved pharmacological activity of Celecoxib when administered as a solid dispersion with cyclodextrin.