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

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 n...

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Bibliographic Details
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
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Summary: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.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-200047795