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Cyclodextrin complexes of valdecoxib: properties and anti-inflammatory activity in rat.
- Source :
-
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V [Eur J Pharm Biopharm] 2005 May; Vol. 60 (1), pp. 39-46. - Publication Year :
- 2005
-
Abstract
- The influence of natural beta-cyclodextrin and its hydrophilic derivatives (HPbetaCd and SBE7betaCd) on the in vitro dissolution rate, in vivo absorption and oral bioavailability of a poorly water soluble anti-inflammatory agent, valdecoxib (VALD) was studied. Equimolar drug-cyclodextrin solid complexes were prepared by kneading and coevaporation methods and characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffraction. In the liquid state, the cyclodextrin complexes were studied using phase solubility analysis, (1)H nuclear magnetic resonance and circular dichroism spectroscopy. Drug solubility and dissolution rate in distilled water were notably improved by employing the betaCds. The DP(15) (i.e. percent of dissolved VALD at 15 min) was 10.5% for the pure drug and 50, 91 and 93% for VALD-betaCd, VALD-HPbetaCd and VALD-SBE7betaCd complexes, respectively. Moreover, it was found that in the, the cyclodextrin complexes of drug showed significant improvement in the anti-inflammatory activity.
- Subjects :
- Animals
Anti-Inflammatory Agents, Non-Steroidal chemistry
Calorimetry, Differential Scanning
Chemistry, Pharmaceutical
Circular Dichroism
Edema chemically induced
Edema prevention & control
Excipients
Isoxazoles chemistry
Kinetics
Magnetic Resonance Spectroscopy
Rats
Solubility
Spectroscopy, Fourier Transform Infrared
Sulfonamides chemistry
X-Ray Diffraction
Anti-Inflammatory Agents, Non-Steroidal adverse effects
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Cyclodextrins chemistry
Isoxazoles administration & dosage
Isoxazoles pharmacology
Sulfonamides administration & dosage
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0939-6411
- Volume :
- 60
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
- Publication Type :
- Academic Journal
- Accession number :
- 15848054
- Full Text :
- https://doi.org/10.1016/j.ejpb.2004.12.005