Preparation and properties of valdecoxib-hydroxypropyl beta-cyclodextrin inclusion complex.
Valdecoxib is a non-steroidal anti-inflammatory drug used in the treatment of rheumatoid and osteoarthritis. It is practically insoluble in water. Incidence of adverse events such as nausea has been reported in some trials. Therefore, an attempt was made to improve the aqueous solubility of the drug by making an inclusion complex using hydroxypropyl beta-cyclodextrin (HPbeta-CD). The complexes were prepared by physical mixture and freeze-drying methods. The different methods employed for evaluation--including differential scanning calorimetry, Fourier transform infrared spectral analysis, and scanning electron microscopy studies--indicated complete formation of the complex by the freeze-drying method in a molar ratio of 1:1. The prepared complexes showed an improved in vitro dissolution profile and better anti-inflammatory activity as compared to the pure drug.
Gowrishankar
P
P
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, India.
Ali
M
M
Baboota
S
S
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology / Q000627:therapeutic use; D002152:Calorimetry, Differential Scanning; D002351:Carrageenan; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013276:Stomach Ulcer / Q000139:chemically induced; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047392:beta-Cyclodextrins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000096926:Benzenesulfonamides
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002351:Carrageenan; D052246:Cyclooxygenase 2 Inhibitors; D007555:Isoxazoles; D013449:Sulfonamides; D047392:beta-Cyclodextrins; C406224:valdecoxib; D000096926:Benzenesulfonamides