TY - JOUR
T1 - Preparation and physicochemical and preclinical evaluations of recrystallized celecoxib
AU - Mutalik, S.
AU - Usha, N.
AU - Ranjith, A.K.
AU - Umesh, S.
AU - Musmade, P.
AU - Anup, N.
N1 - Cited By :2
Export Date: 10 November 2017
CODEN: JPHTE
Correspondence Address: Mutalik, S.; School of Pharmacy, Univeristy of Queensland, Brisbane, QLD 4072, Australia; email: ssmutalik@yahoo.com
Chemicals/CAS: celecoxib, 169590-42-5; polysorbate 80, 8050-83-7, 9005-65-6; Acetic Acid, 64-19-7; celecoxib, 169590-42-5; Cyclooxygenase Inhibitors; Polyethylene Glycols; Polysorbates; Pyrazoles; Solvents; Sulfonamides
Manufacturers: Ranbaxy, India; lupin research park, India; Sigma, United States
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PY - 2007
Y1 - 2007
N2 - The aim of the present study is to increase the aqueous solubility of celecoxib by recrystallization from distilled water, Tween-80, and polyethylene glycol-400. The prepared crystals were evaluated for various physicochemical evaluations, dissolution rate, and in vivo performance like analgesic activity (by writhing and hot plate method) and pharmacokinetics in mice. The practical yield of the crystals ranged between 83 and 98%, and celecoxib content was more than 99%. Celecoxib showed an almost 5-fold increase in solubility when recrystallized in the presence of Tween-80 (2%). The dissolution rates of celecoxib from the co-crystal forms were considerably higher than that of plain celecoxib. The infrared and differential scanning calorimetry studies indicated the absence of a well-defined interaction between celecoxib and carriers. The differential scanning calorimetry and X-ray diffraction studies indicated the amorphization or partial amorphization of the drug. The scanning electron microscopy showed fluffy, porous, and fine particles in recrystallized celecoxib. The particle size of prepared co-crystals was considerably reduced in comparison with plain celecoxib. The crystals prepared with Tween-80 (2%) showed significantly higher analgesic activity than plain celecoxib. In pharmacokinetic study, the prepared crystals exhibited significantly high and rapid absorption along with improved bioavailability.
AB - The aim of the present study is to increase the aqueous solubility of celecoxib by recrystallization from distilled water, Tween-80, and polyethylene glycol-400. The prepared crystals were evaluated for various physicochemical evaluations, dissolution rate, and in vivo performance like analgesic activity (by writhing and hot plate method) and pharmacokinetics in mice. The practical yield of the crystals ranged between 83 and 98%, and celecoxib content was more than 99%. Celecoxib showed an almost 5-fold increase in solubility when recrystallized in the presence of Tween-80 (2%). The dissolution rates of celecoxib from the co-crystal forms were considerably higher than that of plain celecoxib. The infrared and differential scanning calorimetry studies indicated the absence of a well-defined interaction between celecoxib and carriers. The differential scanning calorimetry and X-ray diffraction studies indicated the amorphization or partial amorphization of the drug. The scanning electron microscopy showed fluffy, porous, and fine particles in recrystallized celecoxib. The particle size of prepared co-crystals was considerably reduced in comparison with plain celecoxib. The crystals prepared with Tween-80 (2%) showed significantly higher analgesic activity than plain celecoxib. In pharmacokinetic study, the prepared crystals exhibited significantly high and rapid absorption along with improved bioavailability.
M3 - Article
SN - 1079-7440
VL - 61
SP - 362
EP - 374
JO - PDA Journal of Pharmaceutical Science and Technology
JF - PDA Journal of Pharmaceutical Science and Technology
IS - 5
ER -