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Preparation and Physicochemical and Precliical Evaluations of Recrystallized Celecoxib

Mutalik, S and Usha, N and Ranjith, AK and Umesh, S and Musmade, Prashant B and Anup, N (2007) Preparation and Physicochemical and Precliical Evaluations of Recrystallized Celecoxib. PDA Journal of Pharmaceutical Science and Technology., 61 (5). pp. 362-374.

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: Celecoxib, Recrystallization, Solvent change method, Polyethylene glycol, Tween-80, Analgesic, Pharmacokinetics.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 28 Apr 2012 10:00
Last Modified: 05 Nov 2016 10:00
URI: http://eprints.manipal.edu/id/eprint/76359

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