Abstract

An RP-HPLC analytical method for estimation of valdecoxib in human plasma was developed and validated. Protein precipitation and valdecoxib extraction from plasma (200 μL) was carried out by adding 800 μL perchloric acid (5%, v/v in water) containing nimesulide as the internal standard followed by vortex mixing and centrifugation. The supernatant (20 μL) was then injected onto an ODS C18(25 cm×4.6 mm) column from Shimadzu. The mobile phase comprised of acetonitrile and water (35: 65) with a total run time of 12 min and the wavelength of the detector was set at 244 nm. The extraction recovery of valdecoxib from plasma was >95% and the calibration curve was linear (r2= 0.999) over valdecoxib concentrations ranging from 20 to 1400 μg/mL (n= 10). The method had an accuracy of >92% and LOD and LLOQ of 3.58 μg/mL and 13.45 μg/mL respectively. The method reported is simple, reliable, precise, accurate and has the capability of being used for determination of Valdecoxib in clinical settings.

Highlights

  • Valdecoxib is chemically designated as 4-(5-methyl-3-phenyl-4-isoxazolyl) benzenesulfonamide and is a diaryl substituted isoxazole[1,2] (Figure 1), with the trade name Vx2 (Novartis) has a molecular weight of 314.36. It is commonly used as a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties indicated for oral administration, for the treatment of osteoarthritis and Rheumatoid arthritis[3]

  • The aim of the current study is to develop a simple, rapid and reliable method for estimation of valdecoxib in human plasma using RP

  • Valdecoxib was eluted at 11.250, whereas the internal standard (IS) eluted at 8.783 min and no interfering peaks were observed at the time of valdecoxib peaks or the IS

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Summary

Introduction

Valdecoxib is chemically designated as 4-(5-methyl-3-phenyl-4-isoxazolyl) benzenesulfonamide and is a diaryl substituted isoxazole[1,2] (Figure 1), with the trade name Vx2 (Novartis) has a molecular weight of 314.36. It is commonly used as a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties indicated for oral administration, for the treatment of osteoarthritis and Rheumatoid arthritis[3]. Valdecoxib binds to the cox-2 enzyme and there by prevents its activity in response to stimulation from cytokines This blockade inhibits series of reaction leading to pain. In the first stage the inhibitor interacts at the enzyme surface near the membrane binding region

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