Abstract
Etoricoxib (EXB) is a highly selective cox-2 inhibitor which belongs to the non-steroidal anti-inflammatory drug (NSAID). EXB is a class II drug according to the biopharmaceutical classification system (BCS), which possess a very low aqueous solubility in water. In the present study, many trials were made to improve the aqueous solubility and dissolution rate of EXB by solid dispersion technique.
 Eighteenth EXB formulas were formulated as a solid dispersion using a variety of hydrophilic polymers (as carriers) including poloxamer 407 (PXM 407), poloxamer 188 (PXM 188) and polyethylene glycol 4000 (PEG 4000) at different drug: polymer ratios (1:1, 1:3 and 1:5). These formulas were prepared by two methods; solvent evaporation and fusion method. The prepared formulas were evaluated for practical yield percent (PY %), drug content, saturated solubility and release rate, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD).
 It was found that the solubility was affected by the polymer type and the method of preparation. The polymers (as carriers) used to prepare EXB- solid dispersion showed improvement in the solubility in the following descending order; PXM 407>PXM 188> PEG 4000. The optimum formula (SD15) composed of the drug: PXM 407 at a ratio of 1:5 was prepared by solvent evaporation showed 7.76 folds (676.40%) solubility improvement as compared to pure EXB. The optimum formula showed a release rate of 99.8% through the first 15 min. The advance characterization of the selected formula indicated the possible transformation of the drug to the amorphous state.
 Keywords: EXB, Solid dispersion, PXM 407, PXM 188, PEG 4000.
Highlights
Etoricoxib (EXB) is a cyclooxygenase-2 (COX-2) specific inhibitor which belongs to non-steroidal antiinflammatory drugs (NSAIDS).Cyclooxygenase-2 physiological role is the synthesis of prostanoid mediators of pain, inflammation and fever
Etoricoxib solid dispersion was prepared by solvent evaporation method using different polymers including poloxamer 407 (PXM 407), PEG 4000, and poloxamer 188 (PXM 188) at three different ratios (1:1, 1:3, 1:5) as shown in table [1]
Determination of practical yield percent (PY %) and content of the prepared EXB- solid dispersion The (PY %) of the prepared EXB-solid dispersion was determined to investigate the best method for the preparation of solid dispersion granules
Summary
Etoricoxib (EXB) is a cyclooxygenase-2 (COX-2) specific inhibitor which belongs to non-steroidal antiinflammatory drugs (NSAIDS). Cyclooxygenase-2 physiological role is the synthesis of prostanoid mediators of pain, inflammation and fever. Cyclooxygenase-1 (COX-1), which is presented in the gastrointestinal tract, kidneys and platelets [1]. The potential gastrointestinal adverse effects and impacts on platelet aggregation are less than other non-selective COX inhibitors [2]. Etoricoxib is used to relieve the symptoms of rheumatoid arthritis, osteoarthritis, acute gout, chronic musculoskeletal pain (including chronic low back pain), and primary dysmenorrhoea [3].
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
