Aceclofenac - CAS 89796-99-6
Not Intended for Therapeutic Use. For research use only.
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Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. It has higher anti-inflammatory action than conventional NSAIDs. It is a cytokine inhibitor. It works by blocking the action of a substance in the body called cyclo-oxygenase.
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CAS 89796-99-6 Aceclofenac

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Reference Reading

1.Glucocorticoids and chronotherapy in rheumatoid arthritis.
Cutolo M1. RMD Open. 2016 Mar 18;2(1):e000203. doi: 10.1136/rmdopen-2015-000203. eCollection 2016.
It is evident that the morning symptoms of rheumatoid arthritis (RA) are linked to the circadian abnormal increase in night inflammation, favoured by inadequate cortisol secretion under conditions of active disease. Therefore, exogenous glucocorticoid treatment is recommended in RA at low doses since it may partially act like a 'replacement therapy'. The prevention/treatment of the night upregulation of the immune/inflammatory reaction (and related flare of cytokine synthesis) has been shown to be more effective when exogenous glucocorticoid administration is obtained with a night-time-release formulation. Large-scale trials documented that modified-release prednisone has greater efficacy then morning prednisone for long-term low-dose glucocorticoid treatment in patients with RA, showing at least a more significant reduction in morning joint stiffness. Interestingly, despite a considerably higher cost than conventional prednisone, chronotherapy with night-time-release prednisone was recognised as a cost-effective option for patients with RA not on glucocorticoids who are eligible for therapy with biological disease-modifying antirheumatic drugs (DMARDs).
2.Development and validation of an LC-ESI-MS/MS method for the simultaneous quantification of naproxen and sumatriptan in human plasma: application to a pharmacokinetic study.
Brêtas JM1, César IC2, Brêtas CM1, Teixeira LS3, Bellorio KB3, Mundim IM3, Pianetti GA1. Anal Bioanal Chem. 2016 Mar 28. [Epub ahead of print]
A sensitive and fast liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method was developed and validated for the simultaneous quantification of naproxen and sumatriptan in human plasma. A simple liquid-liquid extraction procedure, with a mixture of ethyl acetate, methyl tert-butyl ether, and dichloromethane (4:3:3, v/v), was used for the cleanup of plasma. Naratriptan and aceclofenac were employed as internal standards. The analyses were carried out using an ACE C18 column (50 × 4.6 mm i.d.; particle size 5 μm) and a mobile phase consisting of 2 mM aqueous ammonium acetate with 0.025 % formic acid and methanol (38:62, v/v). A triple-quadrupole mass spectrometer equipped with an electrospray source in the positive mode was set up in the selective reaction monitoring mode to detect the ion transitions m/z 231.67 → m/z 185.07, m/z 296.70 → m/z 157.30, m/z 354.80 → m/z 215.00, and m/z 336.80 → m/z 97.94 for naproxen, sumatriptan, aceclofenac, and naratriptan, respectively.
3.Development and evaluation of decorated aceclofenac nanocrystals.
Park JJ1, Meghani N1, Choi JS2, Lee BJ3. Colloids Surf B Biointerfaces. 2016 Mar 10;143:206-212. doi: 10.1016/j.colsurfb.2016.03.022. [Epub ahead of print]
This study was aimed at achieving enhanced solubility of aceclofenac (ACF) in nanocrystaline forms (ACF-NC) and evaluating the effects of ACF-NC on cell viability. Decorated ACF-NC were prepared by nano-precipitation with stabilizers. Three kinds of stabilizers were investigated: Tween 80, Poloxamer 407, and PEG 6000. The crystal structure and morphology of ACF-NC were characterized by field emission scanning electron microscopy (FE-SEM) and differential scanning calorimetry (DSC). The solubility of ACF-NC and ACF (pure) was evaluated in different media (pH 1.2 and pH 6.8 buffers and distilled water [DW]). A drug release study was performed in PBS for 24h. Cell viability was evaluated for 24h using a human colon cancer cell-line (HCT-116) and a human breast cancer cell-line (MCF-7). Decorated ACF-NC with a mean size of 725nm were successfully prepared. The solubility of the decorated ACF-NC were 4-7 times higher than that of ACF in DW and pH 6.
4.Novel elastic membrane vesicles (EMVs) and ethosomes-mediated effective topical delivery of aceclofenac: a new therapeutic approach for pain and inflammation.
Sharma G1, Goyal H1, Thakur K1, Raza K2, Katare OP1. Drug Deliv. 2016 Mar 10:1-11. [Epub ahead of print]
CONTEXT: Aceclofenac (ACE) is a systematically designed drug, developed to circumvent the concerns associated with diclofenac. But ACE is also associated with non-steroidal anti-inflammatory drug (NSAIDs)-tagged side effects, although of decreased amplitude.