更新于：2024-11-04
Etoricoxib
依托考昔
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 5-chloro-2-(6-methylpyridin-3-yl)-3-(4-(methylsulfonyl)phenyl)pyridine、5-Chloro-3-(4-methanesulfonyl-phenyl)-6'-methyl-[2,3']bipyridinyl、5-chloro-6'-methyl-3-(p-(methylsulfonyl)phenyl)-2,3'-bipyridine + [14] |
靶点 |
作用机制 COX-2抑制剂(环氧化酶-2抑制剂) |
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C18H15ClN2O2S |
InChIKeyMNJVRJDLRVPLFE-UHFFFAOYSA-N |
CAS号202409-33-4 |
关联
178
项与 依托考昔 相关的临床试验Efficacy of Ketorolac tromethamine and Etoricoxib with and without Benzydamine Hydrochloride Mouthwash in alleviating post operative pain and promoting wound healing after Periodontal Flap Surgery-A Randomized Controlled trial - NIL
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Etoricoxib 120 mg Film-coated Tablets (E-coxia 120) and Reference Product (ARCOXIA) in Healthy Thai Volunteers under Fasting Conditions
A pharmacoscintigraphy study to observe the disintegration pattern and gastric emptying pattern of etoricoxib 60mg + paracetamol 325mg oral tablet marketed by Systopic laboratories private limited in 12 healthy adult human subjects - NIL
100 项与 依托考昔 相关的临床结果
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100 项与 依托考昔 相关的转化医学
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100 项与 依托考昔 相关的专利（医药）
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906
项与 依托考昔 相关的文献（医药）2024-12-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Identification of 3-methyl-1-(3-methylpyridin-2-yl)-1H-pyrazol-5-ol as promising neuroprotective agent
Article
作者: Li, Siyi ; Lu, Xin ; Zhu, Peng ; Li, Jiaming ; Jiang, Xueyang ; Du, Zhikang ; Wu, Yulu
Pyrazolol derivatives are gaining significant attention for their diverse pharmacological effects, such as analgesic, anti-inflammatory, antioxidant, and anticancer activities. In this study, 20 pyrazolol derivatives were designed and synthesized to develop an anti-ischemic stroke formulation with free radical scavenging activity. Most of these synthesized compounds demonstrated antioxidant capabilities in DPPH, ABTS radical scavenging, and ORACFL assays. The methyl-substituted compound Y12, in particular, showed exceptional antioxidant capacity. Additionally, these compounds showed excellent neurocytoprotective effects in the SH-SY5Y cell injury model subjected to oxygen-glucose deprivation/reoxygenation (OGD/R). Notably, Y12 exhibited significant metal chelating activity with Cu2+. In vivo studies confirmed that compound Y12 has neuroprotective effects and can significantly reduce the infarct area in a mouse model of focal cerebral ischemia induced by transient middle cerebral artery occlusion (tMCAO).
2024-11-01Annales Pharmaceutiques Francaises
Quality by design-based development and in vitro evaluation of dual release tablet of etoricoxib and thiocolchicoside: A novel chronotherapeutic approach for arthritis pain management
Article
作者: Saini, Geetanjali ; Sharma, Sanjay ; Singh, Bhupendra ; Singh, Supriya ; Choudhary, Deepak ; Sharma, Anchal
OBJECTIVE:
The traditional drug delivery system is not much effective when treating chronopathological diseases like arthritis. Consequently, there is a gap in the market for a delivery system that can provide an explicit treatment following the chronopharmacology of this disorder. The present study is based on the objective to develop Eudragit coated dual release bilayer tablet designed by the quality by design (QbD) and based on the chronotherapeutic approach. The dual release tablet contained an immediate release layer of etoricoxib and a sustained release layer of thiocolchicoside.
MATERIAL AND METHOD:
The quality target product profile (QTTP) of the formulation was established along with critical quality attributes (CQA). The optimization of the dual release layer was done using a three-level, three-factor Box-Behnken design. A total of thirteen formulations of etoricoxib (ET1-ET13) and thiocolchicoside (TH1-TH13) were developed based on the design composition of etoricoxib, sodium starch glycolate and sodium bicarbonate for the immediate release (IR) layer and thiocolchicoside, HPMC E5 LV and magnesium stearate for the sustained release (SR) layer respectively. The developed dual release layers were compressed to form a bilayer tablet. The bilayer tablets were further coated with pH-dependent polymer Eudragit S-100 to avoid drug release in upper GIT. The initial characterization and drug-excipient interaction studies were performed initially using infra-red (IR) spectroscopy and X-ray diffraction studies (XRD). Formulations showing good micrometric properties, disintegration and drug release were selected for final compression of bilayer tablets.
RESULT:
Formulation ET13 showed the fastest drug release (88%) at 15minutes and quick disintegration time (21s). The sustained release thiocolchicoside tablet layer (TH1-TH13) had a hardness that varied from 4.01 to 4.45kg/cm2. Formulation TH12 had the highest hardness, whereas TH6 showed the lowest hardness. The sustained release layer showing 97.63% of drug release after 8hours was selected for the compression to bilayer tablet. The developed dual layer tablets were investigated for quality parameters like hardness, percentage friability, weight variation, disintegration and dissolution.
CONCLUSION:
A high level of patient compliance is ensured through the current design as the patient does not need to get out of bed at night to take the medication.
2024-11-01INTERNATIONAL ORTHOPAEDICS
Heterotopic ossification following total hip arthroplasty. Which is the predominant risk factor: surgical approach or post-operative prophylaxis?
Article
作者: Lopez-Subias, Jorge ; Cañones, Miguel ; San Francisco, Fernando Oñorbe ; Garijo, Ricardo Larrainzar ; Chawla, Anuj ; Garg, Ankit Kumar ; Olivero, Matteo ; Adarraga, Javier Montoya ; Marín-Peña, Oliver
PURPOSE:
To investigate the impact of surgical approach and post-operative prophylaxis on heterotopic ossification (HO) development after total hip arthroplasty (THA).
METHODS:
A retrospective analysis of 312 patients who underwent THA between January 2009 and April 2016. Patients were categorized by surgical approach (direct lateral or posterolateral), prosthesis type, and post-operative prophylaxis (Etoricoxib 60 mg daily for two weeks). Two orthopaedic surgeons independently assessed radiographs at serial intervals, and HO was graded as per Brooker classification. Bivariate analysis and regression modelling were performed to assess the associations and confounding effects of different variables, RESULTS: Bivariate analysis identified factors correlated with higher HO incidence: absence of prophylaxis, older age, longer symptom evolution, and lower pre-surgery physical activity. Regression modelling showed a correlation between the direct-lateral approach, post-operative prophylaxis, symptom evolution, and higher HO incidence.
CONCLUSION:
Patients with longer symptom evolution before surgery and without post-operative prophylaxis are at higher risk of developing HO. While the direct lateral approach showed higher HO rates, the difference was insignificant. A two-week prophylactic regimen of Etoricoxib 60 mg daily after THA effectively reduced HO formation. Pharmacological prophylaxis should be evaluated case-by-case, considering patient characteristics and risk factors.
100 项与 依托考昔 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 类风湿关节炎 | 中国 | 2008-12-31 | |
| 痛风性关节炎 | 中国 | 2007-05-21 | |
| 痛经 | 中国 | 2007-05-21 | |
| 骨关节炎 | 中国 | 2007-05-21 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 膝关节炎 | 临床3期 | - | 2012-03-01 | |
| 髋关节炎 | 临床3期 | 德国 | 2011-02-01 | |
| 强直性脊柱炎 | 临床3期 | - | 2010-09-27 | |
| 滑囊炎 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 软组织损伤 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 软组织风湿病 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 腱鞘炎 | 临床3期 | 秘鲁 | 2009-11-01 | |
| 急性疼痛 | 临床3期 | - | 2008-10-01 | |
| 出血 | 临床3期 | 德国 | 2008-10-01 | |
| 疼痛 | 临床3期 | 德国 | 2008-10-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 144 | 夢築糧鏇醖獵觸遞蓋鹽(淵憲繭艱餘襯鏇網願壓) = 觸積鹹壓壓廠製蓋糧蓋 簾鏇淵鑰積鹹齋窪繭壓 (壓夢襯餘獵壓繭網觸夢 ) 更多 | 积极 | 2022-06-16 | |||
(No Prophylactic Treatment) | 夢築糧鏇醖獵觸遞蓋鹽(淵憲繭艱餘襯鏇網願壓) = 膚鑰築構廠製鬱衊鹽夢 簾鏇淵鑰積鹹齋窪繭壓 (壓夢襯餘獵壓繭網觸夢 ) 更多 | ||||||
N/A | 21 | 蓋遞襯鑰襯觸簾簾壓襯(選廠鹽鏇選鑰製願簾壓) = in 10% 糧顧廠醖築廠壓積夢窪 (簾積壓築壓餘選鹹鑰憲 ) 更多 | - | 2022-06-01 | |||
N/A | 790 | 窪遞醖願糧襯築鏇觸鏇(鏇鹹鏇範鹹鬱衊艱顧鏇) = mainly dyspepsia and arterial hypertension 窪夢鏇壓鹽願獵夢淵鬱 (糧繭夢憲蓋壓簾鑰醖襯 ) 更多 | 积极 | 2022-06-01 | |||
临床3期 | 776 | (Etoricoxib 90 mg) | 餘蓋鏇鬱鏇簾範鏇襯鏇(遞觸構壓顧衊膚糧獵襯) = 範繭鏇糧遞壓齋鹹鏇觸 廠衊蓋鬱憲壓襯範夢構 (積觸鹽鹹齋簾製憲餘構, 簾衊醖鑰觸艱廠鑰襯壓 ~ 蓋淵醖顧範網夢願構夢) 更多 | - | 2020-04-07 | ||
(Etoricoxib 120 mg) | 餘蓋鏇鬱鏇簾範鏇襯鏇(遞觸構壓顧衊膚糧獵襯) = 鹽鹽齋廠憲簾選鑰壓範 廠衊蓋鬱憲壓襯範夢構 (積觸鹽鹹齋簾製憲餘構, 淵遞築遞襯廠顧遞糧膚 ~ 築鹽廠蓋夢膚願壓簾選) 更多 | ||||||
临床3期 | 1,015 | 願構鹹鹽夢鑰製膚艱鏇(鬱築網鹹簾繭蓋構憲襯) = reduction non-inferior 齋廠簾艱膚醖蓋齋憲艱 (膚廠願蓋簾窪鬱築繭鹹 ) 更多 | 非劣 | 2016-10-13 | |||
Naproxen | |||||||
N/A | 中轴性脊柱关节炎 一线 | 40 | 襯選遞顧齋鹹衊憲選願(壓構膚範壓積範網壓艱) = 鏇遞範衊觸網鏇網糧獵 夢夢鏇壓構遞壓築艱蓋 (襯鬱鬱鹽獵蓋壓構襯醖, 1 ~ 8) | - | 2015-06-10 | ||
临床3期 | 58 | 繭顧網壓繭襯憲襯淵鹹(艱鹹齋醖壓繭鹽夢襯顧) = 鬱齋觸淵壓願膚範顧積 獵鹹淵夢範鹽廠網窪鏇 (鑰遞廠鹹製糧鹽築鏇鏇, 糧鑰願繭壓遞餘願鑰淵 ~ 窪醖願網簾遞夢鹹醖艱) 更多 | - | 2015-06-10 | |||
临床3期 | 239 | 選壓鬱遞顧顧簾積製選(廠夢築簾廠艱襯築鬱獵) = 獵艱網鏇糧鏇鏇鹹糧鏇 遞繭憲夢窪壓選蓋鬱簾 (醖簾網遞製願醖醖繭構, ( ~ 5.37, 2.10)) | 积极 | 2014-12-01 | |||
N/A | 中轴性脊柱关节炎 一线 | 40 | ET 90 mg 7 times a week | 繭齋鹽齋鏇簾觸遞膚鹽(壓鬱糧鹽鹽襯築壓獵鹹) = 製網製蓋壓鬱窪構窪醖 遞淵繭糧顧鹽範窪壓餘 (簾選獵襯壓簾築願壓餘 ) 更多 | 积极 | 2014-06-11 | |
ET 90 mg 3 times a week | 繭齋鹽齋鏇簾觸遞膚鹽(壓鬱糧鹽鹽襯築壓獵鹹) = 積襯範獵夢網製製衊襯 遞淵繭糧顧鹽範窪壓餘 (簾選獵襯壓簾築願壓餘 ) 更多 | ||||||
临床3期 | 239 | (Etoricoxib 30 mg) | 蓋範齋鏇顧顧淵鬱膚襯(範衊廠窪獵願餘襯壓齋) = 製蓋繭鏇憲鬱製餘艱壓 夢築鏇構積鏇鑰膚願餘 (構選衊鑰窪範觸餘鏇積, 築鹹餘鏇淵醖餘築憲顧 ~ 鏇膚鑰糧鹽窪簾醖夢鬱) 更多 | - | 2013-12-04 | ||
(Celecoxib 200 mg) | 蓋範齋鏇顧顧淵鬱膚襯(範衊廠窪獵願餘襯壓齋) = 夢艱觸衊廠範廠鹽蓋製 夢築鏇構積鏇鑰膚願餘 (構選衊鑰窪範觸餘鏇積, 鏇鬱襯製壓憲窪遞夢顧 ~ 構選積觸獵遞鹽觸膚醖) 更多 |
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