更新于：2024-11-14
Dexibuprofen
右布洛芬
更新于：2024-11-14
概要
基本信息
原研机构- |
最高研发阶段批准上市 |
首次获批日期 瑞士 (1998-04-28), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
登录后查看时间轴
结构
分子式C13H18O2 |
InChIKeyHEFNNWSXXWATRW-JTQLQIEISA-N |
CAS号51146-56-6 |
关联
20
项与 右布洛芬 相关的临床试验JC002餐后比较药代动力学临床试验
JC002比较药代动力学临床试验
JC001生物等效性试验（高剂量组）
100 项与 右布洛芬 相关的临床结果
登录后查看更多信息
100 项与 右布洛芬 相关的转化医学
登录后查看更多信息
100 项与 右布洛芬 相关的专利（医药）
登录后查看更多信息
310
项与 右布洛芬 相关的文献（医药）2024-12-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Preparation of two new chiral metal-organic frameworks for lipase immobilization and their use as biocatalysis in the enantioselective hydrolysis of racemic naproxen methyl ester
Article
作者: Ascioglu, Sebahat ; Sayin, Serkan ; Yildirim, Ayse ; Ozyilmaz, Elif ; Yilmaz, Mustafa
Considering the selective pharmacological activity of chiral drugs, it is important to develop new chiral materials to synthesize them. In this work, two new chiral MOFs (UiO-66@Np and UiO-66@Ib) were prepared by the covalent attachment of the chiral compounds (S-naproxen and S-ibuprofen) to the amine-functionalized Zr-MOF (UiO-66-NH2). Then, Candida rugosa lipase (CRL) was immobilized on these chiral MOFs to fabricate two new biocomposites (UiO-66@Np@CRL and UiO-66@Ib@CRL) as effective biocatalysts, which enable significant enhancement in the catalytic activity and enantioselectivity of lipase. The FTIR, SEM, EDX, TGA, and PXRD analyses were carried out to confirm the formation of the biocomposites. The catalytic performances of the biocomposites (UiO-66@Np@CRL and UiO-66@Ib@CRL) were evaluated in the typical hydrolysis of p-nitro-phenyl palmitate (p-NPP) and the catalytic enantioselective hydrolysis of (R,S)-naproxen methyl ester. Under optimal conditions, UiO-66@Np@CRL showed a higher enantiomeric excess of the substrate (ees) value and a 98 % and 50 % conversion rate, respectively, than that of UiO-66@Ib@CRL. Besides, an excellent enantioselectivity (E) value of 458 was obtained in the presence of the biocomposite (UiO-66@Np@CRL). In addition, it was observed that the catalytic activity, conversion rate and ees value of this composite (UiO-66@Np@CRL) remained almost unchanged in reuse after 6 months. The results showed that in enantioselective reactions, the highest conversion and enantioselectivity could be achieved when the chiral compound bound to the MOF and the model compound used are the same.
2024-11-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Ionic liquid supported hydrogel–lipase biocatalytic systems in asymmetric synthesis of enantiomerically pure S-ibuprofen
Article
作者: Fu, Qiang ; Biadasz, Andrzej ; Jesionowski, Teofil ; Nghiem, Long Duc ; Szada, Daria ; Degórska, Oliwia ; Zdarta, Jakub
Novel hydrogel biocatalysts with immobilized lipase, stabilized by ionic liquids (ILs) of different hydrophobicity, were synthesized and evaluated. Variations of the time of immobilization and ratio of substrates during hydrogel synthesis were considered to obtain the most stable biocatalyst with the highest activity. Physicochemical characterization proved the success of the hydrogel synthesis and enzyme deposition on the surface of the support. Nevertheless, the key objective was to produce a biocatalyst for further application in ibuprofen methyl ester resolution, with the aim of obtaining an enantiomerically pure product. The hydrogel biocatalysts obtained in the presence of 5 wt% ILs after 8 h of immobilization achieved the highest activity recovery of 62 %. After 10 reaction cycles, enzymatic activity was still above 60 %, and the negative effect of pH and temperature on the activity of immobilized lipase was much lower than in the case of the free enzyme. After application of the catalyst in the resolution of ibuprofen methyl ester, the enantiomeric excess and conversion rate of the process were obtained for the dynamic kinetic resolution in isooctane. A conversion rate of 95 % was achieved due to the stabilization of the biocatalyst with IL and its resulting high catalytic activity. The study thus provides the pharmaceutical industry with a new potential approach with a strong scientific foundation.
2024-09-13PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers
Article
作者: Dawaba, Hamdy M. ; Bushra, Rabia ; Sayed, Ossama M. ; Aslam, Nousheen ; Rehman, Abdul ; Hanif, Anas M. ; Alam, Shazia ; Dawaba, Aya M.
OBJECTIVE:
This study aimed to develop a stable and scalable enteric film-coated tablet for the gastric irritant dexibuprofen.
METHODS:
Utilizing direct compression with super-disintegration (crospovidone), the optimal core batches were coated with Opadry white seal coat and enterically coated with Eudragit®L100 with pigment (Talc), demonstrating a 12% weight increase; release and integrity were assessed using specific pH buffers and SEM, with stability testing confirming a six-month shelf life at 40 °C and 75% RH.
RESULTS:
The optimized formulation achieved 99.87% release in phosphate buffer within 60 min, maintained integrity for 120 min in acidic conditions, and exhibited superior bioavailability compared to Innovifen with relative bioavailability ≈of 121% and elevated Cmax (18.35 µg/ml compared to 11.1 µg/ml).
CONCLUSION:
These results highlight the potential of this formulation to enhance patient safety and efficacy through delayed enteric technology and fast intestinal release.
100 项与 右布洛芬 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 炎症 | 韩国 | 2007-12-31 | |
| 头痛 | 阿根廷 | - | 2007-04-16 |
| 背痛 | 阿根廷 | - | 2007-04-02 |
| 肌肉骨骼疼痛 | 阿根廷 | - | 2007-04-01 |
| 痛经 | 英国 | - | 2007-03-14 |
| 发热 | 中国 | 2001-01-01 | |
| 骨关节炎 | 中国 | - | 2001-01-01 |
| 类风湿关节炎 | 中国 | - | 2001-01-01 |
| 疼痛 | 瑞士 | - | 1998-05-21 |
| 风湿性疾病 | 瑞士 | - | 1998-04-28 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 镇痛 | 临床2期 | 中国 | 2021-07-13 | |
| 镇痛 | 临床2期 | 中国 | 2021-07-13 | |
| 麻醉 | 临床2期 | 中国 | 2020-11-16 | |
| 麻醉 | 临床2期 | 中国 | 2020-11-16 | |
| 急性疼痛 | 临床2期 | 美国 | 2018-01-12 | |
| 肌痛 | 临床2期 | 美国 | 2015-01-01 |
登录后查看更多信息
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 | 251 | (Active Arm) | 壓網鹹艱鑰簾衊鬱願鏇(廠廠築膚廠艱鏇餘鏇衊) = 鏇網糧獵壓鏇衊選餘淵 築糧艱範襯網積糧顧廠 (範醖網齋醖憲夢顧製膚, 願窪淵廠窪選夢淵製繭 ~ 鏇鬱壓獵壓憲鏇淵廠醖) 更多 | - | 2022-01-25 | ||
Vehicle (Placebo Arm) | 壓網鹹艱鑰簾衊鬱願鏇(廠廠築膚廠艱鏇餘鏇衊) = 積窪鹽醖鹹憲範憲簾襯 築糧艱範襯網積糧顧廠 (範醖網齋醖憲夢顧製膚, 積築襯醖壓齋範顧構窪 ~ 壓齋齋壓簾鏇憲觸糧製) 更多 | ||||||
临床3期 | 263 | 願糧廠醖遞鏇夢夢遞鹹(簾獵糧淵構顧願窪鹽壓) = 繭願鹹簾獵觸廠繭艱簾 築糧蓋鏇築蓋齋醖顧壓 (糧積鏇窪鑰築壓願鹹糧 ) | - | 2018-06-23 | |||
願糧廠醖遞鏇夢夢遞鹹(簾獵糧淵構顧願窪鹽壓) = 廠選積顧蓋範艱鏇膚鑰 築糧蓋鏇築蓋齋醖顧壓 (糧積鏇窪鑰築壓願鹹糧 ) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用