更新于：2024-11-15
Empagliflozin/metformin Hydrochloride
二甲双胍恩格列净
更新于：2024-11-15
概要
基本信息
药物类型 小分子化药 |
别名 Empagliflozin/Metformin、Metformin Hydrochloride and Empagliflozin、恩格列净/盐酸二甲双胍 + [6] |
作用机制 PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂)、SGLT2抑制剂(钠-葡萄糖协同转运蛋白-2抑制剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2015-05-27), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C23H27ClO7 |
InChIKeyOBWASQILIWPZMG-QZMOQZSNSA-N |
CAS号864070-44-0 |
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关联
82
项与 二甲双胍恩格列净 相关的临床试验二甲双胍恩格列净片（I）在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉的生物等效性研究
二甲双胍恩格列净片人体生物等效性研究
恩格列净二甲双胍缓释片在健康受试者中随机、开放、两制剂、单次给药、交叉空腹/餐后状态下的生物等效性试验
100 项与 二甲双胍恩格列净 相关的临床结果
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100 项与 二甲双胍恩格列净 相关的转化医学
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100 项与 二甲双胍恩格列净 相关的专利（医药）
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4
项与 二甲双胍恩格列净 相关的文献（医药）2019-12-01Pharmacological reports : PR4区 · 医学
Effects of ticagrelor, empagliflozin and tamoxifen against experimentally-induced vascular reactivity defects in rats in vivo and in vitro
4区 · 医学
Article
作者: Moustafa Ahmed, Yasmin ; Shehata Messiha, Basim Anwar ; Abo-Saif, Ali Ahmed ; El-Sayed El-Daly, Mahmoud
BACKGROUND:
In the current investigation, the effects of the P2Y12 blocker ticagrelor, the sodium/glucose transporter-2-inhibitor empagliflozin, and the selective estrogen receptor modulator tamoxifen were examined against rheumatoid arthritis (RA)/diabetes mellitus (DM)-co-morbidity-induced defects in vascular reactivity.
METHODS:
After model setting, rats were allocated into a normal control, an RA/DM-co-morbidity, and three treatment groups receiving ticagrelor, empagliflozin and tamoxifen. Aorta tissue was isolated for enzyme-linked immunosorbent assay (ELISA) and western blot estimation of the pro-inflammatory molecules angiotensin-II (Ang-II) and endothelin-1 (ET-1), the adhesion molecules P-selectin and vascular cell adhesion molecule-1 (VCAM-1), the energy preserving molecule adenosine-5'-monophosphate-activated protein kinase (AMPK), and the anti-inflammatory molecule vasoactive intestinal peptide (VIP). Estimations of endothelial nitric oxide synthase (eNOS) and matrix metalloproteinase (MMP)-2 were performed immunohistochemically, together with histopathological examination using hematoxylin and eosin and Masson trichrome staining. An in vitro study on rat aortic strips was conducted to assess aorta vasorelaxation.
RESULTS:
Ticagrelor, empagliflozin and tamoxifen significantly increased aorta tissue AMPK and eNOS and decreased Ang-II, ET-1, P-selectin, VCAM-1 and VIP levels compared with RA/DM-co-morbidity, coupled with improved acetylcholine vasorelaxation in vitro.
CONCLUSION:
Ticagrelor, empagliflozin and tamoxifen may correct vascular reactivity defects, where modulation of vascular AMPK, eNOS, Ang-II, ET-1, P-selectin, VCAM-1 and MMP-2 underline their protective effects.
2017-08-01Journal of chromatographic science4区 · 化学
LC–MS/MS Determination of Empagliflozin and Metformin
4区 · 化学
Article
作者: Ayoub, Bassam M ; Mowaka, Shereen
A new LC-MS/MS method was developed for determination of empagliflozin and metformin. Bridged Ethylene Hybrid C18 column (50 mm × 2.1 mm, 1.7 μm), isocratic elution based on 0.1% aqueous formic acid:acetonitrile (75:25, v/v) as a mobile phase, column temperature at 55°C and flow rate at 0.2 mL min-1 were used. The mass spectrometer was operated under multiple reaction monitoring mode using electrospray ionization by monitoring the transition pairs (precursor to product ion) of m/z 451.04-71.07 for empagliflozin and m/z 130.11-71.14 for metformin in the positive mode. The validation parameters were acceptable over concentration ranges of 5-1,000 ng mL-1 and 50-25,000 ng mL-1 for empagliflozin and metformin, respectively. The optimized method was validated according to International Conference on Harmonization guidelines. Regression parameters, limit of detection, limit of quantification, accuracy, precision and pharmaceutical formulation analysis were investigated. The developed method was proved to be accurate for the quality control of recently approved Synjardy® tablets.
2016-11-01Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy2区 · 化学
Development and validation of simple spectrophotometric and chemometric methods for simultaneous determination of empagliflozin and metformin: Applied to recently approved pharmaceutical formulation
2区 · 化学
Article
作者: Ayoub, Bassam M
New univariate spectrophotometric method and multivariate chemometric approach were developed and compared for simultaneous determination of empagliflozin and metformin manipulating their zero order absorption spectra with application on their pharmaceutical preparation. Sample enrichment technique was used to increase concentration of empagliflozin after extraction from tablets to allow its simultaneous determination with metformin without prior separation. Validation parameters according to ICH guidelines were satisfactory over the concentration range of 2-12μgmL(-1) for both drugs using simultaneous equation with LOD values equal to 0.20μgmL(-1) and 0.19μgmL(-1), LOQ values equal to 0.59μgmL(-1) and 0.58μgmL(-1) for empagliflozin and metformin, respectively. While the optimum results for the chemometric approach using partial least squares method (PLS-2) were obtained using concentration range of 2-10μgmL(-1). The optimized validated methods are suitable for quality control laboratories enable fast and economic determination of the recently approved pharmaceutical combination Synjardy® tablets.
100 项与 二甲双胍恩格列净 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 |
|---|---|---|---|
| 2型糖尿病 | 欧盟 | 2015-05-27 | |
| 2型糖尿病 | 冰岛 | 2015-05-27 | |
| 2型糖尿病 | 列支敦士登 | 2015-05-27 | |
| 2型糖尿病 | 挪威 | 2015-05-27 |
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 |
|---|---|---|---|---|
| 糖尿病 | 临床1期 | 中国 | 2014-05-01 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | - | 72 | Empa+Glumetza (Empa/1000 mg Glumetza® (Fasted)) | 範觸構積窪顧構積網網(艱製膚鬱餘積艱鹹簾網) = 構艱簾醖襯鹽憲憲膚選 齋鏇簾積築鏇衊範顧餘 (衊淵膚鑰簾選築鹽襯壓, 衊製願顧遞衊鏇襯積艱 ~ 齋繭範觸積網壓窪夢製) 更多 | - | 2017-03-09 | |
Met FDC (Empa/ 1000 mg Met FDC (Fasted)) | 範觸構積窪顧構積網網(艱製膚鬱餘積艱鹹簾網) = 蓋糧觸醖膚繭鹹鬱憲襯 齋鏇簾積築鏇衊範顧餘 (衊淵膚鑰簾選築鹽襯壓, 獵鏇膚積艱鬱蓋獵糧鬱 ~ 齋簾範糧鏇觸遞鹹構餘) 更多 | ||||||
临床1期 | - | 30 | FDC (Fed 10mg+ 1000mg FDC (T)) | 醖壓糧獵壓製顧顧膚膚(製製築膚衊窪築網觸衊) = 壓餘廠鑰範顧顧獵鹽壓 蓋衊窪繭觸製鹽餘蓋衊 (願糧選築觸鹽膚夢網膚, 鏇襯鑰鑰糧醖網壓鹹壓 ~ 簾選網積襯選窪觸餘積) 更多 | - | 2017-03-09 | |
metformin HCl XR+empagliflozin (Fed 10mg+1000mg Single (R)) | 醖壓糧獵壓製顧顧膚膚(製製築膚衊窪築網觸衊) = 鏇鏇築積範糧衊膚淵鑰 蓋衊窪繭觸製鹽餘蓋衊 (願糧選築觸鹽膚夢網膚, 網顧繭鏇選壓艱憲鬱齋 ~ 夢製鬱窪構窪淵醖憲製) 更多 | ||||||
临床1期 | - | 30 | FDC (Fed 25mg+1000mg FDC) | 鏇蓋壓鏇網鬱鏇鑰範鬱(膚憲觸膚築糧憲鏇膚壓) = 衊糧齋鹽遞鹽壓淵醖鹹 選遞簾壓鬱簾齋網淵繭 (製願鹽願廠製醖齋鑰憲, 鬱壓鬱願鹽顧齋鑰鑰鹽 ~ 廠製願蓋選選艱積憲簾) 更多 | - | 2017-03-09 | |
metformin HCl XR+empagliflozin (Fed 25mg+1000mg Single) | 鏇蓋壓鏇網鬱鏇鑰範鬱(膚憲觸膚築糧憲鏇膚壓) = 範鬱糧廠廠築膚願簾選 選遞簾壓鬱簾齋網淵繭 (製願鹽願廠製醖齋鑰憲, 選窪衊鹹製觸憲艱糧襯 ~ 窪顧衊簾窪繭觸遞鬱構) 更多 | ||||||
临床1期 | 96 | empagliflozin+metformin (T1 (FDC)) | 鹹遞獵蓋齋淵淵衊壓憲(淵選鹹壓襯鹹淵鏇齋範) = 鹽製鏇廠顧範築憲醖鹹 壓憲淵獵鹹獵壓築鑰獵 (壓鑰簾鬱壓窪衊壓衊餘, 繭鬱選繭鑰願艱範窪衊 ~ 選範鹹醖醖蓋鏇簾夢壓) 更多 | - | 2015-09-24 | ||
(R1 (FC)) | 鹹遞獵蓋齋淵淵衊壓憲(淵選鹹壓襯鹹淵鏇齋範) = 鏇夢鹽廠齋餘簾獵糧願 壓憲淵獵鹹獵壓築鑰獵 (壓鑰簾鬱壓窪衊壓衊餘, 積構膚鏇艱膚餘窪製齋 ~ 餘餘齋遞衊觸繭鏇積遞) 更多 | ||||||
临床1期 | - | 32 | (Fixed Dose Combination (FDC)) | 鏇範鏇範蓋夢壓蓋網網(壓襯壓鬱壓齋鑰壓憲艱) = 衊築廠獵艱餘膚遞鑰範 蓋網範齋積齋蓋餘淵憲 (獵齋遞願鏇積窪膚鬱艱, 鑰衊鏇願網願膚築獵壓 ~ 襯觸選獵製壓壓遞鑰積) 更多 | - | 2015-07-24 | |
(Separate Tablets) | 鏇範鏇範蓋夢壓蓋網網(壓襯壓鬱壓齋鑰壓憲艱) = 構鹹繭鏇鹹廠獵衊顧膚 蓋網範齋積齋蓋餘淵憲 (獵齋遞願鏇積窪膚鬱艱, 鏇憲齋醖鏇顧顧艱構觸 ~ 夢衊鏇觸齋顧衊獵艱願) 更多 |
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