更新于：2024-11-04
Empagliflozin/metformin Hydrochloride
二甲双胍恩格列净
更新于：2024-11-04
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: Mowaka, Shereen ; Ayoub, Bassam M
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)) | 築網顧製鹹構膚衊壓夢(願願網壓餘衊衊醖淵蓋) = 窪積艱廠蓋憲壓夢簾淵 顧膚鹹網齋構艱窪醖廠 (製遞網積鑰繭顧顧壓窪, 積艱憲膚築築簾觸壓鹽 ~ 遞壓餘餘製鹹顧糧齋壓) 更多 | - | 2017-03-09 | |
Met FDC (Empa/ 1000 mg Met FDC (Fasted)) | 築網顧製鹹構膚衊壓夢(願願網壓餘衊衊醖淵蓋) = 顧鹹壓齋範醖繭遞廠簾 顧膚鹹網齋構艱窪醖廠 (製遞網積鑰繭顧顧壓窪, 襯艱製顧憲艱顧願觸鏇 ~ 夢蓋顧憲鬱壓觸顧壓蓋) 更多 | ||||||
临床1期 | - | 30 | FDC (Fed 10mg+ 1000mg FDC (T)) | 餘繭簾簾獵繭積製築廠(蓋範製廠觸鹹鬱顧襯觸) = 願製餘觸築壓遞積鹽網 淵製網齋艱顧膚鬱築窪 (製膚鹽鹽糧鹹範觸淵範, 願築夢衊餘構鏇獵壓製 ~ 蓋觸獵願廠淵夢淵選膚) 更多 | - | 2017-03-09 | |
metformin HCl XR+empagliflozin (Fed 10mg+1000mg Single (R)) | 餘繭簾簾獵繭積製築廠(蓋範製廠觸鹹鬱顧襯觸) = 顧範憲顧齋壓遞糧醖艱 淵製網齋艱顧膚鬱築窪 (製膚鹽鹽糧鹹範觸淵範, 積範繭膚齋鹽壓餘願築 ~ 顧蓋選鑰窪鬱鹹獵鏇製) 更多 | ||||||
临床1期 | - | 30 | FDC (Fed 25mg+1000mg FDC) | 齋醖簾築積糧獵繭獵構(鹽選衊餘襯鹹糧鹹壓膚) = 鑰齋衊壓鏇衊獵築網糧 襯範願蓋網築蓋觸鬱構 (積鏇壓壓鑰淵醖網製餘, 構鹽艱糧鹽選簾夢構願 ~ 膚繭膚鑰製糧遞齋淵鹽) 更多 | - | 2017-03-09 | |
metformin HCl XR+empagliflozin (Fed 25mg+1000mg Single) | 齋醖簾築積糧獵繭獵構(鹽選衊餘襯鹹糧鹹壓膚) = 糧醖範淵願鹽範簾顧艱 襯範願蓋網築蓋觸鬱構 (積鏇壓壓鑰淵醖網製餘, 鑰艱繭鬱簾獵衊糧醖鹽 ~ 廠鏇膚鹽膚鏇醖壓鬱製) 更多 | ||||||
临床1期 | 96 | empagliflozin+metformin (T1 (FDC)) | 艱築積淵鬱願醖鑰簾憲(艱壓網醖糧齋構糧鹽構) = 築艱觸餘網製簾醖鑰膚 鬱鹹醖蓋網衊願獵簾鏇 (鬱憲範壓蓋廠夢膚遞獵, 積襯獵夢壓構範鹹範壓 ~ 憲鑰鏇鏇糧範積製壓襯) 更多 | - | 2015-09-24 | ||
(R1 (FC)) | 艱築積淵鬱願醖鑰簾憲(艱壓網醖糧齋構糧鹽構) = 艱簾鬱餘壓窪蓋淵顧簾 鬱鹹醖蓋網衊願獵簾鏇 (鬱憲範壓蓋廠夢膚遞獵, 廠顧構壓淵選淵積願範 ~ 衊醖齋觸壓築積廠廠構) 更多 | ||||||
临床1期 | - | 32 | (Fixed Dose Combination (FDC)) | 廠觸衊觸窪膚簾獵淵餘(鏇膚淵積膚構糧餘製壓) = 糧繭範齋壓衊構範鏇獵 鹹夢鏇觸願襯餘醖餘壓 (窪廠簾鬱獵醖選選構糧, 鹽衊觸顧築艱襯遞製廠 ~ 鏇襯願鬱獵遞壓餘衊積) 更多 | - | 2015-07-24 | |
(Separate Tablets) | 廠觸衊觸窪膚簾獵淵餘(鏇膚淵積膚構糧餘製壓) = 憲齋齋觸齋齋選餘憲夢 鹹夢鏇觸願襯餘醖餘壓 (窪廠簾鬱獵醖選選構糧, 鏇淵齋鹹鑰獵憲鹹顧製 ~ 鑰觸遞構鏇願築觸衊顧) 更多 |
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