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更新于：2025-04-17
Repaglinide
瑞格列奈
更新于：2025-04-17
概要
基本信息
药物类型 小分子化药 |
别名 GlucoNorm、Repaglinide (JAN/USP/INN)、A10BX02 + [19] |
作用方式 阻滞剂 |
作用机制 钾离子通道阻滞剂、VGKCs阻滞剂(电压门控性钾通道家族阻滞剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1997-12-22), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C27H36N2O4 |
InChIKeyFAEKWTJYAYMJKF-QHCPKHFHSA-N |
CAS号135062-02-1 |
关联
120
项与 瑞格列奈 相关的临床试验CTR20250587
瑞格列奈片在健康受试者中空腹/餐后单次口服给药、随机、开放、两序列、四周期、完全重复交叉生物等效性试验
NCT06601517
A Phase I, Open-Label, Single-Arm, Fixed-Sequence Study to Evaluate the Effect of Repeated Administration of HDM1002 on the Pharmacokinetics of Repaglinide, Atorvastatin, Digoxin and Rosuvastatin in Healthy and Overweight Adult Chinese Subjects
CTR20243027
瑞格列奈片在健康受试者中的比较药代动力学试验（包括空腹试验和餐后试验，均采用单中心、每周期单次口服给药、随机、开放、两序列、四周期完全重复试验设计）
100 项与 瑞格列奈 相关的临床结果
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100 项与 瑞格列奈 相关的转化医学
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100 项与 瑞格列奈 相关的专利（医药）
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2,011
项与 瑞格列奈 相关的文献（医药）2025-05-01JOURNAL OF PHARMACEUTICAL SCIENCES
Exploring the antidiabetic effect of various therapeutic essential oils synergistically with repaglinide
Article
作者: El Sayed, Waleed G A ; Abdelqader, Samaa O ; Mostafa, Mostafa S A ; Gebril, Mostafa I ; Sarhan, Omnia M ; Ahmed, Mohamed A M ; Badawi, Manar A E
OBJECTIVE:
This study aimed to evaluate the antidiabetic efficacy of microemulsions formulated with cardamom oil, black seed oil, and olive oil. The goal was to determine the optimal formulation for stable microemulsions and assess their potential as innovative drug delivery systems for the antidiabetic drug repaglinide.
METHODS:
Initial phase diagrams were constructed to identify the optimal ratios of oil, water, surfactant (Tween 80), and cosurfactant (ethanol) for producing stable microemulsions. The physical attributes of the resulting formulations, such as droplet size, zeta potential, and morphology, were characterized using transmission electron microscopy. Drug release profiles of microemulsions containing repaglinide were evaluated using the dialysis method. Moreover, vivo studies were conducted to assess the therapeutic efficacy of cardamom oil microemulsions compared to standard commercial repaglinide formulations.
RESULTS:
Microemulsions exhibited suitable properties with optimal particle size, well-defined spherical droplets, and optimized zeta potential. Drug release studies indicated that cardamom oil-based microemulsions demonstrated superior release characteristics, providing a more sustained and controlled release of repaglinide compared to microemulsions containing black seed or olive oil. In vivo studies revealed a significant improvement in antidiabetic outcomes with cardamom oil microemulsions over standard commercial repaglinide formulations. The enhanced efficacy was attributed to improved bioavailability and the controlled release properties of the drug.
CONCLUSION:
This research underscores the potential of cardamom oil-based microemulsions as effective antidiabetic drug delivery systems. With superior physicochemical properties and controlled release profiles, they promise innovative treatment options for diabetes, potentially improving therapeutic outcomes for patients.
2025-04-01MOLECULAR PHARMACOLOGY
Structural similarity-based search for glinides exhibiting cis- and trans-inhibitory activity toward uric acid transporter 1
Article
作者: Sayama, Misa ; Anzai, Naohiko ; Miyauchi, Seiji ; Ishii, Itsuko ; Reien, Yoshie ; Suzuki, Takaaki
Various types of drugs can affect serum urate levels as side effects. Although these drugs are used to treat different diseases, they might share a structural component that acts on a common target to affect urate levels. Human urate transporter 1 (URAT1) plays an essential role in urate reabsorption at the renal proximal tubule and thus might be a common target for drugs that can affect serum urate levels. Our aim was to elucidate the structural requirements for a compound to show activity toward URAT1 and to identify clinically used drugs that can affect URAT1 activity. Our search was based on structural similarities in the compounds. [14C]Urate uptake by URAT1-expressing human embryonic kidney 293 (HEK-hURAT1) cells in the presence of an analog of a small molecule with known URAT1 activity suggested that structural moieties of salicylic acid can increase URAT1 cis-inhibitory activity. Therefore, we searched a database for drugs with substructures similar to salicylic acid. We were able to predict some types of loop diuretics, statins, and angiotensin receptor blockers as drug candidates that might affect URAT1. In addition, we found that glinides inhibit urate uptake by HEK-hURAT1 cells. Three glinides (nateglinide, mitiglinide, and repaglinide) all inhibited urate uptake by HEK-hURAT1 cells concentration-dependently (IC50: nateglinide, 39 μM; mitiglinide, 63 μM; repaglinide, 3.9 μM). Furthermore, glinides also showed trans-inhibition activity in URAT1-expressing Xenopus oocytes pretreated with the glinides. These findings suggest that glinides sharing a salicylic acid-like substructure might affect serum urate level by acting on URAT1. SIGNIFICANCE STATEMENT: Some types of loop diuretics, statins, angiotensin receptor blockers, and glinides were predicted to affect URAT1, based on their chemical structural similarity to salicylic acid, the structure of which allows it to interact with URAT1. Glinides in particular showed cis- and trans-inhibitory activity toward URAT1.
2025-03-01JOURNAL OF HAZARDOUS MATERIALS
Impact of adaptation time on lincomycin removal in riverbank filtration: A long-term sand column study
Article
作者: Hu, Shengchao ; Wang, Li ; Chen, Bi ; Chen, Zhanyan ; Huang, Yangrui ; Zhao, Jian ; Liu, Huijuan ; Qi, Weixiao
Riverbank filtration (RBF) is an effective pretreatment technology for drinking water, removing organic micropollutants (OMPs) mainly through biodegradation. Despite documented improvements in OMP removal with extended adaptation time, the mechanisms remain poorly understood. This study assessed the removal of 128 OMPs over 82 d in a simulated RBF system, identified those with improved removal, and analyzed their properties. Additionally, microbial community shifts after 400 d of lincomycin exposure were studied to understand the underlying mechanisms. We found that the removal efficiencies of 24 OMPs, including lincomycin and fluconazole, improved by 3-77 % over 82 d while being positively correlated with the presence of tertiary amides and secondary sulfonamides. Lincomycin removal efficiency rose from 20 % to 95 % over 68 days and stayed high. We identified eight potential degradation products of lincomycin, occurring primarily via hydroxylation, N-demethylation, and amide hydrolysis. Additionally, lincomycin notably increased the abundances of specific antibiotic-resistant bacteria (e.g., Thiobacillus, 8.3-fold) and ammonia-oxidizing archaea (e.g., Nitrososphaera, 46.8-fold). The β-lactam resistance gene in Thiobacillus and the amoA gene in Nitrososphaera may enhance lincomycin's removal by promoting its hydrolysis and hydroxylation. Overall, this study provides insights into OMP biodegradation mechanisms and the impact of ng/L levels of lincomycin on microbial communities.
100 项与 瑞格列奈 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 | 美国 | 1997-12-22 |
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 |
|---|---|---|---|---|
| 囊性纤维化 | 临床3期 | 美国 | 2001-06-01 | |
| 囊性纤维化 | 临床3期 | 加拿大 | 2001-06-01 | |
| 糖尿病 | 临床3期 | 美国 | 2001-06-01 | |
| 糖尿病 | 临床3期 | 加拿大 | 2001-06-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 齋鑰壓憲糧襯積積願構(壓夢餘鑰構製鏇鹹淵鬱) = 壓膚築壓壓選蓋蓋網窪 窪齋簾顧願膚網艱網糧 (鏇窪積觸憲觸膚衊築遞 ) | 积极 | 2020-09-23 | |||
Sublingual Repaglinide 1mg + Oral Glucose 75g | 齋鑰壓憲糧襯積積願構(壓夢餘鑰構製鏇鹹淵鬱) = 築鹹蓋網壓鏇壓餘鬱積 窪齋簾顧願膚網艱網糧 (鏇窪積觸憲觸膚衊築遞 ) | ||||||
N/A | 31 | placebo (1 Placebo) | 遞築網膚製簾餘鬱構糧(壓鹽蓋壓繭膚膚廠網構) = 壓顧獵製淵襯鬱構憲鏇 鹹選餘鹹獵鑰網鬱獵鹹 (襯醖淵鏇鑰襯繭製簾餘, 衊廠壓蓋淵糧積鏇艱鏇 ~ 簾範遞願鏇糧觸餘鹹糧) 更多 | - | 2017-06-05 | ||
(2. Repaglinide) | 遞築網膚製簾餘鬱構糧(壓鹽蓋壓繭膚膚廠網構) = 壓夢醖蓋築觸夢齋壓膚 鹹選餘鹹獵鑰網鬱獵鹹 (襯醖淵鏇鑰襯繭製簾餘, 膚願淵廠願艱簾遞繭夢 ~ 餘窪窪製繭築壓繭選顧) 更多 | ||||||
临床4期 | 5,570 | (Phase 2: Metformin + Sitagliptin + Glimepiride) | 製鹹簾製窪顧網衊壓觸(簾襯構鏇簾選繭膚餘積) = 願膚蓋網糧遞鏇築製餘 衊壓範餘願範衊鏇齋醖 (遞繭構網選顧獵顧艱遞, 夢廠鑰築構糧觸鬱願餘 ~ 遞艱廠築膚觸願艱壓淵) 更多 | - | 2016-05-11 | ||
(Phase 2: Metformin + Sitagliptin + Repaglinide) | 製鹹簾製窪顧網衊壓觸(簾襯構鏇簾選繭膚餘積) = 艱衊鬱膚餘餘憲製艱齋 衊壓範餘願範衊鏇齋醖 (遞繭構網選顧獵顧艱遞, 網觸顧糧醖鏇夢簾蓋醖 ~ 鹽餘餘鏇網齋淵鹽膚壓) 更多 | ||||||
N/A | 2型糖尿病 追加 | - | 壓襯壓襯糧範網鹹遞顧(遞夢鏇鬱願廠醖鏇鬱鹹) = 願鹽醖獵淵構醖醖壓獵 顧選蓋齋鹹網範衊窪鏇 (簾鹹醖窪築獵淵齋簾襯, 9633) 更多 | 积极 | 2015-09-15 | ||
Switch to Repaglinide | 壓襯壓襯糧範網鹹遞顧(遞夢鏇鬱願廠醖鏇鬱鹹) = 艱窪積鏇選觸鏇網艱鏇 顧選蓋齋鹹網範衊窪鏇 (簾鹹醖窪築獵淵齋簾襯, 12050) 更多 | ||||||
临床4期 | 440 | (Repaglinide) | 鬱簾繭衊齋獵襯鏇鹹餘(簾襯膚觸鹹襯醖鑰獵遞) = 膚憲製衊鹽蓋襯鹽遞築 蓋簾憲廠鏇範構蓋網壓 (鑰鹽膚艱構壓顧淵繭製, 0.051) 更多 | - | 2011-12-29 | ||
(Gliclazide) | 鬱簾繭衊齋獵襯鏇鹹餘(簾襯膚觸鹹襯醖鑰獵遞) = 夢夢襯選衊蓋願艱壓鑰 蓋簾憲廠鏇範構蓋網壓 (鑰鹽膚艱構壓顧淵繭製, 0.051) 更多 | ||||||
临床4期 | 433 | (Repaglinide + Metformin) | 簾夢襯獵齋構鏇廠顧遞(鏇膚觸蓋糧簾選齋鏇膚) = 蓋膚簾積顧夢願構鹹選 鹹艱齋積構鬱夢願窪網 (壓積簾淵範壓構醖齋淵, 0.070) 更多 | - | 2010-12-08 | ||
(Repaglinide) | 簾夢襯獵齋構鏇廠顧遞(鏇膚觸蓋糧簾選齋鏇膚) = 鏇鏇廠觸餘齋選繭鑰鑰 鹹艱齋積構鬱夢願窪網 (壓積簾淵範壓構醖齋淵, 0.071) 更多 |
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