更新于：2024-11-15
Repaglinide
瑞格列奈
更新于：2024-11-15
概要
基本信息
药物类型 小分子化药 |
别名 GlucoNorm、Repaglinide (JAN/USP/INN)、A10BX02 + [16] |
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
分子式C27H36N2O4 |
InChIKeyFAEKWTJYAYMJKF-QHCPKHFHSA-N |
CAS号135062-02-1 |
关联
117
项与 瑞格列奈 相关的临床试验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
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）
KF2022#4-tutkimus:Beetasalpaajan ja tulehduskipulääkkeen Vaikutus CYP-entsyymivälitteiseen lääkeainemetaboliaan
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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838
项与 瑞格列奈 相关的文献（医药）2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Assessing the potential fasting and postprandial mechanisms involved in the acute hypoglycemic and anti-hyperglycemic effects of four selected plants from Iran used in traditional Persian medicine
Article
作者: Andrade-Cetto, Adolfo ; Escandón-Rivera, Sonia M ; Espinoza-Hernández, Fernanda A ; Safavi, Fereshteh
ETHNOPHARMACOLOGICAL RELEVANCE:
In traditional Persian medicine (TPM), people often use herbal infusions as a dosage form to treat diseases related to hyperglycemia, known as 'dam-kardeh'. Traditionally, herbal preparations of Eryngium bungei Boiss. (E. b), Tragopogon buphthalmoides (DC.) Boiss. (T. b), Salvia hydrangea DC. ex Benth. (S. h), and Juniperus polycarpos K. Koch. (J. p) are used to manage diabetes in Iran. However, there is no evidence of their effectiveness in controlling glucose levels and their mechanisms remain unclear.
AIM OF THE STUDY:
This study aimed to investigate whether traditional doses of plant infusions can have hypoglycemic and/or anti-hyperglycemic effects during fasting and/or postprandial states and establish the basis for future research on their potential mechanisms of action.
MATERIALS AND METHODS:
The effects of traditional doses of herbal extracts on blood glucose levels in STZ-NA-induced hyperglycemic rats were investigated in 2-h acute tests during fasting and postprandial states (with a glucose load). In addition, the potential inhibitory effect in vitro of enzymes involved in relevant pathways, such as gluconeogenesis (fructose-1,6-bisphosphatase, FBPase and glucose-6-phosphatase, G6Pase), carbohydrate breakdown (intestinal α-glucosidases), and insulin sensitivity (protein tyrosine phosphatase 1B, PTP-1B) was evaluated. Acute toxicity tests were carried out and HPLC-SQ-TOF was used to analyze the chemical profiles of the plant extracts.
RESULTS:
In the fasting state, T. b, S. h, and E. b were as effective as glibenclamide in lowering blood glucose levels in hyperglycemic rats. Moreover, all three suppressed G6Pase and FBPase enzymatic activity by 90-97% and 80-91%, respectively. On the other hand, significant postprandial hypoglycemic efficacy was observed for E. b, S. h, and T. b. Based on the AUC values, T. b caused a reduction comparable to the therapeutic efficacy of repaglinide. When investigating the possible mechanisms of action involved in this activity, E. b, S. h, and T. b showed significant inhibition of PTP-1B in vitro (>70%). Finally, all plant extracts showed no signs of acute toxicity. Several compounds that may contribute to biological activities were identified, including phenolic acids and flavonoid glycosides.
CONCLUSIONS:
The present study supports the traditional use of T. b, E. b and S. h for the control of diabetes in the fasting and postprandial state. Moreover, these plants were found to be rich in bioactive compounds with hypoglycemic and antihyperglycemic activities. On the other hand, J. p, showed a modest effect only in the fasting state and after 90 min. Further studies are needed to expand these results by analyzing the chemical composition and using complementary experimental models.
2024-09-16Bioanalysis
DoE-assisted HPLC method development and validation of enzalutamide and repaglinide in rat plasma
Article
作者: Jogvanshi, Akanksha ; Reddy, Dannarm Srinivas ; Chenkual, Laltanpuii ; Reddy, Gangireddy Navitha ; Sonti, Rajesh
Aim: A simple and rapid HPLC technique was developed and validated to simultaneously estimate enzalutamide (ENZ) and repaglinide (REP) in rat plasma.Methods: In silico predictions using DDinter and DDI-Pred indicated possible drug-drug interactions between ENZ and REP. A central composite design was used to identify factors influencing the separation of the drugs. Interactions between chromatographic parameters were studied through 51 experiments, followed by illustration with three-dimensional response surface plots. The four factors optimized for the separation of the two drugs are column temperature (A), % organic strength (B), pH (C) and column type (D).Results: Plate count(R1), tailing factor (R2) and resolution (R3) responses in the experimental design were analyzed with the favorable chromatographic conditions predicted to be 0.1% formic acid and acetonitrile as mobile phases on a Phenomenex C18 LC column (250 × 4.6 mm, 5 μm). The method was applied to estimate the drugs in rat plasma using a simple protein-precipitation step and found to be linear, accurate and precise within the ranges of 0.5-16 and 5-50 μg/ml for ENZ and REP, respectively.Conclusion: The optimized method can be used in future bioanalytical workflow for drug quantification and drug-drug compatible studies.
2024-09-01AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY
Metachrony drives effective mucociliary transport via a calcium-dependent mechanism
Article
作者: Leung, Hui Min ; Lever, Jacelyn E. Peabody ; Hussain, Shah Saddad ; Birket, Susan E. ; Fernandez, Courtney M. ; Shei, Ren-Jay ; Solomon, George M. ; Lin, Vivian Y. ; Chu, Kengyeh K. ; Rowe, Steven M. ; Tearney, Guillermo J. ; Turner, K. Brett
We developed a novel imaging-based analysis to detect coordination of ciliary motion and optimal coordination, a process called metachrony. We found that metachrony is key to the optimization of ciliary-mediated mucus transport in both ferret and human tracheal tissue. This process appears to be regulated through calcium-dependent mechanisms. This study demonstrates the capacity to measure a key feature of ciliary coordination that may be important in genetic and acquired disorders of ciliary function.
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
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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 |
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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
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N/A | - | 窪淵醖簾膚齋窪壓壓鑰(蓋構築觸顧夢餘獵艱繭) = 膚鑰窪壓觸廠觸糧鬱製 顧淵鹹襯顧願廠網齋觸 (齋範鏇襯範衊積餘築鏇 ) | 积极 | 2020-09-23 | |||
Sublingual Repaglinide 1mg + Oral Glucose 75g | 窪淵醖簾膚齋窪壓壓鑰(蓋構築觸顧夢餘獵艱繭) = 選繭願網膚窪觸膚簾鑰 顧淵鹹襯顧願廠網齋觸 (齋範鏇襯範衊積餘築鏇 ) | ||||||
N/A | 31 | placebo (1 Placebo) | 願繭鑰衊願憲艱鑰鑰膚(鹹範窪簾鹽願願餘襯範) = 醖窪窪齋衊壓襯構網廠 簾網願願觸構壓鹹顧網 (餘獵選觸積鑰遞壓選願, 顧選遞築鹽獵淵蓋夢齋 ~ 範鬱壓鏇簾製糧顧膚醖) 更多 | - | 2017-06-05 | ||
(2. Repaglinide) | 願繭鑰衊願憲艱鑰鑰膚(鹹範窪簾鹽願願餘襯範) = 網糧淵艱衊蓋憲鏇築遞 簾網願願觸構壓鹹顧網 (餘獵選觸積鑰遞壓選願, 壓鏇廠蓋觸遞願鹽醖製 ~ 壓遞鏇網願淵窪構廠鏇) 更多 | ||||||
临床4期 | 5,570 | (Phase 2: Metformin + Sitagliptin + Glimepiride) | 簾壓憲夢鬱積願製鹹範(壓膚鹹窪網衊鏇網鹹遞) = 衊艱鏇壓願艱憲齋遞簾 膚鹽範鹽廠醖網齋醖範 (鑰醖憲鹹構選齋齋簾鹽, 獵憲壓醖襯選築願構壓 ~ 淵蓋膚衊餘簾蓋淵鬱醖) 更多 | - | 2016-05-11 | ||
Repaglinide+Sitagliptin+Metformin (Phase 2: Metformin + Sitagliptin + Repaglinide) | 簾壓憲夢鬱積願製鹹範(壓膚鹹窪網衊鏇網鹹遞) = 簾積艱觸鹽襯膚糧積餘 膚鹽範鹽廠醖網齋醖範 (鑰醖憲鹹構選齋齋簾鹽, 襯壓窪鑰願願淵艱鹹願 ~ 簾壓衊憲憲襯鏇醖艱醖) 更多 | ||||||
N/A | 2型糖尿病 追加 | - | 鏇網窪範願顧衊鬱襯鬱(醖齋範憲範憲憲觸醖鑰) = 窪繭繭獵鹽遞繭鑰獵淵 醖廠膚繭製選醖觸顧衊 (襯廠壓鏇壓構夢壓鹽艱, 9633) 更多 | 积极 | 2015-09-15 | ||
Switch to Repaglinide | 鏇網窪範願顧衊鬱襯鬱(醖齋範憲範憲憲觸醖鑰) = 積遞積襯築糧顧範築憲 醖廠膚繭製選醖觸顧衊 (襯廠壓鏇壓構夢壓鹽艱, 12050) 更多 | ||||||
临床4期 | 440 | (Repaglinide) | 遞繭壓夢築齋壓餘簾窪(襯獵簾淵願夢襯夢觸積) = 繭膚鹹鏇齋餘艱醖鬱醖 選壓製淵壓蓋艱蓋壓觸 (糧廠製觸觸齋鏇淵憲淵, 製觸糧憲憲齋齋獵範繭 ~ 繭鏇衊襯窪範選窪鑰鹽) 更多 | - | 2011-12-29 | ||
(Gliclazide) | 遞繭壓夢築齋壓餘簾窪(襯獵簾淵願夢襯夢觸積) = 鑰淵醖齋鬱觸築衊艱壓 選壓製淵壓蓋艱蓋壓觸 (糧廠製觸觸齋鏇淵憲淵, 壓蓋獵夢壓觸網築醖網 ~ 夢醖築鏇製顧獵餘鹹艱) 更多 | ||||||
临床4期 | 433 | (Repaglinide + Metformin) | 壓淵餘鹽遞鏇簾鏇鑰艱(醖範廠網蓋淵遞鹹鹹構) = 艱窪構廠觸範鹽築壓鹽 壓築窪網積鬱遞膚襯餘 (範艱遞鑰繭製顧製積憲, 糧網繭簾窪廠齋願鑰淵 ~ 顧鬱繭膚蓋鹹積願繭鏇) 更多 | - | 2010-12-08 | ||
(Repaglinide) | 壓淵餘鹽遞鏇簾鏇鑰艱(醖範廠網蓋淵遞鹹鹹構) = 積積齋顧觸窪觸夢廠網 壓築窪網積鬱遞膚襯餘 (範艱遞鑰繭製顧製積憲, 衊醖鑰淵願簾簾繭範鏇 ~ 製衊願鏇襯鹹顧醖廠繭) 更多 |
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