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更新于：2026-01-15
Repaglinide
瑞格列奈
更新于：2026-01-15
概要
基本信息
原研机构 |
权益机构- |
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
122
项与 瑞格列奈 相关的临床试验NCT07340190
A Phase 1b, Open Label, 2-Part Study to Evaluate the Effect of Pelabresib (DAK539/CPI-0610) on the Pharmacokinetics of Repaglinide, Midazolam, and Combined Drospirenone/Ethinyl Estradiol Oral Contraceptive in Patients With Advanced Malignancies
NCT07235748
A Phase 1, Open-label, Single-sequence, 2-period Study to Evaluate the Effect of Multiple Doses of Vorasidenib on the Pharmacokinetics of a Single Dose of Sensitive Index Substrates of Cytochrome P450 2B6, 2C8, 2C9, 2C19, 3A4, and Breast Cancer Resistance Protein in Healthy Adult Participants
NCT07065058
A Phase I, Single-Center, Open-Label, Single-Arm, Fixed-Sequence Clinical Study to Evaluate the Pharmacokinetic Interactions of VCT220 With Repaglinide, Rosuvastatin, and Digoxin in Healthy, Overweight, and Obese Subjects
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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1,334
项与 瑞格列奈 相关的文献（医药）2025-12-01International Journal of Pharmaceutics-X
Optimized buccoadhesive repaglinide-loaded cubogel: In-vitro characterization and in-vivo hypoglycemic activity in a streptozotocin-induced diabetic rat model
Article
作者: Badawi, Alia ; Younes, Nihal Farid ; Latif, Randa ; Hegazy, Khaled
The limited bioavailability of orally administered repaglinide presents a significant challenge in diabetes management, which can be addressed by developing a buccoadhesive drug delivery system. In this study, repaglinide-loaded cubosomes were prepared using a top-down approach and optimized via a 33 Box-Behnken design. The optimized formulation (Opt-RPG-CUB) was characterized for solubilization efficiency (SE%), particle size (PS), zeta potential (ZP), drug release kinetics, and morphology. To further enhance drug delivery, a 22 factorial design was utilized to incorporate varying concentrations of the gelling agents hydroxypropyl methylcellulose or carboxymethyl cellulose into Opt-RPG-CUB, forming repaglinide-loaded cubogels. Upon optimization, the cubogel with the highest desirability function, designated as Opt-RPG-Cubogel, was further evaluated for mucoadhesion, drug release kinetics, rheological properties, ex-vivo buccal permeation, and in-vivo drug permeation by confocal laser scanning microscopy and pharmacodynamic assessment in a streptozotocin-induced diabetic rat model. Results showed that Opt-RPG-CUB exhibited a SE% of 88.01 ± 3.92 %, PS of 252.55 ± 17.18 nm, and ZP of -31.13 ± 1.42 mV, with an extended drug release over 24 h and a cubic nanostructure. Opt-RPG-Cubogel exhibited strong mucoadhesion (>9 h), an extended drug release over 24 h, enhanced mucosal permeation, and improved tissue deposition. Confocal microscopy further confirmed deep mucosal penetration, while in-vivo studies demonstrated a significant reduction in blood glucose levels compared to the control. Overall, these findings highlight the potential of Opt-RPG-Cubogel as a promising buccoadhesive drug delivery system for efficient type II diabetes management.
2025-12-01Alzheimers & Dementia
Effect of diabetes medications on the risk of developing dementia, mild cognitive impairment, or cognitive decline: a systematic review and meta‐analysis
Review
作者: Mukadam, Naheed ; Hui, Esther K ; Kohl, Gianna ; Livingston, Gill
Abstract:
Background:
Diabetes is a risk factor for dementia, but we do not know whether specific diabetes medications ameliorate this risk. Objective: To systematically review and meta‐analyze such medication's effect on the risk of developing dementia, mild cognitive impairment (MCI), or cognitive decline.
Method:
We searched three databases until 21.11.23. We included randomized controlled trials (RCT), cohort, and case‐control studies assessing association between antidiabetic medication and future dementia, MCI, or cognitive decline. We meta‐analyzed studies separately for individual drug classes and their comparators (no medication, placebo, or another drug). We appraised study quality using the Newcastle‐Ottawa Scale and Physiotherapy Evidence Database Scale.
Result:
42 studies fulfilled inclusion criteria. Glucagon‐like peptide‐1 receptor agonists (GLP‐1 RA) versus placebo reduced dementia risk by 53% in 3 RCTs (
n
= 15,820, RR=0.47[0.25,0.86]) and 27% in 3 case‐control studies (
n
= 312,856, RR=0.73[0.54,0.99], I
2
=96%). Repaglinide was superior to glibenclamide by 0.8 points on the Mini‐Mental State Examination scale in another RCT. Meta‐analysis of 7 longitudinal studies showed glitazones (
n
= 1,081,519, RR=0.78[0.76,0.81], I
2
=0%) were associated with reduced dementia risk. Metformin (
n
= 999,349, RR=0.94[0.79,1.13], I
2
=98.4%), sulfonylureas (RR=0.98[0.78,1.22], I
2
=83.3%), dipeptidyl peptidase‐IV inhibitors (DPP‐1V) (
n
= 192,802, RR=0.86[0.65,1.15], I
2
=92.9%) and insulin (
n
= 571,274, RR=1.09[0.95,1.25], I
2
=94.8%) were not. Most studies were observational and limited by confounding by indication.
Conclusion:
In people with diabetes, RCTs consistently showed GLP‐RAs reduce future dementia risk. Glitazones consistently showed protective effects, without heterogeneity, suggesting potential generalizability of these results. Metformin, sulfonylureas, insulin, and DPP‐1V studies had inconsistent findings. If information is available future studies should consider dosage, severity, and duration.
2025-12-01DRUG METABOLISM AND DISPOSITION
Corrigendum to “Human cytochrome P4502C8 metabolizes repaglinide to 4′-hydroxyrepaglinide, not 3′-hydroxyrepaglinide” [Drug Metabolism and Disposition 53 (2025) 100177]
作者: Doran, Angela C ; Walker, Gregory S ; Balesano, Amanda ; Obach, R Scott ; Sharma, Raman
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 | |
| 高血糖 | 临床2期 | 加拿大 | 2003-11-01 | |
| 囊性纤维化相关糖尿病 | 临床阶段不明 | 美国 | 2006-11-01 | |
| 胰腺外分泌功能不全 | 临床阶段不明 | 美国 | 2006-11-01 | |
| 糖尿病前期 | 临床阶段不明 | 美国 | 2006-11-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 31 | placebo (1 Placebo) | 艱窪壓構觸網鏇鹽餘鹹(壓膚積製積窪壓醖遞積) = 餘鬱糧構鹽襯構顧願鹹 糧鬱鑰艱鏇糧積襯鑰壓 (鹹選壓鬱壓築選築齋鹹, 築觸蓋網繭醖範鹹製膚 ~ 壓餘簾網窪鑰遞鹹選鹹) 更多 | - | 2017-06-05 | ||
(2. Repaglinide) | 艱窪壓構觸網鏇鹽餘鹹(壓膚積製積窪壓醖遞積) = 鹹顧遞憲醖繭鑰襯鏇網 糧鬱鑰艱鏇糧積襯鑰壓 (鹹選壓鬱壓築選築齋鹹, 鑰築艱齋網繭壓築壓鏇 ~ 膚範廠鬱觸鏇憲鑰鬱遞) 更多 | ||||||
临床4期 | 5,570 | (Phase 2: Metformin + Sitagliptin + Glimepiride) | 蓋顧餘積構鹽築網鹽襯(製齋淵淵襯憲膚餘醖顧) = 壓構齋鏇壓鹽襯願網網 鹽鹽襯積衊廠鹹夢窪夢 (鹹鬱糧衊築構獵鑰鏇選, 餘糧觸獵齋憲齋壓齋壓 ~ 獵遞鹹襯糧衊憲遞蓋襯) 更多 | - | 2016-05-11 | ||
(Phase 2: Metformin + Sitagliptin + Repaglinide) | 蓋顧餘積構鹽築網鹽襯(製齋淵淵襯憲膚餘醖顧) = 遞鏇鑰構壓蓋膚襯構製 鹽鹽襯積衊廠鹹夢窪夢 (鹹鬱糧衊築構獵鑰鏇選, 艱壓積遞遞壓觸醖製構 ~ 憲遞顧獵壓壓蓋選顧鑰) 更多 | ||||||
临床4期 | 440 | (Repaglinide) | 醖壓襯餘淵鏇鏇觸襯壓(壓廠獵觸鏇觸簾襯鹽簾) = 選衊觸鬱廠憲襯選構製 淵顧顧餘繭齋淵餘選醖 (鏇遞鏇鏇淵構選憲築窪, 0.051) 更多 | - | 2011-12-29 | ||
(Gliclazide) | 醖壓襯餘淵鏇鏇觸襯壓(壓廠獵觸鏇觸簾襯鹽簾) = 蓋襯壓構襯繭簾廠淵鏇 淵顧顧餘繭齋淵餘選醖 (鏇遞鏇鏇淵構選憲築窪, 0.051) 更多 | ||||||
临床4期 | 433 | (Repaglinide + Metformin) | 繭窪淵壓遞築鬱選廠蓋(鹹憲壓構構遞衊壓繭餘) = 窪簾鹽蓋艱築顧構蓋憲 構鑰襯範醖鏇觸壓築艱 (築範積顧構遞衊壓蓋鹽, 0.070) 更多 | - | 2010-12-08 | ||
(Repaglinide) | 繭窪淵壓遞築鬱選廠蓋(鹹憲壓構構遞衊壓繭餘) = 範蓋製鏇構蓋醖蓋顧鹹 構鑰襯範醖鏇觸壓築艱 (築範積顧構遞衊壓蓋鹽, 0.071) 更多 | ||||||
临床4期 | 459 | Insulin plus metformin | 餘淵鑰獵壓餘鏇遞窪窪(願糧鏇憲壓淵鏇遞鬱願) = 築繭醖襯製顧簾網壓鏇 積網廠願範獵餘鏇鏇鹽 (鑰願壓憲鏇糧齋顧繭淵, (1.32)) | - | 2009-11-09 | ||
Insulin plus repaglinide | 餘淵鑰獵壓餘鏇遞窪窪(願糧鏇憲壓淵鏇遞鬱願) = 製夢衊醖顧繭衊簾齋顧 積網廠願範獵餘鏇鏇鹽 (鑰願壓憲鏇糧齋顧繭淵, (0.66)) |
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