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更新于：2025-03-25
Nateglinide
那格列奈
更新于：2025-03-25
概要
基本信息
药物类型 小分子化药 |
别名 Fastic、Glinate、Nageglinide + [38] |
作用方式 拮抗剂、抑制剂 |
作用机制 PPARγ拮抗剂(过氧化物酶体增长因子活化受体γ拮抗剂)、SUR1抑制剂(磺酰脲类受体1抑制剂) |
治疗领域 |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 日本 (1999-06-16), |
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C19H27NO3 |
InChIKeyOELFLUMRDSZNSF-BRWVUGGUSA-N |
CAS号105816-04-4 |
关联
34
项与 那格列奈 相关的临床试验CTR20190942
那格列奈片在健康男性和女性受试者中于餐后情况下进行的单剂量、随机、开放性、 交叉的生物等效性研究。
CTR20181442
单中心、随机开放、双周期双交叉设计评价中国健康受试者单次空腹及餐后口服那格列奈片的人体生物等效性试验
CTR20180642
那格列奈片在健康受试者中的单剂量、随机、开放性、交叉、正式、空腹及餐后生物等效性研究
100 项与 那格列奈 相关的临床结果
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100 项与 那格列奈 相关的转化医学
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100 项与 那格列奈 相关的专利（医药）
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1,258
项与 那格列奈 相关的文献（医药）2025-03-01ANALYTICAL SCIENCES
Microwave-derivatized enhanced-spectrofluorophotometric characterization of nateglinide-loaded solid dispersion adsorbate and greenness profile assessment of method
Article
作者: Prajapati, Pintu ; Shah, Shailesh ; Haque, Anzarul ; Kalam, Mohd Abul
Nateglinide is an oral meglitinide that treats diabetes. Nateglinide was determined in several commercial formulations using chromatographic and spectrophotometric methods in published research. Quality-by-design approach was applied to develop the in-house nateglinide-loaded Solid Dispersion Adsorbate (SDA) for improving bioavailability and solubility. To determine nanogram-level nateglinide concentration for the in-house developed nateglinide-SDA pharmacokinetics required time-consuming and expensive hyphenated analytical techniques such as LC-MS or UPLC-MS. Hence, a sensitive spectrofluorophotometric method was developed to estimate nateglinide using NBD-Cl (7-chloro-4-nitrobenzoxadiazole) as the fluorophore. Microwave-aided chemical derivatization of nateglinide with NBD-Cl sped up sample analysis. Chemical reaction solvents were eco-friendly to safeguard aquatic life and environment. The chemical process was optimized by quality by design approach using screening design and response surface modelling. The fluorescence intensity of nateglinide was found to be linear over the concentration range of 20-250 ng/mL with a correlation coefficient of 0.9978. The limits of detection and quantification were found to be 10 and 20 ng/mL respectively. Precision and robustness investigations of the spectrofluorimetric method showed less than 2% relative standard deviations. Nateglinide-SDA drug-release study and pharmacokinetics were performed using the sensitive spectrofluorophotometric method. The in-house developed nateglinide-SDA released 95% of the drug in 30 min time duration. In-house-developed nateglinide-SDA has 1.5 times the oral bioavailability of commercial formulations due to in-vivo absorption. The published analytical methods were compared to the enhanced-spectrofluorophotometric method for user-friendliness, efficiency, cost-of-analysis, and environmental friendliness. The proposed sensitive-spectrofluorophotometric method was found to be robust, rapid, eco-friendly, cost-effective, and simple for the estimation of nateglinide.
2025-02-17Critical reviews in analytical chemistry
Resolving D-Amino Acid Containing Peptides Using Ion Mobility-Mass Spectrometry: Challenges and Recent Developments
Review
作者: Di, Bin ; Li, Bo ; Abdulbagi, Mohamed
Peptides and proteins having D-amino acids in their sequences are now believed to be widespread among different living organisms. Their significance is attributed to the diverse functions of these molecules, such as having a certain pathological implication or enhancing biological activity. Indeed, some peptide molecules with D-amino acids in their structure have already found their way to clinical use such as the antibacterial gramicidin and the antidiabetic nateglinide. Ion mobility mass spectrometry (IM-MS) added an additional dimension of separation as it depends on ions mobility in the space, which is dependent on their shapes, and the shape depends on the orientation of atoms. Thus, D-amino acids containing peptides (DAACPs) will have different mobility and collision cross-section values than those with L-amino acids. Eventually, this will lead to baseline separation of the two peptides. Additionally, ion mobility can precisely locate the position of D-amino acids by analyzing the difference in the arrival times of the fragment ions. The importance of DAACPs, as well as the difficulties in discovering them, were addressed in this review. Similarly, we emphasized how recent developments in IM-MS have improved their detection and analysis. Consequently, the LC-IM-MS/MS platform appears to be promising in isomeric mixture analysis.
2025-02-01POULTRY SCIENCE
Microbiome and metabolome reveal beneficial effects of baicalin on broiler growth performance and intestinal health
Article
作者: Guo, Yuming ; Lv, Zengpeng ; Nie, Wei ; Lv, Huiyuan ; Ji, Yunru ; Liu, Xingbo
Normal function and health of the intestinal tract were necessary for the growth and development of broilers. Baicalin (BA) possessed a variety of biological activities. The objective of this study was to examine the impact of BA on the growth performance, intestinal barrier function, intestinal microbiota, and mucosal metabolism in broilers. A total of 720 21-day-old broilers were randomly allocated into 3 groups and fed with either basal diet (Con group) or basal diet supplemented with 6 or 12 mg/kg baicalin (BA6 and BA12 groups) for a continuous feeding period of 40 days. Results showed that BA had a trend towards improving (P = 0.086) the 60-day body weight of broilers, and the BA12 group exhibited significantly higher (P < 0.05) average daily gain from day 39 to 60 compared to the Con group. Additionally, in the BA12 group, the ratio of villus height to crypt depth and the expression levels of tight junction protein-related genes significantly increased (P < 0.05), while intestinal permeability significantly decreased (P < 0.05). Supplementation with 12 mg/kg BA significantly enhanced antioxidant capacity, promoted (P < 0.05) crypt proliferation, increased (P < 0.05) immunoglobulin levels, upregulated (P < 0.05) IL-2 and IL-8 mRNA levels, and downregulated (P < 0.05) IL-4 and TGF-β2 mRNA levels. Metabolomics analysis revealed that BA improved the metabolic characteristics of intestinal mucosa, significantly upregulating pathways associated with ascorbate and aldarate metabolism, glyoxylate and dicarboxylate metabolism, phosphatidylinositol signaling system, alpha-linolenic acid metabolism, and galactose metabolism. 16S rRNA sequencing results indicated that BA increased the richness of intestinal microbiota community and the relative abundance of Actinobacteria phylum, while reducing the relative abundance of contains mobile elements, potentially pathogenic, and facultatively anaerobic. Overall, 12 mg/kg BA improved intestinal health by modulating intestinal barrier function, antioxidant capacity, immunity, intestinal microbiota, and intestinal mucosal metabolism levels, ultimately enhancing broiler growth performance.
100 项与 那格列奈 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 | 日本 | 1999-06-16 | |
| 2型糖尿病 | 日本 | 1999-06-16 |
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 |
|---|---|---|---|---|
| 非胰岛素依赖型糖尿病2 | 临床3期 | 日本 | 2005-09-19 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 日本 | 2005-09-19 | |
| 葡萄糖耐受不良 | 临床3期 | 美国 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 中国 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 阿根廷 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 澳大利亚 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 奥地利 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 比利时 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 巴西 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 加拿大 | 2002-01-01 |
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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4期 | 88 | (Nateglinide) | 窪廠構獵鑰顧製積艱膚 = 網簾積積艱選壓鹽築襯 淵築簾鬱淵獵齋範網廠 (製簾壓鑰觸艱餘選夢製, 願夢齋鑰糧衊願鑰製艱 ~ 窪蓋構鏇鏇顧衊顧壓廠) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 窪廠構獵鑰顧製積艱膚 = 蓋廠選壓築壓齋構願夢 淵築簾鬱淵獵齋範網廠 (製簾壓鑰觸艱餘選夢製, 窪衊憲鏇鏇積觸觸顧鬱 ~ 觸構憲願壓窪簾築鹹鹽) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 憲蓋鹹壓製壓夢壓壓淵(範廠鹽壓糧製顧築鏇鏇) = 鹽顧糧簾構選繭製鏇齋 淵鏇蓋淵簾醖糧積襯構 (積繭襯餘窪夢網衊範餘, 遞顧憲選廠齋壓壓鏇醖 ~ 襯鑰餘選網觸醖鑰鬱製) 更多 | - | 2012-10-19 | ||
(Acarbose) | 憲蓋鹹壓製壓夢壓壓淵(範廠鹽壓糧製顧築鏇鏇) = 觸艱糧鑰觸築餘齋齋築 淵鏇蓋淵簾醖糧積襯構 (積繭襯餘窪夢網衊範餘, 襯繭夢衊醖鹹膚簾選壓 ~ 餘餘鬱遞顧夢築廠鑰蓋) 更多 | ||||||
N/A | - | 糧膚憲夢窪鹽觸簾觸觸(艱繭願製繭壓鹹窪築醖) = three episodes of mild hypoglycemia in the C group. These symptoms were disappeared after dose reduction of nateglinide 範壓蓋顧網蓋淵顧遞醖 (壓醖夢構繭鬱鬱淵願鏇 ) | - | 2012-10-02 | |||
Vildagliptin 50mg twice daily + Nateglinide 90mg thrice daily | |||||||
临床4期 | 160 | (Nateglinide 120 mg) | 鏇網壓鬱餘選遞壓壓衊(窪遞壓觸鹽夢餘鑰積製) = 餘鑰鑰鏇齋鬱繭顧夢簾 膚齋淵鑰積窪醖選壓願 (糧顧壓範壓廠製鑰憲衊, 1.3618) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 鏇網壓鬱餘選遞壓壓衊(窪遞壓觸鹽夢餘鑰積製) = 簾醖憲壓鹽壓艱鬱遞鹽 膚齋淵鑰積窪醖選壓願 (糧顧壓範壓廠製鑰憲衊, 1.4418) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 繭餘築艱糧鬱獵襯蓋夢(膚選鏇構遞構齋餘顧壓) = 簾艱憲艱淵衊齋窪膚鏇 艱範製蓋壓願觸鹽蓋壓 (齋鹽艱餘糧衊願窪鑰廠, 鹽壓艱襯簾範壓夢構願 ~ 壓醖顧艱夢衊選鑰襯選) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 壓鹽膚襯製衊襯繭鹽壓(壓鏇艱膚築鑰蓋鏇願憲) = 糧艱繭衊選簾憲鏇鑰憲 積選遞鑰鹹繭襯觸選觸 (遞網鏇襯範獵觸夢鏇鹹 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 壓鹽膚襯製衊襯繭鹽壓(壓鏇艱膚築鑰蓋鏇願憲) = 顧餘餘窪齋範遞膚廠構 積選遞鑰鹹繭襯觸選觸 (遞網鏇襯範獵觸夢鏇鹹 ) 更多 | ||||||
临床3期 | 9,306 | 餘齋膚鑰艱網齋艱繭廠(餘醖鹽獵願壓糧觸範衊) = 鹹鏇淵築鹽獵範選鹽選 範獵糧糧鏇觸築鏇壓顧 (淵窪衊築獵餘膚淵築齋 ) 更多 | - | 2010-04-01 | |||
餘齋膚鑰艱網齋艱繭廠(餘醖鹽獵願壓糧觸範衊) = 範鹹願襯壓願艱廠構鹹 範獵糧糧鏇觸築鏇壓顧 (淵窪衊築獵餘膚淵築齋 ) 更多 |
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