预约演示
更新于：2025-05-16
Glyburide/Metformin Hydrochloride
二甲双胍格列本脲
更新于：2025-05-16
概要
基本信息
药物类型 小分子化药 |
别名 Glibenclamide/metformin、Glucovance、Glyburide/metformin + [48] |
作用方式 激活剂、抑制剂 |
作用机制 PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂)、SUR1抑制剂(磺酰脲类受体1抑制剂) |
治疗领域 |
非在研适应症- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2000-07-31), |
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C27H40Cl2N8O5S |
InChIKeyHCEQQASHRRPQFE-UHFFFAOYSA-N |
CAS号338752-31-1 |
关联
13
项与 二甲双胍格列本脲 相关的临床试验CTR20233289
二甲双胍格列本脲片在中国健康受试者中进行的单中心、随机、开放、单次（空腹/餐后）口服给药、两制剂、两序列、两周期、交叉的人体生物等效性试验
NCT04930744
A Prospective, Randomized Open-Label Phase II Study of the Safety and Tolerability of Metformin in Combination With Standard Antimicrobial Treatment of Pulmonary Tuberculosis in People With TB and Co-infected With HIV
CTR20211771
三门峡赛诺维制药有限公司生产的二甲双胍格列本脲片（Ⅱ）（500 mg/5 mg）与Merk SANTE S.A.S 持证的二甲双胍格列本脲片（商品名：GlucovanceTM，500 mg/5 mg）在健康受试者中的单次给药、随机、开放、两周期、双交叉、空腹及餐后状态下的生物等效性研究
100 项与 二甲双胍格列本脲 相关的临床结果
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100 项与 二甲双胍格列本脲 相关的转化医学
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100 项与 二甲双胍格列本脲 相关的专利（医药）
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32
项与 二甲双胍格列本脲 相关的文献（医药）2023-05-01Clinical pharmacology in drug development
Pharmacokinetic and Bioequivalence Studies of 2 Metformin Glibenclamide Tablets in Healthy Chinese Subjects Under Fasting and Fed Conditions
Article
作者: Chen, Lin ; Huang, Xiaolun ; Li, Xinjing ; Huang, Jiao
Abstract:
The rational combination of oral antidiabetic agents is more likely to provide better glycemic control than monotherapy. Metformin glibenclamide tablets can be used as second‐line therapy for patients with type 2 diabetes mellitus who cannot successfully control their blood glucose levels by diet and exercise plus metformin or sulfonylureas. The aim of this study was to evaluate the bioequivalence and safety of metformin hydrochloride and glibenclamide tablets (500 mg/5 mg) prepared by 2 different vendors in healthy Chinese subjects under fasting and fed conditions. This is an open‐label, single‐center, randomized, 2‐formulation, 2‐period crossover study. After screening, 40 subjects were enrolled in the fasting trial, while 40 subjects were enrolled in the fed trial. Qualified subjects were randomly assigned to receive a monotherapy dose of 500 mg/5 mg of the test or reference formulation, and after a 1‐week washout period, they took the alternative formulation. Blood samples were collected from 24 blood collection sites per cycle for pharmacokinetic analysis until 36 hours after oral administration. In total, 78 subjects completed the study. Under fasting and fed conditions, the geometric mean ratios of maximum plasma concentration, area under the plasma concentration–time curve (AUC) from time 0 to time of last quantifiable drug level , and AUC from time 0 to infinity between the 2 products, as well as the corresponding 90%CIs, were all within the range of 80%–125%. It was found that exposure (AUC from time 0 to infinity) to metformin is decreased by about 25% in the fed state compared to fasting, whereas glibenclamide exposure is increased by about 30% in the fed state. No severe adverse events were observed in the study.
2022-02-17Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals4区 · 医学
Ameliorative effect of flavonoid-rich extracts from Gongronema latifolium against diabetic cardiomyopathy via serpin A3 and socs3-a in streptozocin treated rats
4区 · 医学
Article
作者: Ejeje, Jerius Nkwuda ; Ajiboye, Basiru Olaitan ; Oyinloye, Babatunji Emmanuel ; Omotuyi, Olaposi Idowu ; Brai, Bartholomew I. C. ; Johnson, Oluwafolakemi ; Owolabi, Olutunmise Victoria
INTRODUCTION:
The present study access the effect of the flavonoid-rich extract from Gongronema latifolium against cardiomyopathy streptozotocin-induced diabetic rats.
MATERIALS AND METHODS:
The flavonoid-rich extract from G. latifolium leaf (FREGL) was prepared using a standard method. Diabetes was induced by a single intraperitoneal (i.p.) injection of streptozotocin. The experimental animals were divided into five groups as non-diabetic rats, diabetic control, diabetic rats administered low and high doses of FREGL (13 and 26 mg/kg), and metformin-glibenclamide orally for 21 days. Hence, the experimental animals were sacrificed; blood and heart were harvested to determine diverse biochemical parameters, including the gene expressions of serpin A3 and socs3-a as well as histological examination.
RESULTS:
The results demonstrated that FREGL significantly (p < 0.05) reduced fasting blood glucose, total cholesterol, low density lipoprotein (LDL), triglyceride (TG), lipid peroxidation levels, as well as the activities of lactate dehydrogenase and creatine kinase-MB, including the relative gene expressions of serpin A3 and Socs3-A in diabetic rats. Also, diabetic rats that received different doses of FREGL showed a substantial rise in insulin and high density lipoprotein (HDL) levels, antioxidant enzyme activities, as well as, normal histoarchitecture of the heart tissues.
CONCLUSION:
Therefore, FREGL may be beneficial in alleviating diabetic cardiomyopathy.
2022-01-01European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2区 · 医学
NDMA analytics in metformin products: Comparison of methods and pitfalls
2区 · 医学
Article
作者: Mouton, Bruno ; Goettsche, Anja ; Cimelli, Alexandra ; Keitel, Judith ; Bristow, Tony ; Hickert, Sebastian ; Fritzsche, Matthias ; O'Neill, Nicholas ; Kirsch, Annette ; Guessregen, Brunhilde ; Barrau, Elodie ; Harrison, Mark ; Blom, Giorgio ; Desmartin, Emmanuel ; Reifenberg, Philipp ; Krueger, Phillip ; Schlingemann, Joerg ; Leicht, Stefan ; Seegel, Maic ; Saal, Christoph ; Baranowski, Romane
BACKGROUND:
For nearly three years, the concerns regarding trace levels of N-nitrosamines in pharmaceuticals and the associated cancer risk have significantly expanded and are a major issue facing the global pharmaceutical industry. N-nitrosodimethylamine (NDMA) found in formulations of the popular anti-diabetic drug metformin is a prominent example. This has resulted in product recalls raising the profile within the media. Issues of method robustness, sample preparation and several unexpected sources of nitrosamine contamination have been highlighted as false positive risks. It has become apparent that the identification of the root causes of artefactual formation of nitrosamines must be identified to mitigate risk associated with the analysis.
METHODS:
A comparison study between four laboratories, across three companies was designed, employing orthogonal mass spectrometric methods for the quantification of NDMA in two metformin immediate release (IR) formulations and one extended release (XR) formulation. These were 2x LC-MS/MS, GC-MS/MS and GC-HRMS.
RESULTS:
Good agreement of results was obtained for the IR formulations. However, we measured higher concentrations of NDMA in the XR formulation using GC-MS/MS compared to LC-MS/MS. We could show that this was due to artefactual (in situ) formation of NDMA when samples were extracted with dichloromethane. Removal of dimethylamine (DMA) and nitrite from the extracted sample or the addition of a nitrosation scavenger are shown to be effective remedies. NDMA in situ formation was not observed in 10% MeOH or acetonitrile.
CONCLUSION:
Metformin pharmaceuticals contain traces of the API impurity DMA as well as inorganic nitrite from excipients. This can lead to artefactual formation of NDMA and hence false positive results if DCM is used for sample extraction. Similar artefacts are likely also in other pharmaceuticals if these contain the secondary amine precursor of the respective nitrosamine analyte.
100 项与 二甲双胍格列本脲 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病 | 澳大利亚 | 2004-08-05 | |
| 2型糖尿病 | 美国 | 2000-07-31 |
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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
临床1期 | - | 60 | (Glyburide Metformin) | 窪構選製膚膚鹹願醖餘(觸製窪鹽積構壓遞壓築) = 廠遞襯遞構網膚鬱構淵 餘獵膚簾鏇顧製獵觸選 (範窪壓鏇製壓繭簾鏇淵, 68.08) 更多 | - | 2009-08-04 | |
(Glucovance®) | 窪構選製膚膚鹹願醖餘(觸製窪鹽積構壓遞壓築) = 願壓廠製淵簾簾淵顧顧 餘獵膚簾鏇顧製獵觸選 (範窪壓鏇製壓繭簾鏇淵, 59.87) 更多 | ||||||
临床1期 | - | 60 | (Glyburide Metformin) | 製簾積餘鏇築繭齋網鏇(製繭鑰齋憲觸觸網積鏇) = 蓋餘壓積鬱簾鹽構齋糧 廠製餘簾淵齋廠鹽窪遞 (積積網鏇夢鬱範艱鑰醖, 34.86) 更多 | - | 2009-08-04 | |
(Glucovance®) | 製簾積餘鏇築繭齋網鏇(製繭鑰齋憲觸觸網積鏇) = 顧築製簾廠製齋淵築淵 廠製餘簾淵齋廠鹽窪遞 (積積網鏇夢鬱範艱鑰醖, 52.35) 更多 |
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