更新于：2024-06-24
Glyburide/Metformin Hydrochloride
二甲双胍格列本脲
更新于：2024-06-24
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 |
在研适应症 |
非在研适应症- |
在研机构 |
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
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
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
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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21
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.
2019-01-01Acta endocrinologica (Bucharest, Romania : 2005)4区 · 医学
The Effect of Glucovance Therapy on Biomechanical Deterioration of Bone in Streptozotocin-Induced Diabetic Rats
4区 · 医学
Article
作者: Yildiz, A ; Demirel, C ; Gurgul, S ; Akarsu, E ; Erdal, N ; Korkmaz, H
AIM:
Is to evaluate the influence of glucovance therapy on biomechanical properties of bone in streptozotocin - induced diabetes mellitus (DM) in rats.
MATERIALS AND METHODS:
A total of 28 male Wistar-Albino rats (12-week-old; 210-300 g) were divided into 4 groups including control (C; no treatment; n=7), sham [Sh; distilled water (gavage, for 8 weeks); n=7], diabetes [DM; streptozotocin (45 mg/kg, single i.p injection); n=7] and diabetes+ Glucovance treatment [DM+G; streptozotocin (45 mg/kg, single i.p injection) + Glucovance (Glucovance, 500/5 mg/kg/day/rat, gavage, for 8 weeks); n=7] groups. Body weight, blood glucose levels (BGLs), bone mineral density (BMD) and geometric/mechanical properties of bone tissue were evaluated. BGLs in diabetic rats were significantly increased compared to non-diabetic rats, while the body weights were decreased (p<0.05).
RESULTS:
A significant difference was not detected between groups with regard to cross-sectional area of diaphyseal femur (p>0.05). Maximum load, energy absorption capacity, ultimate stress, ultimate strain, toughness and displacement were shown to decrease and stiffness was shown to increase in DM rats (p<0.05). Ultimate stress and maximum load were significantly increased in DM+G groups compared to DM groups (p<0.05).
CONCLUSION:
Glucovance treatment seems to be effective in restoration of biomechanical deterioration of bone specific to STZ-induced DM.
2016-09-01Journal of hypertension2区 · 医学
OS 02-06 PHYSIOLOGICAL REGULATION OF VASOMOTION BY INTRACELLULAR ATP-MEDIATED SYSTEM IN HUMAN ARTERY
2区 · 医学
Article
作者: Kim, Dae Hoon ; Lee, Sang Jin ; Kim, Chan Hyung ; Lee, Sang Eok ; Kim, Young Chul ; Choi, Woong ; Yun, Hyo-Yung
OBJECTIVE:
Spontaneous oscillation of tone of blood vessel called vasomotion cause vessel to flow blood which is an oscillation of flow into an organ. Microcirculation is sensitive to hypoxic condition and metabolism but mechanism of vasomotion is still poorly understood.
DESIGN AND METHOD:
Purpose: We studied involvement of metabolism-mediated regulation by intracellular ATP level of vasomotion in human gastric artery.
METHODS:
Conventional contractile measuring system and Western blot were used.
RESULTS:
Circular muscle of human gastric artery produced sustained tonic contraction of 1.0 ± 0.19 g by 50 mM high K (n = 36). Pinacidil (10 μM), which is known to activatorof ATP-sensitive K (KATP) channel inhibited vasomotion completely in a reversible manner. Inhibition of vasomotion by activators of KATP channel recovered by glibenclamide. Diazoxide (300 μM), cromakalim (10 μM) nicorandil (10 μM) which is known to activate KATP channel also completely blocked vasomotion in a glibenclamide sensitive manner. Inhibitory effect of these openers of KATP channel on serotonin and norepinephrine-induced contraction were also recoded in a glibenclmide-sensitive manner. In human artery, glucose-free condition which is elated metabolic changes inhibited vasomotion and it was recovered by glibenclamide. Finally, molecular subtypes of KATP channel was defined by Western blot in human artery.
CONCLUSIONS:
Vasomotion of human gastroepiploic artery was inhibited by activation of specific subtypes of KATP channel and alteration of metabolism.
100 项与 二甲双胍格列本脲 相关的药物交易
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外链
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 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) | 鏇壓壓衊鬱窪鬱範鹹蓋(網壓範積遞憲窪糧廠顧) = 選壓繭襯廠願夢窪膚淵 築網鏇蓋簾窪齋簾範鬱 (顧願網蓋網願積淵淵選, 鏇廠構網膚廠築製積膚 ~ 鑰範繭廠繭範襯顧窪憲) 更多 | - | 2009-08-04 | |
(Glucovance®) | 鏇壓壓衊鬱窪鬱範鹹蓋(網壓範積遞憲窪糧廠顧) = 願製鏇願糧蓋獵醖窪廠 築網鏇蓋簾窪齋簾範鬱 (顧願網蓋網願積淵淵選, 範窪遞願簾築顧築鏇網 ~ 簾夢齋鏇齋鹹廠夢願鬱) 更多 | ||||||
临床1期 | - | 60 | (Glyburide Metformin) | 顧鏇憲衊醖壓遞窪鑰鏇(餘構餘淵範積窪網遞憲) = 鹽鏇網餘選顧襯構觸鹽 遞鑰積餘築鬱範齋鏇衊 (糧壓繭願觸憲鬱網鏇鹽, 築衊醖網壓鹹範壓夢製 ~ 蓋鏇構蓋構鏇蓋築範積) 更多 | - | 2009-08-04 | |
(Glucovance®) | 顧鏇憲衊醖壓遞窪鑰鏇(餘構餘淵範積窪網遞憲) = 築夢構遞夢網積齋鹹襯 遞鑰積餘築鬱範齋鏇衊 (糧壓繭願觸憲鬱網鏇鹽, 膚遞齋夢獵膚鏇膚衊製 ~ 淵獵鹽膚餘壓鏇鬱蓋願) 更多 |
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