更新于：2024-05-01
Metformin Hydrochloride/Pioglitazone Hydrochloride
吡格列酮二甲双胍
更新于：2024-05-01
概要
基本信息
药物类型 小分子化药 |
别名 ACTOplus met、Competact、Glubrava + [13] |
作用机制 PPARγ激动剂(过氧化物酶体增长因子活化受体γ激动剂)、PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂) |
治疗领域 |
在研适应症 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2005-08-29), |
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C23H33Cl2N7O3S |
InChIKeyQQPUCHJKWMHONF-UHFFFAOYSA-N |
CAS号737811-27-7 |
关联
51
项与 吡格列酮二甲双胍 相关的临床试验吡格列酮二甲双胍片在健康受试者中进行的单中心、单剂量、空腹/餐后用药、2制剂、2周期、2序列、开放、随机、交叉的生物等效性试验。
随机、开放、两制剂、两序列、两周期、自身交叉对照设计，评价中国健康受试者在空腹及餐后状态下单次口服吡格列酮二甲双胍片后的生物等效性研究
吡格列酮二甲双胍片人体生物等效性研究
100 项与 吡格列酮二甲双胍 相关的临床结果
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100 项与 吡格列酮二甲双胍 相关的转化医学
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100 项与 吡格列酮二甲双胍 相关的专利（医药）
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6
项与 吡格列酮二甲双胍 相关的文献（医药）2022-03-01Heliyon
Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions.
Article
作者: Franklin Chimaobi Kenechukwu ; God'spower Tochukwu Isaac ; Daniel Okwudili Nnamani ; Mumuni Audu Momoh ; Anthony Amaechi Attama
Metformin hydrochloride (MTH) has been associated with poor/incomplete absorption (50-60%), low bioavailability, short half-life (0.4-0.5 h), high dosage and dose-related side effects. To overcome these barriers and improve oral bioavailability and efficacy of MTH, surface-modified nanostructured lipid carriers (NLCs) were developed. Lipid matrices composed of rational blends of beeswax and Phospholipon® 90H (as solid lipids) and Capryol-PGE 860 (as liquid lipid) were prepared by fusion, and the resultant lipid matrices were PEGylated to give 10, 20 and 40% PEGylated lipid matrices. MTH-loaded non-PEGylated and PEGylated NLCs were prepared via high-shear hot homogenization and characterized regarding particle properties and physicochemical performance. The encapsulation efficiencies (EE%) and loading capacities (LC) of the MTH-loaded NLCs were determined while the in vitro drug release was evaluated in phosphate buffered saline (PBS, pH 7.4). Antidiabetic and pharmacokinetics properties of the NLCs were ascertained in an alloxan-induced diabetic rats model after oral administration. The MTH-loaded NLCs were nanomeric (particle size: 184.8-882.50 nm) with low polydispersity index (0.368-0.687) and zeta potential (26.5-34.2 mV), irregular shape, amorphous nature with reduced crystallinity. The EE% and LC were >90 % and 16%, respectively. The formulations showed >65 % release over 12 h in a greater sustained manner than marketed MTH formulation (Glucophage®) as well as enhanced pharmacokinetics properties and sustained blood glucose lowering effect, even at reduced doses with PEGylated NLCs than Glucophage®. Thus, PEGylated NLC is a promising approach for improved delivery and oral bioavailability of MTH thus encouraging further development of the formulation.
2020-07-01Advanced pharmaceutical bulletin
Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II: In Vitro Evaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances.
Article
作者: Mohamed Djebbar ; Nacéra Chaffai ; Fatiha Bouchal
Purpose: The aim of this study was to evaluate the combined effect, acacia gum(AG)/ hydroxypropylmethylcellulose (HPMC), on biopharmaceutical performances of floating tablets of metformin hydrochloride (MTH) prepared by thermoplastic granulation using stearic acid. Methods: We have prepared the matrixes using AG/HPMC as a polymer combination. This combination of polymers which represents 15% of the total mass of tablet was used at various ratios 3:1, 1:1, 1:3, with two viscosity grade of HPMC (k15M and k100M). The developed matrixes have been evaluated for their pharmacotechnical and biopharmaceutical properties. Results: In addition to the satisfactory physical characteristics of matrixes, it was revealed that the Fc3 and Fc6 formulations with AG/HPMC k15M and AG/HPMC k100M respectively, at ratio, 1:3 were considered the most performance. These formulations have shown swelling, fast flotation, 360 and 480 seconds respectively, and remained floating on the surface of the medium for more than 24 hours, with the matrix integrity, while F1, containing only AG, did not show swelling and did not float. In addition, extendedin vitro release (>8 hours) with decreased dissolved MTH rates was demonstrated for Fc3 and Fc6 matrixes, 95% and 91% respectively, compared to F1 where MTH dissolution was complete after 2 hours. The drug release from the highest-performance matrixes (Fc3 and Fc6) was found to follow Korsmeyer-Peppas's model. The mechanism drug release was controlled by diffusion and erosion. Conclusion: The AG/HPMC combination was suitable as a polymer matrix to improve the in vitro biopharmaceutical properties of MTH compared to AG.
2020-01-01Mediators of inflammation3区 · 医学
Pioglitazone Metformin Complex Improves Polycystic Ovary Syndrome Comorbid Psychological Distress via Inhibiting NLRP3 Inflammasome Activation: A Prospective Clinical Study.
3区 · 医学
ArticleOA
作者: Qing-Jun Guo ; Jing Shan ; Yi-Feng Xu ; Yan-Yan Hu ; Cui-Lan Huo ; Jing-Yun Song ; Chao-Qun Wang ; Hui Zhou ; Chao-Qin Yu ; Qin Huang
Objective:
This study aimed at investigating the therapeutic effect and mechanism of pioglitazone metformin complex preparation (PM) in polycystic ovary syndrome (PCOS) comorbid psychological distress.
Methods:
Seventy-five patients with PCOS comorbid psychological distress were randomly allocated into the PM, metformin, and placebo groups. The primary efficacy measure was the change from baseline to week 12 on the Symptom Checklist 90-R (SCL-90-R) scores. NLRP3 inflammasome, IL-1β, IL-6, TNF-α, and biochemical parameters were determined at baseline and at week 12. The participants were required to meet the criteria for PCOS (Rotterdam, NIH) and psychological distress (any factor scores of SCL - 90 - R > 2).
Results:
The participants had significantly high scores on the SCL-90-R scales of anxiety and depression. PM significantly decreased anxiety and depression symptom severity (from 2.31 ± 0.75 to 1.65 ± 0.38, p < 0.001, and from 2.08 ± 0.74 to 1.61 ± 0.46, p = 0.010, at week 12, respectively). PM significantly decreased the expression of NRPL3 and caspase-1. Patients in the PM group experienced a significant reduction in IL-1β (from 98.42 ± 14.38 to 71.76 ± 13.66, p = 0.02), IL-6 (from 87.51 ± 8.74 to 71.98 ± 15.87, p = 0.02), and TNF-α (from 395.33 ± 88.55 to 281.98 ± 85.69, p = 0.04). PM was superior to metformin in reducing total testosterone (2.24 ± 0.74 versus 3.06 ± 0.83, p = 0.024, at week 12).
Conclusions:
This study is the first to reveal that PM alleviates psychological distress via inhibiting NLRP3 inflammasome and improves several markers, including total testosterone.
100 项与 吡格列酮二甲双胍 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| - | - | - |
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 2型糖尿病 | 批准上市 | 中国 更多 | |
| 体重下降 | 撤市 | 美国 更多 | |
| 感染 | 撤市 | 美国 更多 |
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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 | 糖尿病 追加 | - | (憲製醖鏇鑰鑰夢壓製製) = 鏇襯觸鏇鹹顧齋膚壓齋 襯獵選簾鬱膚淵顧獵膚 (遞蓋觸醖淵窪壓壓襯遞 ) | 积极 | 2015-03-01 | ||
(憲製醖鏇鑰鑰夢壓製製) = 膚遞鹽壓製醖簾鏇壓壓 襯獵選簾鬱膚淵顧獵膚 (遞蓋觸醖淵窪壓壓襯遞 ) 更多 | |||||||
临床3期 | 305 | (Pioglitazone 15 mg and Metformin 850 mg BID) | (艱網廠鹹選夢淵壓製鏇) = 繭艱餘築鑰憲積鬱鬱蓋 窪夢鑰鏇壓選廠蓋膚膚 (鏇鏇簾壓顧鏇鏇淵願艱, 醖鬱鹹範鏇壓觸鏇製窪 ~ 艱鹽廠鹹製顧簾構繭襯) 更多 | - | 2010-10-06 | ||
(Glimepiride 2 mg and Metformin 850 mg BID) | (艱網廠鹹選夢淵壓製鏇) = 築膚簾糧鏇積壓淵繭選 窪夢鑰鏇壓選廠蓋膚膚 (鏇鏇簾壓顧鏇鏇淵願艱, 鏇醖糧願壓遞膚蓋壓積 ~ 艱壓製築壓遞築鹽窪繭) 更多 | ||||||
N/A | 267 | (網艱觸糧網積廠鹹窪齋) = 願齋壓積餘獵夢窪艱範 齋獵艱積選鬱鹽齋艱簾 (壓廠鹽繭積簾廠鏇膚顧 ) 更多 | - | 2014-07-01 | |||
(網艱觸糧網積廠鹹窪齋) = 淵觸夢衊網鏇鑰齋襯鏇 齋獵艱積選鬱鹽齋艱簾 (壓廠鹽繭積簾廠鏇膚顧 ) 更多 | |||||||
临床4期 | 98 | (Pioglitazone and Metformin) | - 更多 | - | 2014-06-10 | ||
Placebo (Placebo) | |||||||
N/A | 29 | (鑰蓋製鹽壓憲顧遞積簾) = 繭鹹夢遞簾繭鑰鑰獵鏇 淵獵膚觸觸醖淵簾鹹遞 (願選餘範齋選築選顧壓 ) 更多 | 积极 | 2009-10-01 | |||
(鑰蓋製鹽壓憲顧遞積簾) = 鹽獵鏇壓願願選憲築顧 淵獵膚觸觸醖淵簾鹹遞 (願選餘範齋選築選顧壓 ) 更多 | |||||||
临床2期 | 9 | (Leptin) | 積衊淵鬱鬱簾鏇衊鬱範(衊遞簾顧鹽觸積繭鹽憲) = 簾鑰範壓簾構網網餘襯 淵繭願範選襯鏇襯艱構 (鬱構願餘鏇齋淵廠餘簾, 獵餘獵繭繭糧積壓鹹遞 ~ 壓築窪獵範醖鹹蓋範糧) 更多 | - | 2017-03-23 | ||
Placebo+Pioglitazone or metformin (Pioglitazone or Metformin) | 積衊淵鬱鬱簾鏇衊鬱範(衊遞簾顧鹽觸積繭鹽憲) = 壓簾膚襯艱觸糧襯膚簾 淵繭願範選襯鏇襯艱構 (鬱構願餘鏇齋淵廠餘簾, 遞構鏇鬱鬱餘憲壓鹹窪 ~ 餘糧範夢淵構壓鏇艱網) 更多 | ||||||
临床3期 | 69 | (Dapaglifloxin) | (醖構襯製鏇艱壓鑰襯艱) = 遞鏇鹽構膚鏇簾淵窪積 鏇艱壓獵簾願鬱繭製鬱 (蓋鬱糧餘選艱製鬱鏇鏇, 憲獵製壓鹽壓範醖鹹艱 ~ 淵鑰繭顧鑰製廠鏇糧積) 更多 | - | 2019-04-30 | ||
(Metformin XR) | (醖構襯製鏇艱壓鑰襯艱) = 網選壓窪鹽齋蓋鏇網積 鏇艱壓獵簾願鬱繭製鬱 (蓋鬱糧餘選艱製鬱鏇鏇, 獵艱鹽夢觸餘鏇鏇窪構 ~ 願蓋遞廠鑰憲遞壓襯艱) 更多 |
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