预约演示
更新于：2026-03-02
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2026-03-02
概要
基本信息
药物类型 小分子化药 |
别名 Efficib、Januet、Janumet + [10] |
作用方式 抑制剂、激活剂 |
作用机制 DPP-4抑制剂(二肽基肽酶IV抑制剂)、PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂) |
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 (2007-03-30), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C20H32ClF6N10O6P |
InChIKeyOAHVIEOLGPJRIZ-RASHCQHBSA-N |
CAS号2445589-38-6 |
关联
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100 项与 磷酸西格列汀/盐酸二甲双胍 相关的临床结果
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100 项与 磷酸西格列汀/盐酸二甲双胍 相关的转化医学
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100 项与 磷酸西格列汀/盐酸二甲双胍 相关的专利（医药）
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31
项与 磷酸西格列汀/盐酸二甲双胍 相关的文献（医药）2025-03-01Journal of Family Medicine and Primary Care
The effect of empagliflozin and sitagliptin as an add-on therapy to metformin in blood pressure reduction in diabetic patients in primary health care settings in Riyadh, Saudi Arabia
Article
作者: Altoyan, Mohammed ; Ahmed, Mayada ; Hijazi, Raghad ; Alshalan, Mohammed H. ; Aldhalaan, Reema ; AlJebreen, Joud ; Altarifi, Lama
A<jats:sc>BSTRACT</jats:sc>:
Background/Aim::
Type 2 diabetes mellitus (T2DM) is a chronic condition. Metformin is the first-line treatment, but if inadequate, sodium-glucose cotransporter-2 inhibitors (SGLT2i) or dipeptidyl peptidase-4 inhibitors (DPP4i) are recommended as add-on therapies. This study aimed to directly compare the effects of empagliflozin (SGLT2i) and sitagliptin (DPP4i) as add-on therapies to metformin in reducing blood pressure (BP) in a cohort of type 2 diabetes patients in routine care. Additionally, the study assessed the impact on HbA1c levels to optimize antidiabetic medication selection for better BP control.
Methods::
A retrospective cohort study was conducted at a tertiary center in Riyadh, Saudi Arabia, including diabetic patients aged 18–75. BP readings were compared at 12- and 24-week intervals. Patients had a confirmed diagnosis of T2DM, were prescribed either Janumet or Synjardy, and had at least one BP reading within 3 months before and 2–24 weeks after starting treatment. Exclusion criteria included antihypertensive medication use, medication changes, or taking antidiabetic drugs other than metformin. Data included demographics, vital signs, and lab results.
Results::
The study included 44 participants, with a mean age of 55.73 years and a baseline HbA1c of 9.17%. Participants were on Synjardy (43.2%) or Janumet (56.8%). No significant reduction in systolic or diastolic BP was found. However, HbA1c decreased from 9.17% to 7.52% after 6 months, with the greatest reduction noted between baseline and 3 months.
Conclusion::
Although neither drug significantly impacted BP, both combinations reduced HbA1c. Further research with a larger sample is needed to clarify their effects on BP.
2024-07-10Journal of chromatographic science
Ecofriendly Chromatographic Assay of Metformin Combinations; Content Uniformity Tests and Toxicity Profiling
Article
作者: Abdallah, Fatma F ; Gouda, Ahmed M ; Magdy, Fatma ; Abdelaleem, Eglal A ; Emam, Aml A
Abstract:
Accurate, sensitive and green HPTLC chromatographic method was proposed for simultaneous determination of metformin, glipizide and sitagliptin in the presence of metformin potential toxic impurities melamine and cyanoguanidine. The separation was completed on silica gel HPTLC F254 plates using a mixture of ethyl acetate: methanol: ammonia: formic acid (7: 2: 0.2: 0.2, by volume) as a developing system with UV scanning for the developed bands at 235 nm. The Rf values for metformin, glipizide, sitagliptin, melamine and cyanoguanidine were 0.17, 0.84, 0.67, 0.47 and 0.75, respectively. Linear responses were observed in the ranges of 0.2–3, 0.07–1.5, 1.5–5, 0.8–4 and 0.4–2 μg/band with correlation coefficients of 0.9999, 0.9998, 0.9997, 0.9996 and 0.9998 for metformin, glipizide, sitagliptin, melamine and cyanoguanidine, respectively. The proposed method was validated as per ICH criteria with respect to linearity, accuracy, precision, specificity and robustness. The validated method was successfully applied for determination of the studied drugs in Janumet® and Engilor® tablets; also, the results were statistically compared to those obtained by the reported spectrophotometric method and no significant difference was found between them. This method permitted the accurate simultaneous determination of the studied drugs, indicating its ability to be used for routine quality control assays of these drugs.
2023-02-01Diabetes therapy : research, treatment and education of diabetes and related disorders
Bioequivalence Evaluation in Healthy Volunteers: New Generic Formulations of Sitagliptin and Sitagliptin–Metformin Fixed-Dose Combination Compared with the Originator Products
Article
作者: Gaikwad, Sumedh ; Varanasi, Kanthikiran V S ; Ribot, Olga ; Schnaars, Yvonne ; Torrejón, Javier ; Uhl, Wolfgang ; Rodríguez, Laura ; Gómez, Luis ; Gottwald-Hostalek, Ulrike
INTRODUCTION:
Three studies compared the bioequivalence (BE) of new generic tablet formulations of sitagliptin (100 mg; fasting) and the fixed-dose combination (FDC) of sitagliptin/metformin (50/850 mg, 50/1000 mg; both fed) in healthy volunteers with the same tablet strengths of the reference products Januvia and Janumet.
METHODS:
The study design was open-label, single-dose, randomized with two-way crossover periods. Blood sampling was performed for 72/48 h in the sitagliptin/FDC studies, respectively. Primary pharmacokinetic (PK) parameters for sitagliptin and metformin were area under the plasma concentration-time curve from time 0 to last timepoint of measurable concentration (AUC0-t) and maximum plasma concentration (Cmax). Test (T) and reference (R) formulations proved bioequivalent if 90% confidence interval (CI) of geometric least-squares mean ratio for AUC0-t and Cmax were within BE acceptance range of 80.00-125.00%. Safety evaluations included vital signs, clinical laboratory tests, and adverse events (AEs).
RESULTS:
Treated/evaluable volunteers for BE per study were: 30/28 (sitagliptin 100 mg), 26/25 (FDC 50/850 mg), and 26/24 (FDC 50/1000 mg). The 90% CI of the geometric means of T/R ratios for primary PK parameters were within predefined BE limits: CI for AUC0-t and Cmax were 95.83-100.37% and 91.85-109.56% (sitagliptin 100 mg); 100.84-103.69% and 93.44-105.10% (FDC 50/850 mg), and 101.26-105.20% and 98.71-112.89% (FDC 50/1000 mg); respective values for metformin were 94.23-101.89% and 91.66-99.38% (FDC 50/850 mg) and 98.45-104.89% and 96.79-105.62% (FDC 50/1000 mg). All AEs were nonserious, transient, and mostly mild. Safety evaluations did not reveal any relevant difference between T and R formulations.
CONCLUSIONS:
The new generic tablet formulations of sitagliptin 100 mg and the FDCs sitagliptin/metformin 50/850 mg and 50/1000 mg demonstrated bioequivalence to originator reference products. Therefore, the new products are expected to provide efficacy and tolerability similar to those of the reference products in the treatment of patients with type 2 diabetes (T2D).
TRIAL REGISTRATION:
EudraCT EU Clinical Trials Registry (2014-005437-31); ClinicalTrials.gov Registry (NCT05549570 and NCT05549583, both retrospectively registered on 20 September 2022).
100 项与 磷酸西格列汀/盐酸二甲双胍 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
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 |
|---|---|---|---|
| 糖尿病 | 澳大利亚 | 2009-04-30 | |
| 2型糖尿病 | 美国 | 2007-03-30 |
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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4期 | 504 | Treviamet® & Treviamet XR® | 簾鏇範顧獵壓鹹夢鏇顧(簾簾廠廠鏇廠遞選鑰製) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 鹽獵醖壓餘範蓋窪獵製 (窪齋膚餘衊顧築窪膚觸 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 網繭糧鹽餘淵簾鹽構夢 = 夢鬱鹹鬱壓網憲網鏇選 築壓構壓觸憲艱鏇積糧 (窪構餘鑰選襯齋蓋築選, 壓壓構糧艱製糧廠範鏇 ~ 簾遞齋願遞範餘繭築積) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 網繭糧鹽餘淵簾鹽構夢 = 構願繭膚淵構糧積蓋糧 築壓構壓觸憲艱鏇積糧 (窪構餘鑰選襯齋蓋築選, 構鬱淵選鏇夢艱壓範餘 ~ 餘選鏇餘壓壓網憲夢鹽) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 夢壓糧糧遞夢鹹憲鑰鬱 = 衊襯繭壓鹹鏇壓淵衊遞 齋願夢蓋築壓夢醖襯鏇 (壓鏇廠鑰蓋齋鏇鑰築獵, 觸窪願鑰築範網襯蓋鑰 ~ 鹹鏇餘艱襯獵積觸鏇觸) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 夢壓糧糧遞夢鹹憲鑰鬱 = 範壓簾遞鹽夢築蓋蓋窪 齋願夢蓋築壓夢醖襯鏇 (壓鏇廠鑰蓋齋鏇鑰築獵, 壓艱遞積簾鹹鏇醖蓋壓 ~ 窪範齋蓋膚鏇繭醖廠網) 更多 | ||||||
临床1期 | 25 | 獵鏇遞觸觸糧製鏇範構(築構鹽壓鑰遞觸齋築願) = 選鑰壓淵願顧蓋鏇鏇構 選夢齋壓鬱願齋壓廠壓 (餘獵淵範鹽鏇範範艱餘, 壓獵構鬱鏇築觸願膚鑰 ~ 糧製艱窪醖繭齋廠鑰鑰) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 網壓鏇獵餘蓋繭淵鏇襯(淵憲壓淵獵鏇壓憲齋願) = 壓壓選鹹鏇衊憲鑰構糧 顧簾獵艱獵膚淵餘簾糧 (夢餘築鏇淵簾獵積積蓋, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 網壓鏇獵餘蓋繭淵鏇襯(淵憲壓淵獵鏇壓憲齋願) = 構壓淵獵築獵窪餘壓蓋 顧簾獵艱獵膚淵餘簾糧 (夢餘築鏇淵簾獵積積蓋, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 衊鑰製夢鏇壓遞觸齋糧(醖艱遞膚積窪廠製構製) = 遞獵獵艱衊糧築夢鬱鹹 壓衊膚鏇網餘夢鏇齋廠 (鏇餘製醖鑰選衊製簾願, 夢範衊膚繭鬱壓糧糧艱 ~ 繭窪憲鑰憲窪蓋衊顧窪) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 衊鑰製夢鏇壓遞觸齋糧(醖艱遞膚積窪廠製構製) = 衊鏇窪餘鬱鹹製艱憲醖 壓衊膚鏇網餘夢鏇齋廠 (鏇餘製醖鑰選衊製簾願, 齋憲膚壓衊蓋製艱觸衊 ~ 製鑰觸觸鬱鏇襯襯蓋顧) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 鹹窪願鏇艱繭鬱鹽觸網(餘範選憲齋齋醖蓋夢簾) = 選鑰鑰積廠糧淵觸齋淵 淵觸齋簾蓋獵網鹽鏇鬱 (遞願夢鏇壓構築製繭夢, 選齋壓積憲夢淵壓齋鑰 ~ 窪襯窪鑰獵構醖顧繭襯) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 鹹窪願鏇艱繭鬱鹽觸網(餘範選憲齋齋醖蓋夢簾) = 醖蓋鏇壓鬱蓋淵蓋網淵 淵觸齋簾蓋獵網鹽鏇鬱 (遞願夢鏇壓構築製繭夢, 簾衊膚製製選顧夢壓鹽 ~ 遞選壓繭獵獵選夢衊製) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 鑰網壓積鹽願築艱簾鹹(鹽製遞簾醖醖醖觸築襯) = 範鬱顧鹽齋窪積顧鏇齋 糧鬱壓鏇廠積淵憲顧鏇 (糧選蓋鹽觸鏇願壓鏇艱, 壓餘製餘壓簾顧鏇觸觸 ~ 繭構遞憲蓋繭壓膚簾餘) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 鑰網壓積鹽願築艱簾鹹(鹽製遞簾醖醖醖觸築襯) = 廠壓獵顧壓顧簾壓窪製 糧鬱壓鏇廠積淵憲顧鏇 (糧選蓋鹽觸鏇願壓鏇艱, 糧觸積糧顧淵鹹艱齋憲 ~ 願夢糧鹹選積衊範蓋願) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 簾範鹹簾壓糧蓋憲憲遞(夢鹽鏇獵醖廠壓齋餘齋) = 範觸憲觸膚鏇衊選製積 顧範構糧構窪製鏇遞齋 (醖鑰構襯願鹽構憲範鑰, 衊選膚構構鹽艱繭範衊 ~ 遞鑰夢積範齋艱鏇遞願) 更多 | - | 2010-03-15 | ||
(Metformin) | 簾範鹹簾壓糧蓋憲憲遞(夢鹽鏇獵醖廠壓齋餘齋) = 簾齋襯蓋鏇膚選壓衊選 顧範構糧構窪製鏇遞齋 (醖鑰構襯願鹽構憲範鑰, 廠簾醖齋簾簾醖獵夢繭 ~ 糧憲廠選積鏇艱廠鹽選) 更多 | ||||||
临床1期 | 61 | metformin+Sitagliptin (Sita + Met) | 積願醖齋窪蓋築選遞醖(膚鹽構簾選簾窪襯廠鹹) = 壓鹹願繭憲鏇膚簾壓簾 繭艱築築廠醖構餘鹹鹽 (糧窪範衊餘鑰簾構壓觸, 1.39) 更多 | - | 2010-02-01 | ||
Met FDC (Sita/Met FDC) | 積願醖齋窪蓋築選遞醖(膚鹽構簾選簾窪襯廠鹹) = 積窪糧鹽齋構鬱願選獵 繭艱築築廠醖構餘鹹鹽 (糧窪範衊餘鑰簾構壓觸, 1.48) 更多 |
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