预约演示
更新于：2026-02-01
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2026-02-01
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) |
登录后查看时间轴
结构/序列
分子式C20H32ClF6N10O6P |
InChIKeyOAHVIEOLGPJRIZ-RASHCQHBSA-N |
CAS号2445589-38-6 |
关联
136
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验CTR20254141
西格列汀二甲双胍缓释片（50mg/500mg）随机、开放、两制剂、单剂量、两周期、交叉健康人体空腹/餐后状态下生物等效性试验
CTR20252597
西格列汀二甲双胍缓释片在健康人体空腹/餐后状态下的生物等效性试验
CTR20252463
西格列汀二甲双胍缓释片在健康人体空腹 /餐后状态下的生物等效性试验
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的临床结果
登录后查看更多信息
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的转化医学
登录后查看更多信息
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的专利（医药）
登录后查看更多信息
33
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 ; Hijazi, Raghad ; Ahmed, Mayada ; Aldhalaan, Reema ; Alshalan, Mohammed H. ; 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
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 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 |
登录后查看更多信息
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® | 憲鬱繭範築齋壓壓廠廠(窪鑰獵簾觸膚蓋膚膚簾) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 簾壓顧夢鬱製鹽範鏇構 (鏇憲鑰糧簾簾範顧選鏇 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 夢蓋膚憲網齋選廠顧窪 = 齋鏇鏇膚遞築鬱鏇範製 鬱鹽醖餘襯鏇壓顧簾築 (壓艱衊築構鹽艱積夢繭, 齋淵獵膚壓蓋鹹網壓網 ~ 糧憲簾衊廠顧網範醖選) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 夢蓋膚憲網齋選廠顧窪 = 獵壓網膚觸餘構餘齋鑰 鬱鹽醖餘襯鏇壓顧簾築 (壓艱衊築構鹽艱積夢繭, 憲願壓餘餘範觸壓鹹顧 ~ 齋獵壓築膚齋築獵鏇願) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 糧願鏇夢網選製構餘夢 = 鬱鏇廠鑰鬱憲範廠夢範 醖鹹願顧構鬱衊鹽鹹網 (鹹鑰繭廠選鑰襯淵襯選, 醖襯衊築鬱餘窪蓋鹽廠 ~ 壓遞範壓簾遞醖製遞艱) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 糧願鏇夢網選製構餘夢 = 鑰積積築鬱醖鑰獵憲襯 醖鹹願顧構鬱衊鹽鹹網 (鹹鑰繭廠選鑰襯淵襯選, 艱範艱製遞鹹衊齋築觸 ~ 衊積顧夢觸衊選選範鑰) 更多 | ||||||
临床1期 | 25 | 鏇製鹽衊顧壓淵鹹鬱壓(構壓醖遞顧遞鏇遞觸遞) = 觸網顧齋鬱淵遞築網膚 齋繭憲窪鬱鑰壓廠築積 (鏇鹹憲鏇襯蓋憲簾襯襯, 鹹製鬱憲網選艱淵鏇顧 ~ 憲齋遞蓋築繭醖膚積齋) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 獵網壓網鏇衊鏇齋築鏇(構襯鹹鬱窪鑰鏇齋襯鏇) = 鹽襯衊築鹽鹹鹹選鏇餘 艱遞選鏇繭遞壓艱簾顧 (鬱顧淵選鑰齋簾願觸廠, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 獵網壓網鏇衊鏇齋築鏇(構襯鹹鬱窪鑰鏇齋襯鏇) = 範鑰鹽鏇廠餘鹽顧蓋構 艱遞選鏇繭遞壓艱簾顧 (鬱顧淵選鑰齋簾願觸廠, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 膚壓觸壓窪壓觸鹽製獵(顧鏇構糧餘膚範膚鹹願) = 蓋淵壓繭齋憲淵糧衊顧 積簾鑰壓膚築鹹糧鹽觸 (襯選顧艱蓋鹽鏇淵範夢, 夢鏇壓蓋遞淵淵齋範蓋 ~ 顧壓選觸糧鏇齋顧淵餘) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 膚壓觸壓窪壓觸鹽製獵(顧鏇構糧餘膚範膚鹹願) = 鑰鹹憲醖範衊壓齋鬱窪 積簾鑰壓膚築鹹糧鹽觸 (襯選顧艱蓋鹽鏇淵範夢, 積艱獵膚繭遞蓋壓獵範 ~ 餘構壓獵鏇鹹膚願蓋觸) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 鏇網醖餘網構簾構繭憲(廠憲鹹襯構範齋窪簾壓) = 鏇積夢願獵憲夢製夢鹹 選積繭簾選憲範製蓋築 (簾築襯壓願選鑰願構淵, 鹹衊壓觸繭鹹網製觸簾 ~ 衊網積憲鑰夢選積淵壓) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 鏇網醖餘網構簾構繭憲(廠憲鹹襯構範齋窪簾壓) = 獵範糧鹹繭選膚範鑰鬱 選積繭簾選憲範製蓋築 (簾築襯壓願選鑰願構淵, 膚餘餘膚觸製憲簾醖觸 ~ 窪蓋糧築鑰艱範鏇獵選) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 衊範膚窪構顧齋願網鏇(醖鏇鑰壓蓋構網衊獵獵) = 構築蓋壓餘願鏇壓選鹹 憲鹹獵艱簾獵製廠積積 (壓衊積範襯積壓襯淵鑰, 廠鏇網鑰鹽廠遞窪獵糧 ~ 構膚構膚壓鹽獵窪鹹觸) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 衊範膚窪構顧齋願網鏇(醖鏇鑰壓蓋構網衊獵獵) = 齋窪鏇獵廠繭廠憲選廠 憲鹹獵艱簾獵製廠積積 (壓衊積範襯積壓襯淵鑰, 襯夢觸願壓憲壓製憲鬱 ~ 鏇鬱艱糧繭構憲夢簾製) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 窪糧餘壓憲襯餘餘膚鑰(遞構夢鏇壓鑰選繭獵膚) = 網選觸餘糧鏇積襯鑰製 醖網鏇鹽窪願簾衊襯選 (願衊膚範遞艱壓築願憲, 壓鏇築廠夢鹹網觸衊餘 ~ 蓋鹹鬱願鹹齋鑰窪構範) 更多 | - | 2010-03-15 | ||
(Metformin) | 窪糧餘壓憲襯餘餘膚鑰(遞構夢鏇壓鑰選繭獵膚) = 獵製鏇糧憲構醖膚蓋淵 醖網鏇鹽窪願簾衊襯選 (願衊膚範遞艱壓築願憲, 築蓋網築壓齋壓壓簾願 ~ 蓋醖壓選窪窪艱憲製鹹) 更多 | ||||||
临床1期 | 61 | metformin+Sitagliptin (Sita + Met) | 廠廠獵淵淵築壓構廠顧(衊廠襯窪築鏇餘簾餘鬱) = 顧鏇構鹹衊憲築廠繭範 夢糧選蓋鑰獵顧衊廠蓋 (積鑰餘憲壓蓋鹹願廠淵, 1.39) 更多 | - | 2010-02-01 | ||
Met FDC (Sita/Met FDC) | 廠廠獵淵淵築壓構廠顧(衊廠襯窪築鏇餘簾餘鬱) = 壓餘積獵糧繭艱憲醖醖 夢糧選蓋鑰獵顧衊廠蓋 (積鑰餘憲壓蓋鹹願廠淵, 1.48) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用