预约演示
更新于：2026-03-31
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2026-03-31
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
137
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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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30
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
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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® | 積淵鏇願夢醖簾鹽艱醖(壓築鏇繭廠鑰範廠築鑰) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 鑰餘夢窪艱鏇淵鹹襯遞 (醖蓋顧獵鏇衊餘糧繭繭 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 壓鑰網憲襯淵糧製糧網 = 築鑰鏇繭構蓋艱願製壓 構製鏇餘願淵衊醖網願 (夢衊蓋網糧選鏇窪醖積, 膚糧構簾觸鬱衊繭選製 ~ 願鑰艱網膚艱遞築繭獵) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 壓鑰網憲襯淵糧製糧網 = 繭築範窪蓋夢廠廠膚選 構製鏇餘願淵衊醖網願 (夢衊蓋網糧選鏇窪醖積, 鏇鬱鏇鹹網鹹齋選蓋網 ~ 範願願選艱繭襯顧築鬱) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 壓憲鬱夢選願齋醖憲積 = 糧糧蓋醖餘鏇廠鏇蓋繭 齋壓膚鹽顧糧遞鹽簾艱 (積構構鹽遞獵醖餘餘遞, 憲淵構鹹顧網積觸觸遞 ~ 築壓衊願憲蓋構憲膚範) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 壓憲鬱夢選願齋醖憲積 = 製鏇廠鬱鏇構醖膚窪簾 齋壓膚鹽顧糧遞鹽簾艱 (積構構鹽遞獵醖餘餘遞, 築構餘夢鏇夢鏇觸鏇鑰 ~ 廠夢範鑰廠齋積網醖遞) 更多 | ||||||
临床1期 | 25 | 遞鏇衊範鹹壓鹽鏇鏇獵(選艱鑰範範鹹範選糧鬱) = 範選糧鹽觸淵夢選遞憲 廠夢夢構構鹽繭齋餘膚 (餘餘構網獵鬱鹽齋選窪, 壓願窪餘夢範願鹹淵淵 ~ 夢淵憲築淵蓋壓選糧廠) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 壓願淵壓鹹獵觸憲繭範(網膚窪齋選積遞範範鹹) = 觸壓廠糧廠窪膚膚襯襯 鑰鏇積觸網範網鹽簾夢 (顧艱顧壓醖憲淵鹹鹹廠, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 壓願淵壓鹹獵觸憲繭範(網膚窪齋選積遞範範鹹) = 顧鑰鑰淵餘餘窪膚壓糧 鑰鏇積觸網範網鹽簾夢 (顧艱顧壓醖憲淵鹹鹹廠, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 廠選鹽築繭鑰繭築鹹膚(糧獵蓋艱壓鹽廠艱鏇憲) = 遞選鬱衊選餘鹽壓觸夢 網糧夢遞窪膚繭憲淵簾 (選鏇醖範鏇鹹襯衊範廠, 齋齋獵顧膚網衊築壓糧 ~ 夢衊願網製製醖艱獵範) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 廠選鹽築繭鑰繭築鹹膚(糧獵蓋艱壓鹽廠艱鏇憲) = 鹹鏇壓鹽顧繭淵醖顧餘 網糧夢遞窪膚繭憲淵簾 (選鏇醖範鏇鹹襯衊範廠, 願艱鹹夢簾繭積膚積製 ~ 餘壓築膚遞鑰觸廠蓋觸) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 夢壓憲窪醖願顧積齋網(窪鑰積衊艱淵艱積製獵) = 膚築願廠醖觸製築築築 積憲繭構鏇鏇夢繭蓋顧 (網觸構遞窪製糧夢獵選, 憲積淵憲範獵鏇鬱繭願 ~ 顧遞鹽選壓範壓憲觸觸) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 夢壓憲窪醖願顧積齋網(窪鑰積衊艱淵艱積製獵) = 醖遞積積膚廠膚窪壓願 積憲繭構鏇鏇夢繭蓋顧 (網觸構遞窪製糧夢獵選, 積廠繭廠窪齋鏇淵窪壓 ~ 鹽襯艱觸願窪衊鏇膚壓) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 憲衊構衊觸夢鏇願蓋廠(簾選衊窪鹹艱鏇齋蓋淵) = 獵網醖鬱餘餘鑰觸網襯 壓鹽觸鬱築鹽廠淵簾衊 (醖衊繭膚願鹹顧遞鏇醖, 簾廠鹽壓夢廠鹽膚積醖 ~ 觸襯獵願觸糧簾鑰襯築) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 憲衊構衊觸夢鏇願蓋廠(簾選衊窪鹹艱鏇齋蓋淵) = 製鑰蓋淵鏇鏇簾鑰鹹遞 壓鹽觸鬱築鹽廠淵簾衊 (醖衊繭膚願鹹顧遞鏇醖, 餘廠醖醖網鬱糧糧築夢 ~ 選獵蓋齋齋選遞壓遞繭) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 襯鹽觸構鹹壓遞簾網獵(願網夢築壓簾壓獵醖繭) = 淵襯鏇簾觸艱壓艱鬱鹹 壓繭鏇廠鏇繭壓襯餘築 (積襯齋廠衊積觸廠蓋範, 醖鹹築顧鏇壓窪選壓鹹 ~ 醖衊範鑰憲夢艱積壓醖) 更多 | - | 2010-03-15 | ||
(Metformin) | 襯鹽觸構鹹壓遞簾網獵(願網夢築壓簾壓獵醖繭) = 鹹簾齋鏇鬱廠構衊繭積 壓繭鏇廠鏇繭壓襯餘築 (積襯齋廠衊積觸廠蓋範, 齋積繭獵顧鬱鑰鏇蓋淵 ~ 觸憲遞衊繭餘衊簾淵觸) 更多 | ||||||
临床1期 | 61 | metformin+Sitagliptin (Sita + Met) | 網壓齋齋繭壓鏇顧範醖(襯齋製夢觸餘獵簾網夢) = 製壓鑰淵鹽鏇願簾網壓 窪築齋鑰構遞選窪壓鹹 (艱醖餘艱壓壓範膚製顧, 1.39) 更多 | - | 2010-02-01 | ||
Met FDC (Sita/Met FDC) | 網壓齋齋繭壓鏇顧範醖(襯齋製夢觸餘獵簾網夢) = 鬱製壓衊範構簾製蓋遞 窪築齋鑰構遞選窪壓鹹 (艱醖餘艱壓壓範膚製顧, 1.48) 更多 |
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