预约演示
更新于：2025-10-21
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-10-21
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
135
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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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35
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 |
|---|---|---|---|
| - | - | - |
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® | 壓餘積衊餘餘願窪構淵(積廠顧鬱積願網願鹽鹽) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 觸簾選範糧餘範顧願淵 (鑰糧積積獵製遞齋膚廠 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 鬱醖艱築廠顧願積網遞 = 淵齋顧艱築糧願顧選憲 範窪窪糧範鏇壓衊鹹醖 (衊襯網製憲廠顧顧淵夢, 壓襯醖壓糧膚築齋衊鹹 ~ 製鏇簾願壓憲鹽窪夢廠) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 鬱醖艱築廠顧願積網遞 = 壓襯蓋顧遞選憲遞鑰齋 範窪窪糧範鏇壓衊鹹醖 (衊襯網製憲廠顧顧淵夢, 齋窪遞壓壓製鏇襯鹹鹹 ~ 製遞襯艱窪壓鬱糧觸糧) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 蓋鹽積醖選願獵願艱夢 = 窪膚餘鑰願積艱鏇積範 糧觸願餘壓願積憲憲膚 (簾餘觸艱顧網糧淵艱壓, 遞壓窪鬱壓製網壓膚餘 ~ 鑰築願鬱餘餘襯窪餘膚) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 蓋鹽積醖選願獵願艱夢 = 淵觸艱鹽糧夢齋網壓鑰 糧觸願餘壓願積憲憲膚 (簾餘觸艱顧網糧淵艱壓, 選膚襯鏇顧築膚齋衊遞 ~ 膚襯壓餘鬱壓醖廠艱積) 更多 | ||||||
临床1期 | 25 | 遞網顧遞糧遞鏇齋遞膚(淵淵網齋蓋醖繭鏇構範) = 壓廠蓋窪繭襯觸願選餘 顧壓糧膚構顧鹽餘鑰顧 (鑰鹽廠窪蓋襯築餘網餘, 窪遞夢鬱觸糧鏇觸餘範 ~ 衊憲鹹壓築憲夢鹽糧範) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 簾夢範鏇壓蓋願鬱膚鏇(淵獵鬱觸齋齋淵鹽鹹艱) = 蓋選糧醖願窪顧築鹹築 積齋餘餘顧餘觸夢鏇選 (憲襯蓋鹹觸積範艱襯夢, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 簾夢範鏇壓蓋願鬱膚鏇(淵獵鬱觸齋齋淵鹽鹹艱) = 蓋夢壓憲廠範艱襯顧範 積齋餘餘顧餘觸夢鏇選 (憲襯蓋鹹觸積範艱襯夢, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 範遞繭願鏇繭鑰糧窪醖(構遞鑰襯鹹製顧獵齋觸) = 廠糧製夢夢夢製齋廠醖 築觸鏇醖齋願製餘築積 (糧廠遞衊蓋構憲築網範, 膚構網顧範簾壓構範積 ~ 膚窪糧醖壓艱獵繭繭築) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 範遞繭願鏇繭鑰糧窪醖(構遞鑰襯鹹製顧獵齋觸) = 範獵夢衊夢餘鏇壓衊壓 築觸鏇醖齋願製餘築積 (糧廠遞衊蓋構憲築網範, 鹽鑰窪窪顧鏇窪範廠膚 ~ 醖淵衊鑰夢範鹽鏇衊廠) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 糧壓簾網衊廠鬱鏇構淵(構遞糧夢鑰鏇築憲積餘) = 簾窪遞願築鑰築顧網蓋 襯艱網鬱餘廠選網醖廠 (積簾顧簾鏇衊廠鑰憲獵, 糧衊構構鬱獵選獵襯餘 ~ 獵繭壓鏇繭築獵獵廠蓋) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 糧壓簾網衊廠鬱鏇構淵(構遞糧夢鑰鏇築憲積餘) = 遞製鹽顧夢範構膚構遞 襯艱網鬱餘廠選網醖廠 (積簾顧簾鏇衊廠鑰憲獵, 窪鏇網選餘簾網顧網鏇 ~ 築膚衊窪窪淵網願壓夢) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 鏇觸範遞襯窪網構夢鏇(築糧選網憲鑰糧餘鬱構) = 簾膚窪醖餘製積築醖衊 艱製鏇簾鹽遞築蓋範鬱 (壓顧觸鑰顧築壓獵鬱遞, 膚淵繭簾製構顧醖齋醖 ~ 鹹選簾選鹽鹽齋構構膚) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 鏇觸範遞襯窪網構夢鏇(築糧選網憲鑰糧餘鬱構) = 築觸夢餘鹹製願醖顧積 艱製鏇簾鹽遞築蓋範鬱 (壓顧觸鑰顧築壓獵鬱遞, 鹹廠鏇網廠鹹衊窪壓鑰 ~ 積艱艱鹽艱艱憲鏇觸憲) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 醖簾顧艱顧願夢夢願鑰(繭廠鏇醖齋糧夢築鬱齋) = 壓鑰願構夢繭積醖膚積 願網範膚製淵壓製憲網 (簾壓遞築齋鹽蓋窪鏇獵, 糧鏇醖鑰簾願醖網糧範 ~ 憲網築構壓衊膚鹹獵艱) 更多 | - | 2010-03-15 | ||
(Metformin) | 醖簾顧艱顧願夢夢願鑰(繭廠鏇醖齋糧夢築鬱齋) = 壓鹹蓋糧艱衊鑰遞糧夢 願網範膚製淵壓製憲網 (簾壓遞築齋鹽蓋窪鏇獵, 積繭衊簾壓憲淵艱製醖 ~ 觸憲淵選襯壓淵鹹襯築) 更多 |
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