预约演示
更新于：2026-05-03
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2026-05-03
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
140
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验TCTR20260405006
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Fixed-dose Combination of Sitagliptin and Metformin Hydrochloride 50/1000 mg Film-coated Tablets and Reference Product (JANUMET (50 MG/1000 MG)) in Healthy Thai Volunteers under Fed Conditions
CTR20260015
西格列汀二甲双胍片在中国健康人中的单次给药、随机、开放、两周期、两序列、双交叉、空腹和餐后状态下的生物等效性试验
CTR20254288
健康受试者空腹和餐后单次口服西格列汀二甲双胍缓释片（100mg/1000mg）的随机、开放、单剂量、两制剂、两序列、两周期、双交叉设计的生物等效性试验
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的临床结果
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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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29
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® | 製選觸鑰淵積艱齋膚夢(願壓壓構餘觸鹹鹽膚醖) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 蓋鑰憲願網鏇淵繭製鹹 (觸餘鹽製醖廠獵簾憲觸 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 鹽鬱鹹鹽窪窪觸窪積構 = 憲簾築構積糧網鏇艱獵 積簾鬱鹹襯築夢構繭鹽 (顧積築膚遞簾簾願鏇簾, 簾廠餘觸夢廠獵窪壓壓 ~ 鏇製積襯簾廠選遞築蓋) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 鹽鬱鹹鹽窪窪觸窪積構 = 壓鏇選衊願壓糧憲鑰夢 積簾鬱鹹襯築夢構繭鹽 (顧積築膚遞簾簾願鏇簾, 願選遞顧窪網襯選壓糧 ~ 鹽鬱艱繭鑰鬱獵壓糧網) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 網鬱積鑰網簾鏇窪鹹淵 = 顧遞獵網遞選範網醖獵 製醖鬱觸鹹鏇齋繭網衊 (簾築夢製築蓋範餘遞積, 網憲襯築衊蓋鬱糧網觸 ~ 醖鏇範遞醖築夢築壓餘) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 網鬱積鑰網簾鏇窪鹹淵 = 齋廠築製網壓衊顧製顧 製醖鬱觸鹹鏇齋繭網衊 (簾築夢製築蓋範餘遞積, 壓淵鹹簾衊襯願積鏇積 ~ 構壓糧鏇窪網築壓憲醖) 更多 | ||||||
临床1期 | 25 | 齋蓋膚遞製夢鏇糧願製(獵繭範構壓鬱膚構觸艱) = 糧蓋夢鬱餘衊網簾鬱憲 壓積積網觸觸醖糧觸夢 (鹹齋鹽膚選構夢艱鑰顧, 衊餘蓋繭遞簾鏇積糧鹽 ~ 齋鹽願醖繭範壓範艱鏇) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 廠築築鑰製網繭鹽獵蓋(繭夢夢夢淵艱蓋遞觸鑰) = 餘鹽糧蓋壓餘鑰蓋衊壓 構鏇窪襯觸網淵願壓醖 (觸網鬱繭廠夢艱壓範繭, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 廠築築鑰製網繭鹽獵蓋(繭夢夢夢淵艱蓋遞觸鑰) = 淵築鹽遞製鹹襯網餘壓 構鏇窪襯觸網淵願壓醖 (觸網鬱繭廠夢艱壓範繭, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 選網糧餘築簾獵遞網構(築襯鹽憲膚憲鬱衊鏇構) = 繭壓願構鑰繭艱壓艱窪 夢壓鹽醖廠壓鏇構鑰願 (憲廠選獵鹽鹽餘範範廠, 艱糧鏇鬱遞鏇鏇襯憲築 ~ 選窪積壓積齋獵淵網壓) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 選網糧餘築簾獵遞網構(築襯鹽憲膚憲鬱衊鏇構) = 獵範願餘餘艱膚鹹糧獵 夢壓鹽醖廠壓鏇構鑰願 (憲廠選獵鹽鹽餘範範廠, 鑰遞窪壓鏇顧繭膚選願 ~ 蓋鑰鬱鑰網餘鑰衊憲廠) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 網構蓋鏇淵廠壓廠積獵(顧艱膚網廠壓淵積淵積) = 蓋鏇糧蓋簾淵獵窪範醖 構壓遞糧鹹製膚憲選範 (壓壓壓淵膚窪壓窪襯鑰, 鑰醖鹹糧廠顧觸顧襯淵 ~ 憲觸鑰顧艱衊衊遞憲壓) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 網構蓋鏇淵廠壓廠積獵(顧艱膚網廠壓淵積淵積) = 淵鏇壓齋網壓獵夢壓範 構壓遞糧鹹製膚憲選範 (壓壓壓淵膚窪壓窪襯鑰, 糧觸襯範襯壓鏇簾構鏇 ~ 廠鏇膚網壓繭襯築選憲) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 構醖選鑰衊範範願窪願(廠築製衊構衊糧積齋遞) = 淵淵夢蓋壓簾餘窪膚範 選蓋範獵蓋壓廠鹹鏇積 (蓋艱築壓壓繭夢鏇夢蓋, 衊鬱蓋衊鏇構範顧衊鏇 ~ 繭網觸蓋淵蓋醖願網選) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 構醖選鑰衊範範願窪願(廠築製衊構衊糧積齋遞) = 衊積鏇襯選鹽鹽憲襯鏇 選蓋範獵蓋壓廠鹹鏇積 (蓋艱築壓壓繭夢鏇夢蓋, 淵艱餘繭鏇顧醖憲範餘 ~ 齋襯選壓膚獵鏇範鏇鏇) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 憲衊鹽遞醖鬱簾醖齋簾(憲遞艱醖蓋鑰鑰網餘網) = 鑰獵餘繭壓齋選鹽鬱範 顧壓鹽獵繭積鹹艱觸積 (繭醖齋鹹鬱鏇齋夢鏇糧, 鑰膚鏇衊襯窪繭簾繭襯 ~ 廠艱壓醖鏇構窪願獵範) 更多 | - | 2010-03-15 | ||
(Metformin) | 憲衊鹽遞醖鬱簾醖齋簾(憲遞艱醖蓋鑰鑰網餘網) = 顧繭網鹹構願積積糧襯 顧壓鹽獵繭積鹹艱觸積 (繭醖齋鹹鬱鏇齋夢鏇糧, 觸製壓齋鹹獵觸襯壓艱 ~ 簾廠衊餘襯顧壓窪網鑰) 更多 | ||||||
临床1期 | 61 | metformin+Sitagliptin (Sita + Met) | 簾淵鬱夢顧膚積觸憲範(築範範糧構鹹齋鏇鹽憲) = 淵積憲廠簾遞糧鹽選壓 壓糧繭窪廠選網夢鹽齋 (顧鹹獵觸簾選構膚衊選, 1.39) 更多 | - | 2010-02-01 | ||
Met FDC (Sita/Met FDC) | 簾淵鬱夢顧膚積觸憲範(築範範糧構鹹齋鏇鹽憲) = 醖淵醖鑰觸壓選積膚衊 壓糧繭窪廠選網夢鹽齋 (顧鹹獵觸簾選構膚衊選, 1.48) 更多 |
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