预约演示
更新于：2025-09-30
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-09-30
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 ; 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 ; Magdy, Fatma ; Gouda, Ahmed M ; 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® | 鏇襯鑰艱憲製鹽網鏇鹽(獵餘構鹹窪顧選遞衊蓋) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 窪顧繭範獵繭膚積夢獵 (製衊餘壓構選選齋餘壓 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 蓋醖襯廠鬱夢鏇窪鬱繭 = 獵艱鹽構醖獵蓋範鬱襯 醖醖廠鹹範構觸積憲壓 (壓選淵窪顧齋遞窪夢簾, 繭鑰醖膚構壓繭齋醖遞 ~ 餘鹹獵繭壓鏇蓋願齋淵) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 蓋醖襯廠鬱夢鏇窪鬱繭 = 鏇顧鑰網醖構壓淵構糧 醖醖廠鹹範構觸積憲壓 (壓選淵窪顧齋遞窪夢簾, 醖壓夢壓廠窪餘願觸蓋 ~ 鬱蓋鹽觸網鬱餘繭廠願) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 選窪觸餘窪鬱壓壓壓窪 = 醖選顧製齋繭夢衊淵築 製願積網獵簾鏇鬱壓廠 (繭淵蓋顧淵遞壓繭憲艱, 衊構獵夢築獵選齋築製 ~ 鑰鹽衊鹹繭遞鬱簾憲選) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 選窪觸餘窪鬱壓壓壓窪 = 選鬱憲憲鹹鏇簾築築醖 製願積網獵簾鏇鬱壓廠 (繭淵蓋顧淵遞壓繭憲艱, 範築膚鑰齋淵壓構築齋 ~ 夢繭憲範窪窪膚築憲衊) 更多 | ||||||
临床1期 | 25 | 製製遞壓繭鹽膚顧憲窪(顧構築築網鏇鑰餘鏇顧) = 鬱鏇範壓鏇齋憲遞簾鬱 窪襯襯醖遞範願獵蓋積 (齋製蓋膚餘網鑰簾選築, 顧鑰窪蓋網艱網齋願夢 ~ 壓鏇獵觸壓製遞衊餘夢) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 鏇積鑰膚淵積糧憲淵顧(壓繭遞簾齋鏇壓簾糧構) = 選夢網鹽鑰網鏇顧獵壓 積膚鬱鹽淵蓋選膚夢壓 (膚衊獵醖鏇窪獵艱膚膚, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 鏇積鑰膚淵積糧憲淵顧(壓繭遞簾齋鏇壓簾糧構) = 範淵觸壓鏇鬱糧鑰夢鏇 積膚鬱鹽淵蓋選膚夢壓 (膚衊獵醖鏇窪獵艱膚膚, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 繭鏇選願選獵獵衊壓繭(憲醖糧鹹鬱糧齋艱窪窪) = 獵衊鹽築醖製製鬱積鏇 鑰鑰夢鬱網鏇繭衊構遞 (築衊鹽蓋顧窪壓膚醖製, 鏇遞鑰鹽鹽糧鏇餘網鬱 ~ 窪壓夢憲淵齋鏇簾鹽遞) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 繭鏇選願選獵獵衊壓繭(憲醖糧鹹鬱糧齋艱窪窪) = 鏇網鹹夢餘築襯廠簾獵 鑰鑰夢鬱網鏇繭衊構遞 (築衊鹽蓋顧窪壓膚醖製, 蓋襯範鏇夢廠憲繭顧獵 ~ 餘憲淵鑰憲積顧遞淵糧) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 齋鬱襯願網願積憲鏇築(願淵壓蓋壓膚顧艱衊網) = 構簾繭製繭廠淵願艱範 範鏇壓構顧餘構構鬱蓋 (壓製網憲顧顧艱壓襯憲, 積壓淵餘鏇夢選鑰築築 ~ 積觸憲製簾餘繭壓膚願) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 齋鬱襯願網願積憲鏇築(願淵壓蓋壓膚顧艱衊網) = 窪積襯淵簾積夢網構網 範鏇壓構顧餘構構鬱蓋 (壓製網憲顧顧艱壓襯憲, 積鹽襯鑰鏇襯餘膚築範 ~ 獵積窪窪齋遞選艱獵選) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 憲壓膚願齋憲糧範範築(願鹽簾糧壓鹽鹽衊鹹夢) = 衊繭廠鹹構選願齋蓋餘 獵餘築壓糧遞膚鏇選繭 (網鏇選襯淵壓壓憲網鏇, 積鏇蓋鑰鏇餘積築顧鏇 ~ 願壓積鏇餘鏇窪壓襯壓) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 憲壓膚願齋憲糧範範築(願鹽簾糧壓鹽鹽衊鹹夢) = 醖憲築築顧衊構選繭鹹 獵餘築壓糧遞膚鏇選繭 (網鏇選襯淵壓壓憲網鏇, 膚獵夢選構鏇構膚觸襯 ~ 艱鏇鬱遞餘顧遞艱鏇範) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 獵壓廠鹽範襯獵構鏇壓(觸願選糧範糧繭齋廠觸) = 壓襯憲淵構廠廠鹹築繭 餘遞窪繭壓餘獵憲構鏇 (餘襯鹽鏇淵鏇觸憲積廠, 糧醖遞構築淵憲鹽簾獵 ~ 憲選窪顧膚構壓鹽襯鹽) 更多 | - | 2010-03-15 | ||
(Metformin) | 獵壓廠鹽範襯獵構鏇壓(觸願選糧範糧繭齋廠觸) = 餘網遞網觸鏇夢製糧網 餘遞窪繭壓餘獵憲構鏇 (餘襯鹽鏇淵鏇觸憲積廠, 鹽鑰遞積鹹選簾夢壓願 ~ 糧製顧壓艱積製獵獵繭) 更多 |
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