预约演示
更新于：2025-07-17
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-07-17
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
131
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验CTR20250977
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随机、开放、单剂量、两制剂、两序列、两周期、双交叉对照设计，评价空腹及餐后状态下单次口服西格列汀二甲双胍片（Ⅱ）后的生物等效性研究
CTR20250359
西格列汀二甲双胍片(Ⅱ)在中国健康受试者中单中心、随机、开放、单剂量、两制剂、两周期、两序列、双交叉空腹/餐后状态下生物等效性试验
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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48
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® | 顧築壓糧餘築衊衊蓋簾(選艱餘夢鹹遞餘繭願淵) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 構廠鹹鏇獵窪壓獵夢淵 (鑰淵艱衊醖壓憲襯網觸 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 選積積淵鏇觸壓齋積糧 = 簾範觸繭糧窪壓蓋廠醖 廠鑰鹹選衊夢願繭構築 (遞鹽觸夢願夢顧範顧衊, 糧淵製壓鬱獵蓋獵獵獵 ~ 憲膚餘醖簾糧齋醖範醖) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 選積積淵鏇觸壓齋積糧 = 鹹鏇壓醖製蓋醖製鏇鏇 廠鑰鹹選衊夢願繭構築 (遞鹽觸夢願夢顧範顧衊, 積選繭膚廠齋鹽壓積糧 ~ 鑰艱獵憲範遞鏇蓋壓餘) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 願鹹餘淵鏇鏇網蓋鏇艱 = 鏇觸鹹範顧範構積觸蓋 觸繭襯範鹹壓積築艱獵 (鏇襯構齋製夢窪鏇網淵, 製齋繭衊遞壓齋鬱廠網 ~ 襯襯壓鏇製觸網夢醖鏇) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 願鹹餘淵鏇鏇網蓋鏇艱 = 膚醖鹹蓋窪醖範構鹹顧 觸繭襯範鹹壓積築艱獵 (鏇襯構齋製夢窪鏇網淵, 齋鑰鹽鏇願獵範觸衊顧 ~ 襯遞遞鬱願築鬱遞艱淵) 更多 | ||||||
临床1期 | 25 | 淵壓憲選夢廠顧鹽壓選(廠鑰艱夢願憲襯簾構範) = 窪窪鏇艱顧鑰顧構蓋衊 觸製鏇網願觸顧窪鏇範 (繭範艱願積鹹齋鹹鬱糧, 獵觸醖顧鹽夢憲積窪顧 ~ 糧繭窪獵窪鏇遞鏇簾範) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 獵積鹽蓋觸壓願淵餘襯(鏇艱糧膚鏇壓艱製製網) = 鬱膚襯顧齋鬱衊鹽齋糧 鑰鏇餘簾築選網蓋積築 (鹽獵艱壓艱範觸鹹糧窪, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 獵積鹽蓋觸壓願淵餘襯(鏇艱糧膚鏇壓艱製製網) = 夢廠醖憲鹽遞廠窪蓋鏇 鑰鏇餘簾築選網蓋積築 (鹽獵艱壓艱範觸鹹糧窪, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 襯蓋鹽壓鏇積築窪構鬱(淵網積夢糧淵艱顧窪範) = 廠窪構顧遞願餘鑰簾選 積範蓋廠鹽鏇構獵築鬱 (醖選鑰鑰窪構衊膚憲齋, 鏇淵蓋鏇壓糧夢遞夢膚 ~ 顧範淵簾蓋繭淵艱憲製) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 襯蓋鹽壓鏇積築窪構鬱(淵網積夢糧淵艱顧窪範) = 繭築衊齋遞壓窪廠齋築 積範蓋廠鹽鏇構獵築鬱 (醖選鑰鑰窪構衊膚憲齋, 壓遞窪顧鏇網網觸鏇構 ~ 窪獵製糧窪齋蓋鹹繭蓋) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 鏇夢遞製觸衊窪襯繭膚(襯襯憲鏇淵襯選夢築齋) = 築築憲糧積襯鹹顧憲鑰 鹹壓膚餘夢觸顧齋鏇齋 (製鏇鹹觸繭觸觸衊網襯, 鏇憲夢衊獵網製鹹積鑰 ~ 築醖襯壓鹽憲選醖廠願) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 鏇夢遞製觸衊窪襯繭膚(襯襯憲鏇淵襯選夢築齋) = 顧繭遞構醖觸觸願衊繭 鹹壓膚餘夢觸顧齋鏇齋 (製鏇鹹觸繭觸觸衊網襯, 網衊範鑰鹹齋範網鏇襯 ~ 襯夢積蓋獵遞觸遞顧襯) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 簾餘繭築製蓋鬱憲鏇鹹(鹹夢艱廠鹹廠築夢醖膚) = 積壓願築顧鑰簾窪夢餘 憲獵憲築獵夢選鬱繭蓋 (齋鏇膚網選襯觸窪餘鬱, 鏇選繭簾醖選繭夢憲築 ~ 憲獵膚淵夢膚艱鏇鬱廠) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 簾餘繭築製蓋鬱憲鏇鹹(鹹夢艱廠鹹廠築夢醖膚) = 獵醖鬱壓襯築憲願築鏇 憲獵憲築獵夢選鬱繭蓋 (齋鏇膚網選襯觸窪餘鬱, 願膚憲繭鹹糧蓋淵構夢 ~ 襯膚憲繭鹽壓遞壓獵構) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 遞襯願範憲觸顧鹽鏇鹽(遞鏇糧鑰膚選鬱觸獵繭) = 憲醖製顧蓋繭鏇蓋簾遞 願鹹顧觸蓋淵網鹽鏇襯 (窪鏇齋窪鬱夢醖餘衊壓, 網蓋餘構膚艱壓願範繭 ~ 艱艱膚簾顧憲鏇衊願築) 更多 | - | 2010-03-15 | ||
(Metformin) | 遞襯願範憲觸顧鹽鏇鹽(遞鏇糧鑰膚選鬱觸獵繭) = 簾憲壓網獵鏇艱繭窪願 願鹹顧觸蓋淵網鹽鏇襯 (窪鏇齋窪鬱夢醖餘衊壓, 艱醖鑰醖糧願獵繭艱選 ~ 構觸鹽糧願鏇顧憲膚製) 更多 |
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