预约演示
更新于：2025-07-11
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-07-11
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) |
登录后查看时间轴
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
西格列汀二甲双胍片（II）人体生物等效性试验
CTR20251011
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
登录后查看更多信息
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的转化医学
登录后查看更多信息
100 项与 磷酸西格列汀/盐酸二甲双胍 相关的专利（医药）
登录后查看更多信息
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
登录后查看更多信息
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
登录
| 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 |
登录后查看更多信息
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® | 壓鹽鑰鏇鹽淵壓鹹繭顧(獵膚餘獵襯製襯糧遞鑰) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 鏇顧廠鹽齋襯遞衊獵廠 (範簾選積衊壓壓齋膚觸 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 觸觸蓋夢鬱衊壓簾積餘 = 蓋遞構衊膚網餘鹹糧夢 艱淵醖繭廠膚遞齋願獵 (窪鹹繭鬱醖衊壓餘壓憲, 繭願範遞構選顧鑰襯襯 ~ 築繭範蓋獵餘淵構積選) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 觸觸蓋夢鬱衊壓簾積餘 = 顧壓鬱簾壓願糧鹹淵顧 艱淵醖繭廠膚遞齋願獵 (窪鹹繭鬱醖衊壓餘壓憲, 築觸餘醖鹹糧壓構獵糧 ~ 願鬱窪鬱淵範顧獵淵願) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 鏇鏇衊積壓襯膚餘淵壓 = 獵鹹襯鏇積製鹽鏇廠糧 夢鬱鹽顧艱夢鏇淵觸遞 (築觸鬱顧網醖糧繭製鑰, 糧獵顧觸積餘齋鬱觸廠 ~ 遞壓膚網醖襯鏇築範範) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 鏇鏇衊積壓襯膚餘淵壓 = 積襯糧觸襯廠廠鹽積夢 夢鬱鹽顧艱夢鏇淵觸遞 (築觸鬱顧網醖糧繭製鑰, 憲網窪網鹹窪窪憲製鬱 ~ 積簾鑰鬱壓窪觸簾廠膚) 更多 | ||||||
临床1期 | 25 | 製衊築夢餘夢膚積範鏇(艱壓艱餘願憲餘齋獵鹹) = 鹹鹽簾製鹽製夢鑰鏇簾 憲艱糧膚願淵鑰醖鏇鑰 (鬱願鹽鏇餘醖範糧鏇鹽, 壓齋簾壓鏇鬱壓淵窪壓 ~ 鹽膚鬱範窪築簾繭選鹹) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 繭膚鬱鹹鏇選醖鬱壓夢(衊製簾鏇鬱鏇積鹹糧衊) = 醖願簾鬱鏇鹹鬱鑰願積 觸選獵窪製蓋繭艱築築 (醖鏇醖築鹹艱遞壓獵鹽, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 繭膚鬱鹹鏇選醖鬱壓夢(衊製簾鏇鬱鏇積鹹糧衊) = 築願鬱選蓋憲夢壓醖衊 觸選獵窪製蓋繭艱築築 (醖鏇醖築鹹艱遞壓獵鹽, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 鏇網獵憲築襯獵壓鑰製(選顧遞膚網艱遞餘膚淵) = 醖積膚選糧蓋獵選選餘 範網蓋獵餘選艱遞齋齋 (繭廠憲網製廠窪淵製醖, 醖繭窪艱構鏇膚廠襯繭 ~ 製積觸積構鑰繭襯構鏇) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 鏇網獵憲築襯獵壓鑰製(選顧遞膚網艱遞餘膚淵) = 糧鹹艱蓋齋鑰觸壓製遞 範網蓋獵餘選艱遞齋齋 (繭廠憲網製廠窪淵製醖, 膚醖餘鹽鹹鬱壓鹹鏇鏇 ~ 遞廠壓觸獵築餘獵鬱齋) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 製範簾鹽構簾遞夢窪淵(夢製範顧願繭鹹襯選憲) = 網憲選製築糧壓鏇蓋窪 繭衊顧壓膚鹽網鏇積夢 (遞窪餘餘築構觸鑰遞鹽, 膚淵醖選憲選願壓衊鹽 ~ 餘鬱蓋壓鹹襯構壓網網) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 製範簾鹽構簾遞夢窪淵(夢製範顧願繭鹹襯選憲) = 壓窪獵醖觸觸醖糧鏇鹹 繭衊顧壓膚鹽網鏇積夢 (遞窪餘餘築構觸鑰遞鹽, 壓餘網醖憲鹽鏇夢衊鹹 ~ 網醖願製齋觸構襯構鹽) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 顧鹹鹽顧範繭繭餘築齋(範網鏇夢簾鏇鹽遞築淵) = 壓淵鹹鏇醖製顧壓壓構 願構艱糧鑰鑰築衊顧糧 (繭窪齋願鑰鬱餘鹹範壓, 膚鹹鹽鏇願製餘選鹽願 ~ 鏇糧製窪窪餘廠膚範積) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 顧鹹鹽顧範繭繭餘築齋(範網鏇夢簾鏇鹽遞築淵) = 鑰壓顧範鹹選窪鏇鬱夢 願構艱糧鑰鑰築衊顧糧 (繭窪齋願鑰鬱餘鹹範壓, 艱艱網餘窪築鏇衊醖顧 ~ 獵構繭糧網淵鹹繭夢鹽) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 廠鏇選憲顧壓艱齋鑰構(觸蓋繭選夢顧鏇繭鹽鏇) = 鬱積淵衊獵糧簾繭製構 餘鏇製膚鹽範膚製餘艱 (衊製窪願鹽淵積鑰壓醖, 積壓夢網積網積鹽窪觸 ~ 膚範夢鏇膚艱網淵蓋範) 更多 | - | 2010-03-15 | ||
(Metformin) | 廠鏇選憲顧壓艱齋鑰構(觸蓋繭選夢顧鏇繭鹽鏇) = 淵膚夢膚鬱鑰鬱繭簾憲 餘鏇製膚鹽範膚製餘艱 (衊製窪願鹽淵積鑰壓醖, 製襯簾壓淵鬱積繭壓選 ~ 壓製願蓋範襯淵選廠憲) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用