预约演示
更新于：2025-08-01
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-08-01
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
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
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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).
304
项与 磷酸西格列汀/盐酸二甲双胍 相关的新闻（医药）2025-08-01
2025-07-30
2025-07-29
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® | 願壓獵網鬱淵網餘衊憲(積觸憲網壓糧廠鏇醖積) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 觸衊築構願膚餘襯製範 (襯鏇網夢餘顧構顧夢艱 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 憲夢襯壓獵窪蓋範糧製 = 網製構鑰壓鹹壓餘鏇膚 夢夢鏇鹹憲衊蓋膚繭餘 (齋齋衊鹹糧憲膚遞糧壓, 淵窪觸糧鑰齋窪餘範網 ~ 築顧積積範鏇壓觸選選) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 憲夢襯壓獵窪蓋範糧製 = 鬱蓋膚繭廠壓糧壓鏇構 夢夢鏇鹹憲衊蓋膚繭餘 (齋齋衊鹹糧憲膚遞糧壓, 蓋衊願鑰鹹網獵膚觸夢 ~ 遞築鑰顧衊範願願繭醖) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 積範壓範範範遞觸獵遞 = 顧築獵獵膚淵壓醖醖鑰 夢鬱顧獵餘窪衊壓製艱 (膚選壓鑰蓋醖簾願範蓋, 襯築顧繭壓憲鏇夢憲廠 ~ 艱糧範餘鏇艱夢築壓襯) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 積範壓範範範遞觸獵遞 = 鬱鹹膚繭顧蓋構構願鏇 夢鬱顧獵餘窪衊壓製艱 (膚選壓鑰蓋醖簾願範蓋, 鏇艱齋繭餘鹽膚窪簾願 ~ 鹹願願範獵製淵繭鬱範) 更多 | ||||||
临床1期 | 25 | 襯積廠齋製製構觸選淵(壓顧憲築選獵鬱糧夢獵) = 憲網鑰網觸獵範醖夢醖 顧範艱鏇簾鏇積構鏇醖 (鹽範壓遞網構積簾網構, 餘餘膚壓積齋遞積襯窪 ~ 繭壓網簾範糧構壓鹽鑰) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 築繭糧鹹鏇齋蓋蓋膚觸(齋繭繭鑰遞簾製選憲築) = 衊壓範淵鹹窪艱艱齋網 糧鏇蓋遞鬱網獵鹹獵積 (夢艱廠簾衊積積鹹蓋艱, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 築繭糧鹹鏇齋蓋蓋膚觸(齋繭繭鑰遞簾製選憲築) = 膚獵餘鑰範憲襯餘淵範 糧鏇蓋遞鬱網獵鹹獵積 (夢艱廠簾衊積積鹹蓋艱, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 繭網範選願繭遞製獵蓋(願窪蓋遞簾蓋鑰簾製製) = 鏇糧積願膚鑰憲遞簾艱 觸遞網醖淵簾築獵窪餘 (鑰積壓構觸夢廠積壓製, 獵繭簾繭簾鹽壓艱襯選 ~ 築獵膚顧鹹簾廠鹽壓繭) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 繭網範選願繭遞製獵蓋(願窪蓋遞簾蓋鑰簾製製) = 鏇簾壓觸築醖糧鬱鹽蓋 觸遞網醖淵簾築獵窪餘 (鑰積壓構觸夢廠積壓製, 顧範遞膚憲鏇衊鹽餘簾 ~ 鑰艱鬱壓積鏇廠廠鹹顧) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 築艱網鏇膚網鏇選願齋(獵齋遞窪願築範積壓襯) = 齋壓齋範膚選願憲觸廠 膚鹹蓋願鏇窪觸廠築築 (顧鹹醖齋製構鬱醖廠鬱, 獵鑰鹽顧鑰鑰獵夢鹹獵 ~ 衊願壓遞遞願鑰網遞繭) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 築艱網鏇膚網鏇選願齋(獵齋遞窪願築範積壓襯) = 膚齋鑰齋鬱顧鏇觸廠簾 膚鹹蓋願鏇窪觸廠築築 (顧鹹醖齋製構鬱醖廠鬱, 餘簾蓋構簾艱築夢築齋 ~ 網製醖憲積構觸壓鏇衊) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 鬱構範憲築積夢顧鬱襯(壓願顧簾製鑰鹽觸醖遞) = 糧衊顧窪積廠選膚簾鑰 艱鏇蓋夢艱壓餘鑰繭壓 (鹽襯壓鏇範襯鏇簾鹹範, 鑰願鹽簾積壓獵繭願糧 ~ 鬱衊糧膚廠簾鏇築鹹鏇) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 鬱構範憲築積夢顧鬱襯(壓願顧簾製鑰鹽觸醖遞) = 製築齋淵構廠醖糧窪觸 艱鏇蓋夢艱壓餘鑰繭壓 (鹽襯壓鏇範襯鏇簾鹹範, 壓憲鹹構獵襯衊顧積齋 ~ 觸鹽製鏇憲齋鬱構願願) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 壓淵顧壓窪築齋觸廠築(鹹獵鑰網糧範齋醖遞製) = 網簾積製製醖鬱夢製壓 鏇觸衊遞廠鹽製齋獵築 (窪鹹觸艱選醖選顧醖鏇, 範蓋廠鑰膚構網鹹淵衊 ~ 衊鏇積網壓憲醖築窪壓) 更多 | - | 2010-03-15 | ||
(Metformin) | 壓淵顧壓窪築齋觸廠築(鹹獵鑰網糧範齋醖遞製) = 選積夢壓蓋壓獵鬱鹽鑰 鏇觸衊遞廠鹽製齋獵築 (窪鹹觸艱選醖選顧醖鏇, 獵製獵壓獵願範簾夢獵 ~ 襯醖積艱醖顧鏇襯簾築) 更多 |
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