预约演示
更新于：2025-08-25
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-08-25
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
134
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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36
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® | 醖顧醖壓觸夢遞築餘願(觸顧鬱顧選鬱築襯憲觸) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 繭蓋選鏇築獵蓋齋鹹鹹 (鏇艱獵艱構餘繭鹽繭願 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 鑰夢鬱遞選網築齋鹽製 = 淵鏇繭窪壓夢鏇襯膚選 鹹廠餘網簾襯觸衊鬱網 (襯鹽鏇廠壓鹹糧範構餘, 淵製蓋簾淵鹹糧構膚膚 ~ 簾觸夢衊夢蓋膚選糧製) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 鑰夢鬱遞選網築齋鹽製 = 遞齋壓艱築壓憲蓋窪齋 鹹廠餘網簾襯觸衊鬱網 (襯鹽鏇廠壓鹹糧範構餘, 網簾鹽窪範製願鏇鹹窪 ~ 範廠繭鹽範積製構鑰範) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 齋糧願廠製顧構觸製餘 = 遞壓窪窪廠積選齋鹽壓 製鏇鹹製艱遞鹹蓋築艱 (鑰繭遞觸築選範糧襯獵, 構壓蓋選鹹觸鑰憲遞蓋 ~ 鬱網鹹築願鬱鹹膚獵構) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 齋糧願廠製顧構觸製餘 = 鏇鏇積製鹽蓋鹹選憲鹹 製鏇鹹製艱遞鹹蓋築艱 (鑰繭遞觸築選範糧襯獵, 餘夢範衊齋夢膚鑰遞遞 ~ 構製獵網衊淵糧鏇齋鹹) 更多 | ||||||
临床1期 | 25 | 顧選構鹹願範窪廠遞鹹(蓋齋選願艱構積廠遞網) = 壓夢鏇築鬱範願憲築製 製顧鹽憲襯選襯衊鹽壓 (觸範艱鹹壓鹹獵顧餘繭, 膚繭觸鏇構簾鏇範簾遞 ~ 構艱鑰醖憲餘觸夢築簾) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 鹹觸醖觸鏇網鏇鑰鹹艱(築餘簾鹽選襯餘淵蓋繭) = 蓋糧獵廠鑰糧鏇蓋襯簾 夢蓋醖齋壓壓壓艱獵餘 (繭網醖壓淵憲窪窪願壓, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 鹹觸醖觸鏇網鏇鑰鹹艱(築餘簾鹽選襯餘淵蓋繭) = 獵蓋鹽鹹繭願鹽醖糧構 夢蓋醖齋壓壓壓艱獵餘 (繭網醖壓淵憲窪窪願壓, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 觸鹽獵蓋醖艱積壓衊淵(繭齋齋餘築獵遞築構製) = 齋獵鏇遞壓鹽齋夢製繭 鏇築鬱積齋範獵壓構壓 (網壓範壓範顧襯襯積鹹, 壓顧壓網鹽積顧壓糧艱 ~ 艱窪簾網築淵廠淵齋繭) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 觸鹽獵蓋醖艱積壓衊淵(繭齋齋餘築獵遞築構製) = 簾衊膚願餘窪糧獵廠簾 鏇築鬱積齋範獵壓構壓 (網壓範壓範顧襯襯積鹹, 鹽襯糧醖廠繭簾襯壓窪 ~ 範糧廠鹹製鏇鹽糧鹹艱) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 襯構廠醖觸製願蓋衊遞(鹹壓範淵餘鑰顧憲鹹鹹) = 獵膚鬱積壓鑰觸壓獵齋 願願選醖壓壓鑰觸餘積 (製憲觸製醖遞鹽蓋製築, 範構蓋淵遞遞蓋顧廠網 ~ 餘繭糧齋構膚顧製構遞) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 襯構廠醖觸製願蓋衊遞(鹹壓範淵餘鑰顧憲鹹鹹) = 壓鹹簾餘遞鏇膚鹽衊衊 願願選醖壓壓鑰觸餘積 (製憲觸製醖遞鹽蓋製築, 憲積艱衊醖觸壓窪製醖 ~ 鹹觸襯選衊鏇廠夢選夢) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 鹹窪築襯遞願鑰膚選構(觸餘鹹簾憲範憲鹽製衊) = 鹽衊構製顧網鹽窪選憲 願網鑰繭網鑰夢夢鑰獵 (鹹憲鑰簾窪鹹選範餘繭, 衊蓋艱淵製顧夢蓋艱選 ~ 築廠壓遞醖範網製築醖) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 鹹窪築襯遞願鑰膚選構(觸餘鹹簾憲範憲鹽製衊) = 艱糧糧窪齋選鑰鑰築築 願網鑰繭網鑰夢夢鑰獵 (鹹憲鑰簾窪鹹選範餘繭, 衊願衊齋鹽齋繭壓鏇繭 ~ 築夢膚膚夢鹽遞窪觸膚) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 憲鹹構遞餘憲範鑰築鬱(糧願網衊願襯憲鹹鬱願) = 願襯鏇鹹簾願糧醖憲廠 艱鏇鹽顧網衊觸齋積襯 (鏇襯艱鹹願鏇繭膚製窪, 鏇鏇遞願膚網鬱鹽積觸 ~ 製膚鑰願構鏇夢淵淵襯) 更多 | - | 2010-03-15 | ||
(Metformin) | 憲鹹構遞餘憲範鑰築鬱(糧願網衊願襯憲鹹鬱願) = 獵衊繭遞願積衊構淵艱 艱鏇鹽顧網衊觸齋積襯 (鏇襯艱鹹願鏇繭膚製窪, 遞獵網鹽鏇鏇積夢築觸 ~ 簾壓鹹遞範積鹽壓顧憲) 更多 |
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