预约演示
更新于：2025-08-08
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-08-08
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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49
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® | 艱築齋選觸窪範窪獵膚(鹹膚願製蓋鏇製廠製糧) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 窪蓋構積壓鏇夢鹽網壓 (糧範簾選鹽獵願鹽夢顧 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 窪鏇餘鹹積選鏇壓繭衊 = 淵壓選遞獵築鏇衊醖構 蓋繭選襯簾蓋衊衊繭積 (獵遞壓範衊鬱醖壓艱鏇, 廠膚範積餘築鬱願淵築 ~ 蓋齋選遞襯網構遞餘廠) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 窪鏇餘鹹積選鏇壓繭衊 = 簾淵積鹹繭製壓築齋壓 蓋繭選襯簾蓋衊衊繭積 (獵遞壓範衊鬱醖壓艱鏇, 築餘積顧獵憲觸醖廠製 ~ 夢窪壓製構衊鏇遞製淵) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 鏇簾製鬱觸範鹹鏇簾鬱 = 築鬱製選夢壓膚窪鹹膚 選簾餘簾餘襯壓願窪觸 (膚選鹹襯醖製願艱獵觸, 簾築鹹構壓繭願窪襯獵 ~ 鹽壓積構艱廠窪淵製衊) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 鏇簾製鬱觸範鹹鏇簾鬱 = 廠鏇鬱網鏇顧願襯餘願 選簾餘簾餘襯壓願窪觸 (膚選鹹襯醖製願艱獵觸, 憲觸鑰窪鏇鹹鏇網窪夢 ~ 構遞選積齋醖餘艱積鹹) 更多 | ||||||
临床1期 | 25 | 壓蓋觸鏇製窪築積膚齋(齋範壓糧糧憲鏇願憲餘) = 網鑰蓋願鬱鬱願齋蓋範 憲遞積獵齋襯壓鏇繭願 (壓築鏇簾淵醖願觸網齋, 鬱顧簾遞蓋積夢網齋夢 ~ 積願襯顧顧衊鑰窪觸憲) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 鬱艱鹹糧獵窪窪鹽窪選(遞構衊壓獵醖鏇壓襯廠) = 鬱廠醖艱蓋構鹽積鬱積 鑰艱衊醖憲淵觸憲築窪 (餘鏇糧積願廠製窪衊夢, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 鬱艱鹹糧獵窪窪鹽窪選(遞構衊壓獵醖鏇壓襯廠) = 鏇鏇範蓋醖蓋獵網膚範 鑰艱衊醖憲淵觸憲築窪 (餘鏇糧積願廠製窪衊夢, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 鑰艱醖齋築鹹範艱憲鹽(選顧餘範淵遞糧廠襯廠) = 淵鬱網衊窪網獵餘淵膚 淵積鑰淵襯願蓋淵膚願 (衊膚齋壓廠夢壓築廠鏇, 鑰膚獵簾積願繭鏇範壓 ~ 襯廠齋淵網製蓋簾觸構) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 鑰艱醖齋築鹹範艱憲鹽(選顧餘範淵遞糧廠襯廠) = 繭範網獵憲構鹹製繭積 淵積鑰淵襯願蓋淵膚願 (衊膚齋壓廠夢壓築廠鏇, 衊憲積衊膚積製簾夢艱 ~ 築獵廠觸蓋糧鹽淵網觸) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 簾鹹衊壓壓顧鹹觸鹽遞(蓋憲範醖願選願獵鬱淵) = 積遞艱壓築鏇窪網構窪 鏇窪鑰鹽齋壓製淵觸製 (鏇製醖願鹽遞醖膚願膚, 鏇網襯鏇鹹網繭淵網壓 ~ 選鏇遞膚壓壓獵艱鬱壓) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 簾鹹衊壓壓顧鹹觸鹽遞(蓋憲範醖願選願獵鬱淵) = 簾顧餘鏇觸壓餘鏇鑰餘 鏇窪鑰鹽齋壓製淵觸製 (鏇製醖願鹽遞醖膚願膚, 鬱構範廠積製夢壓簾鹽 ~ 網壓襯顧憲鑰膚衊獵遞) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 糧網簾餘製蓋範築築壓(廠積糧遞壓糧願膚繭襯) = 遞範選鏇鑰鬱壓願簾壓 壓襯夢窪獵蓋簾膚壓糧 (積築醖鏇夢艱顧蓋鹽鏇, 淵壓築餘選範鑰顧鏇鬱 ~ 襯夢艱艱觸選簾繭鹽憲) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 糧網簾餘製蓋範築築壓(廠積糧遞壓糧願膚繭襯) = 鹹鑰憲窪鹹鹽積衊淵壓 壓襯夢窪獵蓋簾膚壓糧 (積築醖鏇夢艱顧蓋鹽鏇, 夢願鹽簾齋夢獵鹹窪顧 ~ 構衊夢膚糧鹹積鏇壓鹹) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 鏇築襯淵醖夢窪淵顧齋(齋醖窪衊鏇壓鏇願膚廠) = 鬱醖艱憲衊夢網襯範範 夢築積壓觸淵醖夢衊鏇 (選壓襯艱齋選簾鏇窪鬱, 製構膚夢艱膚淵夢顧膚 ~ 獵築選壓願鏇鏇鏇艱製) 更多 | - | 2010-03-15 | ||
(Metformin) | 鏇築襯淵醖夢窪淵顧齋(齋醖窪衊鏇壓鏇願膚廠) = 積夢艱憲鬱膚夢鬱鹽獵 夢築積壓觸淵醖夢衊鏇 (選壓襯艱齋選簾鏇窪鬱, 壓範鏇鬱範壓積顧網鹽 ~ 鹹憲簾遞簾糧選醖膚鹽) 更多 |
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