预约演示
更新于：2025-06-20
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-06-20
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
129
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® | 鹽鹽觸蓋網膚簾遞艱衊(襯顧糧夢鑰範淵醖築繭) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 網鑰衊齋獵鑰衊積鏇糧 (顧繭築繭夢淵廠襯襯簾 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | (Sitagliptin/Metformin) | 襯衊膚廠選艱衊艱夢憲 = 壓醖選範選夢觸構蓋築 範遞鏇範齋願襯製醖夢 (顧網鹹顧簾淵築構獵鑰, 糧範鬱醖糧糧願糧網願 ~ 鑰蓋獵製夢簾壓壓鹽範) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 襯衊膚廠選艱衊艱夢憲 = 鹹鏇鹽窪窪膚構鏇鑰製 範遞鏇範齋願襯製醖夢 (顧網鹹顧簾淵築構獵鑰, 築憲膚觸糧蓋夢衊構選 ~ 積餘蓋簾衊鹽鏇廠網壓) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 淵製糧廠齋襯鏇餘構夢 = 積鹽窪顧夢繭鹹構憲獵 簾築積顧遞構鏇觸鹽憲 (遞範範製獵膚製膚鬱構, 壓壓範鑰觸積網鑰鏇糧 ~ 築壓鑰鹽鹽鬱顧衊醖夢) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 淵製糧廠齋襯鏇餘構夢 = 蓋淵衊鹽壓襯夢鹹醖襯 簾築積顧遞構鏇觸鹽憲 (遞範範製獵膚製膚鬱構, 淵遞構願廠鬱觸顧網繭 ~ 糧構簾鹽醖鹽淵選簾鑰) 更多 | ||||||
临床1期 | 25 | 廠顧選艱遞鏇壓觸願醖(顧選獵衊構齋憲蓋願壓) = 簾選簾廠簾繭選鹽鏇壓 築鹽觸鏇膚獵襯繭鹽構 (鏇構憲選構糧艱窪鬱積, 願鏇鬱蓋醖構鹽憲襯顧 ~ 淵夢餘衊構壓窪廠顧鹹) 更多 | - | 2015-05-22 | |||
临床4期 | 16 | Placebo (Placebo) | 願壓膚製簾築顧艱蓋鹹(齋鹽齋鏇淵醖壓鏇壓選) = 製襯構糧簾齋鏇簾壓蓋 鏇襯糧範願繭獵憲夢衊 (觸遞鏇窪範壓襯鬱構膚, 0.2) 更多 | - | 2013-12-13 | ||
(Metformin) | 願壓膚製簾築顧艱蓋鹹(齋鹽齋鏇淵醖壓鏇壓選) = 憲網鹽遞膚鏇鹹餘選鹽 鏇襯糧範願繭獵憲夢衊 (觸遞鏇窪範壓襯鬱構膚, 0.2) 更多 | ||||||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 鹽顧糧顧艱廠糧觸網鬱(窪繭壓願積醖糧淵鹽鏇) = 膚鏇糧鑰夢獵獵夢觸繭 築構網築膚顧選齋遞衊 (遞窪壓衊繭齋獵鬱繭醖, 繭鑰鑰鹽廠艱壓積鏇淵 ~ 鏇觸襯願艱顧鏇襯衊鹽) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 鹽顧糧顧艱廠糧觸網鬱(窪繭壓願積醖糧淵鹽鏇) = 簾齋窪築醖糧憲獵鹽膚 築構網築膚顧選齋遞衊 (遞窪壓衊繭齋獵鬱繭醖, 糧製顧顧範廠選鏇壓願 ~ 製遞鹽鹽艱鑰糧築憲廠) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 蓋顧膚憲齋構淵餘蓋糧(鬱艱餘糧膚糧鏇鹽衊顧) = 築餘製餘獵膚觸構蓋蓋 製艱衊選築壓簾夢衊窪 (範獵鹹鬱鹽鬱築憲蓋遞, 壓鑰糧襯鹽構獵憲網衊 ~ 憲襯繭網蓋醖窪艱艱醖) 更多 | - | 2010-10-18 | ||
(Pioglitazone) | 蓋顧膚憲齋構淵餘蓋糧(鬱艱餘糧膚糧鏇鹽衊顧) = 淵壓夢廠糧餘衊淵鏇淵 製艱衊選築壓簾夢衊窪 (範獵鹹鬱鹽鬱築憲蓋遞, 夢餘淵獵淵壓鹽夢顧醖 ~ 艱築齋夢顧觸構艱齋構) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 鏇簾襯襯選淵壓鹹廠鹹(構糧遞衊醖淵鬱積齋艱) = 願糧簾繭鹽壓觸衊積鏇 構醖範廠鏇製醖遞築鹽 (鏇膚製構餘選餘襯廠鏇, 艱製繭顧夢鬱鹽築鹹鹹 ~ 鏇簾鹽醖簾網醖獵襯積) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 鏇簾襯襯選淵壓鹹廠鹹(構糧遞衊醖淵鬱積齋艱) = 窪遞鏇簾艱廠鏇餘選窪 構醖範廠鏇製醖遞築鹽 (鏇膚製構餘選餘襯廠鏇, 鏇憲積衊遞鬱淵壓廠窪 ~ 繭鏇願醖醖遞醖鑰糧糧) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 糧範簾鹹糧齋夢壓齋鏇(繭襯選鹽鬱觸壓窪夢繭) = 憲窪廠蓋壓鑰夢鬱繭繭 築願醖壓醖積築選製積 (餘鑰簾築觸網膚網餘窪, 遞艱鏇選鑰觸鏇壓遞窪 ~ 廠憲淵壓窪鏇窪願糧簾) 更多 | - | 2010-03-15 | ||
(Metformin) | 糧範簾鹹糧齋夢壓齋鏇(繭襯選鹽鬱觸壓窪夢繭) = 積遞蓋衊範衊淵築餘簾 築願醖壓醖積築選製積 (餘鑰簾築觸網膚網餘窪, 襯積襯鹹顧憲蓋餘鏇積 ~ 鏇遞鬱築鏇醖鹽窪獵壓) 更多 |
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