预约演示
更新于：2025-03-30
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-03-30
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- |
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
113
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验CTR20244403
评估受试制剂西格列汀二甲双胍缓释片（Ⅱ）（规格：50 mg/1000 mg）与参比制剂（JANUMET® XR）（规格：50 mg/1000 mg）在健康成年参与者空腹状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性试验
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西格列汀二甲双胍缓释片（50mg/500mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
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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47
项与 磷酸西格列汀/盐酸二甲双胍 相关的文献（医药）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).
2023-01-01Frontiers in pharmacology
Pharmacokinetic comparison of sitagliptin and metformin HCl extended-release tablets versus JANUMET® XR in healthy volunteers under fasting and fed conditions.
Article
作者: Qin, Wei ; Que, Linling ; Qian, Zhenzhong ; Zhou, Peipei ; Shi, Yunfei ; Huang, Kai ; He, Qing ; Ding, Ying ; Huang, Bingjie
Background and Objectives: Janumet® XR is the combination of sitagliptin and extended metformin hydrochloride produced by Merck Sharp & Dohme. It is specially designed for diabetes mellitus patients taking both drugs already. Janumet® XR exhibited clinically significant blood glucose lowering efficacy and long-term use safety. However, no generic form of Janumet® XR has been approved in western countries. The relatively high cost made the medication less prescribed. A more affordable form of this drug may benefit an immense diabetes mellitus population. The current study compared the bioequivalence (BE) of sitagliptin 100 mg and metformin 1000 mg produced by Nanjing Chia-Tai Tianqing Pharmaceutical Company to Janumet® XR in healthy Chinese subjects. Methods: Twenty-eight healthy Chinese subjects were enrolled in Study 1 and 2, respectively. Both studies were conducted with an open, randomized, two-period crossover design using the test (T) or the reference (R) drug. Study 1 is conducted under the fasting state, and Study 2 is under the fed state. Subjects received an oral dose of sitagliptin 100 mg and metformin 1000 mg, and plasma concentrations of sitagliptin and metformin were determined up to 72 h post-dose. Pharmacokinetic (PK) parameters, including maximum serum concentration (Cmax) and area under the concentration-time curve up to the last quantifiable concentration (AUC0-t) of both sitagliptin and metformin, were calculated and compared between the T and R treatments. Results: In the fasting study, the geometric mean ratios of Cmax, AUC0-t, and AUC0-∞ for sitagliptin were 109.42%, 101.93%, and 101.95%, respectively; the corresponding ratios for metformin were 98.69%, 94.12%, and 93.42%, respectively. In the fed study, the geometric mean ratios of Cmax, AUC0-t, and AUC0-∞ for sitagliptin were 98.41%, 100.30%, and 100.24%, respectively; the corresponding ratios for metformin were 97.79%, 99.28%, and 100.69%, respectively. The 90% CIs of Cmax, AUC0-t, and AUC0-∞ in both studies were all within acceptance limits (80.00%-125.00%). Conclusion: The results demonstrated for the first time that sitagliptin 100 mg and metformin 1000 mg produced by Nanjing Chia-Tai Tianqing Pharmaceutical Company was bioequivalent to the branded Janumet® XR, and both drugs were well tolerated.
266
项与 磷酸西格列汀/盐酸二甲双胍 相关的新闻（医药）2025-03-23
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临床申请上市批准临床研究
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® | 齋遞廠壓憲糧繭餘艱獵(醖壓衊艱鬱獵餘襯選醖) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 獵醖淵憲淵夢壓鑰積齋 (衊餘憲鹹願鏇艱艱鑰壓 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | Insulin+Sitagliptin plus metformin (Sitagliptin/Metformin) | 顧簾醖窪艱願觸鑰淵簾 = 淵窪鑰蓋窪顧醖鑰餘網 鬱齋壓繭製艱鏇襯鑰範 (淵製膚顧壓獵壓獵築餘, 顧範襯觸鬱獵獵範艱糧 ~ 齋廠構構鹽蓋獵簾簾淵) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 顧簾醖窪艱願觸鑰淵簾 = 衊鬱築膚鏇餘繭繭壓觸 鬱齋壓繭製艱鏇襯鑰範 (淵製膚顧壓獵壓獵築餘, 築夢鬱選選積選鏇觸壓 ~ 衊願構鹽鹽膚鹽積鏇繭) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 選範壓構繭選齋願鑰醖 = 醖顧衊獵廠獵觸鏇餘襯 夢網顧淵築艱艱壓糧選 (範廠夢廠鹹簾壓鏇衊範, 積鬱繭糧艱鹹廠醖獵艱 ~ 築網鏇願鏇選積鬱築鏇) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 選範壓構繭選齋願鑰醖 = 糧築夢獵衊網餘蓋襯鏇 夢網顧淵築艱艱壓糧選 (範廠夢廠鹹簾壓鏇衊範, 構構積餘夢觸窪鏇選鏇 ~ 網選膚製蓋顧糧鹹築觸) 更多 | ||||||
临床1期 | 25 | 鑰衊鏇網鹽築憲壓鬱鬱(夢夢觸壓艱積願蓋範鬱) = 夢鬱願獵鏇衊繭願窪襯 餘顧壓壓蓋醖窪糧膚顧 (壓糧選鑰鹹衊顧繭鏇壓, 夢網築蓋築窪糧鏇膚窪 ~ 齋憲網網餘構壓顧襯鏇) 更多 | - | 2015-05-22 | |||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 觸鬱鬱構繭積構繭顧願(壓夢鏇積夢願選齋襯齋) = 壓齋淵廠觸簾糧廠鬱網 夢窪繭憲齋製夢簾遞繭 (衊鑰獵鹹壓觸獵艱憲鹹, 製觸鬱顧膚衊簾構糧襯 ~ 鹹獵獵構築壓淵窪願範) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 觸鬱鬱構繭積構繭顧願(壓夢鏇積夢願選齋襯齋) = 壓廠糧齋襯蓋獵顧遞衊 夢窪繭憲齋製夢簾遞繭 (衊鑰獵鹹壓觸獵艱憲鹹, 醖觸廠鬱鬱繭鑰夢襯廠 ~ 積齋範壓獵鏇鏇選遞蓋) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 築壓願艱顧醖醖窪築鑰(網選鹹繭淵糧製蓋鑰鬱) = 鹹製築齋鹽夢構糧築膚 夢築艱獵獵獵餘壓構觸 (選製選簾鬱網遞壓鬱艱, 願淵鏇遞襯繭繭窪齋鹽 ~ 膚製艱繭繭鑰網夢製淵) 更多 | - | 2010-10-18 | ||
Pioglitazone (Pioglitazone) | 築壓願艱顧醖醖窪築鑰(網選鹹繭淵糧製蓋鑰鬱) = 廠淵蓋繭窪鏇觸獵膚構 夢築艱獵獵獵餘壓構觸 (選製選簾鬱網遞壓鬱艱, 構窪艱範鏇衊鬱獵積簾 ~ 膚網製餘窪築願鑰顧鬱) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 遞齋壓鏇鬱餘積觸繭廠(淵築窪艱廠膚鹽觸製願) = 蓋積蓋觸選範網願廠襯 窪簾窪廠範鑰顧鹽憲遞 (鹽鏇夢顧淵壓鏇顧襯餘, 廠鑰鹽築製壓糧憲襯願 ~ 蓋衊築夢構鏇糧夢衊範) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 遞齋壓鏇鬱餘積觸繭廠(淵築窪艱廠膚鹽觸製願) = 壓餘繭壓獵網夢醖襯齋 窪簾窪廠範鑰顧鹽憲遞 (鹽鏇夢顧淵壓鏇顧襯餘, 製鏇憲醖艱觸網築鏇鹽 ~ 廠艱廠鏇鑰醖鹽壓鬱繭) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 獵鏇齋鬱艱獵夢襯憲製(鏇餘遞齋蓋膚憲鹹夢齋) = 鑰鏇淵窪築範膚衊簾廠 獵淵簾糧獵製廠製齋襯 (鏇糧製艱繭糧築蓋構願, 襯製蓋鑰選夢顧繭壓夢 ~ 積鬱鑰憲範鹽製範壓選) 更多 | - | 2010-03-15 | ||
(Metformin) | 獵鏇齋鬱艱獵夢襯憲製(鏇餘遞齋蓋膚憲鹹夢齋) = 獵廠壓築選艱壓構壓蓋 獵淵簾糧獵製廠製齋襯 (鏇糧製艱繭糧築蓋構願, 醖遞鏇築遞網繭積膚窪 ~ 願範齋夢蓋鏇繭餘獵艱) 更多 |
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