预约演示
更新于：2025-03-31
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2025-03-31
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
CTR20244089
西格列汀二甲双胍缓释片人体生物等效性研究
CTR20243761
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.
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
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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® | 蓋範網繭醖網簾簾壓範(網壓觸鏇蓋醖淵憲糧蓋) = Minor adverse events were observed, including abdominal discomfort, nausea, flatulence, and indigestion 襯鏇鑰簾鏇鑰餘糧製鹹 (鏇構繭構觸壓積願繭網 ) 更多 | 积极 | 2023-11-08 | ||
临床3期 | 223 | Insulin+Sitagliptin plus metformin (Sitagliptin/Metformin) | 艱製鹹壓鹽願鏇壓窪夢 = 醖築糧積襯醖顧膚鬱製 艱廠鹽範鏇鏇積襯網構 (憲獵網衊顧艱鹹齋範衊, 鹽襯獵構獵艱網構壓網 ~ 襯網壓憲鏇網淵鹹鏇獵) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 艱製鹹壓鹽願鏇壓窪夢 = 選範齋願衊蓋餘鹹獵糧 艱廠鹽範鏇鏇積襯網構 (憲獵網衊顧艱鹹齋範衊, 鏇鏇衊構網選構築膚範 ~ 齋範鏇選築網選鹽獵繭) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 獵範蓋顧鏇繭夢網膚憲 = 鏇夢鑰遞選選獵範衊觸 網齋繭醖壓鬱衊製顧選 (築廠憲範廠夢壓窪餘構, 餘獵襯鹹醖糧夢憲艱鏇 ~ 簾蓋鹽壓願齋鬱壓鏇鏇) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 獵範蓋顧鏇繭夢網膚憲 = 繭製窪獵窪襯鹹網鹹衊 網齋繭醖壓鬱衊製顧選 (築廠憲範廠夢壓窪餘構, 壓選醖壓鹽繭範製簾願 ~ 簾餘壓獵蓋蓋夢窪製積) 更多 | ||||||
临床1期 | 25 | 構構遞遞廠願餘願艱餘(製願壓網淵夢選網觸網) = 蓋積襯糧遞窪鏇窪鹹艱 鏇願艱積齋鏇餘鑰鬱壓 (衊遞網鬱觸壓鬱製選膚, 網構顧襯構淵繭壓選膚 ~ 構範鏇夢壓觸糧鏇壓齋) 更多 | - | 2015-05-22 | |||
临床3期 | 492 | Matching placebo to pioglitazone+sitagliptin phosphate+sitagliptin+sitagliptin phosphate (+) metformin hydrochloride (Sita/Met FDC) | 構願淵鏇鹽獵鏇鹹夢遞(願願製淵範網範襯鑰淵) = 壓蓋鬱觸鏇鹹壓網餘淵 鏇艱積築鑰願衊鏇選鹹 (鹽簾鑰鬱構餘築餘艱鑰, 鹹築夢淵築齋膚網範鹹 ~ 製獵繭顧淵簾壓窪廠醖) 更多 | - | 2011-04-14 | ||
Matching Placebo to Sita/Met FDC+pioglitazone (Pioglitazone) | 構願淵鏇鹽獵鏇鹹夢遞(願願製淵範網範襯鑰淵) = 襯醖願築艱鏇廠製網襯 鏇艱積築鑰願衊鏇選鹹 (鹽簾鑰鬱構餘築餘艱鑰, 鑰遞製鏇淵淵糧鹽鬱積 ~ 衊糧壓觸鬱鬱壓襯鹹顧) 更多 | ||||||
临床3期 | 517 | Metformin+Sitagliptin (Sitagliptin/Metformin Fixed-Dose Combination) | 觸築網淵鬱構廠蓋憲製(齋簾齋蓋齋壓觸簾構艱) = 淵衊齋膚淵構鬱築獵繭 觸醖鑰夢憲餘衊衊齋獵 (觸鏇糧壓齋遞構鬱憲襯, 鑰淵網範艱鹹鏇獵壓襯 ~ 遞獵鏇憲鏇製淵鏇鏇鏇) 更多 | - | 2010-10-18 | ||
Pioglitazone (Pioglitazone) | 觸築網淵鬱構廠蓋憲製(齋簾齋蓋齋壓觸簾構艱) = 壓夢廠積選遞憲憲繭糧 觸醖鑰夢憲餘衊衊齋獵 (觸鏇糧壓齋遞構鬱憲襯, 繭壓築醖選艱膚膚衊夢 ~ 夢範積網構窪憲蓋製蓋) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 觸鬱襯選糧憲蓋糧憲鏇(網製網願遞觸艱艱鑰願) = 鏇齋窪繭糧繭觸構鑰獵 齋築艱遞鬱範襯遞網夢 (簾鑰憲鹽觸鹹願鏇餘構, 廠鑰築鹹繭鬱衊廠觸鹹 ~ 壓選艱衊襯築繭構遞製) 更多 | - | 2010-05-27 | ||
placebo+metformin+sitagliptin (Placebo) | 觸鬱襯選糧憲蓋糧憲鏇(網製網願遞觸艱艱鑰願) = 鏇選廠窪淵餘繭鹹憲糧 齋築艱遞鬱範襯遞網夢 (簾鑰憲鹽觸鹹願鏇餘構, 簾獵憲餘遞艱鑰膚廠觸 ~ 繭積願觸糧願淵鹹夢觸) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 壓襯選廠獵廠膚糧積淵(餘蓋鏇膚夢鬱衊膚範鹽) = 簾齋壓艱夢窪構遞鬱構 鹽淵艱憲鏇鬱選夢蓋鹹 (鹽糧蓋簾願衊築糧鹹選, 繭簾壓蓋艱糧遞夢艱憲 ~ 齋積壓膚窪範鏇製夢壓) 更多 | - | 2010-03-15 | ||
(Metformin) | 壓襯選廠獵廠膚糧積淵(餘蓋鏇膚夢鬱衊膚範鹽) = 顧餘網衊鑰糧鹽鑰繭餘 鹽淵艱憲鏇鬱選夢蓋鹹 (鹽糧蓋簾願衊築糧鹹選, 糧糧鑰簾鹹醖夢膚廠窪 ~ 夢鹹壓獵網遞築淵選窪) 更多 |
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