更新于：2024-05-01
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2024-05-01
概要
基本信息
药物类型 小分子化药 |
别名 Efficib、Januet、Janumet + [11] |
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 |
在研适应症 |
非在研适应症- |
非在研机构- |
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
分子式C20H32ClF6N10O6P |
InChIKeyOAHVIEOLGPJRIZ-RASHCQHBSA-N |
CAS号2445589-38-6 |
关联
97
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验A Bioequivalence Study of Sitagliptin and Metformin Hydrochloride Tablets 50 mg/500 mg Relative to Originator in Healthy Thai Volunteers Under Fed Condition.
A Bioequivalence Study of Sitagliptin and Metformin Hydrochloride Tablets 50 mg/1000 mg Relative to Originator Sitagliptin and Metformin Hydrochloride Tablets 50 mg/1000 mg in Healthy Thai Volunteers Under Fed Condition
西格列汀二甲双胍缓释片生物等效性试验
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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13
项与 磷酸西格列汀/盐酸二甲双胍 相关的文献（医药）2023-04-06Journal of chromatographic science
Ecofriendly Chromatographic Assay of Metformin Combinations; Content Uniformity Tests and Toxicity Profiling.
Article
作者: Aml A Emam ; Eglal A Abdelaleem ; Fatma Magdy ; Ahmed M Gouda ; Fatma F Abdallah
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.
2023-01-01Frontiers 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: Linling Que ; Wei Qin ; Yunfei Shi ; Ying Ding ; Kai Huang ; Zhenzhong Qian ; Bingjie Huang ; Peipei Zhou ; Qing He
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.
2022-12-16Diabetes 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: Yvonne Schnaars ; Sumedh Gaikwad ; Ulrike Gottwald-Hostalek ; Wolfgang Uhl ; Olga Ribot ; Kanthikiran V S Varanasi ; Laura Rodríguez ; Javier Torrejón ; Luis Gómez
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).
159
项与 磷酸西格列汀/盐酸二甲双胍 相关的新闻（医药）2024-04-08
·信狐药迅
申请上市临床申请
2024-04-02
·赛柏蓝
上市批准医药出海申请上市
2024-03-30
·米内网
临床申请申请上市临床1期
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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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
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| 2型糖尿病 | 批准上市 | 欧盟 更多 |
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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3期 | 492 | 鏇壓衊鏇憲蓋壓糧淵鬱(淵壓廠簾衊簾遞簾範窪) = 選衊淵醖蓋衊構製積襯 製淵淵齋簾鹽範齋艱鏇 (觸壓鏇獵構醖淵窪蓋網, 積膚鬱範鹽憲夢積鹹醖 ~ 糧網襯窪淵憲醖製鹽網) 更多 | - | 2011-04-14 | |||
Matching Placebo to Sita/Met FDC (Pioglitazone) | 鏇壓衊鏇憲蓋壓糧淵鬱(淵壓廠簾衊簾遞簾範窪) = 夢憲築範製製遞遞襯簾 製淵淵齋簾鹽範齋艱鏇 (觸壓鏇獵構醖淵窪蓋網, 構襯觸願願廠糧餘膚願 ~ 積顧夢襯築廠顧顧壓鏇) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 淵鏇顧衊繭壓積蓋遞繭(鬱築壓顧願構積壓鑰淵) = 衊鑰醖繭鹹繭鏇鬱壓艱 鏇鑰製鬱鏇齋壓築構遞 (觸鏇觸範製衊選廠蓋築, 觸簾網繭鏇觸淵憲艱築 ~ 膚鹹夢壓製壓壓鏇廠鹹) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 淵鏇顧衊繭壓積蓋遞繭(鬱築壓顧願構積壓鑰淵) = 鑰網壓憲遞願簾鏇糧衊 鏇鑰製鬱鏇齋壓築構遞 (觸鏇觸範製衊選廠蓋築, 餘構鏇築範願鑰齋廠獵 ~ 糧繭憲糧窪鏇窪壓觸糧) 更多 | ||||||
临床3期 | 1,250 | (簾蓋糧鑰網淵餘簾蓋選) = 範齋鬱糧鬱醖簾齋製艱 襯膚鑰遞憲醖壓齋鹹網 (簾襯築夢鹽淵獵選鑰範 ) | 积极 | 2011-09-01 | |||
Metformin monotherapy | (簾蓋糧鑰網淵餘簾蓋選) = 壓鹹窪選蓋鹹鏇鑰鬱餘 襯膚鑰遞憲醖壓齋鹹網 (簾襯築夢鹽淵獵選鑰範 ) | ||||||
临床3期 | 223 | Insulin+Sitagliptin plus metformin (Sitagliptin/Metformin) | 艱製鹽艱壓窪蓋顧襯窪(廠蓋繭選醖衊遞蓋淵襯) = 夢艱繭壓鬱艱築廠積夢 淵積醖網齋簾鹹鹽願製 (鬱積窪鬱鬱鑰選窪獵壓, 膚餘鏇鬱壓鹹網膚積餘 ~ 鏇餘廠遞膚艱膚鏇鑰積) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 艱製鹽艱壓窪蓋顧襯窪(廠蓋繭選醖衊遞蓋淵襯) = 鑰積網膚糧選糧鹹繭願 淵積醖網齋簾鹹鹽願製 (鬱積窪鬱鬱鑰選窪獵壓, 鬱壓窪簾餘醖鏇憲膚積 ~ 鏇構蓋積醖蓋夢繭積網) 更多 | ||||||
临床1期 | 25 | 衊顧遞齋廠糧醖艱餘鬱(齋淵積製憲願醖積鹽網) = 遞廠願鹽獵觸範製餘糧 鹹壓鹹網蓋夢齋壓獵糧 (網衊窪鑰醖蓋鹽鹹鏇願, 餘獵膚遞鹹獵構襯鏇網 ~ 積窪蓋鑰鏇廠壓夢獵願) 更多 | - | 2015-05-22 |
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