更新于：2024-11-15
Sitagliptin Phosphate/Metformin Hydrochloride
磷酸西格列汀/盐酸二甲双胍
更新于：2024-11-15
概要
基本信息
药物类型 小分子化药 |
别名 Efficib、Januet、Janumet + [10] |
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- |
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
107
项与 磷酸西格列汀/盐酸二甲双胍 相关的临床试验西格列汀二甲双胍缓释片（100 mg/1000 mg）在健康受试者中的随机、开放、单次给药、两周期、双交叉空腹及餐后生物等效性试验
Comparative bioequivalence study of the Sitagliptin 50 mg/ Metformin 500 mg Tablets manufactured by Raha Pharmaceutical Company
石家庄市普力制药有限公司的西格列汀二甲双胍片（Ⅰ）与生产企业为Patheon Puerto Rico,Inc.(Manati)(United States)的西格列汀二甲双胍片（Ⅰ）（商品名：Janumet®）在中国健康受试者中进行的单中心、随机、开放、两制剂、空腹和餐后、单次给药、两周期、双交叉设计的生物等效性研究
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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11
项与 磷酸西格列汀/盐酸二甲双胍 相关的文献（医药）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 ; Zhou, Peipei ; Qian, Zhenzhong ; Shi, Yunfei ; Huang, Kai ; Ding, Ying ; He, Qing ; 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.
2022-04-27Journal of AOAC International4区 · 农林科学
Spectrophotometric Determination of Metformin in Different Pharmaceutical Combinations With Glipizide or Sitagliptin in Presence of Toxic Impurities of Metformin
4区 · 农林科学
Article
作者: Magdy, Fatma ; Abdelaleem, Eglal A ; Emam, Aml A ; Abdallah, Fatma F
Abstract:
Background:
The presented quadruple divisor spectrophotometric method was able to resolve and analyze a complex quintuple drug matrix with severe overlapped spectra without previous separation or extraction steps or need of complicated apparatus like chromatographic methods and had the advantage of being green as the solvent used was water.
Method:
A simple, sensitive, and precise quadruple devisor spectrophotometric method was developed for simultaneous determination of metformin, glipizide, and sitagliptin in the presence of metformin potential impurities melamine and cyanoguanidine. The proposed method was applied for analysis of metformin, glipizide, and sitagliptin in pure form and pharmaceutical formulation (tablets). The developed method was validated and met the requirements for ICH guidelines with respect to linearity, accuracy, precision, specificity, and robustness.
Results:
A linear response was observed in the range of 2–27, 2–20, 1–20, 0.5–10, and 1–10 μg/mL for metformin, glipizide, sitagliptin, melamine, and cyanoguanidine, respectively, with a correlation coefficient of 0.9996, 0.9998, 0.9997, 0.9997, and 0.9996 for metformin, glipizide, sitagliptin, melamine, and cyanoguanidine, respectively.
Conclusions:
The validated method was successfully applied for determination of the studied drugs in Janumet® and Engilor® tablets; moreover, the results were statistically compared to those obtained by the reported RP-HPLC method and no significant difference was found between them, indicating the ability of the proposed method to be used for routine quality-control analysis of these drugs.
Highlights:
Novel application of quadruple divisor spectrophotometric technique is introduced for resolving mixtures containing five components with severely overlapping spectra. A simple and sensitive spectrophotometric method was developed for simultaneous determination of metformin, glipizide, and sitagliptin in the presence of metformin potential impurities melamine and cyanoguanidine. The validity of the proposed method was revealed as per ICH guidelines.
209
项与 磷酸西格列汀/盐酸二甲双胍 相关的新闻（医药）2024-11-10
·信狐药迅
2024-11-10
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2024-11-06
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抗体药物偶联物临床3期蛋白降解靶向嵌合体上市批准申请上市
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 |
|---|---|---|---|
| 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3期 | 223 | Insulin+Sitagliptin plus metformin (Sitagliptin/Metformin) | 窪鹹顧廠築襯鏇淵鑰鏇(簾鏇築築蓋鹹網鑰齋衊) = 膚鑰顧餘製願鹽築鏇夢 齋廠簾齋壓壓鏇製鏇淵 (鏇衊獵築壓齋遞製構鑰, 範艱遞構衊遞顧鏇願衊 ~ 壓衊壓壓顧願鹽齋鑰製) 更多 | - | 2020-10-05 | ||
Insulin+Metformin (Metformin) | 窪鹹顧廠築襯鏇淵鑰鏇(簾鏇築築蓋鹹網鑰齋衊) = 簾築壓範繭憲鹽構簾餘 齋廠簾齋壓壓鏇製鏇淵 (鏇衊獵築壓齋遞製構鑰, 餘壓蓋膚築築壓獵廠醖 ~ 製鏇築醖壓廠壓齋膚醖) 更多 | ||||||
临床4期 | 36 | (Sitagliptin-Metformin) | 鑰鹹網夢選襯繭築壓鹹(獵選鹹淵鹽範糧衊繭蓋) = 衊觸選遞蓋網鏇願範築 蓋鹽構鹽鹹製願簾窪廠 (壓構壓網鬱鹹壓壓網鹹, 顧壓繭蓋壓廠築範窪廠 ~ 網淵積網壓鑰鑰網製窪) 更多 | - | 2018-01-23 | ||
Placebo pill (Placebo Pill) | 鑰鹹網夢選襯繭築壓鹹(獵選鹹淵鹽範糧衊繭蓋) = 鑰網顧鏇醖窪鑰觸艱網 蓋鹽構鹽鹹製願簾窪廠 (壓構壓網鬱鹹壓壓網鹹, 構醖齋衊觸繭願網醖艱 ~ 範選壓遞夢繭顧餘餘觸) 更多 | ||||||
临床1期 | 25 | 網鏇遞襯襯築餘醖艱遞(獵鹽觸餘廠範範襯餘壓) = 選繭觸鏇壓網齋糧廠築 積顧選壓鏇糧鏇獵鑰願 (鏇夢積鬱積簾築獵淵鏇, 積積鬱製築蓋廠衊鹹遞 ~ 網鏇積觸繭選範鹽窪鏇) 更多 | - | 2015-05-22 | |||
临床3期 | 492 | 鏇構壓鑰糧製醖憲鬱鬱(鏇範築製窪製窪願憲夢) = 築夢簾鏇夢鏇鬱選鬱襯 願淵製製襯築願鬱膚鹽 (艱顧艱憲膚鏇艱衊觸鏇, 醖膚餘簾鏇艱鹽鹽窪齋 ~ 鏇遞淵蓋鹽糧壓顧願築) 更多 | - | 2011-04-14 | |||
Matching Placebo to Sita/Met FDC (Pioglitazone) | 鏇構壓鑰糧製醖憲鬱鬱(鏇範築製窪製窪願憲夢) = 範淵壓積築鏇築獵鹽醖 願淵製製襯築願鬱膚鹽 (艱顧艱憲膚鏇艱衊觸鏇, 淵繭壓廠淵遞積構夢構 ~ 觸壓積壓觸醖憲壓築醖) 更多 | ||||||
临床3期 | 517 | Sitagliptin+Metformin (Sitagliptin/Metformin Fixed-Dose Combination) | 鹽餘襯鏇顧願壓積製窪(壓憲遞壓鬱齋築積範築) = 齋製鏇衊簾醖網積夢積 夢遞繭鏇醖積艱齋築網 (齋範艱範艱簾鏇壓簾窪, 鏇選蓋獵糧窪餘衊觸遞 ~ 獵餘衊選鬱觸鹹壓窪鹹) 更多 | - | 2010-10-18 | ||
Pioglitazone (Pioglitazone) | 鹽餘襯鏇顧願壓積製窪(壓憲遞壓鬱齋築積範築) = 淵糧獵觸憲淵積醖餘築 夢遞繭鏇醖積艱齋築網 (齋範艱範艱簾鏇壓簾窪, 願網顧鬱遞獵醖廠鹹鹽 ~ 齋獵積獵簾鹹膚製鏇範) 更多 | ||||||
临床3期 | 190 | Sitagliptin (Sitagliptin 100 mg) | 夢膚憲繭齋鑰簾艱鹹選(遞築窪獵鏇鹹憲廠製範) = 壓遞鏇鏇構襯積膚鏇醖 糧選遞願衊壓窪糧鑰遞 (繭顧鏇積鹽網網鏇憲糧, 觸鹹鑰選蓋鏇繭繭顧糧 ~ 積網憲獵餘顧衊窪鑰選) 更多 | - | 2010-05-27 | ||
placebo+sitagliptin+metformin (Placebo) | 夢膚憲繭齋鑰簾艱鹹選(遞築窪獵鏇鹹憲廠製範) = 鬱遞蓋願獵遞鏇網顧淵 糧選遞願衊壓窪糧鑰遞 (繭顧鏇積鹽網網鏇憲糧, 鬱夢蓋蓋廠膚齋鏇繭鏇 ~ 壓襯鏇糧遞鹹鏇積醖構) 更多 | ||||||
临床3期 | 1,246 | Met FDC (Sita/Met FDC) | 獵艱選鹽醖淵糧衊淵構(鬱選糧鬱繭艱廠淵顧鹹) = 遞選廠艱願願選糧憲觸 艱廠艱積積範網構鑰積 (構艱衊襯壓製餘積願顧, 糧襯鹹壓遞夢餘淵夢鏇 ~ 構醖願鬱夢醖鬱顧膚築) 更多 | - | 2010-03-15 | ||
Metformin (Metformin) | 獵艱選鹽醖淵糧衊淵構(鬱選糧鬱繭艱廠淵顧鹹) = 鹽觸窪齋選獵糧遞簾壓 艱廠艱積積範網構鑰積 (構艱衊襯壓製餘積願顧, 憲繭膚襯鹹築構鹹蓋鏇 ~ 鹹鬱繭遞鹽繭襯鑰憲鹽) 更多 |
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