Dapagliflozin Impurities and Dapagliflozin
Daicel Pharma synthesizes Dapagliflozin impurities of exceptional quality, such as 1α-Methoxy Dapagliflozin, 4-Deschloro-4-bromo Dapagliflozin, 5-bromo-2-chloro-4′-ethoxydiphenylmethane, Dapagliflozin Hydroxy Impurity, Dapagliflozin Tetraacetate, and Monoacetyl Dapagliflozin. These impurities are crucial to assess the purity, reliability, and safety of an active pharmaceutical ingredient, Dapagliflozin. Besides, Daicel Pharma provides custom synthesis of Dapagliflozin impurities to meet clients’ demands for delivery worldwide.
Dapagliflozin [CAS: 461432-26-8], a selective inhibitor of sodium-glucose cotransporter subtype 2 (SGLT2), exhibits potent antihyperglycemic activity. This selective inhibition of SGLT2 enhances its effectiveness in improving glycemic control in adults with type 2 diabetes when used in conjunction with diet and exercise. Dapagliflozin helps individuals seeking to manage their blood glucose levels.
Dapagliflozin: Use and Commercial Availability
Dapagliflozin, available under the brand name Farxiga, improves glycemic control in adult patients with type 2 diabetes mellitus. It is useful where metformin is not suitable due to intolerance or in addition to other medications for treating type 2 diabetes. Additionally, it treats symptomatic chronic heart failure with reduced ejection fraction and chronic kidney disease in adults.
Dapagliflozin Structure and Mechanism of Action
The chemical name of Dapagliflozin is (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol. Its chemical formula is C21H25ClO6, and its molecular weight is approximately 408.9 g/mol.
Dapagliflozin inhibits Sodium-glucose cotransporter 2 (SGLT2) and reduces the reabsorption of filtered glucose. It decreases the renal threshold for glucose while increasing urinary glucose excretion.
Dapagliflozin Impurities and Synthesis
During the synthesis1, storage, or degradation of Dapagliflozin, impurities generate. These impurities can originate from various sources, including raw materials, reaction by-products, or degradation of the drug substance. Analytical techniques like HPLC, LC, and MS help identify and quantify these impurities. Strict control measures are necessary to ensure the quality and safety of Dapagliflozin, including setting impurity specifications and implementing robust manufacturing processes.
Daicel Pharma offers a Certificate of Analysis (CoA) for Dapagliflozin impurity standards, such as 1α-Methoxy Dapagliflozin, 4-Deschloro-4-bromo Dapagliflozin, 5-bromo-2-chloro-4′-ethoxydiphenylmethane, Dapagliflozin Hydroxy Impurity, Dapagliflozin Tetraacetate, and Monoacetyl Dapagliflozin, generated from an analytical facility compliant with cGMP standards. The CoA includes a comprehensive characterization report comprising data from techniques like 1H NMR, 13C NMR, IR, MASS, and HPLC purity2. Furthermore, on request, we give additional data like 13C-DEPT and CHN. Daicel Pharma can synthesize unknown Dapagliflozin impurities or degradation products. A complete characterization report accompanies every delivery.
- Ellsworth, Bruce; Washburn, William N.; Sher, Philip M.; Wu, Gang; Meng, Wei, C-Aryl Glucoside SGLT2 Inhibitors, Bristol-Myers Squibb Company, United States, EP1224195B1, May 18, 2005
- Sanagapati, Manasa; Dhanalakshmi, K.; Nagarjunareddy, G.; Sreenivasa, S., Development and validation of a RP-HPLC method for the estimation of dapagliflozin in API, International Journal of Pharmaceutical Sciences and Research, Volume: 5, Issue: 12, Pages: 5394-5397, 2014
Frequently Asked Questions
Some impurities in Dapagliflozin may interfere with its pharmacokinetic or pharmacodynamic properties, potentially affecting its absorption, distribution, metabolism, or excretion in the body.
Yes, the control of genotoxic impurities is of utmost importance in Dapagliflozin due to its potentially harmful effects on DNA and increased risk of cancer. There are stringent limits set for genotoxic impurities.
Regulatory authorities such as the FDA and EMA provide guidelines and regulations regarding controlling impurities in Dapagliflozin, ensuring compliance with quality standards.
Acetonitrile is a solvent used for analyzing many impurities in Dapagliflozin.
Dapagliflozin impurities are stored at a controlled room temperature between 2-8 °C or as indicated on the Certificate of Analysis (CoA).
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