Carvedilol Impurities and Carvedilol
Daicel Pharma synthesizes Carvedilol impurities of exceptional quality, such as (R)- N-Benzyl Carvedilol, (R)-(+)-Carvedilol, (S)- N-Benzyl Carvedilol, and more. These impurities are crucial to assess the purity, reliability, and safety of Carvedilol, an active pharmaceutical ingredient. Besides, Daicel Pharma provides custom synthesis of Carvedilol impurities to meet clients’ demands for delivery worldwide.
Carvedilol [CAS: 72956-09-3] is a third-generation beta-blocker treating mild to severe heart failure. It can block beta1 and beta2 receptors and also exhibits alpha1-adrenergic blocking properties. This drug treats conditions such as high blood pressure, stable angina pectoris, and congestive heart failure.
Carvedilol: Use and Commercial Availability
Carvedilol is a non-selective adrenergic blocker that treats congestive heart failure. It also treats hypertension and stable angina pectoris. It is a highly lipophilic non-selective beta-adrenoceptor antagonist. It has alpha1-blocking action, promotes peripheral vasodilatation, and also possesses free radical scavenging and antimitogenic effects. The drug is available under Carvedilol Phosphate, Coreg, and Coreg CR.
Carvedilol Structure and Mechanism of Action
The chemical name of Carvedilol is 1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol. Its chemical formula is C24H26N2O4, and its molecular weight is approximately 406.5 g/mol.
Carvedilol has alpha1-adrenergic receptor antagonist properties with peripheral vasodilating effects. It inhibits apoptosis and reduces vascular smooth muscle migration.
Carvedilol Impurities and Synthesis
During the synthesis1 and storage of Carvedilol, impurities can form, which affect the drug’s efficacy and safety. It is vital to control and monitor these impurities as they can alter the pharmacological profile of the drug, leading to potential adverse effects. The International Council for Harmonization (ICH) guidelines provide specific limits for these impurities to ensure the safety and quality of the drug product. Thus, rigorous testing and monitoring of Carvedilol impurities are necessary to ensure its safety and efficacy.
Daicel Pharma offers a Certificate of Analysis (CoA) for Carvedilol impurity standards, such as (R)- N-Benzyl Carvedilol, (R)-(+)-Carvedilol, (S)- N-Benzyl Carvedilol, and more, generated from an analytical facility compliant with cGMP standards. The CoA includes a comprehensive characterization report comprising data from various techniques like 1H NMR, 13C NMR, IR, MASS, and HPLC purity2. Furthermore, we can give additional data like 13C-DEPT and CHN on request. Daicel Pharma can synthesize unknown Carvedilol impurities or degradation products and labeled compounds to assess the effectiveness of Carvedilol. We also give highly pure deuterium-labeled Carvedilol Labelled Standard for bioanalytical research such as BA/BE studies. A complete characterization report accompanies every delivery.
- Wiedemann, Fritz; Kampe, Wolfgang; Thiel, Max; Sponer, Gisbert; Roesch, Egon; Dietmann, Karl, Derivatives Of Carbazolyl-4-Oxypropanolamine, Methods For Their Preparation And Medicines Containing Them, Boehringer Mannheim G.m.b.H., Federal Republic of Germany, EP4920B1, August 5, 1981
- Reiff, K., High-performance liquid chromatographic method for the determination of carvedilol and its demethyl metabolite in body fluids, Journal of Chromatography, Biomedical Applications, Volume: 413, Pages: 355-62, 1987
Frequently Asked Questions
Impurities in Carvedilol form due to various reasons such as impurities in starting materials, reaction by-products, degradation of the drug substance during storage or manufacturing, or environmental factors.
Impurities in Carvedilol are identified using analytical techniques such as high-performance liquid chromatography (HPLC), liquid chromatography (LC), mass spectrometry (MS), etc.
The limits for impurities in Carvedilol set by regulatory agencies are ≤0.2% for individuals and ≤0.5% for total impurities.
Impurity standards in Carvedilol help identify and quantify impurities in the drug substance. They are also used to develop and validate analytical methods for impurity identification and quantification.
Carvedilol 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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