Everything You Need to Know About Bisoprolol Fumarate_ Swapnroop Drugs & Pharmaceuticals_ APIMANUFACTURER_EXPORTER
1. What is Bisoprolol Fumarate API?
Bisoprolol Fumarate is the active pharmaceutical ingredient (API) in various cardiovascular drugs. It is a beta-blocker, specifically a selective beta-1 adrenergic antagonist. It works by blocking the beta-1 receptors in the heart, which reduces the effects of stress hormones like adrenaline. This leads to a slower heart rate, decreased blood pressure, and a reduction in the heart's workload. As a result, it is used to treat a variety of cardiovascular conditions.
Chemical Structure:
Bisoprolol is derived from the aryloxypropanolamine class, which includes other beta-blockers like metoprolol. Its fumarate salt form is a combination of bisoprolol with fumaric acid, enhancing its solubility and stability in pharmaceutical formulations.
2. What is Bisoprolol Fumarate used for?
Therapeutic Uses:
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Hypertension (High Blood Pressure): By lowering heart rate and the force of heart contractions, Bisoprolol helps reduce overall blood pressure.
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Chronic Heart Failure (CHF): Bisoprolol improves the heart’s ability to pump blood by reducing the heart rate and improving heart function. It is part of a treatment regimen for stable, chronic heart failure, usually in combination with other medications like ACE inhibitors and diuretics.
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Angina Pectoris: It is used to manage chest pain related to angina by reducing the heart's oxygen demand.
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Atrial Fibrillation: Bisoprolol is used to control the heart rate in atrial fibrillation, where the heart beats irregularly and too fast.
Mechanism of Action:
Bisoprolol selectively blocks the beta-1 receptors in the heart, leading to reduced sympathetic nervous system activity. This results in:
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Decreased heart rate (negative chronotropy)
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Reduced force of contraction (negative inotropy)
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Decreased rate of impulse conduction through the AV node (negative dromotropy)
These effects lead to a reduction in blood pressure and the workload on the heart.
3. What are the physicochemical properties of Bisoprolol Fumarate?
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Molecular Formula: C18H31NO4
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Molecular Weight: 325.45 g/mol
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Appearance: White to off-white crystalline powder.
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Solubility: Slightly soluble in water and more soluble in organic solvents like methanol and ethanol, which makes it easier to formulate into tablets.
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Melting Point: 151–155°C
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pH (in solution): It typically has a pH in the range of 5–7 when dissolved in water.
The fumarate salt form increases the drug’s bioavailability and stability compared to the base form, which is critical for therapeutic efficacy.
4. How is Bisoprolol Fumarate synthesized?
Synthesis Process: The synthesis of Bisoprolol involves multiple steps, typically starting with the preparation of an aryloxypropanolamine intermediate. Here’s a simplified version of the synthesis pathway:
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Step 1 – Synthesis of Aryloxypropanolamine:
The reaction involves the alkylation of a phenolic intermediate with an alcohol group, forming an aryloxypropanolamine compound. -
Step 2 – Formation of Bisoprolol:
The intermediate undergoes further reactions, typically involving a condensation process, to form Bisoprolol. -
Step 3 – Fumarate Salt Formation:
Bisoprolol is then reacted with fumaric acid to form Bisoprolol Fumarate. The fumarate salt improves solubility and stability, allowing the drug to be formulated effectively for oral administration.
Challenges in Synthesis:
Maintaining high purity and yield of Bisoprolol Fumarate is important during synthesis. Impurities or incomplete reactions can affect the drug's quality, requiring stringent control over reaction conditions.
5. What are the different dosage forms of Bisoprolol Fumarate?
The most common dosage forms include:
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Oral Tablets: These are the primary dosage form, available in varying strengths (e.g., 2.5 mg, 5 mg, 10 mg).
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Oral Liquid Formulations: Some formulations are available in liquid form for patients who have difficulty swallowing tablets.
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Combination Tablets: Bisoprolol may also be found in combination with other antihypertensive agents, such as diuretics or calcium channel blockers, to improve therapeutic outcomes.
6. How are Bisoprolol Fumarate dosage forms prepared?
Preparation Process:
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Granulation: The active ingredient, Bisoprolol Fumarate, is mixed with excipients like binders, fillers, and disintegrants in a powder form. The mixture is often granulated to improve flow properties.
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Compression: The granules are then compressed into tablets using a tablet press. This process ensures the tablets are uniform in size and weight.
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Coating: Some tablets may be coated to protect the drug from degradation by light or moisture or to provide a controlled release of the drug.
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Quality Control: After manufacturing, the tablets undergo rigorous testing for content uniformity, dissolution rate, and stability to ensure consistency and efficacy.
7. What is the appropriate dosage form of Bisoprolol Fumarate?
The oral tablet is the standard and most commonly prescribed dosage form. It allows for convenient, controlled administration, ensuring the right amount of medication reaches the bloodstream. In patients with difficulty swallowing pills, the liquid formulation can be considered.
8. When should Bisoprolol Fumarate be taken?
Bisoprolol Fumarate is typically taken once daily. It can be taken in the morning or evening, depending on the patient’s preference, but it should be taken at the same time every day to maintain steady blood levels.
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With or without food: It can be taken with or without food, although taking it with food may help reduce any stomach upset.
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Important Consideration: The dosage is usually initiated at a lower level and gradually increased to avoid side effects like bradycardia (slow heart rate).
9. What are the effects and side effects of Bisoprolol Fumarate?
Effects:
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Primary: Reduction in heart rate, blood pressure, and heart workload. These effects improve the symptoms of hypertension, heart failure, and angina.
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Secondary: Improved survival rates in heart failure patients, reduced hospitalizations, and improved exercise tolerance.
Side Effects:
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Common: Fatigue, dizziness, cold extremities, and headache.
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Serious: Bradycardia, hypotension, respiratory distress (particularly in asthma or COPD patients), heart block, or worsening of heart failure.
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Rare but Severe: Severe allergic reactions, heart failure exacerbation, and depression.
Monitoring: Regular monitoring of blood pressure and heart rate is important, especially during the initial stages of treatment.
10. How is Bisoprolol Fumarate tested?
Quality Control Testing:
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Purity Testing: High-performance liquid chromatography (HPLC) or other techniques ensure the active ingredient is present in the required amounts.
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Dissolution Testing: Ensures the tablets release the active ingredient at the correct rate.
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Microbiological Testing: To ensure the product is free from harmful microorganisms.
Pharmacokinetic Testing: Measures the absorption, distribution, metabolism, and excretion (ADME) of Bisoprolol Fumarate to understand how the drug behaves in the body.
11. What tests are performed on Bisoprolol Fumarate?
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Content Uniformity Test: Ensures that each tablet contains the correct dose of Bisoprolol.
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Dissolution Rate: Determines the rate at which the drug is released into the bloodstream.
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Stability Testing: Monitors how the drug holds up over time under various conditions (temperature, humidity, light).
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Microbial Testing: Ensures that the drug is free from microbial contamination.
12. What are the challenges in manufacturing Bisoprolol Fumarate API?
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Purity Control: Achieving high purity of Bisoprolol Fumarate in synthesis, as impurities could lead to suboptimal therapeutic effects.
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Solubility: Ensuring the fumarate salt is soluble enough for optimal absorption and therapeutic action.
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Stability: Bisoprolol Fumarate must remain stable during manufacturing, storage, and transportation to ensure efficacy.
13. What are the challenges in manufacturing Bisoprolol Fumarate dosage forms?
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Uniform Distribution: Ensuring that Bisoprolol is evenly distributed within each tablet and that there is no segregation during processing.
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Dissolution Rate Control: Ensuring that the tablet dissolves at the correct rate to release the drug effectively.
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Stability of the Finished Product: The product needs to withstand environmental conditions like temperature, humidity, and light.
14. What are the storage conditions for Bisoprolol Fumarate?
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Temperature: Store at room temperature (between 20°C and 25°C).
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Protection from Moisture and Light: Store in a dry place, away from direct sunlight.
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Packaging: Keep in the original blister packs or bottles to protect from contamination and degradation.
15. What is the packaging for Bisoprolol Fumarate?
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Blister Packs: Protect each individual dose from moisture, contamination, and degradation.
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Bottles: For larger quantities, often used in long-term treatments.
16. What is the shelf life of Bisoprolol Fumarate?
Typically, the shelf life of Bisoprolol Fumarate tablets is 2 to 3 years when stored under the recommended conditions. Always check the expiry date on the packaging.
17. What should the label claim for Bisoprolol Fumarate include?
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Drug Name: Bisoprolol Fumarate
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Strength: The dosage strength (e.g., 2.5 mg, 5 mg, 10 mg)
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Indications: Conditions it treats (e.g., hypertension, chronic heart failure)
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Administration Instructions: How to take it (e.g., with or without food)
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Storage Information: Keep in a dry place, away from light.
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Expiry Date: Ensure the drug is used before the stated expiration date.
Manufacturer Name: Swapnroop Drugs & Pharmaceutical
18. Where can Bisoprolol Fumarate be procured?
Bisoprolol Fumarate can be procured from:
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