Montelukast Sodium: Understanding Its Role in Respiratory Health, Allergies, and Asthma Management_Swapnroop Drugs & Pharmaceuticals_APIMANUFACTURER_Exporter#apimanufacturer
Montelukast Sodium: Understanding Its Role in Respiratory Health, Allergies, and Asthma Management
1. What is Montelukast Sodium API?
Montelukast Sodium is a leukotriene receptor antagonist (LTRA) that helps in managing and preventing asthma and allergic rhinitis. It works by blocking leukotrienes, chemicals in the body that cause inflammation, bronchoconstriction, and mucus production.
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IUPAC Name: Sodium 1-[[[(1R)-1-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetate.
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Molecular Formula: C35H35ClNNaO3S
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Molecular Weight: 608.18 g/mol
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CAS Number: 151767-02-1
2. What is Montelukast Sodium used for?
Primary Uses
✅ Asthma Management: Prevents and controls chronic asthma by reducing airway inflammation.
✅ Exercise-Induced Bronchoconstriction (EIB): Helps prevent breathing difficulties triggered by physical activity.
✅ Allergic Rhinitis (Hay Fever): Relieves symptoms like sneezing, runny nose, and nasal congestion.
Off-Label Uses
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Treating chronic urticaria (hives).
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Managing aspirin-induced asthma.
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Potential role in COVID-19 management due to its anti-inflammatory properties.
3. What are the physicochemical properties of Montelukast Sodium?
| Property | Description |
|---|---|
| Appearance | White to off-white powder |
| Solubility | Freely soluble in water & methanol, slightly soluble in ethanol |
| Melting Point | 138-140°C |
| pH (Solution) | 7.0 – 8.5 |
| Partition Coefficient (log P) | 8.79 |
| Polymorphic Forms | Exhibits polymorphism; different forms have varying stability and bioavailability. |
4. How is Montelukast Sodium synthesized?
Montelukast Sodium synthesis is a multi-step organic reaction involving several intermediates:
Step-by-Step Synthesis Process
1️⃣ Formation of the Chiral Side Chain:
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The chiral side chain is synthesized via enantioselective reduction of ketone intermediates.
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Catalysts such as BINAP-ruthenium complexes are used.
2️⃣ Preparation of the Quinoline Derivative:
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7-chloro-2-methylquinoline undergoes Friedel–Crafts acylation to obtain an intermediate.
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This intermediate is coupled with the chiral side chain in the presence of organolithium reagents.
3️⃣ Sulfur Addition & Cyclization:
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The compound is subjected to thiolation to introduce a sulfur-containing moiety.
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Cyclization follows to form the final Montelukast structure.
4️⃣ Sodium Salt Formation:
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The free acid is neutralized with sodium hydroxide (NaOH) to form Montelukast Sodium.
5️⃣ Purification & Crystallization:
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Purification is carried out using chromatographic techniques.
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Crystallization ensures high purity and stability.
π¬ Key Challenges in Synthesis:
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Achieving high enantioselectivity and purity.
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Controlling polymorphic transformations.
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Ensuring high yield with minimal side reactions.
5. What are the different dosage forms of Montelukast Sodium?
| Dosage Form | Strengths | Use Case |
|---|---|---|
| Tablets | 10 mg | Adults & Adolescents (≥15 years) |
| Chewable Tablets | 4 mg, 5 mg | Children (2-14 years) |
| Oral Granules | 4 mg | Infants (6 months - 5 years) |
6. How are Montelukast Sodium dosage forms prepared?
Montelukast Sodium is blended with excipients to form stable dosage forms.
Tablet Formulation Process
1️⃣ Blending: Montelukast Sodium + excipients (lactose, microcrystalline cellulose).
2️⃣ Granulation: Wet or dry granulation to improve flow properties.
3️⃣ Compression: Tablets are formed using high-speed rotary presses.
4️⃣ Coating: Film-coated to enhance stability and mask taste.
5️⃣ Packaging: Blister packs or HDPE bottles with desiccants to protect from moisture.
7. What is the appropriate dosage form of Montelukast Sodium?
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Adults & Adolescents (≥15 years): 10 mg tablet once daily.
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Children (6-14 years): 5 mg chewable tablet once daily.
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Children (2-5 years): 4 mg chewable tablet or granules.
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Infants (6 months-2 years): 4 mg oral granules.
8. When should Montelukast Sodium be taken?
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Asthma: In the evening for better symptom control.
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Exercise-Induced Bronchospasm: At least 2 hours before exercise.
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Allergic Rhinitis: Anytime, but consistency is key.
9. What are the effects and side effects of Montelukast Sodium?
Effects:
✅ Prevents airway inflammation.
✅ Reduces asthma attacks.
✅ Alleviates allergy symptoms.
Side Effects:
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Common: Headache, dizziness, stomach upset.
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Rare: Neuropsychiatric effects (mood changes, hallucinations).
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Severe (Rare): Anaphylaxis, liver dysfunction.
10. How is Montelukast Sodium tested?
✅ Identification Tests: FTIR, HPLC, UV Spectroscopy.
✅ Assay for Potency: HPLC with UV detection.
✅ Impurity Analysis: LC-MS for residual solvents & degradation products.
✅ Dissolution Test: Ensures drug release meets USP/EP standards.
11. What are the challenges in manufacturing Montelukast Sodium?
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Moisture Sensitivity: Needs controlled humidity (<30%).
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Polymorphism Issues: Affects solubility and bioavailability.
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High Manufacturing Cost: Due to complex synthesis steps.
12. Storage, Packaging & Shelf Life
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Storage Conditions: 15-30°C, dry place, away from light.
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Packaging: Blister packs, HDPE bottles with desiccants.
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Shelf Life: 2-3 years under proper storage conditions.
13. Where can Montelukast Sodium be procured?
Top API Manufacturers:
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Swapnroop Drugs & Pharmaceuticals
+91 9420294801 |
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