"Tiotropium Bromide API (CAS No. 136310-93-5) – Properties, Uses, Synthesis, and Dosage Forms"

 

🌿 What is Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 🌿

Tiotropium Bromide API is a high-purity active pharmaceutical ingredient (API) produced by Swapnroop Drugs & Pharmaceuticals for use in respiratory medicine formulations. It belongs to the class of long-acting muscarinic antagonists (LAMAs), also called anticholinergics.

💡 Key Highlights:

• Pharmacological Role: Tiotropium bromide is designed to provide once-daily bronchodilation by selectively blocking muscarinic M₃ receptors in the airway smooth muscles. This results in airway relaxation, improved airflow, and long-term relief for patients with obstructive lung diseases.

• Primary Applications: It serves as the foundation API in inhalation therapies for chronic obstructive pulmonary disease (COPD) and is also prescribed in some cases of moderate to severe asthma as an add-on therapy.

• Chemical Identity:

  • CAS No.: 136310-93-5

  • Molecular Formula: C₁₉H₂₂BrNO₄S₂

  • Form: Typically supplied as tiotropium bromide monohydrate, a stable crystalline powder.

• Physicochemical Traits:

  • Appearance: White to yellowish crystalline powder

  • Solubility: Sparingly soluble in water, freely soluble in methanol and DMSO

  • Stability: Hygroscopic; stable under recommended storage conditions

🔬 Why it’s important:
As an API, Tiotropium Bromide enables pharmaceutical companies to develop dry powder inhalers (DPI), soft-mist inhalers (SMI), and capsule-based inhalation systems that improve patients’ quality of life by reducing breathlessness, controlling symptoms, and lowering the risk of COPD exacerbations.

✨ In summary:
Tiotropium Bromide API from Swapnroop Drugs & Pharmaceuticals is a trusted, globally compliant respiratory care API, manufactured under stringent cGMP practices to ensure purity, consistency, and therapeutic reliability.

🌿 Q2. What is Tiotropium Bromide API by Swapnroop Drugs & Pharmaceuticals used for? 🌿

Tiotropium Bromide API is primarily used to formulate inhalation medicines for long-term maintenance therapy in:

• Chronic Obstructive Pulmonary Disease (COPD) 🌬️ – reduces airflow obstruction, improves lung function, decreases breathlessness, and lowers the frequency of exacerbations.

• Asthma (add-on therapy) 🫁 – prescribed in moderate to severe persistent asthma when patients remain symptomatic despite inhaled corticosteroids and long-acting beta agonists.

• Improving quality of life 💙 – helps patients carry out daily activities by providing 24-hour bronchodilation with once-daily dosing.

It is not intended for acute rescue therapy but rather as a preventive and maintenance treatment.

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🧪 Q3. What are the physicochemical properties of Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 🧪

• Chemical Name: Tiotropium Bromide Monohydrate

• CAS Number: 136310-93-5

• Molecular Formula: C₁₉H₂₂BrNO₄S₂ · H₂O

• Molecular Weight: ~472.4 g/mol (anhydrous form)

• Appearance: White to yellowish crystalline powder

• Solubility:

  • Sparingly soluble in water 💧

  • Freely soluble in methanol and DMSO

  • Practically insoluble in non-polar solvents (like methylene chloride)

• Stability: Hygroscopic; stable when stored in airtight containers at room temperature under dry conditions

• Melting/Decomposition: Decomposes at ~225–235 °C

These properties make it suitable for inhalation dosage forms, ensuring controlled delivery to the respiratory tract.

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⚙️ Q4. How is Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals synthesized? ⚙️

The synthesis of Tiotropium Bromide involves multi-step organic synthesis, generally starting from thiophene derivatives and progressing through quaternization steps to form the bromide salt:

1. Preparation of tropane intermediate 🧪 – Tropine or related bicyclic structures are synthesized or sourced as precursors.

2. Coupling with thiophene derivatives 🌿 – Introduction of thiophene-based moieties for desired pharmacological activity.

3. Esterification & functional group modifications 🔄 – Steps to obtain the required ester functionalities.

4. Quaternization with bromide ⚡ – Final reaction where a bromide ion is introduced, forming the stable crystalline salt (tiotropium bromide).

5. Crystallization & purification ✨ – The API is crystallized as a monohydrate to achieve required purity and physicochemical stability.

Swapnroop Drugs & Pharmaceuticals manufactures this under cGMP guidelines, ensuring compliance with pharmacopeial standards and international regulatory requirements.

💊 Q5. What are the different dosage forms of Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 💊

Tiotropium Bromide API is mainly developed into inhalation-based dosage forms because it acts locally in the lungs:

• Dry Powder Inhalers (DPI) 🌬️ – e.g., capsule-based inhalers where the powder is inhaled using devices such as HandiHaler®.

• Soft Mist Inhalers (SMI) 💧 – liquid formulations that create a fine mist for deeper lung deposition (e.g., Respimat®).

• Inhalation Capsules 💊 – containing tiotropium powder for device-specific inhalation.

• Nebulizer Solutions (in some regions) 🫁 – less common, but available for hospital or clinical use.

These forms ensure direct delivery to the lungs, maximizing efficacy while minimizing systemic exposure.

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⚗️ Q6. How are Tiotropium Bromide API dosage forms prepared? ⚗️

• Dry Powder Inhalers (DPI):

  • The API is micronized to achieve a respirable particle size (usually 1–5 μm).

  • It is blended with carriers like lactose monohydrate to ensure flow and dosing uniformity.

  • Filled into capsules or blister packs for inhalation devices.

• Soft Mist Inhalers (SMI):

  • Tiotropium Bromide is dissolved in sterile aqueous solution.

  • Filled into cartridge-based delivery systems that create a fine mist without propellants.

• Capsules for Inhalation:

  • Pre-metered capsules containing precise amounts of DPI formulation are sealed.

  • These are inserted into specific inhaler devices before use.

Each step is carefully controlled to maintain particle size distribution, purity, and aerodynamic properties essential for lung targeting.

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✅ Q7. What is the appropriate dosage form of Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? ✅

• The most appropriate and widely used dosage form is inhalation therapy (DPI or SMI), as it delivers the drug directly to the bronchial smooth muscles where it acts.

• For COPD patients, once-daily DPI capsules or SMI sprays are the gold standard.

• Choice of dosage form depends on:

  • Patient profile (ability to handle inhaler devices) 👵👨‍🦳

  • Therapeutic need (maintenance vs hospital setting) 🏥

  • Device preference and availability 🫁

In summary: DPI capsules and soft mist inhalers are the most appropriate dosage forms for Tiotropium Bromide API, ensuring effective, safe, and convenient long-term respiratory management. 🌿

🕒 Q8. When should Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals be taken? 🕒

• Once Daily Dosing: Tiotropium Bromide is typically administered once daily, due to its long-acting bronchodilator effect (lasting 24 hours).

• Timing: It can be taken at the same time each day, morning or evening, depending on patient preference for routine. ⏰

• Not for Acute Attacks: It is not a rescue medication – it should never be used for sudden breathing problems or acute bronchospasm. 🚫

• Consistency Matters: Regular use is essential for maintaining open airways and preventing COPD/asthma symptoms.

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🌬️ Q9. What are the effects and side effects of Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 🌬️

✅ Effects (Therapeutic Benefits):

• Relieves bronchospasm by relaxing airway smooth muscles.

• Improves lung function (FEV₁) and oxygen flow.

• Reduces shortness of breath, wheezing, and chest tightness.

• Lowers frequency of exacerbations and hospitalizations.

• Enhances exercise tolerance and daily activity performance. 🏃‍♂️💨

⚠️ Possible Side Effects:

• Common: Dry mouth 👅, sore throat, cough, constipation, blurred vision.

• Less common: Dizziness, headache, urinary retention, palpitations.

• Rare but serious: Hypersensitivity reactions, paradoxical bronchospasm, glaucoma worsening (if powder/mist gets into eyes).

• Systemic side effects are rare due to its local action in the lungs.

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🔬 Q10. How is Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals tested? 🔬

To ensure quality, safety, and efficacy, Swapnroop performs rigorous API testing under cGMP and pharmacopeial standards (e.g., USP, EP, IP):

• Identification Tests 🧪 – Confirm chemical identity using Infrared Spectroscopy (IR), NMR, and Mass Spectrometry.

• Assay (Potency Test): Quantification of Tiotropium Bromide content using HPLC (High-Performance Liquid Chromatography).

• Impurity & Related Substances Profile: Detection of organic and inorganic impurities using LC-MS, GC, and TLC.

• Particle Size Distribution: Laser diffraction or microscopy for inhalation-grade powders.

• Moisture Content: Karl Fischer titration to ensure stability.

• Polymorphic Form Analysis: X-ray diffraction (XRD) to verify crystalline structure (monohydrate form).

• Microbial Limits & Sterility (for inhalation solutions): Ensuring product is free of harmful microbial contamination.

These tests guarantee that the API meets international regulatory standards for safety and performance in inhaled drug formulations.

📦 Q14. What are the storage conditions for Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 📦

• Store in airtight, well-closed containers to protect from moisture and air.

• Recommended temperature: 15–30 °C (room temperature). 🌡️

• Protect from direct light and humidity, as Tiotropium Bromide is hygroscopic. 💧

• For long-term stability, it should be kept in controlled room conditions as per ICH guidelines (temperature + relative humidity).

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🎁 Q15. What is the packaging for Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? 🎁

Tiotropium Bromide API is packaged to preserve stability and comply with international shipping standards:

• Primary Packaging:

  • Double-layered polyethylene (LDPE/HDPE) bags, heat-sealed to protect from moisture.

  • Sometimes includes aluminium foil liners for extra protection.

• Secondary Packaging:

  • HDPE/Plastic or Fiber Drums (25 kg or 50 kg capacity).

  • Clearly labeled with product name, batch number, manufacturing/expiry date, net weight, and storage instructions.

• Tamper-Evident Seals: Ensure product integrity during transport.

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⏳ Q16. What is the shelf life of Tiotropium Bromide API manufactured by Swapnroop Drugs & Pharmaceuticals? ⏳

• Typical Shelf Life: 24–36 months (2–3 years) when stored under recommended conditions.

• Shelf life may vary depending on:

  • Packaging type (moisture barrier efficiency).

  • Storage conditions (temperature and humidity).

• Stability studies conducted under ICH Q1A guidelines determine the final assigned shelf life for each production batch.

✨ In summary: Proper storage + moisture-proof packaging ensures Tiotropium Bromide API retains its potency, purity, and stability for up to 3 years.