"Tizanidine Hydrochloride API (CAS No. 51329-02-3) – Properties, Uses, Synthesis, and Dosage Forms"

 

Q1. What is Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals? 💊✨

Short Answer:
Tizanidine Hydrochloride is a centrally acting α₂-adrenergic agonist used as a muscle relaxant. It is primarily developed as an active pharmaceutical ingredient (API) for the treatment of muscle spasticity and related neuromuscular conditions.

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Detailed Description (In-Depth) 🌟

1. Pharmacological Class & Mechanism 🔬

• Tizanidine Hydrochloride belongs to the α₂-adrenergic receptor agonist class.

• It works by inhibiting presynaptic motor neurons in the central nervous system (CNS), which reduces spasticity and muscle tone.

• Effects are centrally mediated, making it effective for spinal cord injuries, multiple sclerosis, and post-stroke spasticity. 🧠💪

2. Clinical Uses & Therapeutic Significance 🏥💚

• Muscle Spasticity Relief 💪 – Helps relax tight, stiff, or contracted muscles.

• Neuromuscular Disorders 🧬 – Used in multiple sclerosis, cerebral palsy, spinal cord injury, or post-stroke rehabilitation.

• Adjunct Therapy 🔹 – Can be used alongside physiotherapy or other supportive care to improve mobility and comfort.

3. Chemical Identity & Formulation 🧪

• IUPAC Name: 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine hydrochloride

• CAS Number: 51329-02-3

• Molecular Formula: C₉H₈ClN₅S·HCl

• Molecular Weight: 280.2 g/mol

• Form: White to off-white crystalline powder, water-soluble for oral or compounded dosage forms.

4. Physicochemical Characteristics ⚗️

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in water and slightly soluble in organic solvents like ethanol

• Stability: Stable under dry conditions, sensitive to light and moisture

• Melting Point: ~225–227°C

5. Manufacturing Importance 🏭

• Tizanidine Hydrochloride API is used to formulate tablets, capsules, or oral solutions for clinical use.

• Requires cGMP-compliant chemical synthesis to ensure purity, consistency, and bioavailability.

• Supports the production of safe and effective muscle relaxant therapies for patients worldwide. 🌍

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✨ Summary:
Tizanidine Hydrochloride API by Swapnroop Drugs & Pharmaceuticals is a centrally acting α₂-adrenergic agonist, essential for muscle spasticity management. Its high-quality crystalline form and cGMP production ensure it is safe, potent, and reliable for pharmaceutical dosage forms. 💊💪

🌿 Q2. What is Tizanidine Hydrochloride API by Swapnroop Drugs & Pharmaceuticals used for? 🌿

Therapeutic Uses:

• Muscle Spasticity Relief 💪 – Effective in reducing stiffness and involuntary muscle contractions.

• Neurological Disorders 🧠 – Used in multiple sclerosis, spinal cord injuries, cerebral palsy, and post-stroke spasticity.

• Adjunct Therapy 🔹 – Helps improve mobility, posture, and comfort when combined with physiotherapy.

• Pain Management ⚡ – Indirectly reduces pain associated with muscle spasms.

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

• Chemical Name: Tizanidine Hydrochloride

• CAS Number: 51329-02-3

• Molecular Formula: C₉H₈ClN₅S·HCl

• Molecular Weight: 280.2 g/mol

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in water; slightly soluble in ethanol

• Stability: Stable in dry conditions, sensitive to moisture and light

• Melting Point: ~225–227°C

• pH: Slightly acidic in aqueous solution

• Hygroscopicity: Minimal, but requires controlled storage conditions

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⚙️ Q4. How is Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals synthesized? ⚙️

Tizanidine Hydrochloride is synthesized via multi-step organic chemical synthesis:

1. Benzothiadiazole Core Formation 🧪 – Construction of the core ring system via cyclization of appropriate precursors.

2. Chlorination Step ⚗️ – Introduction of chlorine at the 5-position to yield 5-chloro intermediate.

3. Amine Substitution 🔄 – Incorporation of the imidazoline group to form the active Tizanidine base.

4. Hydrochloride Salt Formation 💧 – Conversion of Tizanidine base into hydrochloride salt for enhanced stability and solubility.

5. Purification & Drying ✨ – Crystallization and drying to obtain high-purity API.

6. Quality Control Testing 🔬 – Ensures identity, purity, and compliance with pharmacopeial standards.

This process ensures that Swapnroop Drugs & Pharmaceuticals produces API of consistent potency, high purity, and suitable for pharmaceutical dosage forms.

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

• Tablets 💊 – Most common oral dosage form, available in 2 mg and 4 mg strengths.

• Oral Capsules 🏺 – For controlled-release formulations or patient convenience.

• Oral Solution / Suspension 🥛 – Used for patients who have difficulty swallowing tablets.

• Compounded Forms ⚗️ – May be prepared in hospital pharmacies for specific dosing requirements.

All dosage forms are optimized for systemic absorption, providing effective muscle relaxation and symptom control.

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⚗️ Q6. How are Tizanidine Hydrochloride API dosage forms prepared? ⚗️

• Tablets:

  • API is blended with excipients like fillers, binders, disintegrants, and lubricants ⚖️.

  • The mixture is compressed into tablets using a tablet press 🏭.

  • Film coating may be applied for taste masking or controlled release 🌈.

• Oral Solutions/Suspensions:

  • API is dissolved or suspended in suitable solvents with stabilizers 💧.

  • Flavoring agents and preservatives may be added for palatability and stability 🍓.

• Capsules:

  • API is blended with excipients and filled into gelatin or HPMC capsules 🏺.

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✅ Q7. What is the appropriate dosage form of Tizanidine Hydrochloride manufactured by Swapnroop Drugs & Pharmaceuticals? ✅

• Primary Form: Oral tablets 💊 – standard for outpatient therapy.

• Oral Solution: 🥛 – For pediatric, geriatric, or dysphagic patients.

• Dosage strength is selected based on clinical condition and patient tolerance (often starting low and titrated).

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🕒 Q8. When should Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals be taken? 🕒

• Dosing Schedule: Typically 3 times daily, depending on spasticity severity and physician prescription.

• Timing: Can be taken with or without food; avoid abrupt cessation to prevent rebound hypertension ⚠️.

• Start Low, Titrate Slowly: Initial doses are 2 mg, gradually increased to optimize effect and minimize side effects 💊.

• Monitoring: Blood pressure and liver function may be monitored during therapy 🩺.

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

Therapeutic Effects:

• Muscle Relaxation 💪 – Reduces spasticity and involuntary muscle contractions.

• Pain Relief ⚡ – Alleviates discomfort associated with muscle stiffness.

• Improved Mobility 🚶 – Enhances functional movement and quality of life for patients with neuromuscular conditions.

Common Side Effects:

• CNS Effects: Drowsiness 😴, dizziness 🌀, fatigue 😓

• Cardiovascular: Hypotension (low blood pressure) 🩸, bradycardia (slow heart rate) ❤️

• Gastrointestinal: Dry mouth 😛, nausea 🤢

• Other: Weakness, mild liver enzyme elevation ⚠️

Important Note: Effects are dose-dependent; gradual titration is recommended to minimize adverse effects.

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🔬 Q10. How is Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals tested? 🔬

Tizanidine Hydrochloride API undergoes rigorous quality control testing to ensure safety, efficacy, and compliance:

• Identity Tests 🧪 – Confirm chemical structure using HPLC, IR, and NMR spectroscopy.

• Purity Assays ✨ – HPLC ensures API purity ≥98%.

• Impurity Profiling ⚗️ – Detects residual solvents, unreacted intermediates, and degradation products.

• Moisture Content 💧 – Measured by Karl Fischer titration to ensure stability.

• pH and Solubility Testing ⚖️ – Ensures consistent formulation performance.

• Microbial Testing 🦠 – Confirms absence of contamination for injectable or compounded forms.

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🧪 Q11. What tests are performed on Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals? 🧪

Additional analytical and quality checks include:

• Melting Point Determination 🌡️ – Confirms crystalline purity and stability.

• Spectroscopic Analysis 🔬 – UV, IR, and NMR for structural verification.

• Chromatographic Assays 🏭 – HPLC or GC to quantify impurities and ensure batch consistency.

• Assay of Active Ingredient 💊 – Confirms correct API content per pharmacopeial standards.

• Stability Testing 📆 – ICH-guided studies under varied temperature, humidity, and light conditions.

• Dissolution & Solubility Tests 💧 – Relevant for oral dosage forms to ensure bioavailability.

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⚙️ Q12. What are the challenges in manufacturing Tizanidine Hydrochloride API by Swapnroop Drugs & Pharmaceuticals? ⚙️

Manufacturing Tizanidine Hydrochloride API involves several challenges:

1. Multi-step Synthesis Complexity 🧪 – Requires precise chemical reactions for high yield and purity.

2. Purity Control ✨ – Removal of unreacted intermediates and by-products is critical.

3. Moisture & Light Sensitivity 🌡️ – The crystalline API can degrade if exposed to humidity or light.

4. Regulatory Compliance 📜 – cGMP standards must be strictly followed for batch consistency.

5. Analytical Verification 🔬 – Accurate identification, assay, and impurity testing require advanced instrumentation.

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💊 Q13. What are the challenges in manufacturing Tizanidine Hydrochloride dosage forms by Swapnroop Drugs & Pharmaceuticals? 💊

• Dose Accuracy ⚖️ – Ensuring uniform API distribution in tablets or capsules.

• Stability Issues ❄️ – Preventing degradation during formulation and storage.

• Excipients Compatibility ⚗️ – Selection of fillers, binders, and coatings that do not affect API efficacy.

• Patient Compliance 👵👨‍🦳 – Designing tablets, capsules, or solutions that are easy to swallow and administer.

• Quality Control 🧪 – Continuous testing for dissolution, uniformity, and microbial safety.

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🌡️ Q14. What are the storage conditions for Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals? 🌡️

• Temperature: Store at 20–25°C, protected from excess heat or freezing 🌡️.

• Moisture Protection: Keep in airtight, moisture-resistant containers 💧.

• Light Sensitivity: Store away from direct sunlight ☀️.

• Handling: Use standard laboratory precautions; avoid contamination.

• Stability Monitoring: Regular checks ensure potency, purity, and physical integrity throughout storage.

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📦 Q15. What is the packaging for Tizanidine Hydrochloride API manufactured by Swapnroop Drugs & Pharmaceuticals? 📦

• Primary Packaging:

  • High-density polyethylene (HDPE) bottles 🧴 – protects against moisture and contamination.

  • Desiccant inclusion 💧 – maintains low humidity inside the container.

  • Sealed foil or laminated bags 🛡️ – optional for bulk API transport.

• Secondary Packaging:

  • Cartons with protective inserts 📦 – safeguards the primary container during storage and shipping.

  • Labeling: Includes batch number, manufacturing date, expiration date, storage instructions, and safety information.

• Special Considerations:

  • Packaging materials are chosen to prevent light and moisture exposure, ensuring API stability.

  • Suitable for transport under controlled conditions to maintain quality.

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

• Typical Shelf Life: 24–36 months when stored under recommended conditions (20–25°C, protected from light and moisture).

• Post-Opening / Handling: Ensure containers are tightly sealed and avoid prolonged exposure to humidity.

• Stability Monitoring: Conducted per ICH guidelines, including temperature, humidity, and light stress tests to verify potency, purity, and physical integrity.

• Expiry: Clearly marked on packaging to ensure safe and effective use.

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