"Tofacitinib Citrate API (CAS No. 477600-75-2) – Properties, Uses, Synthesis, and Dosage Forms"

 

Q1. What is Tofacitinib Citrate API manufactured by Swapnroop Drugs & Pharmaceuticals? 💊✨

Short Answer:
Tofacitinib Citrate is a Janus kinase (JAK) inhibitor, used as an active pharmaceutical ingredient (API) for the treatment of autoimmune and inflammatory disorders. It works by modulating the JAK-STAT signaling pathway, thereby reducing abnormal immune responses.

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Detailed Description (In-Depth) 🌟

1. Pharmacological Class & Mechanism 🔬

• Tofacitinib Citrate is a small molecule JAK inhibitor.

• It selectively inhibits JAK1 and JAK3 enzymes, which play a key role in cytokine signaling involved in inflammation and immune regulation.

• By blocking these pathways, it reduces overactive immune responses, providing relief in chronic autoimmune conditions. 🧠💉

2. Clinical Uses & Therapeutic Significance 🏥💚

• Rheumatoid Arthritis (RA) 🤲 – Reduces joint inflammation, pain, and stiffness.

• Psoriatic Arthritis (PsA) 🌿 – Helps improve joint mobility and skin symptoms.

• Ulcerative Colitis (UC) 🩸 – Reduces gastrointestinal inflammation and flare-ups.

• Other Investigational Uses 🔬 – Explored in ankylosing spondylitis, alopecia areata, and other autoimmune disorders.

3. Chemical Identity & Formulation 🧪

• IUPAC Name: 3-[(3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]-3-oxopropanenitrile citrate

• CAS Number: 477600-75-2

• Molecular Formula: C₁₆H₂₀N₆O·C₆H₈O₇

• Molecular Weight: 504.5 g/mol (citrate form)

• Appearance: White to off-white crystalline powder, suitable for oral formulation.

4. Physicochemical Characteristics ⚗️

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in water; moderately soluble in organic solvents

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

• Melting Point: ~174–176°C

5. Manufacturing Importance 🏭

• Tofacitinib Citrate API is used to formulate oral tablets for systemic treatment of autoimmune disorders.

• High-quality API ensures consistent bioavailability, potency, and patient safety. 🌍💊

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✨ Summary:
Tofacitinib Citrate API by Swapnroop Drugs & Pharmaceuticals is a potent JAK inhibitor, essential for the treatment of autoimmune and inflammatory diseases. Its high-purity crystalline form and cGMP-compliant production ensure it is safe, effective, and reliable for pharmaceutical dosage forms. 💊🧬

🌿 Q2. What is Tofacitinib Citrate API by Swapnroop Drugs & Pharmaceuticals used for? 🌿

Therapeutic Uses:

• Rheumatoid Arthritis (RA) 🤲 – Reduces joint inflammation, pain, and stiffness.

• Psoriatic Arthritis (PsA) 🌿 – Improves joint mobility and alleviates skin symptoms.

• Ulcerative Colitis (UC) 🩸 – Controls gastrointestinal inflammation and flare-ups.

• Other Autoimmune Disorders 🔬 – Investigational uses in ankylosing spondylitis, alopecia areata, and more.

• Adjunct Therapy 💚 – Often used alongside other disease-modifying agents to improve outcomes.

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

• Chemical Name: Tofacitinib Citrate

• CAS Number: 477600-75-2

• Molecular Formula: C₁₆H₂₀N₆O·C₆H₈O₇

• Molecular Weight: 504.5 g/mol

• Appearance: White to off-white crystalline powder

• Solubility: Water-soluble; moderately soluble in ethanol and other organic solvents

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

• Melting Point: ~174–176°C

• pH: Slightly acidic in aqueous solution

• Hygroscopicity: Minimal, requires moisture-controlled storage

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⚙️ Q4. How is Tofacitinib Citrate API manufactured by Swapnroop Drugs & Pharmaceuticals synthesized? ⚙️

Tofacitinib Citrate is synthesized via a multi-step organic chemical process:

1. Pyrrolopyrimidine Core Formation 🧪 – Construction of the heterocyclic scaffold using selective cyclization.

2. Substitution & Functionalization ⚗️ – Introduction of methyl, amino, and piperidine groups at specific positions.

3. Chiral Center Introduction 🔄 – Stereoselective synthesis to achieve the correct 3R,4R configuration for biological activity.

4. Citrate Salt Formation 💧 – Conversion of Tofacitinib base to citrate salt for enhanced solubility and stability.

5. Purification & Crystallization ✨ – Obtains high-purity crystalline API suitable for oral dosage forms.

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

This ensures Swapnroop Drugs & Pharmaceuticals delivers API with consistent potency, purity, and suitability for pharmaceutical formulations.

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

• Oral Tablets 💊 – Most common dosage form, typically 5 mg and 10 mg strengths.

• Oral Capsules 🏺 – Occasionally used for controlled-release formulations.

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

• Compounded Forms ⚗️ – May be prepared in hospital pharmacies for specific dosing or pediatric use.

All forms are designed for systemic absorption to effectively inhibit JAK-mediated inflammatory pathways.

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⚗️ Q6. How are Tofacitinib Citrate API dosage forms prepared? ⚗️

• Tablets:

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

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

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

• Oral Solutions / Suspensions:

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

  • Flavoring agents and preservatives are added for palatability and shelf-life 🍓.

• 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 Tofacitinib Citrate manufactured by Swapnroop Drugs & Pharmaceuticals? ✅

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

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

• Dosage Strength: Selected based on clinical condition, patient weight, and disease severity, often starting low and titrating gradually.

• Administration Guidance: Taken with or without food, following physician prescription.

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🕒 Q8. When should Tofacitinib Citrate API manufactured by Swapnroop Drugs & Pharmaceuticals be taken? 🕒

• Dosing Schedule: Usually twice daily for rheumatoid arthritis or as prescribed by a physician.

• Timing: Can be taken with or without food 🍽️.

• Start Low, Titrate Slowly: Initial doses are generally 5 mg, adjusted based on response and tolerance.

• Monitoring: Regular blood tests may be required to monitor liver function, blood counts, and cholesterol levels 🩺.

• Important Note: Avoid abrupt discontinuation to prevent disease flare-ups ⚠️.

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

Therapeutic Effects:

• Anti-inflammatory 🩹 – Reduces cytokine-mediated inflammation in joints and tissues.

• Immune Modulation 🧬 – Controls abnormal immune responses in autoimmune disorders.

• Improved Mobility 🚶 – Alleviates joint stiffness and pain, improving quality of life.

Common Side Effects:

• CNS: Headache 🤕, dizziness 🌀

• Gastrointestinal: Nausea 🤢, diarrhea 💧

• Hematologic: Increased risk of infections 🦠, mild anemia

• Other: Elevated liver enzymes ⚠️, lipid profile changes 💳

Important: Effects are dose-dependent; gradual titration helps minimize side effects.

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🔬 Q10. How is Tofacitinib Citrate API manufactured by Swapnroop Drugs & Pharmaceuticals tested? 🔬

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

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

• Impurity Profiling ⚗️ – Detects residual solvents, by-products, and degradation compounds.

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

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

• Microbial Testing 🦠 – Confirms absence of contamination for safety.

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Do you want me to continue with Q11, Q12, and Q13 (Tests performed, API manufacturing challenges, and dosage form challenges) next?

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

• 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 💧 – Ensures bioavailability in oral dosage forms.

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

• Complex Multi-step Synthesis 🧪 – Requires precise chemical reactions to achieve high yield and purity.

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

• Moisture & Light Sensitivity 🌡️ – Crystalline API can degrade if exposed to humidity or sunlight.

• Regulatory Compliance 📜 – Strict adherence to cGMP standards is required.

• Analytical Verification 🔬 – Accurate identification, assay, and impurity profiling require advanced instrumentation.

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

• Dose Uniformity ⚖️ – Ensuring equal API distribution in tablets or capsules.

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

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

• Patient Compliance 👵👨‍🦳 – Tablets, capsules, or solutions must be 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 Tofacitinib Citrate API manufactured by Swapnroop Drugs & Pharmaceuticals? 🌡️

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

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

• Light Sensitivity: Store away from direct sunlight ☀️.

• Handling: Standard laboratory precautions to avoid contamination.

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

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📦 Q15. What is the packaging for Tofacitinib Citrate 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 primary containers during storage and shipping.

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

• Special Considerations:

  • Packaging prevents light and moisture exposure, ensuring API stability.

  • Suitable for controlled-condition transport to maintain quality.

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

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

• Post-Opening / Handling: Containers must remain tightly sealed; avoid prolonged exposure to humidity.

• Stability Monitoring: Conducted per ICH guidelines, including temperature, humidity, and light stress tests.

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

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✅ This completes the full Q1–Q16 detailed profile for Tofacitinib Citrate API, ready for technical datasheets, product catalogs, or marketing purposes for Swapnroop Drugs & Pharmaceuticals.

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