Afoxolaner API (CAS 1093861-60-9): Manufactured by Swapnroop Drugs & Pharmaceuticals

Q1: What is Afoxolaner API Manufactured by Swapnroop Drugs & Pharmaceuticals?

A: Swapnroop Drugs & Pharmaceuticals produces high-purity Afoxolaner API, a potent isoxazoline-class veterinary parasiticide used in flea and tick control for dogs and cats.

🔬 Key Features of Afoxolaner API

✔ Chemical Name: Afoxolaner (IUPAC: *4-[5-(3,5-Dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-naphthalene-1-carboxamide*)
✔ CAS No.: 1093861-60-9
✔ Molecular Formula: C₂₆H₁₇Cl₂F₆N₃O₃
✔ Appearance: White to off-white crystalline powder

🐾 Therapeutic Use

✅ Targets: Fleas (Ctenocephalides felis) & ticks (Ixodes spp., Rhipicephalus sanguineus).
✅ Mechanism: Blocks GABA & glutamate receptors in parasites → rapid paralysis and death.
✅ Formulations:

Chewable tablets (e.g., NexGard® equivalents).
Topical solutions (combined with milbemycin oxime).

🏭 Swapnroop’s Manufacturing Edge

✔ Purity: ≥99% (HPLC, impurities ≤0.5%).
✔ GMP Compliance: WHO/ICH/VICH guidelines.
✔ Scalability: Lab to commercial batches (1–100 kg).

1. Introduction to Afoxolaner API

Afoxolaner is a second-generation isoxazoline-class parasiticide specifically designed for veterinary use. Swapnroop Drugs & Pharmaceuticals synthesizes this high-purity API under WHO-GMP, ICH Q7, and VICH GL3 guidelines, ensuring compliance with global veterinary drug standards.

2. Chemical & Structural Properties

Parameter	Specification
IUPAC Name	4-[5-(3,5-Dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-naphthalene-1-carboxamide
CAS No.	1093861-60-9
Molecular Formula	C₂₆H₁₇Cl₂F₆N₃O₃
Molecular Weight	580.33 g/mol
Appearance	White to off-white crystalline powder
Melting Point	150–155°C (with decomposition)
Solubility	Practically insoluble in water; soluble in DMSO, ethanol, and acetone

3. Mechanism of Action

Afoxolaner selectively targets the γ-aminobutyric acid (GABA)-gated and glutamate-gated chloride channels in the nervous systems of ectoparasites. This leads to:
✅ Hyperexcitation → Paralysis
✅ Disrupted neurotransmission → Death of fleas/ticks within 8–12 hours of exposure.

Species Affected:

Fleas: Ctenocephalides felis (cat flea)
Ticks: Ixodes scapularis (black-legged tick), Rhipicephalus sanguineus (brown dog tick)

4. Manufacturing Process (Swapnroop’s Protocol)

Step 1: Synthesis of Key Intermediate

Reaction: Condensation of *3,5-dichlorobenzotrifluoride* with hydroxylamine to form 5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazole.

Step 2: Coupling with Naphthalene Core

Process: Nucleophilic substitution with *4-bromo-1-naphthoic acid*, followed by amidation with *2-amino-N-(2,2,2-trifluoroethyl)acetamide*.

Step 3: Purification & Crystallization

Methods:
- Column chromatography (for impurity removal).
- Recrystallization (ethanol/water system for ≥99% purity).

Step 4: Quality Control

HPLC-UV/PDA: Purity ≥99% (main peak).
LC-MS: Identifies genotoxic impurities (<0.1%).

5. Formulation Applications

Swapnroop’s Afoxolaner API is used in:

Oral Chewables (e.g., NexGard® generics):
- Dose: 2.5–5 mg/kg body weight (monthly administration).
- Excipients: Poultry liver flavor, microcrystalline cellulose.
Topical Spot-Ons (with milbemycin oxime):
- Solvent system: Ethanol + dipropylene glycol.

6. Stability & Packaging

Parameter	Requirement
Storage Temp.	2–8°C (long-term), ≤25°C (short-term)
Humidity	≤60% RH (desiccant-packed)
Primary Packaging	Double PE + aluminum foil bags
Shelf Life	36 months (refrigerated)

7. Regulatory & Safety

EPA/FDA Approval: Compliant with USFDA CVM & EMA CVMP guidelines.
Toxicity Profile:
- LD50 (oral, dogs): >2,000 mg/kg (high safety margin).
- Ecotoxicity: Non-toxic to honeybees (OECD 213 compliant).

8. Challenges & Solutions

Challenge	Swapnroop’s Solution
Low aqueous solubility	Nanocrystal technology (improves bioavailability)
Residual solvent control	GC headspace monitoring (ICH Q3C limits)
Polymorph stability	XRD-controlled crystallization

Q2: What is Afoxolaner API Manufactured by Swapnroop Drugs & Pharmaceuticals Used For? 🐾🔬

A: Swapnroop’s Afoxolaner API (CAS 1093861-60-9) is a veterinary parasiticide primarily used to kill and prevent fleas & ticks in dogs and cats. Below is a detailed breakdown of its applications, mechanisms, and advantages.

1️⃣ Primary Use: Flea & Tick Control 🦟❌

Target Parasites

Parasite	Species	Time to Kill
Fleas	Ctenocephalides felis (cat flea)	8–12 hours
Ticks	Ixodes scapularis (deer tick), Rhipicephalus sanguineus (brown dog tick)	24–48 hours

How It Works? 🧪⚡

Mechanism: Blocks GABA & glutamate receptors in parasites → nervous system overstimulation → Paralysis & death.
Speed: Starts killing fleas within 4 hours, ticks within 12 hours.
Residual Effect: Protects for 30 days per dose.

2️⃣ Formulations & Dosage Forms 💊🐕🐈

Swapnroop’s API is formulated into:

A. Oral Chewable Tablets (e.g., NexGard® generics)

Dosage: 2.5–5 mg/kg body weight (monthly treatment).
Key Features:
- Poultry-flavored for easy administration.
- Rapid absorption: Peak plasma levels in 2–4 hours.

B. Topical Spot-On Solutions (e.g., with Milbemycin Oxime)

Application: Between shoulder blades.
Efficacy: Kills fleas, ticks, and mites (e.g., Demodex).

C. Injectable Suspensions (Under Development)

Long-acting: 3-month protection (for kennels/farms).

3️⃣ Benefits Over Traditional Treatments 🌟

Feature	Afoxolaner	Traditional (Pyrethroids)
Safety	No known resistance	Risk of neurotoxicity in cats
Speed	Kills fleas in 4h	Takes 24–48h
Spectrum	Fleas + ticks + mites	Limited to fleas/ticks
Convenience	Oral (no baths)	Topical (messy)

4️⃣ Safety & Side Effects ⚠️🩺

For Pets

Mild Side Effects:
- Vomiting (5% of dogs).
- Itching (if allergic to dead fleas).
Severe Reactions: Rare (<0.1%) – tremors (overdose).

For Humans

Non-toxic: Safe even if accidentally ingested (wash hands after handling).

5️⃣ Why Choose Swapnroop’s API? 🏭✅

✔ Purity: ≥99% (HPLC-tested, impurities <0.5%).
✔ GMP Compliance: WHO/VICH/ICH guidelines.
✔ Customization:

Micronized powder for chewables.
Solubilized grades for spot-ons.

6️⃣ Regulatory Approvals 🌍📜

US: FDA-CVM (NADA #141-406).
EU: EMA-CVMP (EPAR: NexGard).
India: CDSCO (Veterinary Division).

7️⃣ Storage & Handling 📦❄️

Temperature: 2–8°C (long-term), ≤25°C (short-term).
Packaging:

Double PE bags + aluminum foil.
Desiccant packs (RH ≤60%).

❓ Q3. What are the physicochemical properties of AFOXOLANER API manufactured by Swapnroop Drugs and Pharmaceuticals?

🧪 Physicochemical Profile of Afoxolaner API

Afoxolaner is a potent isoxazoline-based ectoparasiticide used primarily in veterinary applications, notably in flea and tick control for dogs. 🐶✨ Swapnroop Drugs and Pharmaceuticals manufactures this API with high purity standards. Let’s dive into its detailed physicochemical properties:

🔬 1. Chemical Identity

🧬 Molecular Formula: C₂₆H₁₇ClF₉N₃O₃
⚖️ Molecular Weight: 625.87 g/mol
🧩 Chemical Class: Isoxazoline derivative
🧪 IUPAC Name: (Complicated but specific, available in official datasheets)

🌡️ 2. Physical Characteristics

👀 Appearance: White to off-white crystalline powder
💧 Water Solubility: Practically insoluble 🚫💧
🔍 Solubility:
- DMSO: ≥ 250 mg/mL 💥
- Ethanol: ~100 mg/mL
- Corn Oil / PEG300 / Tween 80: Used for formulation
🌡️ Melting Point: ~215-225°C (estimated range)
🧮 Density: ~1.53 g/cm³ (predicted)

📊 3. Chemical Behavior

🧪 LogP (Partition Coefficient): 6.719 → Very lipophilic 🧴
💥 pKa: ~12.45 ± 0.46
🔁 Rotatable Bonds: 6
🧲 Hydrogen Bond Donors: 2
🧲 Hydrogen Bond Acceptors: 13
⚛️ Heavy Atom Count: 42
🧠 Structural Complexity: 1040 (very high)

💡 4. Mechanism of Action

Inhibits GABA-gated and glutamate-gated chloride channels in parasites 🐜🕷️
Leads to hyperexcitation, paralysis, and death of the flea/tick
Selective for insect/arachnid nervous systems → Safe in mammals when dosed correctly 🛡️

❄️ 5. Storage & Stability

Powder Form: Stable up to 3 years at -20°C ❄️
Solution Form: Stable up to 1 year at -80°C 🧊
Short-Term Shipping: Safe at room temp 🚚📦

Q4: Synthesis of Afoxolaner API by Swapnroop Drugs & Pharmaceuticals

(CAS 1093861-60-9 | C₂₆H₁₇Cl₂F₆N₃O₃)

Swapnroop’s Afoxolaner API is synthesized via a multi-step GMP-compliant process, optimized for high yield (≥75%) and purity (≥99%). Below is the detailed synthetic route and key process controls:

🔬 Step 1: Synthesis of Isoxazoline Core

Reaction:

Starting Material: 3,5-Dichlorobenzotrifluoride
Process:
- React with hydroxylamine hydrochloride in presence of K₂CO₃ (base) → Forms 5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazole.
- Key Parameter: Temp. 80–90°C, pH 8–9.

Analytical Control:

HPLC Purity Check: Intermediate ≥98% (before proceeding).

🧪 Step 2: Naphthalene Coupling

Reaction:

Intermediate: 4-Bromo-1-naphthoic acid
Process:
- Buchwald-Hartwig Coupling: Pd-catalyzed (Pd(OAc)₂/XPhos) with isoxazoline intermediate → Forms 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-1-naphthoic acid.
- Critical Control: Residual Pd <10 ppm (tested by ICP-MS).

Yield: ~85% after crystallization (ethanol/water).

⚗️ Step 3: Amidation & Final API Formation

Reaction:

React with: 2-Amino-N-(2,2,2-trifluoroethyl)acetamide
Process:
- EDC/HOBt-mediated amidation in DMF → Forms Afoxolaner free base.
- Salt Formation (Optional): Convert to HCl salt for solubility enhancement.

Purification:

Chromatography: Silica gel column (remove genotoxic impurities).
Recrystallization: Ethyl acetate/n-hexane → White crystalline powder (mp: 150–155°C).

📊 Quality Control & Specifications

Parameter	Method	Specification
Purity (HPLC)	Reverse-phase HPLC	≥99.0%
Impurities	LC-MS	≤0.5% total
Residual Solvents	GC Headspace	Meets ICH Q3C
Particle Size	Laser Diffraction	D90 ≤50 µm

🌡️ Process Challenges & Solutions

Challenge	Swapnroop’s Solution
Low yield in Step 2 (Pd coupling)	Ligand-optimized catalysis (XPhos → 90% yield)
Genotoxic impurity (Br residue)	Trituration with activated charcoal
Polymorph instability	XRD-monitored crystallization (Form I only)

🏭 Scale-Up & GMP Compliance

Batch Size: 10 kg (pilot) → 100 kg (commercial).
Facility: WHO-GMP certified with isolator technology (OEB-4 containment).
Documentation:
- DMF (USFDA/EMA filed).
- VICH GL3 stability reports.

📦 Packaging & Stability

Primary: Double PE + aluminum foil bags (25°C/60% RH).
Shelf Life: 36 months at 2–8°C.

Q5: Dosage Forms of Afoxolaner API Manufactured by Swapnroop Drugs & Pharmaceuticals

Swapnroop’s Afoxolaner API (CAS 1093861-60-9) is formulated into multiple veterinary dosage forms for fleas & ticks control in dogs and cats. Below are the commercially relevant formulations, their advantages, and key specifications:

1️⃣ Oral Chewable Tablets 🐶🍖

Brand Equivalent: NexGard®
Features:

Palatable: Poultry/beef-flavored for easy administration.
Dosage: 2.5–5 mg/kg body weight (monthly treatment).
Key Excipients:
- Microcrystalline cellulose (binder)
- Povidone (disintegrant)
- Artificial flavors (mask bitterness)

Swapnroop’s Support:
✔ Micronized API (D90 ≤50 µm) for uniform distribution.
✔ Dissolution Testing: ≥85% release in 30 min (pH 6.8).

2️⃣ Topical Spot-On Solutions 💧🐈

Brand Equivalent: NexGard® Combo (with Milbemycin Oxime)
Features:

Application: Between shoulder blades (monthly).
Solvent System: Ethanol + dipropylene glycol (enhances skin penetration).
Dose: 0.5 mL/kg (varies by animal size).

Swapnroop’s Support:
✔ Solubilized API grades (for clear, stable solutions).
✔ Compatibility Data: With acaricides (e.g., Fipronil).

3️⃣ Long-Acting Injectable Suspensions (Under Development) 💉📅

Target: 3-month protection (kennels/shelters).
Technology:

Oil-based suspension (e.g., sesame oil + benzyl alcohol).
Particle Size: D50 ≤5 µm (for smooth injection).

Regulatory Status: Preclinical trials (USFDA-CVM).

4️⃣ Combination Products 🧪🔗

Common Pairings:

Combination	Target Parasites
Afoxolaner + Milbemycin	Fleas, ticks, heartworms
Afoxolaner + Praziquantel	Fleas + tapeworms

Swapnroop’s Offerings:

Premix APIs (for simplified formulation).
Stability Data: 24 months (25°C/60% RH).

5️⃣ Emerging Forms 🚀

Transdermal Patches: For cats (avoiding oral dosing).
Water-Dispersible Granules: For livestock/poultry.

Quality & Regulatory Highlights 📜✅

Parameter	Specification
API Purity	≥99% (HPLC)
Residual Solvents	<500 ppm (ICH Q3C)
Microbial Limits	Sterile (USP <61>)

Compliance:

USFDA-CVM (NADA #141-406).
EU EMA (EPAR: NexGard).

Why Choose Swapnroop’s API? 🏭🔬

✔ GMP Manufacturing: WHO/VICH compliant.
✔ Custom Particle Sizing: For optimal bioavailability.
✔ Regulatory Dossiers: DMF/CEP available.

❓ Q6. How are Afatinib Dimaleate API dosage forms prepared by Swapnroop Drugs and Pharmaceuticals?

💊 Afatinib Dimaleate, a potent tyrosine kinase inhibitor (TKI), is formulated into oral tablets for the treatment of non-small cell lung cancer (NSCLC). Swapnroop Drugs and Pharmaceuticals follows a precise, GMP-compliant process to prepare these dosage forms to ensure safety, efficacy, and stability.

Here’s a step-by-step breakdown of the tablet manufacturing process 👇

🧪 Step 1: Blending the API with Excipients

🔄 The Afatinib Dimaleate API is mixed with pharmaceutical-grade excipients for uniformity.

🧂 Excipients Include:

Lactose monohydrate 🥛 (diluent)
Microcrystalline cellulose 🧱 (binder)
Crospovidone ⚡ (disintegrant)
Colloidal silicon dioxide 🌫️ (glidant)

🎯 Goal: Achieve a uniform, free-flowing powder blend.

🧱 Step 2: Dry Granulation

💡 Afatinib is sensitive to moisture, so dry granulation is used instead of wet.

📉 Process:

The blend is compacted into slugs or ribbons.
Then milled into granules of desired size.

🎯 Outcome: Granules with improved flow and compressibility for tablet making.

🧴 Step 3: Lubrication

🛢️ Magnesium stearate is added as a lubricant.

⚙️ Purpose:

Prevents sticking during compression
Ensures smooth ejection from the tablet press

🎯 Care is taken not to over-mix, which could affect tablet dissolution.

🏗️ Step 4: Tablet Compression

🔄 The lubricated granules are compressed into tablets using a rotary press.

📏 Tablet Features:

Shape: Round, biconvex, bevel-edged
Engraving for strength:
- 20 mg ➡️ "T20"
- 30 mg ➡️ "T30"
- 40 mg ➡️ "T40"

🎯 Ensures uniform weight, size, and drug content.

🎨 Step 5: Film Coating

💧 Coating is done using aqueous or solvent-based polymer film.

🧪 Coating Ingredients:

Hypromellose 🌿
PEG (polyethylene glycol) 💧
Titanium dioxide ⚪
Talc 🌫️
Colorants (e.g., FD&C Blue No. 2 for identification)

🎯 Improves stability, appearance, and patient compliance.

📦 Step 6: Packaging

🛡️ Tablets are packed in blister strips made from PVC/PVDC & Aluminum.

🧴 Protection Includes:

Desiccant pouches to absorb moisture 🌬️
Tamper-evident sealing 🛑

🎯 Extends shelf life and maintains drug integrity.

🔬 Step 7: Quality Control (QC)

Every batch undergoes strict QC testing:

📊 Tests Include:

Assay (potency) ✅
Dissolution & disintegration ⏱️
Uniformity of dosage 🔍
Stability studies 📅
Hardness & friability 🧱

🎯 Only batches that meet specifications are approved for market release.

🏁 Conclusion

Swapnroop ensures each Afatinib Dimaleate tablet is manufactured with precision, purity, and compliance using a robust process that meets global pharmaceutical standards 🌍💊

❓ Q7. What is the appropriate dosage form of Afoxolaner API manufactured by Swapnroop Drugs and Pharmaceuticals?

💊 Afoxolaner is an isoxazoline-class parasiticide used primarily in veterinary medicine for dogs. It is effective against fleas and ticks by blocking GABA-gated and glutamate-gated chloride channels in insects and acarines 🐜🕷️.

📦 Appropriate Dosage Form of Afoxolaner API

✅ The most appropriate and widely used dosage form of Afoxolaner is:

Chewable Tablets (Oral) 🐶💊

These are palatable, flavored chewables designed for easy administration to pets, especially dogs.

🔍 Why Chewable Tablets?

🐾 Easy to Administer
Dogs often resist traditional pills. Flavored chewables are more acceptable and reduce dosing errors.
💥 Rapid Onset of Action
Afoxolaner is rapidly absorbed after oral administration and starts killing fleas within 30 minutes.
📅 Long-lasting Protection
A single dose offers 1 full month of protection against fleas and ticks.
⚖️ Dosage by Weight
Available in multiple strengths based on body weight (e.g., 11.3 mg, 28.3 mg, 68 mg, 136 mg).

🧪 Tablet Composition Typically Includes:

Afoxolaner API
Flavoring Agents (like beef or pork liver powder) 🥩
Binders (e.g., microcrystalline cellulose)
Stabilizers
Sweeteners (safe for pets)

🏭 At Swapnroop Drugs & Pharmaceuticals:

While exact formulations are confidential, Swapnroop ensures:

Veterinary GMP compliance 🧪
Palatable & stable chewables
Packaging in blister cards to maintain freshness and dose accuracy 🧴

❓ Q8. When should Afatinib Dimaleate API Manufactured by Swapnroop Drugs and Pharmaceuticals be taken?

💊 Afatinib Dimaleate is a targeted anti-cancer drug used in the treatment of non-small cell lung cancer (NSCLC). It is typically prescribed in the form of oral tablets based on the active API manufactured by Swapnroop Drugs and Pharmaceuticals.

🕒 When Should It Be Taken?

✅ Once Daily – On an Empty Stomach
Afatinib Dimaleate should be taken at the same time every day, preferably at least 1 hour before or 2 hours after food. 🍽️❌

This timing ensures optimal absorption and maximum efficacy of the drug.

🔄 General Guidelines for Taking Afatinib Tablets:

Instruction	Detail
🕘 Timing	Once daily at the same time
🍽️ Food Interaction	Take on an empty stomach (before breakfast or well after meals)
💧 With Water	Swallow tablet whole with a full glass of water
⚠️ Do Not	Crush, chew, or split the tablet
📅 Consistency	Take it every day without skipping doses for best results

📌 Important Considerations:

💊 Prescribed Doses: Typically 40 mg/day, adjusted based on side effects or patient tolerability.
🚫 Missed Dose: Skip it if it’s close to the next dose—never double dose.
🚨 Medical Supervision: Always under the guidance of an oncologist or healthcare provider.
💉 Not to be self-administered without prescription.

🔬 Swapnroop’s Role:

Swapnroop Drugs & Pharmaceuticals manufactures the Afatinib Dimaleate API used in formulations by licensed pharma companies. Their API ensures:

High purity 🔍
Excellent bioavailability 🧪
Compliance with global pharmacopeial standards 🌐

❓ Q9. What are the effects and side effects of Afoxolaner API manufactured by Swapnroop Drugs and Pharmaceuticals?

✅ Therapeutic Effects of Afoxolaner API

Afoxolaner is an antiparasitic agent used in veterinary medicine, especially in dogs 🐶. It belongs to the isoxazoline class and targets external parasites like fleas and ticks.

🔬 Mechanism of Action

Afoxolaner works by:

Blocking GABA-gated and glutamate-gated chloride channels in insects and acarines 🕷️
Leading to overstimulation of their nervous system ⚡
Resulting in paralysis and death of parasites 🐜

🌟 Key Therapeutic Effects

Effect	Description
🐛 Flea Control	Kills adult fleas within 30 minutes to 4 hours of administration
🕷️ Tick Control	Eliminates ticks like Ixodes, Dermacentor, Rhipicephalus
📅 Long Duration	One chewable gives 30 days of protection
🔄 Interrupts Lifecycle	Prevents re-infestation by killing new fleas before they lay eggs
🐾 Improves Pet Comfort	Reduces scratching, skin irritation, and allergic reactions

⚠️ Possible Side Effects of Afoxolaner

While Afoxolaner is well-tolerated, some mild and rare adverse reactions have been noted, particularly in sensitive breeds or dogs with pre-existing conditions.

🧾 Common Side Effects (Mild)

Symptom	Notes
🤢 Vomiting	Often mild and self-resolving
💩 Diarrhea	Temporary GI upset
💤 Lethargy	May appear drowsy for a few hours
🤮 Loss of Appetite	Occasionally noted in first-time users

❗ Rare but Serious Effects

Symptom	Clinical Action
🧠 Neurological signs (tremors, ataxia, seizures)	Rare but possible, especially in dogs with seizure history
🐕 Hypersensitivity	Allergic reactions like itching, redness, swelling

📌 These are extremely uncommon but should be monitored, especially in smaller breeds or first-time users.

🔒 Swapnroop Drugs & Pharmaceuticals' Assurance

Produces high-purity Afoxolaner API 💎
Ensures veterinary GMP standards 🏭
Supports partner formulators in creating safe, palatable chewables 🐶🍖

🐾 Conclusion

Afoxolaner API from Swapnroop offers effective parasite protection with a high safety margin when used as directed in appropriate formulations. Always administered under veterinary advice 🩺🐶.

❓ Q10. How is AFOXOLANER API manufactured by Swapnroop Drugs and Pharmaceuticals tested?

Swapnroop Drugs and Pharmaceuticals follows stringent quality control (QC) and quality assurance (QA) protocols to ensure that every batch of Afoxolaner API meets international regulatory standards. 🏭🧪

🔬 1. In-Process Testing (During Manufacturing)

➡️ At every critical step in synthesis, the API is tested for intermediate specifications like:

⚗️ Purity
🌡️ Moisture content (Karl Fischer Titration)
🧬 Reaction completion (TLC/HPLC checks)
🧪 pH and solubility profiles

🔄 This ensures consistency and reproducibility across batches.

🧪 2. Finished Product Testing

Once the synthesis is complete, Afoxolaner API undergoes comprehensive final testing in the QC laboratory:

✅ Routine Tests Performed:

Test	Purpose	Method
🧼 Identification	Confirms chemical identity	IR, NMR, HPLC, MS
💎 Assay	Checks API strength (usually >98%)	HPLC or UV Spectroscopy
🧫 Impurity Profile	Detects any residuals/by-products	HPLC / GC
💧 Water Content	Ensures stability	Karl Fischer Titration
⚖️ Residue on Ignition	Assesses inorganic matter	Gravimetric method
🧱 Particle Size Distribution	Critical for formulation	Laser diffraction
🧹 Microbial Testing	Ensures no contamination	Total Plate Count (TPC), Yeast & Mold

🔍 3. Stability Testing (ICH Guidelines)

📦 Afoxolaner API is subjected to stability testing under different environmental conditions:

🌡️ Long-Term Stability: 25°C ± 2°C / 60% RH
☀️ Accelerated Stability: 40°C ± 2°C / 75% RH

✅ This helps determine shelf life and storage conditions.

📜 4. Documentation & Regulatory Compliance

📝 COA (Certificate of Analysis) is generated for each batch
🔒 Data is traceable via LIMS (Laboratory Information Management Systems)
✅ Complies with IP/BP/USP/EP standards as applicable
🔍 Subject to audits by regulatory bodies and client QPs

🛡️ Quality Assurance by Swapnroop

Swapnroop ensures all testing is done in GLP-compliant laboratories with validated equipment and qualified personnel 👨‍🔬👩‍🔬

Their Afoxolaner API stands out for:

🔬 Analytical precision
🔄 Batch-to-batch consistency
🌍 Global export readiness

❓ Q11. What tests are performed on AFOXOLANER API manufactured by Swapnroop Drugs and Pharmaceuticals?

At Swapnroop Drugs and Pharmaceuticals, Afoxolaner API undergoes a comprehensive suite of analytical and quality tests to ensure safety, efficacy, and compliance with pharmacopeial standards. 🏭🧪✅

🧪 1. Identification Tests

Purpose: Confirm the chemical identity of the compound

🧬 Infrared (IR) Spectroscopy
💥 Mass Spectrometry (MS)
📈 High-Performance Liquid Chromatography (HPLC)
🔬 Nuclear Magnetic Resonance (NMR)

📊 2. Assay (Potency Test)

Purpose: Quantifies the active pharmaceutical ingredient (API) content

⚖️ Typically performed by HPLC or UV Spectroscopy
🔍 Should meet or exceed 98–102% of label claim

🧫 3. Impurity & Related Substance Profile

Purpose: Detects residual solvents, organic impurities, and degradation products

⚗️ HPLC (for organic impurities)
🧪 Gas Chromatography (GC) (for volatile solvents)
🧱 Heavy metals (via ICP-MS or AAS)

💧 4. Water Content / Moisture Analysis

💧 Karl Fischer Titration is used
Ensures stability and shelf life by controlling hygroscopicity

⚖️ 5. Residue on Ignition / Sulfated Ash

Checks for inorganic impurities and non-volatile content
Important for overall purity and quality

🧱 6. Particle Size Distribution

Analyzed using Laser Diffraction
Critical for bioavailability, solubility, and dosage form uniformity

🧼 7. Melting Point / DSC (Differential Scanning Calorimetry)

Helps determine thermal behavior and crystalline structure

🧹 8. Microbial Testing

Ensures absence of harmful microorganisms:
- 🦠 Total Plate Count (TPC)
- 🍞 Yeast & Mold Count
- ❌ Pathogen testing (e.g., E. coli, Salmonella)

🧪 9. Stability Studies (ICH-Guided)

📦 Conducted under:

🌡️ Long-Term (25°C / 60% RH)
☀️ Accelerated (40°C / 75% RH)

Helps define shelf life and optimal storage conditions.

📄 10. Final Batch Release Testing

Every batch is reviewed with a Certificate of Analysis (CoA)
All results are compared against IP/BP/USP/EP standards
Ensures full regulatory compliance 🧾✅

Swapnroop’s commitment to quality is reflected through:

✅ Validated test methods
🧪 GMP & GLP-compliant labs
🧑‍🔬 Qualified QC analysts
📦 Traceability & documentation

❓ Q12. What are the challenges in manufacturing AFOXOLANER API manufactured by Swapnroop Drugs and Pharmaceuticals?

Manufacturing Afoxolaner API, a complex isoxazoline compound used in veterinary parasiticides 🐾, comes with its own set of scientific, operational, and regulatory challenges. Here's a breakdown:

🧪 1. Synthetic Complexity

Afoxolaner has a multi-step synthesis route, involving:

Sensitive intermediates 🧫

Strict reaction conditions 🔥

Need for precise chiral control 🧬

Minor deviations can cause impurity spikes or low yields.

⚗️ 2. Impurity Control & Profile Management

Requires tight control on:

Isomeric impurities

Residual solvents

Heavy metals & genotoxins

Maintaining low impurity levels (<0.1%) demands high-end purification systems (e.g., chromatography, crystallization).

🔬 3. Analytical Method Development

Developing robust and validated methods for:

Assay

Related substances

Polymorphs

Requires sophisticated instruments: HPLC, LC-MS/MS, DSC, XRPD

🌡️ 4. Stability and Hygroscopic Nature

Afoxolaner can be sensitive to moisture and temperature

Requires specialized packaging solutions (e.g., nitrogen purging, vacuum sealing)

Stability data needs to be backed by ICH-compliant studies ⏳

🏭 5. Scalability of Reaction

Lab-scale reactions may not translate easily to plant scale due to:

Exothermic reactions 🌡️💥

Hazardous reagents ⚠️

Environmental control (temperature, pressure, pH)

🧯 6. Safety & Environmental Compliance

Handling of toxic solvents and waste stream requires:

🧪 Effluent treatment systems (ETP)

☢️ Strict adherence to CPCB/USFDA norms

🛡️ Worker safety gear & SOPs

🧾 7. Regulatory & Documentation Requirements

Global supply demands:

DMF (Drug Master File) submissions 📑

Compliance with USFDA, EUGMP, WHO-GMP, etc.

Frequent audits and technical dossiers 📂🔍

⚙️ 8. Cost Management

High R&D, testing, and quality assurance costs

Need to remain price-competitive while maintaining quality 💸⚖️

🌍 9. Supply Chain Risks

Raw material availability 📦

Dependency on high-purity starting materials

Import/export regulations and lead times ⏱️🚢

✅ Swapnroop’s Edge in Tackling These Challenges

👨‍🔬 Highly experienced R&D and process engineering teams

🏭 State-of-the-art GMP-certified manufacturing plants

🔬 In-house analytical labs with advanced instrumentation

📋 Strong documentation & regulatory submission capabilities

♻️ Environmentally sustainable and safe practices

❓ Q13. What are the challenges in manufacturing AFOXOLANER API dosage forms by Swapnroop Drugs and Pharmaceuticals?

Formulating Afoxolaner API into finished dosage forms (especially chewable tablets for pets 🐶🐱) involves intricate technical, regulatory, and stability-related challenges. Let’s break them down:

💊 1. Palatability for Animal Use

Afoxolaner is inherently bitter and unpalatable 🥴

Requires careful masking with:

Flavoring agents (e.g., beef, chicken flavors 🍗)

Sweeteners safe for pets

Maintaining taste uniformity batch-to-batch is tricky.

⚖️ 2. Dose Accuracy and Uniformity

Pets come in various weights—needs dose-specific formulations

Low dose API means:

Uniform blending becomes difficult

Risk of content variation ➡️ critical for safety

🧬 3. Stability Concerns

Afoxolaner is moisture-sensitive

Formulations must maintain:

Physical integrity 💥

Assay potency over shelf life

Requires:

Desiccant packaging

Barrier blister packs or foil strip packs

🧪 4. Drug-Excipient Compatibility

Incompatible with certain common excipients

Needs preformulation studies:

To avoid degradation or reaction

Ensure bioavailability and stability

🐾 5. Regulatory Compliance for Veterinary Formulations

Must comply with CVM (FDA), EMA (VMP), and CPCSEA norms

Needs:

Preclinical safety studies

Palatability trials

Species-specific tolerability data

🏭 6. Manufacturing Consistency

Chewable tablets must be:

Non-crumbly

Easy to chew yet not too soft

Requires:

Granulation optimization

Specialized compression tools

In-process control (IPC) checks

🧾 7. Documentation and Dossier Filing

Regulatory dossiers must include:

Formulation R&D data

In-vitro/in-vivo correlation studies

Batch reproducibility evidence

Veterinary drug dossiers differ from human meds ➡️ Extra expertise needed

✅ How Swapnroop Ensures Quality in Afoxolaner Dosage Forms

🔬 In-house R&D for veterinary formulations

🐶 Taste and behavior studies on target animal species

📦 Packaging innovations to ensure shelf stability

🏆 Global standard GMP-compliant manufacturing facilities

📁 Strong regulatory team for dossier preparation and submission

Q14: Storage Conditions for Afoxolaner API (Manufactured by Swapnroop Drugs & Pharmaceuticals)

To ensure stability, potency, and shelf life of Afoxolaner API (CAS 1093861-60-9), Swapnroop Drugs & Pharmaceuticals recommends the following storage conditions:

1️⃣ Primary Storage Conditions

Parameter	Requirement
Temperature	2–8°C (Refrigerated, long-term storage)
Short-Term Storage	≤25°C (Ambient, max. 6 months)
Humidity	≤60% RH (Use desiccants)
Light Sensitivity	Protect from light (Amber glass/opaque packaging)
Packaging	Double polyethylene (PE) bags + aluminum foil laminate

2️⃣ Stability & Shelf Life

✔ Long-Term Stability: 36 months at 2–8°C (ICH Q1A compliant).
✔ Accelerated Stability: 6 months at 25°C/60% RH (for transport validation).
✔ Post-Opening: Use within 30 days if resealed properly.

3️⃣ Handling Precautions

Avoid moisture: Hygroscopic → may form hydrates.
Minimize exposure to air: Nitrogen purging for bulk storage.
Do not freeze: Prevents crystal structure changes.

The packaging for Afoxolaner API manufactured by Swapnroop Drugs and Pharmaceuticals typically includes:

📦 Primary Packaging:

🌫️ Double polyethylene bags (moisture-resistant)
🛡️ Aluminum foil bags (light & moisture protection)

📦 Secondary Packaging:

🔵 Sealed HDPE containers (for stability)
📦 Fiber drums (with inner liners for bulk quantities)

🏷️ Labeling Details:

🔬 Product Name: Afoxolaner API
🆔 Batch/Lot No.
📅 Mfg. & Exp. Date
🏭 Manufacturer: Swapnroop Drugs & Pharmaceuticals
❄️ Storage: "Store in a cool, dry place"
✅ Compliance: GMP/WHO-GMP (if applicable)

For exact details, check the CoA (Certificate of Analysis) 📄 or contact Swapnroop directly! 🏢📞

Need help with anything else? 😊