Comprehensive Overview of DOCETAXEL TRIHYDRATE (CAS No. 114977-28-5) Manufactured by Swapnroop Drugs & Pharmaceuticals

Q1: What is DOCETAXEL TRIHYDR

ATE manufactured by Swapnroop Drugs & Pharmaceuticals?

DOCETAXEL TRIHYDRATE is a chemotherapeutic active pharmaceutical ingredient (API) widely used in cancer treatment. Manufactured by Swapnroop Drugs & Pharmaceuticals, it is a semi-synthetic analogue of paclitaxel derived from the European yew tree (Taxus baccata). This drug belongs to the taxane class of antineoplastic agents and works by disrupting the microtubule network within cancer cells, which is essential for cell division. By stabilizing microtubules and preventing their disassembly, DOCETAXEL TRIHYDRATE effectively halts mitosis, leading to programmed cell death (apoptosis) of rapidly dividing cancer cells. 🎯

Key Highlights:

Class: Taxane antineoplastic agent
Use: Treatment of various cancers, including breast, lung, prostate, stomach, and head and neck cancers.
Mechanism: Inhibits microtubule depolymerization, preventing cell division.
Form: Trihydrate form refers to the molecule bound with three water molecules, affecting its stability and solubility. 💧
Manufacturing: Swapnroop Drugs & Pharmaceuticals produces high-purity DOCETAXEL TRIHYDRATE following strict quality controls to ensure efficacy and safety. 🏭

DOCETAXEL TRIHYDRATE is a cornerstone in chemotherapy protocols because of its potency and ability to target cancer cells with precision, although it requires careful handling due to its potent cytotoxic nature. ⚠️

Q2: What is DOCETAXEL TRIHYDRATE by Swapnroop Drugs and Pharmaceuticals used for?

DOCETAXEL TRIHYDRATE is primarily used as a chemotherapy drug to treat various types of cancers. Manufactured by Swapnroop Drugs & Pharmaceuticals, it serves as a powerful antineoplastic agent targeting rapidly dividing cancer cells. Its applications include treatment for:

🎗️ Breast Cancer: Often used in both early-stage and metastatic breast cancer to reduce tumor size or control progression.
🎗️ Non-Small Cell Lung Cancer (NSCLC): Administered alone or in combination with other drugs for advanced lung cancer.
🎗️ Prostate Cancer: Particularly effective in hormone-refractory (resistant) prostate cancer cases.
🎗️ Gastric (Stomach) Cancer: Used in advanced stages to help control tumor growth.
🎗️ Head and Neck Cancers: Sometimes part of combination therapy for squamous cell carcinomas.

How it works:

DOCETAXEL TRIHYDRATE disrupts the microtubule network inside cells, preventing them from dividing and proliferating. This leads to cancer cell death and helps shrink tumors or slow their progression. 🛑

Because of its strong effect, DOCETAXEL is used carefully under medical supervision and often combined with other therapies to increase its effectiveness.

Q3: What are the physicochemical properties of DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

DOCETAXEL TRIHYDRATE is a complex molecule with distinct physicochemical properties that influence its stability, formulation, and therapeutic performance. Here are the key properties:

🧪 Chemical Name: Docetaxel trihydrate
🧪 Molecular Formula: C₄₃H₅₃NO₁₄ · 3H₂O (including trihydrate)
🧪 Molecular Weight: Approximately 861.9 g/mol (anhydrous form is ~807.9 g/mol)

Physical Appearance:

White to off-white crystalline powder
Odorless or faintly characteristic

Solubility:

Poorly soluble in water (due to lipophilic nature)
Soluble in organic solvents like ethanol, methanol, and chloroform
Trihydrate form helps improve stability but still requires special formulation techniques for injectable dosage forms 💧

Melting Point:

Around 232–237 °C (with decomposition)

Stability:

Sensitive to light and moisture; requires protection from humidity and direct sunlight during storage
The trihydrate form improves chemical stability compared to the anhydrous form

Optical Activity:

DOCETAXEL is optically active due to several chiral centers in its structure, contributing to its biological activity 🎯

Partition Coefficient (Log P):

Approximately 4.1, indicating it is lipophilic, which affects its absorption and distribution in the body.

pH:

Generally stable in neutral to slightly acidic conditions; degradation can occur under strong acidic or basic environments.

Q4: How is DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals synthesized?

The synthesis of DOCETAXEL TRIHYDRATE is a complex, multi-step process involving both natural extraction and sophisticated chemical modifications. Here’s an in-depth overview of the synthesis pathway typically followed by manufacturers like Swapnroop Drugs & Pharmaceuticals:

1. Starting Material – Natural Extraction:

DOCETAXEL is a semi-synthetic derivative of paclitaxel, which is originally isolated from the needles and twigs of the European yew tree (Taxus baccata). Paclitaxel serves as the key precursor molecule.

2. Semi-Synthesis Process:

The isolated paclitaxel undergoes chemical modifications to improve its solubility, stability, and therapeutic properties.
Key steps include esterification and functional group transformations that convert paclitaxel into docetaxel’s distinct molecular structure.
This involves selective protection and deprotection of hydroxyl groups, acylation at specific positions, and modifications of side chains.

3. Hydration Step:

The final product is converted into its trihydrate form by carefully controlling crystallization conditions, adding three molecules of water per docetaxel molecule to enhance stability and handling.

4. Purification:

High-performance purification methods such as chromatography (e.g., preparative HPLC) are employed to ensure the docetaxel trihydrate is of pharmaceutical grade purity (>99%).
Removal of residual solvents, impurities, and by-products is critical for safety.

5. Quality Control:

Rigorous analytical testing including NMR, mass spectrometry, IR spectroscopy, and HPLC validates the identity, purity, and potency of the final API.

Summary:

This synthesis blends natural product isolation with chemical synthesis and precise purification to produce a highly potent chemotherapy agent. Manufacturing DOCETAXEL TRIHYDRATE demands advanced facilities and stringent quality standards, such as those maintained by Swapnroop Drugs & Pharmaceuticals. 🏭⚗️

Q5: What are the different dosage forms of DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

DOCETAXEL TRIHYDRATE, due to its potent anticancer activity and physicochemical properties, is primarily available in the following dosage forms:

💉 1. Injectable Form (Intravenous Injection):

This is the most common and clinically used form of docetaxel.
Usually supplied as a sterile lyophilized powder or concentrate solution that is reconstituted with a suitable diluent (e.g., saline or dextrose solution) before intravenous administration.
The injectable dosage form is designed for controlled delivery directly into the bloodstream to maximize efficacy and minimize degradation.

💊 2. Lyophilized Powder for Injection:

Freeze-dried powder that improves the stability and shelf-life of the drug.
Reconstituted just prior to use to maintain potency.
Often contains excipients like polysorbate 80 to aid solubilization.

⚠️ Note:
Currently, oral or other non-injectable dosage forms of docetaxel are not common due to poor oral bioavailability and high toxicity concerns.

Q6: How are DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals dosage forms prepared?

The preparation of DOCETAXEL TRIHYDRATE dosage forms, primarily injectable formulations, involves several critical steps to ensure safety, efficacy, and stability:

1. API Handling and Quality Control:

High-purity DOCETAXEL TRIHYDRATE API is first tested for identity, purity, and potency.
The API must meet strict pharmacopeial standards before use.

2. Formulation Development:

Since DOCETAXEL TRIHYDRATE is poorly soluble in water, the formulation usually includes solubilizing agents such as polysorbate 80 and ethanol.
For lyophilized powder, excipients that stabilize the drug during freeze-drying (e.g., mannitol) are added.

3. Mixing:

The API is blended uniformly with excipients under controlled temperature and humidity to maintain stability.
The mixture is prepared in a sterile environment (cleanroom) to avoid contamination.

4. Sterile Filtration and Filling:

For liquid concentrates, the formulation undergoes sterile filtration to remove any microbes.
The drug product is filled into sterile vials under aseptic conditions.

5. Lyophilization (Freeze-Drying):

When preparing lyophilized powder, the filled vials are frozen and then dried under vacuum to remove water by sublimation.
This process extends shelf life and enhances stability.

6. Sealing and Labeling:

Vials are sealed with sterile stoppers and aluminum caps.
Labels are applied with batch information, dosage instructions, and expiry date.

7. Quality Control Testing:

Final dosage forms are tested for sterility, endotoxins, potency, particulate matter, and appearance.

Q7: What is the appropriate dosage form of DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

The most appropriate and widely used dosage form of DOCETAXEL TRIHYDRATE manufactured by Swapnroop Drugs & Pharmaceuticals is the sterile injectable formulation, typically administered by intravenous infusion. Here’s why:

💉 Injectable Formulation:

Due to its poor oral bioavailability and high first-pass metabolism, oral dosage forms of docetaxel are not feasible or effective.
The injectable dosage ensures rapid and complete delivery of the drug directly into the bloodstream, allowing it to reach cancer cells efficiently.
This form can be precisely dosed and adjusted based on patient condition and treatment protocol.

⚖️ Lyophilized Powder or Concentrate:

Usually supplied as a lyophilized powder that is reconstituted before administration, ensuring drug stability and a longer shelf life.
Alternatively, concentrate solutions are available for dilution prior to infusion.

🎯 Clinical Use:

This dosage form is used for treatment of cancers like breast, lung, prostate, gastric, and head and neck cancers.
The dosage and infusion rate are carefully controlled to balance efficacy and minimize side effects.

Q8: When should DOCETAXEL TRIHYDRATE API Manufactured by Swapnroop Drugs and Pharmaceuticals be taken?

DOCETAXEL TRIHYDRATE, being a potent chemotherapy drug, is administered under strict medical supervision and should only be taken when prescribed by an oncologist as part of a cancer treatment regimen. Here are key points about its timing and administration:

⏰ Timing of Administration:

DOCETAXEL is usually given as an intravenous infusion over about 1 hour, once every 3 weeks (21-day cycle), though schedules can vary based on cancer type and patient response.
It is generally administered in a hospital or clinical setting where medical staff can monitor for side effects and manage supportive care.

⚠️ Pre-Treatment Requirements:

Patients are often pre-medicated with corticosteroids (e.g., dexamethasone) 1 day before and after the infusion to reduce side effects like fluid retention and hypersensitivity reactions.
Blood counts and liver function tests must be checked before each dose to ensure the patient is fit for treatment.

🩺 Do NOT self-administer:

DOCETAXEL must never be self-administered or taken orally.
It requires trained healthcare professionals to prepare, dose, and monitor treatment carefully.

In short, DOCETAXEL TRIHYDRATE should be taken only as an intravenous infusion in a controlled clinical environment according to a prescribed schedule, with all necessary precautions and monitoring by healthcare providers.

Q9: What are the effects and side effects of DOCETAXEL TRIHYDRATE manufactured by Swapnroop Drugs and Pharmaceuticals?

Effects:

DOCETaxel trihydrate is a powerful chemotherapy agent used to treat various cancers by inhibiting cell division. It works by stabilizing microtubules, which are essential for mitosis, thereby causing cancer cells to stop dividing and undergo programmed cell death (apoptosis). This leads to:
🎯 Reduction in tumor size
🎯 Slowing or stopping the progression of cancer
🎯 Improved survival rates in cancers such as breast, lung, prostate, gastric, and head and neck cancers.

Common Side Effects:

Because DOCETAXEL targets rapidly dividing cells, it can also affect healthy cells, causing several side effects:

Bone marrow suppression: Lowered white blood cells (neutropenia), red blood cells (anemia), and platelets (thrombocytopenia), increasing infection risk and causing fatigue or bleeding. 🩸
Hair loss (alopecia): Temporary hair thinning or loss. 💇‍♀️
Nausea and vomiting: Often managed with antiemetics. 🤢
Fluid retention and edema: Swelling in hands, feet, or face; corticosteroids are used to reduce this. 💧
Peripheral neuropathy: Tingling, numbness, or pain in hands and feet due to nerve effects. 🦶
Mouth sores and mucositis: Painful inflammation of mouth lining.
Fatigue and weakness: Common during chemotherapy cycles.

Serious but less common side effects:

Allergic or hypersensitivity reactions (rash, itching, breathing difficulty)
Liver toxicity or abnormal liver function tests
Severe infections due to immune suppression
Cardiac effects in rare cases

Monitoring and Management:

Patients receiving DOCETAXEL require close monitoring for side effects, and supportive treatments are often given to manage symptoms and maintain quality of life during therapy.

Q10: How is DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals tested?

DOCETAXEL TRIHYDRATE undergoes rigorous testing during and after manufacturing to ensure its quality, purity, safety, and efficacy before it reaches patients. Swapnroop Drugs & Pharmaceuticals implements comprehensive analytical and quality control measures, including:

Key Testing Procedures:

Identity Testing:
- Confirm the chemical structure using techniques like Nuclear Magnetic Resonance (NMR) spectroscopy, Infrared (IR) spectroscopy, and Mass Spectrometry (MS).
- Ensures the compound is indeed DOCETAXEL TRIHYDRATE.
Purity and Assay:
- High-Performance Liquid Chromatography (HPLC) is used to measure the purity and quantify the API content.
- Tests for related substances and impurities to ensure they are within acceptable limits.
Moisture Content:
- Karl Fischer titration or loss on drying tests to measure water content, crucial for the trihydrate form.
Residual Solvent Analysis:
- Gas Chromatography (GC) is used to detect and quantify any residual organic solvents used during synthesis.
Sterility Testing (for dosage forms):
- Ensures the injectable product is free from microbial contamination.
Endotoxin Testing:
- Detects bacterial endotoxins using the Limulus Amebocyte Lysate (LAL) assay, critical for injectable forms.
Physical Tests:
- Appearance, color, particle size, and melting point verification.
Stability Testing:
- Accelerated and long-term stability studies under controlled temperature and humidity conditions to confirm shelf life and storage requirements.

These tests ensure that DOCETAXEL TRIHYDRATE manufactured by Swapnroop Drugs & Pharmaceuticals meets stringent regulatory standards for pharmaceutical use, guaranteeing patient safety and therapeutic effectiveness.

Q11: What tests are performed on DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

To ensure the quality, safety, and efficacy of DOCETAXEL TRIHYDRATE, Swapnroop Drugs & Pharmaceuticals performs the following key tests during and after manufacturing:

1. Identity Tests:

NMR (Nuclear Magnetic Resonance) Spectroscopy
IR (Infrared) Spectroscopy
Mass Spectrometry (MS)
UV-Visible Spectroscopy

2. Purity and Assay:

High-Performance Liquid Chromatography (HPLC) for assay and related impurities
Thin Layer Chromatography (TLC) for impurity profiling

3. Moisture Content:

Karl Fischer Titration or Loss on Drying test

4. Residual Solvents:

Gas Chromatography (GC) to detect organic solvents used during synthesis

5. Microbial Tests (for injectable forms):

Sterility Test
Bacterial Endotoxin Test (LAL test)

6. Physical Characterization:

Melting Point Determination
Particle Size Analysis
Appearance and Color Inspection

7. Stability Testing:

Accelerated and long-term stability studies under ICH guidelines to assess degradation and shelf life

Q13: What are the challenges in manufacturing DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals dosage forms?

Manufacturing dosage forms of DOCETAXEL TRIHYDRATE, particularly injectable forms, presents several unique challenges:

1. Poor Water Solubility:

DOCETAXEL is highly lipophilic and poorly soluble in water, requiring the use of solvents like polysorbate 80 and ethanol to formulate injectable solutions.
Achieving a stable, homogeneous formulation without precipitation is technically demanding.

2. Sterility and Aseptic Processing:

Since DOCETAXEL dosage forms are administered intravenously, they must be sterile.
Manufacturing requires strict aseptic conditions and validated sterilization processes to prevent contamination.

3. Stability Issues:

The drug is sensitive to light, moisture, and temperature, so maintaining stability throughout manufacturiQ14: What are the storage conditions for DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

Proper storage of DOCETAXEL TRIHYDRATE is crucial to maintain its stability, potency, and safety. The recommended storage conditions are:

Storage Recommendations:
- Temperature: Store at 2°C to 8°C (refrigerated conditions). Avoid freezing. ❄️
- Light Protection: Keep the product protected from light to prevent degradation. Store in the original packaging or amber-colored containers. 🌑
- Humidity: Maintain in a dry place with controlled humidity to preserve the trihydrate form and prevent moisture-related degradation.
- Handling: Avoid exposure to excessive heat or moisture during transportation and storage.
- Shelf Life: Adhere strictly to the labeled expiration date. Use before expiry for maximum efficacy.
Additional Tips:

Store out of reach of children.
Do not use the product if the vial is damaged or the solution appears cloudy or discolored.

Q15: What is the packaging for DOCETAXEL TRIHYDRATE Manufactured by Swapnroop Drugs and Pharmaceuticals?

DOCETAXEL TRIHYDRATE is packaged with strict attention to maintaining its stability, sterility, and safety:

Primary Packaging:
- Sterile glass vials (usually amber-colored) to protect from light and contamination.
- Vials are sealed with rubber stoppers and aluminum crimp caps to ensure airtight closure.
Secondary Packaging:
- Vials are packed in protective cartons or boxes with cushioning materials to prevent damage during transport.
- Packaging includes clear labeling with batch number, manufacturing and expiry dates, storage instructions, and handling precautions.
Tamper-Evident Seals:
- Ensures the integrity and safety of the product.

Q16: What is the shelf life of DOCETAXEL TRIHYDRATE manufactured by Swapnroop Drugs and Pharmaceuticals?

The typical shelf life of DOCETAXEL TRIHYDRATE is 24 months (2 years) when stored under recommended conditions (2°C to 8°C, protected from light and moisture).
Shelf life is determined through stability studies following ICH guidelines to ensure the drug maintains its potency and safety over time.
Using the product beyond its expiration date is not recommended as it may lose effectiveness or degrade

ng, storage, and transportation is challenging.
Lyophilization (freeze-drying) is often used to improve stability but adds complexity to production.

4. Handling and Safety:

DOCETAXEL is cytotoxic, posing health risks to manufacturing personnel.
Facilities need appropriate containment systems and protective measures to ensure worker safety.

5. Precise Dosage and Uniformity:

Injectable dosage forms require precise dosing and uniform drug distribution in each vial to ensure patient safety and efficacy.
This demands rigorous process control and quality assurance.

6. Regulatory Requirements:

Injectable products must meet stringent regulatory standards for sterility, endotoxin levels, particulate matter, and potency.