Tetracaine Freebase (CAS 94-24-6) – Premium Pharmaceutical Intermediate for Advanced Anesthetic Formulations

Tetracaine Freebase (CAS 94-24-6) is the fundamental organic compound, or “freebase” form, of the potent long-acting local anesthetic Tetracaine. Unlike its water-soluble hydrochloride salt counterpart, the freebase offers distinct advantages in specific pharmaceutical applications due to its unique physicochemical properties, particularly its lipid solubility. This makes it an invaluable intermediate for research, development, and the manufacture of innovative anesthetic delivery systems.

Manufactured under strict cGMP (current Good Manufacturing Practices) guidelines, our Tetracaine Freebase is characterized by its exceptional purity and consistency, providing formulators and researchers with a reliable and versatile building block for advanced pharmaceutical products.

Key Features & Advantages:

• High Lipid Solubility: The freebase form exhibits significantly greater lipophilicity than the salt, enhancing its permeability through lipid-rich biological membranes like the skin and cornea. This property is crucial for developing high-efficiency topical and transdermal formulations.

• Exceptional Purity: Meets stringent quality control specifications for identity, assay, and impurities, ensuring predictable performance and stability in your formulations.

• Critical Formulation Intermediate: Serves as the essential starting material for creating various salt forms, prodrugs, and novel delivery vehicles such as liposomes, microspheres, and lipid-based nanoemulsions.

• Research Versatility: The preferred chemical form for analytical method development, pharmacokinetic studies, and investigating structure-activity relationships (SAR) due to its unmodified molecular structure.

• Optimized for Organic Solubility: Freely soluble in organic solvents like ethanol, methanol, chloroform, and DMSO, facilitating its use in non-aqueous formulations and research applications.

Chemical Specifications:

• Chemical Name: 2-(Dimethylamino)ethyl 4-(butylamino)benzoate

• Synonyms: Amethocaine Freebase; Tetracaine Base

• CAS Number: 94-24-6

• Molecular Formula: C₁₅H₂₄N₂O₂

• Molecular Weight: 264.36 g/mol

• Appearance: White to off-white crystalline powder or lumps.

• Solubility: Very slightly soluble in water. Freely soluble in organic solvents (ethanol, methanol, chloroform, diethyl ether).

• Melting Point: ~41°C – 44°C (Note: The freebase has a significantly lower melting point than the hydrochloride salt).

• pKa: ~8.5

Mechanism of Action:

As the active moiety, the Tetracaine freebase is intrinsically linked to the mechanism of anesthesia. In its un-ionized (freebase) form, it demonstrates higher lipid solubility, allowing it to more readily diffuse through the nerve sheath and neuronal membrane. Once inside the cell (pH lower), a significant portion converts to the ionized (cationic) form, which is the active species that binds reversibly to intracellular voltage-gated sodium channels. This binding inhibits sodium ion influx, preventing depolarization and the propagation of nerve impulses, resulting in a reversible local anesthesia.

Applications & Intended Use:

This product is a Pharmaceutical Intermediate intended exclusively for research, development, and pharmaceutical manufacturing.

Its primary applications include:

• Advanced Topical/Transdermal Systems: The ideal formulator’s choice for creating patches, creams, gels, and ointments where high skin permeability is desired for enhanced efficacy.

• Salt Formation & Prodrug Synthesis: Used as the primary precursor in the synthesis of Tetracaine Hydrochloride and other salt forms, or to create novel prodrugs with tailored properties.

• Novel Drug Delivery Systems (NDDS): Incorporated into lipid-based carriers like liposomes, nanoemulsions, and micelles to improve bioavailability, control release kinetics, and target specific tissues.

• Analytical & Research Applications: Serves as a reference standard in HPLC, GC-MS, and other analytical techniques for quality control of final drug products. Essential for basic pharmacological research and bioavailability studies.

• Specialized Ophthalmic Solutions: Used in the development of non-aqueous or oil-based ophthalmic formulations.

Packaging & Storage:

To preserve its integrity and prevent degradation, Tetracaine Freebase is packaged with care:

• Inner Bags: Sealed airtight inside double polyethylene bags to protect from moisture.

• Outer Packaging: Secure, light-resistant fiber drums or HDPE containers.

• Inert Atmosphere: Optionally available packaged under an inert gas (Nitrogen or Argon) to prevent oxidation.

• Standard Sizes: Available from gram-scale for R&D to multi-kilogram quantities for manufacturing, with custom packaging available.

Storage Conditions: Store in a cool, dry, well-ventilated place. Must be stored refrigerated or at controlled room temperature due to its relatively low melting point. Keep the container tightly closed and sealed under an inert atmosphere if possible. Protect from light and moisture.

Quality & Compliance:

Every batch is produced under a rigorous quality management system and is accompanied by a comprehensive Certificate of Analysis (CoA), providing full analytical traceability and confirming compliance with stated specifications.