Vilazodone Hydrochloride is a pharmaceutical active ingredient belonging to the class of serotonergic antidepressant compounds. It is the hydrochloride salt of vilazodone and is used in the manufacture of oral pharmaceutical formulations for the treatment of major depressive disorder (MDD) in adults.
Vilazodone Hydrochloride is chemically identified as 2-benzofurancarboxamide, 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]-, hydrochloride (1:1). It has the molecular formula C26H28ClN5O2 and a molecular weight of approximately 477.99 g/mol. Its CAS Number is 163521-08-2.
Vilazodone is a centrally acting serotonergic compound with a dual pharmacological profile. It acts as a selective serotonin reuptake inhibitor (SSRI) and also as a partial agonist at the 5-HT1A receptor. The antidepressant activity is associated with enhancement of serotonergic neurotransmission through serotonin reuptake inhibition together with 5-HT1A receptor activity.
Vilazodone Hydrochloride is generally described as a white to cream-colored powder or solid. Regulatory information identifies the substance as slightly hygroscopic and notes that it can exist in multiple crystalline polymorphic forms. Form IV was selected during the original pharmaceutical development program.
The substance is practically insoluble in water. A pharmaceutical product monograph reports water solubility below 0.1 mg/mL, while it is freely soluble in methanol and has greater solubility in selected organic solvents.
Vilazodone Hydrochloride has a relatively high melting/decomposition temperature. Public sources report values around 277–290°C, depending on crystalline form and analytical conditions. Because polymorphism can affect thermal behavior, the exact observed melting or decomposition profile can vary with the solid form.
Vilazodone Hydrochloride is primarily used as an API for oral solid pharmaceutical formulations.
Its major pharmaceutical application is:
Vilazodone Hydrochloride is marketed in tablet formulations in strengths including 10 mg, 20 mg and 40 mg.
Vilazodone has a combined serotonergic mechanism. It selectively inhibits the serotonin transporter, thereby reducing serotonin reuptake and increasing serotonergic activity in the central nervous system.
In addition, vilazodone acts as a partial agonist at 5-HT1A serotonin receptors. The exact contribution of the 5-HT1A activity to the overall antidepressant effect has not been completely established, but both pharmacological properties form the basis of its mechanism of action.
Polymorphism is an important consideration for Vilazodone Hydrochloride because different crystalline forms can have different physicochemical properties, including solubility, thermal behavior and processing characteristics.
Regulatory and patent literature describes several crystalline forms of Vilazodone Hydrochloride. Form IV was selected for pharmaceutical development, and its crystal structure and physical properties were investigated during development.
Therefore, control of crystalline form, identity, chemical purity and residual solvents can be important during API manufacturing and pharmaceutical formulation.
Vilazodone Hydrochloride can be characterized using several analytical techniques, including:
Published analytical research has specifically developed stability-indicating HPLC methods for Vilazodone Hydrochloride and identified process impurities such as Vilazodone Acid (Impurity A) and Vilazodone Ester (Impurity B). The methods were also evaluated under acidic, basic, oxidative, thermal and humidity stress conditions.
Impurity profiling is an important part of Vilazodone Hydrochloride API quality control. Process-related impurities can originate from intermediates, reaction steps or incomplete conversion during synthesis.
Published analytical work specifically identifies Vilazodone Acid and Vilazodone Ester as process-related impurities and demonstrates their separation from the main API by stability-indicating HPLC.
For commercial pharmaceutical API, the final impurity specification should be established using validated analytical procedures and the applicable regulatory filing or customer-approved specification.
Vilazodone Hydrochloride is practically insoluble in water. A pharmaceutical product monograph reports water solubility below 0.1 mg/mL and describes the substance as freely soluble in methanol, slightly soluble in ethanol and practically insoluble in water.
Public technical information also reports good solubility in DMSO.
Vilazodone Hydrochloride intended for pharmaceutical manufacturing should be controlled for identity, assay, related substances, water content, residual solvents and physical characteristics.
Because the API can exhibit different crystalline forms, manufacturing processes should maintain appropriate control over crystallization and drying conditions. Appropriate packaging and moisture protection are also important because the material has been described as slightly hygroscopic.
Vilazodone Hydrochloride API is suitable for pharmaceutical companies involved in antidepressant formulation development, generic drug manufacturing and oral solid dosage development.
The API can be used in the development and manufacture of immediate-release tablets and other pharmaceutical dosage forms where Vilazodone is the active pharmaceutical ingredient.
Swapnroop Drugs & Pharmaceuticals provides Vilazodone Hydrochloride API for pharmaceutical development, formulation and manufacturing requirements, subject to applicable quality specifications and regulatory requirements.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 99.0–101.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.50% |
| Total Impurities | NMT 1.0% |
| Melting Point | Approximately 277–290°C |