Vortioxetine is a synthetic antidepressant active pharmaceutical ingredient belonging to the multimodal serotonergic antidepressant class. In pharmaceutical products, the most established salt form is Vortioxetine Hydrobromide (HBr). Vortioxetine hydrochloride (HCl) is a chemically defined alternative salt form of the same parent active moiety.
Vortioxetine is marketed in the United States as TRINTELLIX and was previously marketed as Brintellix in some markets. The FDA-approved product contains the beta polymorph of Vortioxetine Hydrobromide. The active ingredient is used in the treatment of major depressive disorder in adults.
Vortioxetine Hydrobromide is chemically identified as 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine hydrobromide. Its empirical formula is C18H22N2S·HBr, corresponding to C18H23BrN2S, with a molecular weight of 379.36 g/mol. Its CAS Number is 960203-27-4.
The FDA describes Vortioxetine Hydrobromide as a white to very slightly beige powder that is slightly soluble in water. USP similarly describes the substance as a white to very slightly beige powder and reports that it is soluble in ethanol and methanol and slightly soluble in water.
The hydrobromide salt is the form used in the FDA-approved immediate-release tablet formulation. The amount of Vortioxetine Hydrobromide in the finished product is adjusted to provide the labeled amount of vortioxetine active moiety. For example, FDA labeling identifies 6.355 mg, 12.71 mg and 25.42 mg of Vortioxetine Hydrobromide as equivalent to 5 mg, 10 mg and 20 mg of vortioxetine, respectively.
Vortioxetine Hydrochloride is another salt form of the same parent compound. PubChem identifies its molecular formula as C18H23ClN2S, molecular weight as 334.9 g/mol, and CAS Number as 960203-28-5.
The molecular difference between the HBr and HCl forms results from the counterion. Therefore, their molecular weights, formulas and certain physicochemical properties differ even though the parent vortioxetine moiety remains the same.
For pharmaceutical documentation, the salt form should always be stated explicitly. A specification or certificate for Vortioxetine Hydrobromide should not automatically be represented as a specification for Vortioxetine Hydrochloride.
Vortioxetine is a serotonergic antidepressant with a multimodal pharmacological profile. The FDA describes its activity as involving inhibition of the serotonin transporter together with activity at several serotonin receptor subtypes. It has high-affinity binding to the serotonin transporter and also exhibits 5-HT3 receptor antagonism and 5-HT1A receptor agonism, among other serotonergic activities.
The combined serotonergic activity distinguishes vortioxetine from conventional selective serotonin reuptake inhibitors that primarily act through serotonin transporter inhibition.
The exact contribution of each receptor activity to the overall antidepressant effect has not been fully established. Vortioxetine is nevertheless classified pharmacologically as a serotonergic antidepressant.
Vortioxetine API is relevant to pharmaceutical manufacturers and developers working on antidepressant formulations and central nervous system products. As a Vortioxetine HBr/HCl API manufacturer and supplier in India, the material can be positioned for pharmaceutical development and manufacturing applications requiring controlled-quality vortioxetine salt material.
Quality control should distinguish between the hydrobromide and hydrochloride forms. Identity, assay, related substances, residual solvents, water content and other applicable quality attributes should be evaluated using validated analytical procedures appropriate to the selected salt.
For Vortioxetine Hydrobromide, USP has proposed a drug-substance monograph based on validated analytical procedures, including liquid chromatographic testing for assay and organic impurities. USP also lists reference standards for Vortioxetine Hydrobromide and specified related compounds.
Vortioxetine is used as an antidepressant for the treatment of major depressive disorder in adults. The established pharmaceutical product uses Vortioxetine Hydrobromide as the active ingredient.
Vortioxetine Hydrobromide immediate-release tablets are available in strengths corresponding to 5 mg, 10 mg, 15 mg and 20 mg of vortioxetine in current European regulatory guidance.
The API is therefore relevant to pharmaceutical manufacturing involving oral antidepressant formulations and CNS-focused pharmaceutical development.
Vortioxetine Hydrobromide has a molecular weight of 379.36 g/mol and is described as a white to very slightly beige powder. FDA labeling reports that it is slightly soluble in water.
USP describes Vortioxetine Hydrobromide as soluble in ethanol and methanol and slightly soluble in water.
A product monograph reports that Vortioxetine Hydrobromide has a melting point of approximately 231°C and an aqueous solubility of approximately 1.3 mg/mL as vortioxetine base at ambient temperature, with the saturated solution at approximately pH 5.5. At pH 7.4, the reported solubility is approximately 50 µg/mL as vortioxetine base. These values are physicochemical reference data and should not automatically be entered as API release limits.
A separate thermal study reported a melting temperature of approximately 504 ± 0.5 K, equivalent to about 230.9 ± 0.5°C, for Vortioxetine Hydrobromide.
Quality control of Vortioxetine API should include appropriate identity, assay and purity testing. For Vortioxetine Hydrobromide, chromatographic methods are particularly relevant for assay and related-substance evaluation.
USP's proposed Vortioxetine Hydrobromide monograph describes liquid chromatographic procedures for assay and organic impurities and a gas chromatographic procedure for additional organic impurities. USP also identifies specific Vortioxetine related compounds for reference-standard purposes.
Important quality attributes may include identity, assay, individual impurities, total impurities, residual solvents, water content and other process-related or degradation-related impurities.
For Vortioxetine Hydrochloride, the applicable specification should be established independently because the HCl salt has a different molecular formula and molecular weight from the HBr salt.
Vortioxetine is a specialized CNS API with a multimodal serotonergic mechanism. The selection of salt form is an important consideration during pharmaceutical development because the counterion can influence molecular weight, crystallinity, solubility and other physicochemical properties.
Vortioxetine Hydrobromide is the established pharmaceutical salt in the FDA-approved product. Vortioxetine Hydrochloride should be identified separately wherever it is used as a pharmaceutical development material.
Analytical characterization should therefore confirm the intended salt form, chemical identity, assay and impurity profile before the material is used in finished pharmaceutical manufacturing.
Vortioxetine API should be stored and handled according to the applicable API specification, validated stability data, safety documentation and pharmaceutical manufacturing requirements.
Packaging should protect the material from environmental conditions that could affect its chemical or physical quality. Temperature, humidity, light exposure and container-closure requirements should be established from product-specific stability studies.
Manufacturing facilities should use appropriate procedures for sampling, weighing, handling and storage to maintain API quality and minimize contamination.
Vortioxetine is an important CNS pharmaceutical ingredient used in antidepressant formulations. The hydrobromide salt has an established pharmaceutical application and regulatory history, while the hydrochloride form represents a distinct salt of the same parent compound.
For pharmaceutical manufacturers and developers, accurate control of salt identity, assay, purity and related substances is important for consistent product quality.
Vortioxetine can therefore be categorized as a CNS API, antidepressant API, serotonergic API and pharmaceutical active ingredient, with Vortioxetine Hydrobromide being the principal established pharmaceutical salt.
Vortioxetine is a synthetic serotonergic antidepressant API. The established pharmaceutical form is Vortioxetine Hydrobromide, with the molecular formula C18H22N2S·HBr, molecular weight 379.36 g/mol, and CAS Number 960203-27-4. FDA describes it as a white to very slightly beige powder that is slightly soluble in water.
Vortioxetine Hydrochloride is a distinct salt form with molecular formula C18H23ClN2S, molecular weight 334.9 g/mol, and CAS Number 960203-28-5.
For pharmaceutical manufacturing, the HBr and HCl forms should be documented separately, with their respective molecular identities and quality specifications. Vortioxetine Hydrobromide is particularly relevant to oral antidepressant formulations and current pharmaceutical development.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Melting Point | Approximately 231°C |