Duloxetine HCl

Sinónimos: (S)-N-Methyl-3-(1-naphthyloxy)-3-(2-thienyl)propan-1-amine hydrochloride, LY248686, Duloxetine hydrochloride, Cymbalta, Yentreve, Ariclaim, Xeristar

Duloxetine HCl is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that has become a cornerstone in the treatment of major depressive disorder, generalized anxiety disorder, and neuropathic pain. As a hydrochloride salt, it offers improved aqueous solubility and stability compared to the free base, making it the preferred form for oral solid dosage formulations. The compound was originally developed by Eli Lilly and received FDA approval in 2004 under the brand name Cymbalta.

Chemically, duloxetine HCl is a naphthalenyloxy-substituted thiophene propanamine. Its structure features a chiral center, and the active pharmaceutical ingredient is the (S)-enantiomer, which is significantly more potent than the (R)-enantiomer. The molecule’s lipophilic naphthalene and thiophene rings facilitate blood-brain barrier penetration, while the secondary amine side chain is responsible for its interaction with serotonin and norepinephrine transporters. This dual mechanism distinguishes it from selective serotonin reuptake inhibitors (SSRIs) and contributes to its broader efficacy profile.

From a manufacturing perspective, duloxetine HCl is synthesized through a multi-step process that typically starts from 1-naphthol and 2-acetylthiophene, followed by a resolution step to isolate the desired (S)-enantiomer. The final hydrochloride salt is crystallized to high purity, with particle size distribution carefully controlled to ensure consistent dissolution and bioavailability in finished dosage forms. Our material is produced under cGMP conditions and is supported by a comprehensive regulatory package, including DMF and CEP where applicable.

Función

• SNRI activity: Inhibits serotonin and norepinephrine reuptake, enhancing neurotransmitter availability in the synaptic cleft.
• Antidepressant effect: Improves mood and reduces anxiety symptoms in major depressive disorder and generalized anxiety disorder.
• Analgesic properties: Effective in managing chronic musculoskeletal pain, diabetic peripheral neuropathic pain, and fibromyalgia.
• Anxiolytic action: Reduces excessive worry and tension through modulation of serotonergic and noradrenergic pathways.
• Stability and solubility: The hydrochloride salt ensures consistent dissolution and shelf-life in oral formulations.

Source & Standardization

• Source: Synthetic chemical synthesis, starting from 1-naphthol and 2-acetylthiophene.
• Standardization: Assay 98.0% – 102.0% (HPLC, on dried basis), with strict control of chiral purity.
• Forms: White to off-white crystalline powder, milled to a defined particle size range.
• Aplicaciones: Antidepressant and analgesic medications, generic drug development, and clinical research.

Especificaciones

Documentation & Supply

• Monthly capacity: 10 metric tons
• Plazo de entrega: 3-5 días laborables (artículos en stock)
• Documentación: COA, MSDS, TDS, DMF (where applicable), and CEP upon request
• Embalaje: 25 kg fiber drum with double polyethylene bags, or as per customer requirements

Solicitud de presupuesto

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