Venlafaxine HCl

Venlafaxine HCl

Nazwa produktu Venlafaxine HCl
Numer CAS 99300-78-4
Wzór cząsteczkowy C17H27NO2·HCl
Masa cząsteczkowa 313.86 g/mol
Wygląd Biały lub prawie biały krystaliczny proszek
Oznaczenie (HPLC) 98.0% – 102.0% (on dried basis)
Rozpuszczalność Soluble in water, methanol; slightly soluble in ethanol
Przechowywanie Store in tight containers, protected from light
Opakowanie 25 kg fiber drum with double polyethylene liners

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Venlafaxine HCl Structure

Synonimy: (±)-1-[2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride, Wy-45030, Venlafaxine hydrochloride, Effexor, Trevilor, Dobupal

Venlafaxine HCl is the hydrochloride salt of venlafaxine, a bicyclic phenylethylamine derivative that acts as a serotonin-norepinephrine reuptake inhibitor (SNRI). First approved in the 1990s, it has become a mainstay in the treatment of major depressive disorder, generalized anxiety disorder, and panic disorder. Its distinct pharmacological profile—weak dopamine reuptake inhibition at higher doses—sets it apart from selective serotonin reuptake inhibitors (SSRIs).

Chemically, venlafaxine HCl is a racemic mixture of two enantiomers, with the (R)-enantiomer primarily responsible for norepinephrine reuptake inhibition and the (S)-enantiomer for serotonin reuptake inhibition. This dual action contributes to its broad efficacy across mood and anxiety disorders. The hydrochloride salt form offers improved aqueous solubility and stability, making it suitable for a range of immediate-release and extended-release oral dosage forms.

Manufacturers and CDMOs rely on venlafaxine HCl as a key API for generic formulations, particularly extended-release capsules and tablets. The compound is also a frequent subject in bioequivalence studies and analytical method development, given its well-characterized pharmacokinetics and established therapeutic window. Its patent-expired status has made it a high-volume item in the global generic market.

Funkcja

  • Serotonin reuptake inhibition: Blocks serotonin transporter (SERT), increasing synaptic serotonin levels.
  • Norepinephrine reuptake inhibition: Inhibits norepinephrine transporter (NET), enhancing noradrenergic neurotransmission.
  • Dopamine reuptake inhibition: Mild inhibition at higher doses, contributing to broader mood effects.
  • Antidepressant activity: Alleviates symptoms of major depressive disorder.
  • Anxiolytic activity: Reduces anxiety in generalized anxiety disorder and panic disorder.

Source & Standardization

  • Źródło: Synthetic chemical process starting from cyclohexanone and 4-methoxyphenylacetic acid derivatives.
  • Manufacturing: Multi-step organic synthesis followed by salt formation and recrystallization.
  • Standardization: Complying with EP, USP, and IP monographs; typical assay 98.0%–102.0% (HPLC).
  • Forms: White to off-white crystalline powder.
  • Zastosowania: Generic antidepressants, extended-release formulations, clinical research.

Dane techniczne

Parametr Specyfikacja
Oznaczenie (HPLC) 98.0% – 102.0%
Identyfikacja IR, HPLC retention time conforms to standard
Strata przy suszeniu ≤ 0,5%
Popiół po spaleniu ≤ 0,11 TP3T
Metale ciężkie ≤ 20 ppm
Wartości graniczne dla mikroorganizmów Total aerobic count ≤ 1000 CFU/g; Yeast & Mold ≤ 100 CFU/g; E. coli absent

Documentation & Supply

  • Miesięczna wydajność: 5 metric tons
  • Czas realizacji: 3–5 dni roboczych (towary dostępne w magazynie)
  • Dokumentacja: COA, MSDS, TDS, DMF available upon request
  • Opakowanie: 25 kg fiber drum with double polyethylene liners, or as per customer requirements

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