Dapoxetine hydrochloride RC00264

Manufacturer: Hangzhou Royalchem Co.,LTD.

Website:   www.cnroyalchem.com

【 Providing a complete set of intermediates and impurities for Dapoxetine 】

【 Providing a complete set of intermediates and impurities for Dapoxetine 】

【 Providing a complete set of intermediates and impurities for Dapoxetine 】

Here is a detailed product description for  Dapoxetine Hydrochloride (CAS 129938-20-1)  in English:

Chemical Identification:

Chemical Name:  (S)-(+)-N,N-Dimethyl-(α)-[2-(1-naphthalenyloxy)ethyl]benzenemethanamine hydrochloride

Synonyms:  Dapoxetine HCl; (+)-Dapoxetine hydrochloride; Dapoxetini hydrochloridum; Priligy (brand name for the finished product)

CAS Registry Number:  129938-20-1

Molecular Formula:  C 21 H 23 NO · HCl

Molecular Weight:  341.87 g/mol (hydrochloride salt)

Physical Description:

Dapoxetine hydrochloride is typically a  white to off-white crystalline powder .

It is  hygroscopic  (absorbs moisture from the air).

Solubility:  Freely soluble in water, methanol, and ethanol; slightly soluble in isopropyl alcohol; practically insoluble in acetone, ethyl acetate, and hexane.

Chemical Properties:

Chirality:  Dapoxetine is the pharmacologically active  S-(+)-enantiomer .

Salt Form:  It exists as the  hydrochloride salt  for pharmaceutical use, enhancing solubility and stability.

Pharmacological Classification:

Category:  Selective Serotonin Reuptake Inhibitor (SSRI) - Short-acting.

Primary Indication:  Treatment of  premature ejaculation (PE)  in adult men aged 18 to 64 years. It is specifically indicated for on-demand use.

Mechanism of Action:

Dapoxetine hydrochloride is a potent and  selective inhibitor  of the serotonin (5-hydroxytryptamine or 5-HT) transporter.

By blocking the reuptake of serotonin into presynaptic neurons, it increases serotonin levels in the synaptic cleft within the central nervous system (CNS), particularly in the ejaculatory centers of the spinal cord and hypothalamus.

This enhanced serotonergic neurotransmission is believed to  delay the ejaculatory reflex , increasing intravaginal ejaculatory latency time (IELT).

Key Pharmacokinetic Properties:

Absorption:  Rapidly absorbed after oral administration. Time to peak plasma concentration (T max ) is approximately 1-2 hours.

Food Effect:  Absorption is delayed by high-fat meals, potentially reducing peak exposure (C max ) by about 10% and delaying T max  by approximately 30 minutes. Efficacy is not significantly altered.

Distribution:  Extensive distribution (~99% protein bound, primarily to albumin and α1-acid glycoprotein). Volume of distribution is large (~77 L).

Metabolism:  Extensively metabolized primarily in the liver by multiple cytochrome P450 (CYP) enzymes, including CYP3A4, CYP2C19, CYP2D6, and flavin-containing monooxygenase (FMO1). Major metabolites include dapoxetine-N-oxide and desmethyldapoxetine.

Elimination:  Rapidly eliminated with a mean  elimination half-life of approximately 1.5-1.6 hours . Excreted primarily as metabolites in the urine (mean 42%, mainly as conjugates) and feces (mean 36%, mainly as unconjugated metabolites). Less than 2% is excreted unchanged.

Pharmaceutical Use:

Active Pharmaceutical Ingredient (API):  Dapoxetine hydrochloride is the active substance used in the manufacture of  immediate-release oral tablets  (e.g., 30 mg and 60 mg strengths).

Dosage Form:  Tablets are intended for "on-demand" administration (taken 1-3 hours prior to anticipated sexual activity), not for continuous daily dosing like most SSRIs.

Handling and Safety (API Level):

Handling Precautions:  Handle in accordance with good industrial hygiene and safety procedures. Avoid contact with eyes, skin, and clothing. Avoid formation of dust and aerosols. Use appropriate engineering controls (e.g., local exhaust ventilation). Personnel should wear suitable protective clothing, gloves, and eye/face protection.

Storage:  Store in a tightly closed container, protected from light and moisture, at controlled room temperature (typically 15-30°C or as specified by the manufacturer). Store under an inert atmosphere if hygroscopic nature is significant.

Stability:  Stable under recommended storage conditions. Refer to the Certificate of Analysis (CoA) for specific retest/expiry dates.