Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor(SSRI).Dapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Premature ejaculation (

Synthesis of [11C]dapoxetine.HCl, a serotonin re-uptake inhibitor: biodistribution in rat and preliminary PET imaging in the monkey.[Pubmed:9234326]

Nucl Med Biol. 1994 May;21(4):669-75.

[11C]Dapoxetine.HCl, S-(+)-N,N-dimethyl-a-[2-(naphthalenyloxy)ethyl] benzenemethanamine hydrochloride, a potent serotonin re-uptake inhibitor was prepared from its mono-methyl precursor, S-(+)-N-methyl-a-[2-(naphthalenyloxy)ethyl]benzene methanamine hydrochloride. Biodistribution was determined in rats at 5, 30 and 60 min after injection and preliminary PET studies were performed in a Rhesus monkey. 11CH3I was bubbled into a solution of S-(+)-N-methyl-alpha-[2-(naphthalenyloxy)ethyl]benzene methanamine hydrochloride (3.0 mg in DMSO) and the mixture was heated at 110 degrees C for 8 min. [11C]Dapoxetine.HCl was purified by HPLC on a C18 cartridge eluted with MeOH:phosphate buffer, pH 7,2 (75:25) with a 10% yield (end of synthesis). The time required for the synthesis was 40 min, from the end of bombardment. Radiochemical purity of the final product was > 99% and specific activity was routinely > 400 mCi/mumol [EOS]. In the biodistribution studies the highest concentration (%ID/g +/- SEM) of dapoxetine.HCl was detected in lung: 4.56 +/- 0.27 (5 min), 1.28 +/- 0.18 (30 min) and 0.67 +/- 0.04 (60 min). Brain accumulation was 0.76 +/- 0.02 (5 min), 0.46 +/- 0.04 (30 min) and 0.27 +/- 0.01 (60 min). Preliminary PET studies demonstrated significant displaceable binding in the cerebral cortex and subcortical grey matter. These results demonstrate that [11C]dapoxetine.HCl can be prepared in high purity and may be useful for the in vivo evaluation of serotonin re-uptake mechanisms.

Stability indicating HPLC-UV method for determination of dapoxetine HCl in pharmaceutical product.[Pubmed:25265818]

Acta Pol Pharm. 2014 May-Jun;71(3):393-400.

A stability-indicating HPLC-UV method for the determination of dapoxetine hydrochloride in solution and pharmaceutical product was developed. The mobile phase was composed of acetonitrile and 0.2 M ammonium acetate buffer at 50 : 50 ratio. The chromatographic parameters, theoretical plates (N), tailing factor (T), capacity factor (k') and peak asymmetry factor (As) were calculated. Stress degradation studies, namely, acid, alkali, oxidation, heat and UV light, were performed. The analyte was eluted at 5.8 min using gradient system at a flow rate of 1.5 mL/min. The theoretical plates count was > 2000, tailing factor < 1.54, capacity factor > 5.38 and peak asymmetry factor was < 1.10. The method was linear from 1 to 40 microg/mL with a correlation coefficient of 0.9994. The intraday precision and accuracy values were 0.14-1.54% and 0.63-1.83%, respectively. On the other hand, the interday precision and accuracy results were 0.49-1.83% and 1.15-1.85%, respectively. The drug solution was stable at ambient room temperature (26 degrees C) for 48 h. Dapoxetine HCI was found susceptible to oxidation and degraded slightly under acid and alkali conditions but was stable under UV light and heat. No interference from tablet excipiets and degradation products was found. Hence, the method can be employed as a stability-indicating method for the determination of Dapoxetine HCl in pharmaceutical products.