Dual-purpose vardenafil hydrochloride/dapoxetine hydrochloride orodispersible tablets: in vitro formulation/evaluation, stability study and in vivo comparative pharmacokinetic study in healthy human subjects

Abstract

Erectile dysfunction (ED) is the most important disorder after premature ejaculation for sexual activity in men. Vardenafil hydrochloride (VH) is an oral therapy for the treatment of erectile dysfunction. VH oral disintegrating tablets (ODTs) have been prepared by freeze drying technique to improve its dissolution profile and the overall clinical performance. Dapoxetine hydrochloride (DH) was added to the best three formulae of the prepared VH ODTs to treat premature ejaculation. All the ODTs formulae were evaluated for weight variation, friability, drug content, in vitro disintegration time, wetting time, and the dissolution study. Gelatin as a matrix former with N-methylpyrrolidone as a solubilizer in VH/DH ODTs improved the dissolution rate and extent of release of VH and DH with 100% of drug being dissolved after 15 min. In vivo study results from six healthy male volunteers showed shorter T_max of VH from VH/DH ODT of 0.583 ± 0.129 h and shorter T_max of DH from VH/DH ODT of 0.625 ± 0.137 h and showed AUC_0–12 of VH from VH/DH ODT of 39.234 ± 10.932 ng/mlh¹ and AUC_0–12 of DH from VH/DH ODT of 531.681 ± 129.544 ng/mlh¹, with relative bioavailability values of 100.9 and 85%, respectively, compared to (Levitra^®) and (Priligy^®).

Keywords:

• Vardenafil hydrochloride
• dapoxetine hydrochloride
• erectile dysfunction
• premature ejaculation
• oral disintegrating tablet

Acknowledgements

The authors are thankful to the management of Drug Research Center, Egypt; Quality Control Department of UniPharma Company, Egypt; Quality Control Department of DELTA Pharma Company, Egypt; Grand Pharma, Egypt; Averros Pharma, Egypt and Dr Nabil Hussein Youssef (quality director) at Multicare Pharma, Egypt for providing the necessary materials, facilities and consultation for carrying out the in vitro and in vivo research work.

Disclosure statement

The authors alone are responsible for the content and writing of this article and reports that there is no conflict of interest.