Dual-purpose Vardenafil hydrochloride/Dapoxetine hydrochloride Orodispersible Tablets: in-vitro Formulation/Evaluation, Stability Study and in-vivo Comparative Pharmacokinetic Study in Healthy Human Subjects.

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Dual-purpose Vardenafil hydrochloride/Dapoxetine hydrochloride Orodispersible Tablets: in-vitro Formulation/Evaluation, Stability Study and in-vivo Comparative Pharmacokinetic Study in Healthy Human Subjects.

Drug Dev Ind Pharm. 2018 Jan 11;:1-39

Authors: El-Refaie K, Teaima MH, El-Nabarawi MA

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 minutes. In-vivo study results from six healthy male volunteers showed shorter Tmax of VH from VH/DH ODT of 0.583±0.129 hr and shorter Tmax of DH from VH/DH ODT of 0.625±0.137 hr and showed AUC0-12 of VH from VH/DH ODT of 39.234±10.932 ng mL-1 h-1 and AUC0-12 of DH from VH/DH ODT of 531.681±129.544 ng mL-1 h-1, with relative bioavailability values of 100.9% and 85% respectively compared to (Levitra®) and (Priligy®).

PMID: 29325456 [PubMed - as supplied by publisher]

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