Rapid-Onset Sildenafil Sublingual Drug Delivery Systems: In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits

Ming Thau Sheu, Chien Ming Hsieh, Ray Neng Chen, Po Yu Chou, Hsiu O. Ho

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

The aim of the present study was to prepare sublingual delivery systems for sildenafil and evaluate its relative bioavailability after sublingual administration in rabbits to attain a rapid onset of action with good efficacy at lower doses. For sublingual application, sildenafil and its citrate were formulated in 2 different dosage forms: the first was a sublingual spray consisting of sildenafil in 2 microemulsion systems, oleic acid or propylene glycol (PG), and the second was sublingual tablets prepared with various granulated sublingual sprays adsorbed onto a silicate adsorbant (Florite® R), binders (Cyclocel® or EMDEX®), and disintegrants (Ac-Di-Sol® or Kollidon® CL). Results showed that sublingual absorption of sildenafil spray prepared with PG was fairly rapid. At a 0.5-mg dose, the mean onset of action was 1.3 ± 0.6 min and lasted for about 1.5 h according to the pharmacokinetic studies. In vivo studies also showed that for sublingual tablets formulated with sildenafil in PG adsorbed onto Florite® R at a 1:1 weight ratio then mixed with Cycloel® and Ac-Di-Sol®, the onset action was fast at 1.9 ± 0.4 min and lasted for about 1 h at 0.5 mg. These findings suggest the potential for the sublingual delivery of sildenafil instead of the conventional oral administration.

Original languageEnglish
Pages (from-to)2774-2781
Number of pages8
JournalJournal of Pharmaceutical Sciences
Volume105
Issue number9
DOIs
Publication statusPublished - Sep 1 2016

Keywords

  • bioavailability
  • erectile dysfunction
  • sildenafil
  • sublingual spray
  • sublingual tablets

ASJC Scopus subject areas

  • Pharmaceutical Science

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