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

5 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

Fingerprint

Drug Delivery Systems
Pharmacokinetics
Rabbits
Propylene Glycol
Polymethyl Methacrylate
Tablets
Sublingual Administration
Transcobalamins
Povidone
Silicates
Dosage Forms
Oleic Acid
Biological Availability
Oral Administration
Sildenafil Citrate
Weights and Measures

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

@article{dd9e2bba26974373b4b148e7c06fb307,
title = "Rapid-Onset Sildenafil Sublingual Drug Delivery Systems: In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits",
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{\circledR} R), binders (Cyclocel{\circledR} or EMDEX{\circledR}), and disintegrants (Ac-Di-Sol{\circledR} or Kollidon{\circledR} 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{\circledR} R at a 1:1 weight ratio then mixed with Cycloel{\circledR} and Ac-Di-Sol{\circledR}, 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.",
keywords = "bioavailability, erectile dysfunction, sildenafil, sublingual spray, sublingual tablets",
author = "Sheu, {Ming Thau} and Hsieh, {Chien Ming} and Chen, {Ray Neng} and Chou, {Po Yu} and Ho, {Hsiu O.}",
year = "2016",
month = "9",
day = "1",
doi = "10.1016/j.xphs.2016.01.015",
language = "English",
volume = "105",
pages = "2774--2781",
journal = "Journal of Pharmaceutical Sciences",
issn = "0022-3549",
publisher = "John Wiley and Sons Inc.",
number = "9",

}

TY - JOUR

T1 - Rapid-Onset Sildenafil Sublingual Drug Delivery Systems

T2 - In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits

AU - Sheu, Ming Thau

AU - Hsieh, Chien Ming

AU - Chen, Ray Neng

AU - Chou, Po Yu

AU - Ho, Hsiu O.

PY - 2016/9/1

Y1 - 2016/9/1

N2 - 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.

AB - 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.

KW - bioavailability

KW - erectile dysfunction

KW - sildenafil

KW - sublingual spray

KW - sublingual tablets

UR - http://www.scopus.com/inward/record.url?scp=84982840896&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84982840896&partnerID=8YFLogxK

U2 - 10.1016/j.xphs.2016.01.015

DO - 10.1016/j.xphs.2016.01.015

M3 - Article

VL - 105

SP - 2774

EP - 2781

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

SN - 0022-3549

IS - 9

ER -