Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency

Int J Pharm. 2014 May 15;466(1-2):286-95. doi: 10.1016/j.ijpharm.2014.03.001. Epub 2014 Mar 4.

Abstract

The aim of the present study was to prepare the particulate taste-masking system to mask the bitter taste of sildenafil citrate (SC), a well-known phosphodiesterase-5 inhibitor used for erectile dysfunction (ED) and pulmonary artery hypertension (PAH). It was evaluated for the taste masking efficiency by the in vitro measurement using electronic tongue (e-tongue) system and the in vivo human panel sensory test. Microcapsules were prepared by microencapsulation with a gastro-soluble polymer, Eudragit(®) E100 (E100), using a spray drying technique at four different weight ratios (2:1, 1:1, 1:2, and 1:3). Characters of prepared microcapsules and the effect of polymer ratio on the taste masking were investigated. The particle morphology and the distribution of SC in microcapsules were observed by SEM-EDS and physical properties were evaluated by PXRD, Raman spectroscopy, and DSC. By drug dissolution studies at pH 1.2 buffer and DW, it was found that E100 was not able to alter the drug release in stomach. As the result of taste evaluation studies, there were a good correlation (R(2)=0.9867) between the weight ratio of polymer and the taste masking efficiency expressed in the distances on the PCA map of the e-tongue data, and a relevance of the e-tongue measurement with the result of sensory test.

Publication types

  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemistry*
  • Adult
  • Capsules
  • Drug Compounding
  • Electrical Equipment and Supplies
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Male
  • Phosphodiesterase 5 Inhibitors / chemistry*
  • Phosphodiesterase 5 Inhibitors / pharmacology*
  • Piperazines / chemistry*
  • Piperazines / pharmacology*
  • Polymers / chemistry*
  • Purines / chemistry
  • Purines / pharmacology
  • Sildenafil Citrate
  • Single-Blind Method
  • Solubility
  • Sulfones / chemistry*
  • Sulfones / pharmacology*
  • Taste / drug effects*
  • Young Adult

Substances

  • Acrylates
  • Capsules
  • Eudragit E100
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Polymers
  • Purines
  • Sulfones
  • Sildenafil Citrate