Release characteristics of quinupramine from the ethylene-vinyl acetate matrix

Int J Pharm. 2006 Jun 6;315(1-2):134-9. doi: 10.1016/j.ijpharm.2006.03.019. Epub 2006 Mar 27.

Abstract

An ethylene-vinyl acetate (EVA) matrix containing quinupramine was prepared in an attempt to develop a controlled delivery system for quinupramine. Permeation studies of quinupramine through the EVA copolymer membrane were carried out using a two-chamber diffusion cell. The rate of drug permeation through the EVA membrane was proportional to the PEG 400 volume fraction. The release of quinupramine from the EVA matrix was examined using a modified Franz diffusion cell. A plasticizer was added to prepare the pore structure of the EVA matrix in order to increase the rate of drug release. The effects of PEG 400, membrane thickness, drug concentration, temperature, and plasticizer on drug release rate were investigated. The drug release rate from the EVA matrix increased with increasing PEG 400 volume fraction, temperature and drug loading dose. The activation energy for drug release was 5.91, 5.39, 4.68 and 4.52 kcal/mol for a loading dose of 0.5%, 1%, 1.5%, and 2%, respectively. Among the plasticizers used, diethyl phthalate showed the best results. The release of quinupramine from the EVA matrix follows a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The controlled release of quinupramine was achieved using the EVA polymer including a plasticizer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Delayed-Action Preparations / chemistry*
  • Delayed-Action Preparations / pharmacokinetics*
  • Dibenzazepines / administration & dosage
  • Dibenzazepines / pharmacokinetics*
  • Diffusion
  • Kinetics
  • Permeability
  • Plasticizers
  • Polyethylene Glycols
  • Polyvinyls / pharmacokinetics*
  • Porosity
  • Quinuclidines / administration & dosage
  • Quinuclidines / pharmacokinetics*
  • Temperature
  • Thermodynamics

Substances

  • Delayed-Action Preparations
  • Dibenzazepines
  • Plasticizers
  • Polyvinyls
  • Quinuclidines
  • ethylenevinylacetate copolymer
  • quinupramine
  • Polyethylene Glycols