In vitro drug release studies of polymeric freeze-dried wafers and solvent-cast films using paracetamol as a model soluble drug

Int J Pharm. 2009 Aug 13;378(1-2):66-72. doi: 10.1016/j.ijpharm.2009.05.038. Epub 2009 May 27.

Abstract

Drug dissolution and release characteristics from freeze-dried wafers and solvent-cast films prepared from sodium carboxymethylcellulose (CMC) have been investigated to determine the mechanisms of drug release from the two systems. The formulations were prepared by freeze-drying (wafers) or drying in air (films), the hydrated gel of the polymer containing paracetamol as a model soluble drug. Scanning electron microscopy (SEM) was used to examine differences between the physical structure of the wafers and films. Dissolution studies were performed using an exchange cell and drug release was measured by UV spectroscopy at 242 nm. The effects of drug loading, polymer content and amount of glycerol (films) on the release characteristics of paracetamol were investigated. The release profiles of paracetamol from the wafers and films were also compared. A digital camera was used to observe the times to complete hydration and dissolution of the wafers containing different amounts of CMC and how that impacts on drug release rates. Both formulations showed sustained type drug release that was modelled by the Korsmeyer-Peppas equation. Changes in the concentration of drug and glycerol (films) did not significantly alter the rate of drug release while increasing polymer content significantly decreased the rate of drug release from both formulations. The results show that the rate of paracetamol release was faster from the wafers than the corresponding films due to differences in their physical structures. The wafers which formed a porous network, hydrated faster than the more dense and continuous, (non-porous) sheet-like structure of the films.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetaminophen / administration & dosage
  • Acetaminophen / chemistry*
  • Carboxymethylcellulose Sodium / chemistry*
  • Chemistry, Pharmaceutical / methods
  • Delayed-Action Preparations
  • Freeze Drying
  • Gels
  • Glycerol / chemistry*
  • Microscopy, Electron, Scanning
  • Polymers / chemistry*
  • Porosity
  • Solubility
  • Solvents / chemistry
  • Time Factors

Substances

  • Delayed-Action Preparations
  • Gels
  • Polymers
  • Solvents
  • Acetaminophen
  • Carboxymethylcellulose Sodium
  • Glycerol