Influence of the composition of glycerides on the solid-state behaviour and the dissolution profiles of solid lipid extrudates

Int J Pharm. 2009 Nov 3;381(2):184-91. doi: 10.1016/j.ijpharm.2009.03.002. Epub 2009 Mar 19.

Abstract

A monoacid triglyceride and a partial glyceride were extruded below their melting ranges alone and together in different mixture ratios to investigate the influence of the chemical composition of the lipid matrix on the solid-state properties and dissolution characteristics. The partial glyceride exhibits a faster release of the drug compared to the triglyceride due to its surfactant properties. The lipid mixtures show rather complex solid-state behaviour and hence unexpected dissolution characteristics. Adding 10% (w/w) partial glyceride to a triglyceride matrix led to increased incidence of the unstable alpha-form of the triglyceride leading to recrystallization of the stable beta-form over time which causes fractal structures on the extrudate surface which decrease the dissolution rate. Adding 50% (w/w) partial glyceride to the triglyceride matrix also results in tristearin alpha-formation subsequently followed by recrystallization to the beta-form. But as 50% of the matrix consists of the partial glyceride the dissolution rate was faster than the rate obtained by pure triglyceride or the 9+1 (w/w) mixture of triglyceride and partial glyceride. The results of this study help in understanding the complex solid-state behaviour of solid lipid extrudates with different composition and to manufacture suitable lipid-based oral dosage forms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Crystallization
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Drug Compounding / methods*
  • Drug Storage
  • Glycerides / chemistry*
  • Hot Temperature
  • Lipids / chemistry*
  • Powder Diffraction
  • Powders / chemistry
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Surface Properties
  • Surface-Active Agents / chemistry
  • Theophylline / chemistry
  • Transition Temperature
  • Triglycerides / chemistry

Substances

  • Drug Carriers
  • Glycerides
  • Lipids
  • Powders
  • Surface-Active Agents
  • Triglycerides
  • glyceryl monostearate
  • Theophylline
  • tristearin