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Characterization of a diltiazem-lambda carrageenan complex.

M C Bonferoni1, S Rossi, F Ferrari

  • 1Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100, Pavia, Italy.

International Journal of Pharmaceutics
|June 27, 2000
PubMed
Summary
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Lambda carrageenan binds diltiazem HCl, influencing drug release from hydrophilic matrix systems. This interaction is pH-insensitive but affected by ionic strength, crucial for drug delivery formulation.

Area of Science:

  • Pharmaceutical Sciences
  • Polymer Chemistry

Background:

  • Diltiazem HCl is a calcium channel blocker used in treating cardiovascular conditions.
  • Lambda carrageenan is a natural sulfated polysaccharide with potential applications in drug delivery.

Purpose of the Study:

  • To investigate the interaction between lambda carrageenan and diltiazem HCl.
  • To quantify the binding capacity of lambda carrageenan for diltiazem.
  • To assess the impact of this interaction on diltiazem release from hydrophilic matrix systems.

Main Methods:

  • Dialysis equilibria were employed to determine binding capacity.
  • Matrix tablets with varying lambda carrageenan concentrations were prepared.
  • Drug release profiles were analyzed.
  • X-ray and Differential Scanning Calorimetry (DSC) were used for solid-state characterization.

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Main Results:

  • A significant interaction and binding capacity between lambda carrageenan and diltiazem HCl were observed.
  • The binding capacity was found to be largely insensitive to pH (1.8-6.8) but decreased with increasing ionic strength, indicating ionic bond involvement.
  • Drug release from matrix tablets correlated with lambda carrageenan content, demonstrating the interaction's relevance to drug delivery.
  • Solid-state analysis provided preliminary characterization of the diltiazem-carrageenan complex.

Conclusions:

  • Lambda carrageenan effectively binds diltiazem HCl, influencing its release kinetics in hydrophilic matrices.
  • The diltiazem-carrageenan interaction is primarily governed by ionic forces and is robust across a relevant pH range.
  • Understanding this interaction is vital for optimizing diltiazem HCl formulations using lambda carrageenan as a matrix former.