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Spray-dried microparticulate systems containing acetaminophen.

A Billon1, B Bataille, M Delalonde

  • 1Université Montpellier 1, UFR Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacie Galénique, Pharmacotechnie et Biopharmacie, EA 3008 Génie des Procédés et Sciences des Aliments', France.

Journal of Microencapsulation
|February 12, 2002
PubMed
Summary

Sodium carboxymethylcellulose (NaCMC) microparticles effectively sustained acetaminophen release for 6-8 hours. Microcrystalline cellulose (MCC) showed minimal drug release, highlighting NaCMC

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery Systems

Background:

  • Developing sustained-release formulations is crucial for improving drug efficacy and patient compliance.
  • Cellulose derivatives are widely explored as excipients in drug delivery due to their biocompatibility and versatility.
  • Acetaminophen is a common analgesic and antipyretic requiring effective delivery systems for prolonged action.

Purpose of the Study:

  • To investigate the preparation and acetaminophen release profiles from spray-dried microparticles.
  • To evaluate the performance of two cellulose derivatives, microcrystalline cellulose (MCC) and sodium carboxymethylcellulose (NaCMC), as sustaining agents.
  • To understand the influence of dissolution medium pH on drug release kinetics.

Main Methods:

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  • Spray-drying technique was employed for microparticle preparation.
  • In-vitro dissolution studies were conducted using acetaminophen-loaded microparticles in media of varying pH.
  • Drug release mechanisms were analyzed based on polymer-drug interactions and matrix properties.

Main Results:

  • Microcrystalline cellulose (MCC) exhibited rapid acetaminophen release, with complete dissolution within 1 hour, due to adsorption effects.
  • Sodium carboxymethylcellulose (NaCMC) significantly retarded acetaminophen release, extending it over 6-8 hours.
  • Drug release from NaCMC matrices was dependent on the plasticizer and dissolution medium pH, primarily governed by diffusion through the swollen polymer.

Conclusions:

  • Sodium carboxymethylcellulose (NaCMC) is a promising agent for developing sustained-release acetaminophen formulations.
  • The reduced hydrophilicity of NaCMC in acidic media contributes to delayed gel formation and sustained drug release.
  • Understanding pH-dependent polymer behavior is key to optimizing drug release from cellulose-based microparticulate systems.