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Formulation factors affecting drug release from poly(lactic acid) (PLA) microcapsule tablets.

A Kader1, R Jalil

  • 1Faculty of Pharmacy, University of Dhaka, Bangladesh. Kader_A@guilfordpharm.com

Drug Development and Industrial Pharmacy
|March 5, 1999
PubMed
Summary

This study developed a sustained-release phenobarbital (PB) microcapsule tablet using poly(lactic acid) (PLA). The microcapsule tablets effectively controlled PB release, showing potential for sustained drug delivery.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Developing sustained-release (SR) formulations is crucial for improving drug efficacy and patient compliance.
  • Phenobarbital (PB) is an antiepileptic drug requiring controlled release to maintain therapeutic levels.

Purpose of the Study:

  • To prepare and characterize a sustained-release phenobarbital microcapsule tablet using poly(lactic acid) (PLA).
  • To evaluate the effect of formulation variables and processing parameters on drug release kinetics and tablet performance.

Main Methods:

  • Microencapsulation of phenobarbital using low and high molecular weight poly(lactic acid) (PLA).
  • Direct compression of microcapsules and physical mixtures into tablets.
  • Assessment of drug release profiles, tablet properties (hardness, friability, tensile strength), and microcapsule morphology.

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Main Results:

  • Successfully prepared PB microcapsules with high loading capacity and unimodal size distribution.
  • Drug release was influenced by PLA ratios, with higher L-PLA content increasing release.
  • Microcapsule tablets demonstrated significantly lower drug release compared to matrix tablets or free microcapsules.
  • Tablet adjuvants, compression pressure, and microcapsule loading affected release kinetics, with mechanical destruction of microcapsules observed.

Conclusions:

  • Poly(lactic acid) microcapsules can be successfully formulated into sustained-release tablets.
  • Tablet processing parameters can be optimized to control drug release without compromising tablet integrity.
  • This approach offers a viable strategy for developing sustained-release phenobarbital formulations.