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Related Experiment Videos

Gastro-resistant microspheres containing ketoprofen.

G F Palmieri1, G Bonacucina, P Di Martino

  • 1Università di Camerino, Dipartimento di Scienze Chimiche, Italy. gianpalm@camserv.unicam.it

Journal of Microencapsulation
|January 29, 2002
PubMed
Summary
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Ketoprofen gastroresistant microspheres were successfully prepared using Eudragit polymers, offering good gastroresistance and tablet compressibility. These microspheres effectively prevent drug release in acidic conditions.

Area of Science:

  • Pharmaceutical Technology
  • Materials Science

Background:

  • Ketoprofen microspheres require gastroresistance for effective oral delivery.
  • Spray-drying is a common method for microsphere preparation, but drug recrystallization can be a challenge.

Purpose of the Study:

  • To prepare and characterize ketoprofen gastroresistant microspheres using various pH-dependent polymers.
  • To evaluate the impact of polymer choice on microsphere properties, compressibility, and in vitro drug release.
  • To assess the gastroresistance of formulated tablets.

Main Methods:

  • Spray-drying of ketoprofen with Eudragit S, Eudragit L, CAP, CAT, and HPMCP.
  • Characterization using scanning electron microscopy, differential scanning calorimetry, and X-ray diffractometry.
  • In vitro dissolution studies and tablet compaction analysis.

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Main Results:

  • Eudragit L/S microspheres exhibited comparable compressibility to microcrystalline cellulose, unlike cellulosic derivatives.
  • All microspheres demonstrated good gastroresistance, with acrylic polymers being more effective than cellulosic ones at low pH.
  • Tablet compression eliminated polymer-dependent differences in drug release, achieving near-zero release in 0.1 N HCl.

Conclusions:

  • Eudragit polymers are suitable for preparing ketoprofen gastroresistant microspheres with good compressibility.
  • The compression process into tablets ensures robust gastroresistance, irrespective of the enteric polymer used.
  • Spray-dried microspheres offer a viable approach for developing gastro-protected ketoprofen formulations.