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Sustained-release butorphanol microparticles.

H C Chang1, L C Li

  • 1Abbott Laboratories, Department 97d, Abbott Park, IL 60064-3500, USA.

Drug Development and Industrial Pharmacy
|July 20, 2000
PubMed
Summary
This summary is machine-generated.

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Biodegradable microparticles were created using P(FAD-SA) and P(CPP-SA) copolymers for sustained butorphanol release over 48 hours. Spray-dried microspheres showed rapid drug release within 2 hours.

Area of Science:

  • Polymer science
  • Materials science
  • Pharmaceutical technology

Background:

  • Biodegradable polymers are crucial for controlled drug delivery systems.
  • Butorphanol is an analgesic with potential for sustained release formulations.
  • Developing microparticulate drug delivery systems requires careful selection of polymers and fabrication methods.

Purpose of the Study:

  • To prepare and characterize butorphanol-loaded microparticles using biodegradable copolymers P(FAD-SA) and P(CPP-SA).
  • To investigate the in vitro drug release profiles of butorphanol from these microparticles.
  • To evaluate the influence of fabrication methods, drug loading, particle size, and copolymer composition on drug release.

Main Methods:

  • Melt compounding and milling were used to prepare butorphanol-loaded microparticles with P(FAD-SA) and P(CPP-SA) copolymers.

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  • In vitro drug release studies were conducted at 37°C in water for injection.
  • Scanning electron microscopy (SEM) was employed to analyze particle morphology and surface characteristics.
  • Spray-drying was used as an alternative method to prepare butorphanol-encapsulated microspheres with P(FAD-SA).

    • Main Results:

    • Butorphanol was released in a sustained manner from melt-compounded microparticles, reaching ~100% release in 48 hours.
    • Drug release was influenced by drug loading and microparticle size but not significantly by copolymer composition.
    • SEM revealed irregular shapes and uneven surfaces for melt-compounded particles.
    • Spray-dried microspheres (2-10 microns) exhibited smooth surfaces and rapid drug release (>92% in 2 hours).

    Conclusions:

    • Biodegradable copolymers P(FAD-SA) and P(CPP-SA) can be fabricated into microparticles for butorphanol delivery.
    • Melt compounding and milling yield sustained drug release, while spray-drying results in rapid release.
    • Particle characteristics and fabrication methods significantly impact butorphanol release kinetics.