Preparation of 3,4-diaminopyridine microparticles by solvent-evaporation methods. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue International Journal of Pharmaceutics Année : 2002

Preparation of 3,4-diaminopyridine microparticles by solvent-evaporation methods.

Résumé

The present study compares two methods of preparation of microparticles of 3,4-diaminopyridine (3,4-DAP) for the treatment for multiple sclerosis and Lambert-Eaton myasthenia syndrome. Poly( epsilon -caprolactone) microparticles were prepared with a solvent-evaporation W/O method. The 3,4-DAP was dispersed in dichloromethane, leading to a suspension. The dispersion and the solidification of the dichloromethane droplets in an aqueous phase have led to microparticles of 55.3+/-34.7 microm. The incorporation of the drug by milligram of powder was very low (1.91 micrograms/mg) and the scanning electron microscopy (SEM) did not show any crystal but marks of dissolved crystals were observed on the polymeric surface. EudragitRS microspheres containing 3,4-DAP were prepared by a solvent-evaporation technique using light mineral oil as continuous phase. The drug and the polymer were completely dissolved in an acetone solution, used as discontinuous phase. This formulation have led to a higher incorporation of the drug (88.25 micrograms/mg). The particle size was 91.8+/-44.3 microm. The observation, by SEM, shows many crystals on the surface and inside the microparticles. A slow-release of the drug in a phosphate buffer pH 7.4 was observed (50% in 60 min and about 70% in 4 h).
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Dates et versions

hal-00399627 , version 1 (27-06-2009)

Identifiants

  • HAL Id : hal-00399627 , version 1
  • PUBMED : 12176246

Citer

Stéphane Gibaud, Aurélie Bonneville, Alain Astier. Preparation of 3,4-diaminopyridine microparticles by solvent-evaporation methods.. International Journal of Pharmaceutics, 2002, 242 (1-2), pp.197-201. ⟨hal-00399627⟩
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