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

Autor: Aurélie Bonneville, Alain Astier, Stéphane Gibaud
Přispěvatelé: Gibaud, Stéphane, Cibles thérapeutiques, formulation et expertise pré-clinique du médicament (CITHEFOR), Université de Lorraine (UL)
Rok vydání: 2002
Předmět:
MESH: Microscopy
Electron
Scanning
MESH: Delayed-Action Preparations
Scanning electron microscope
Drug Compounding
Polyesters
MESH: Microspheres
Acrylic Resins
Pharmaceutical Science
MESH: Solvents
030226 pharmacology & pharmacy
Dosage form
Excipients
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Polymer chemistry
MESH: Particle Size
4-Aminopyridine
Particle Size
Microparticle
MESH: Excipients
Dichloromethane
MESH: Acrylic Resins
Aqueous two-phase system
[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences
MESH: Polyesters
Microspheres
[SDV.SP] Life Sciences [q-bio]/Pharmaceutical sciences
MESH: 4-Aminopyridine
chemistry
Delayed-Action Preparations
MESH: Drug Compounding
Polycaprolactone
Microscopy
Electron
Scanning
Solvents
Amifampridine
Drug carrier
Caprolactone
030217 neurology & neurosurgery
Nuclear chemistry
Zdroj: International Journal of Pharmaceutics
International Journal of Pharmaceutics, Elsevier, 2002, 242 (1-2), pp.197-201
ISSN: 0378-5173
DOI: 10.1016/s0378-5173(02)00157-6
Popis: International audience; 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).
Databáze: OpenAIRE
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