| 摘要 |
A sustained-release porous microparticle for pulmonary delivery of a protein drug is provided to reduce destruction of microparticles by macrophages by having suitable particle size, improve stability and distribution uniformity of a protein drug, and release the drug for a long period of time without initial burst. A sustained-release porous microparticle comprises a protein drug as an active ingredient, cyclodextrin derivatives, viscous hydrophilic polymer, biodegradable polymer, sucrose acetate isobutyrate and aqueous coating materials, and has an average particle diameter of 5-100 mum. A process for preparing the sustained-release porous microparticle comprises the steps of: (1) solubilizing cyclodextrin derivatives, viscous hydrophilic polymer and a protein drug in water to prepare an inner water phase; (2) adding biodegradable polymer and sucrose acetate isobutyrate into organic solvent to prepare an organic phase; (3) mixing the inner water phase with the organic phase to prepare a first emulsion; and (4) spraying the first emulsion to an outer aqueous continuous phase containing aqueous coating materials.
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