MICROPARTICLES BASED ON AN AMPHIPHILIC COPOLYMER AND ON ACTIVE INGREDIENT(S) WITH MODIFIED RELEASE AND PHARMACEUTICAL FORMULATIONS CONTAINING SAME

摘要

Polymeric microparticle (I) comprising an active ingredient is claimed. The polymer present in (I) is amphiphilic, biodegradable, hydro-soluble copolymer with hydrophobic and hydrophilic groups, spontaneously forms a colloidal suspension of nanoparticles in water at a pH of 7 under isotonic condition. (I) is non-covalently bonded to the active ingredient and obtained by atomization of a solution or a colloidal suspension of (I), has a size of 0.5-100 mu m, preferably 2-40 mu m and is dispersible in colloidal suspension measured by a dispersibility test described in the given specification. Independent claims are included for: (1) a process of preparing (I) comprising atomizing a solution or a colloidal suspension of (I); (2) a liquid/solid pharmaceutical formulation for the sustained release of the active ingredient comprising a less viscous colloidal suspension; (3) requirements for a reconstitution process comprising (I) and a reconstituting liquid like an aqueous liquid, water (non)miscible organic liquid; and (4) a reconstitution process comprising mixing and agitating the given requirements.