Process for producing drug-containing microspheres by oil-in-wat

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form

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424490, 424450, A61K 950, A61K 914

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active

059809477

ABSTRACT:
Formation of a drug into microspheres by an oil-on-water solvent evaporation process in which a mixed solvent of at least one water-insoluble solvent and at least one water-miscible solvent is used as a solvent of an oil phase. A fatty acid or a salt thereof or at least one glycerin fatty acid ester and/or at least one propylene glycol fatty acid ester are added to the mixed solvent. The oil phase may also comprise the mixed solvent; a fatty acid or a salt thereof; and at least one glycerin fatty acid ester and/or at least one propylene glycol fatty acid ester. This oil phase is mixed and emulsified with an aqueous phase to form an oil-in-water emulsion. The emulsion with a drug contained therein is then subjected to an oil-in water solvent evaporation to produce the microspheres. The resulting drug-containing microspheres contain the drug at a high concentration and slowly release from the initial stage after administration.

REFERENCES:
patent: 4542025 (1985-09-01), Tice
patent: 4671954 (1987-06-01), Goldberg
patent: 4933105 (1990-06-01), Fong
patent: 4954298 (1990-09-01), Yamamoto
patent: 4954338 (1990-09-01), Mattox
patent: 4994281 (1991-02-01), Muranishi

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