Method for producing sustained release microsphere preparation

Details Method for producing sustained release microsphere preparation Method for producing sustained release microsphere preparation

1993-07-12

1996-09-17

Azpuru, Carlos A.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424451, 424489, 424497, 424498, 424501, 514963, 42840221, 264 41, 264 46, A61K 948, A61K 914, A61K 916, A61K 950

Patent

active

055566421

ABSTRACT:
A method for producing sustained release microsphere preparation for water-soluble medicament, which has high incorporation efficiency of the medicament and low initial burst, which comprises dissolving water-soluble pharmaceutical active ingredient and water-insoluble biodegradable polymer in one or two solvents in which both can dissolve, removing the solvent to give a solid dispersion having the water-soluble pharmaceutical active ingredient dispersed into said biodegradable polymer at molecular level, and further, dissolving said solid dispersion in an organic solvent being water-immiscible and having a boiling point of below 100.degree. C., and adding the resulting oil phase into an aqueous phase containing emulsifying agent to give O/W emulsion, and followed by removing the organic solvent from the oil phase of the resulting emulsion.

REFERENCES:
patent: 3976071 (1976-08-01), Sadek
patent: 4384975 (1983-05-01), Fong
patent: 4479911 (1984-10-01), Fong
patent: 4933105 (1990-06-01), Fong
Hiroshi Yuasa et al, Application of the Solid Dispersion Method to Controlled Release of Medicine. I. Controlled Release of Water Soluble Medicine by Using Solid Dispersion, Chem. Pharm. Bull. 39(2) 465-467 (1991).

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