Method for producing sustained release microsphere preparation

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

A - Human Necessities

61

K

A61K 9/16 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 9/52 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2099941

A method for producing a sustained release microsphere preparation for a water-soluble medicament, which has a high incorporation efficiency of the medicament and a low initial burst, comprises dissolving a water-soluble pharmaceutical active ingredient and a 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 the biodegradable polymer at the molecular level, and dissolving the solid dispersion in an organic solvent that is water-immiscible and has a boiling point below 100°C, and adding the resulting oil phase into an aqueous phase containing an emulsifying agent to give an O/W emulsion, followed by removing the organic solvent from the oil phase of the resulting emulsion.

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