Takeda Chemical Industries, Inc.

Shigehiro Higuchi

Naoru Hamaguchi

Muneo Nonomura

Nobuyuki Takechi

Toshiharu Beppu

Motoya Ohshika

This invention provides a method for producing a microparticle which comprises pulverizing a solid preparation comprising a compound represented by the formula: ##STR1## wherein ring A is an optionally substituted benzene ring; R is a hydrogen atom or an optionally substituted hydrocarbon group; B is an optionally esterified or amidated carboxyl group; X is --CH(OH)-- or --CO--; k is 0 or 1; and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof and a biodegradable polymer of .alpha.-hydroxycarboxylic acid in the presence of a pulverizing auxiliary, which can provide microparticles which are less adhesive and involve less aggregation and are thus excellent in drug entrapment ratio and control of drug-release in a desired particle size.

Method for producing a microparticle

A freeze-dried preparation comprising a bioactive substance having an optionally substituted amidino group and a disaccharide which stabilizes the bioactive substance; and a process for making the preparation are described.

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Amagasaki, Japan

Shigehiro Higuchi