Toyo Jozo Kabushiki Kaisha

Toyo Jozo Company, Ltd.

Jinnosuke Abe

Tadashiro Fujii

Masataka Morishita

Mitsuru Fukushima

Yoshihito Inaba

Sadami Kobari

Kentaro Fujimoto

Kazuyoshi Nishiie

Akiho Nagata

Tetsuo Watanabe

Teruo Take

Microcapsules are made by (a.) dispersing or dissolving a core substance in a film-forming polymer solution, (b.) emulsifying in fine droplets the resulting dispersion or solution in a vehicle which is poorly miscible with the solvent of the polymer solution and which doesn't dissolve said polymer to prepare an emulsion, and (c.) adding to the emulsion a non-solvent for the polymer wherein the non-solvent is miscible with the solvent, poorly miscible with the vehicle, and does not dissolve the polymer, whereby the solvent is removed by being absorbed by non-solvent emulsion droplets to precipitate the polymer film around the core substance.

Preparation of microcapsules

Novel diacyl penicillins of the formula ##EQU1## wherein R is alkyl, cycloalkyl, aryl, aralkyl, phenoxyalkyl, heterocyclic carboxyl excepting isoxazole carboxyl derivatives, or ##SPC1## In which benzene ring A may optionally be substituted and B represents a protective group for the amino group, and X is a protective group for the carboxyl group, are produced by reacting a benzyl penicillin ester of the formula ##EQU2## wherein X is as defined above, with a chlorinating agent in the presence of tertiary organic base to obtain an imide chloride group-incorporated compound of the formula ##EQU3## and then reacting the compound of the last-named formula with carboxylate of the formula

Diacyl penicillins and methods for their production

Growing community of inventors

Shizuoka, Japan

Jinnosuke Abe