PROCESS FOR THE PRODUCTION OF DRUG FORMULATIONS FOR ORAL ADMINISTRATION

摘要

The present invention provides a simple and mild process for the preparation of nano- and/or microparticles, which particles contain one or more therapeutic agents dispersed in non-crystalline form in a matrix containing one or more polymers selected from cellulose ethers, cellulose esters, copolymers of methacrylic acid with one or more (meth) acrylic acid esters, copolymers of two or more (meth) acrylic acid esters and mixtures thereof, as well as pharmaceutical formulations containing the nano- and/or microparticles.

主权项

1. A process for the production of nano- and/or microparticles, which particles contain one or more therapeutic agents dispersed in non-crystalline form in a matrix containing one or more polymers selected from cellulose ethers, cellulose esters, copolymers of methacrylic acid with one or more (meth)acrylic acid esters, copolymers of two or more (meth)acrylic acid esters and mixtures thereof, said process comprising the steps of
a) providing a solution containing
a1) the one or more therapeutic agents in dissolved form;a2) the one or more polymers in dissolved form, anda3) a solvent mixture containing (i) at least one solvent S1 which is fully miscible with water, and which is a solvent for the one or more therapeutic agents and a solvent for the one or more polymers, and (ii) at least one solvent S2 which is fully miscible with solvent S1 and which is partially miscible with water; b) adding an aqueous surfactant solution with a volume of at least 2 times the volume of the solution provided in step a) to the solution provided in step a) while the solution provided in step a) is stirred, and c) allowing the nano- and/or microparticles to form via extraction of the solvents S1 and S2 into the aqueous surfactant solution.