Multilayered pharmaceutically active compound-releasing microparticles in a liquid dosage form

A controlled-release multilayer microparticle containing a pharmaceutically active compound, said microparticle being intended for oral administration or direct administration in the stomach in the form of a liquid pharmaceutical composition and said microparticle comprising:

• a core comprising the pharmaceutically active compound, said pharmaceutically active compound being esomeprazole;
• a controlled-release intermediate coating layer;
• an outmost external protection coating layer surrounding the controlled-release intermediate coating layer and consists essentially of a mixture of
• a) a hydrophilic gastro-soluble component which is insoluble in aqueous media at a pH of between 7.5 and 8.5 and is a cationic polymer based on dimethylaminomethyl methacrylate, butyl methacrylate, and methyl methacrylate,
• b) a hydrophobic and/or insoluble component which is glyceryl monostearate, and
• c) talc,
• wherein the weight ratio of the hydrophilic gastro-soluble component/hydrophobic and/or insoluble component is between 1/1 and 30/1 and
• wherein said controlled-release multilayer microparticle is stable for at least one week when stored at 2-8° C. in a liquid medium having a pH>6 and <8.5.

A controlled-release multilayer microparticle containing a pharmaceutically active compound, said microparticle being intended for oral administration or direct administration in the stomach in the form of a liquid pharmaceutical composition and said microparticle comprising:

• a core comprising the pharmaceutically active compound, said pharmaceutically active compound being esomeprazole;
• a controlled-release intermediate coating layer;
• an outmost external protection coating layer surrounding the controlled-release intermediate coating layer and consists of a mixture of
• a) a hydrophilic gastro-soluble component which is insoluble in aqueous media at a pH of between 7.5 and 8.5 and is a cationic polymer based on dimethylaminomethyl methacrylate, butyl methacrylate, and methyl methacrylate
• b) a hydrophobic and/or insoluble component which is glyceryl monostearate,
• c) talc and
• d) silica and/or aluminum oxide and/or magnesium stearate and/or titanium dioxide and/or iron oxide and/or calcium carbonate,
• wherein the weight ratio of the hydrophilic gastro-soluble component/hydrophobic and/or insoluble component is between 1/1 and 30/1 and
• wherein said controlled-release multilayer microparticle is stable for at least one week when stored at 2-8° C. in a liquid medium having a pH>6 and <8.5.