Gastroretentive controlled release microspheres for improved drug delivery

A method for the treatment or prophylaxis of a disease, the method comprising

• administering to a patient in need of such treatment or prophylaxis a composition comprising a microsphere which comprises
• an active ingredient effective against the disease, wherein the ingredient is in the inner core of the microsphere,
• a rate controlling layer of a water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of a cationic polymer.

A kit of parts for use in the treatment of H. pylori infection, the kit comprising

• a composition comprising an H2-antagonist, a proton pump inhibitor, or an antacid, and
• a composition comprising a microsphere which comprises
• an active ingredient useful in the treatment of Helicobacter pylori, wherein the ingredient is in the inner core of the microsphere,
• a rate controlling layer of a water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of a cationic polymer.

A process for the preparation of a composition for the controlled release of an active ingredient in the stomach environment over a prolonged period of time, the process comprising

• preparing an oil-in-water or a water-in-oil-in-water emulsion comprising the active ingredient, a water insoluble polymer and a cationic polymer, and
• spray drying the emulsion to yield microspheres having
• the active ingredient in the inner cores of the microspheres,
• a rate controlling layer of the water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of the cationic polymer.

A method of delivering a therapeutic agent to the stomach of a patient, the method comprising

• administering to the patient a composition comprising a microsphere which comprises
• the therapeutic agent in the inner core of the microsphere,
• a rate controlling layer of a water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of a cationic polymer.

A method of enhancing the gastrorentention of an active ingredient in the stomach of a patient, the method comprising

• administering to the patient the active ingredient in a composition comprising a microsphere which comprises
• the active ingredient in the inner core of the microsphere,
• a rate controlling layer of a water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of a cationic polymer.

A method of enhancing the gastrointestinal absorption of a drug which has a limited absorption capacity in the small intestine of a patient, the method comprising

• administering to the patient the drug in a composition comprising a microsphere which comprises
• the drug in the inner core of the microsphere,
• a rate controlling layer of a water insoluble polymer, and
• an outer layer of a bioadhesive agent in the form of a cationic polymer.