Producing solid oral dosage form, useful as e.g. anti-ulcer drugs, comprises mixing pyridylmethylsulfinyl benzimidazole with alumina and optionally auxiliary agents and converting into a suitable solid application form

摘要

#CMT# #/CMT# Producing solid oral dosage form comprises mixing an optionally substituted 2-(pyridylmethylsulfinyl)-1H-benzimidazole with alumina and optionally auxiliary agents and converting the mixture into a suitable solid dosage form. #CMT# : #/CMT# An independent claim is included for a pharmaceutical composition comprising an optionally substituted 2-(pyridylmethylsulfinyl)-1H-benzimidazole and alumina. #CMT#ACTIVITY : #/CMT# Gastrointestinal-Gen; Antiulcer. No biological data given. #CMT#MECHANISM OF ACTION : #/CMT# Proton pump inhibitor. #CMT#USE : #/CMT# The dosage form is useful as an anti-ulcer agent and as an agent for treating/preventing the over-production of gastric acid related diseases. #CMT#ADVANTAGE : #/CMT# The optionally substituted 2-(pyridylmethylsulfinyl)-1H-benzimidazole is chemically and physically stable in the solid oral application form. #CMT#PHARMACEUTICALS : #/CMT# Preferred Components: The pyridylmethylsulfinyl benzimidazole is esomeprazole in the form of magnesium salt dihydrate. The alumina has a Brunner Emmett Teller (BET) surface area of 100 m 2>/g. The mixture of pyridylmethylsulfinyl benzimidazole and alumina in compacted, tableted, pelleted or extruded form is provided with a polymer coating, which dissolves at a pH of >= 5. The pharmaceutical composition comprises a stabilizing intermediate layer below the polymer layer. #CMT#EXAMPLE : #/CMT# Esomeprazole (40 g) and amorphous alumina (80 g) were mixed intensively and then magnesium stearate was added. The mixture was pressed into tablets of 2 mm diameter. The hydroxypropyl methylcellulose was provided as an insulation layer for the tablets and coated with an enteric coating. Then the mini-tablets were filled into gelatin capsules.