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Stable Formulation

IP.com Disclosure Number: IPCOM000011024D
Publication Date: 2003-Feb-09
Document File: 1 page(s) / 72K

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Stabilized pharmaceutical formulation of acid labile benzimidazole compound and its preparation

Substituted benzimidazole are substituted sulfoxides, such as 2-({[4-(3- Methoxypropoxy)-3-methyl-2- pyridyl]methyl}sulfinyl)-1H-benzimidazole sodium,

which are potent inhibitors of gastric secretion. These compounds are susceptible to degradation and/or transformation in acidic media.

In order to provide a pharmaceutical composition containing such an acid labile substance, which will not degrade in the GI tract, the dosage form should be enteric- coated. However, pharmaceutically acceptable enteric coating materials often contain acidic reacting groups. Therefore, direct coating of the acid susceptible drug with these enteric coatings may cause degradation of the acid labile substance.

A large number of publications and patent applications are available, describing enteric coated pharmaceutical formulations of labile benzimidazoles.

Our work herein disclosed relates to a stabilized pharmaceutical composition in the form of a tablet core comprising the benzimidazole derivative drug, an intermediate coating layer based on a water soluble polymer and an enteric coating layer.

The cores contain the active substance; a binder consisting of an inert polymer such as hydroxypropyl methylcellulose, hydroxypropy cellulose, sodium carboxymethyl cellulose; an inert filler such as microcrystalline cellulose, lactose , mannitol; an alkaline reacting agent such as basic inorganic salts (magnesium carbonate, magnesi...