Pharmaceutical preparation in the form of an effervescent...

A - Human Necessities – 61 – K

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A61K 31/445 (2006.01) A61K 9/16 (2006.01) A61K 9/46 (2006.01)

Patent

CA 2127352

The pharmaceutical preparation in the form of an effervescent and/or disintegrating tablet or an instant granulate contains at least one taste irritating agent and at least one matrix delaying the release of the agent which is intimately mixed with the agent particles or envelops them and is applied to a substrate. The preparation in aqueous solution at room temperature releases at most 65 and preferably at most 50 % of the agent within some 2 minutes, but in 0.1n HCl at 38°C releases over 70 and preferably 80 % of the agent within at most 20 and preferably at most 15 minutes. The matrix preferably contains at least one fatty acid ester and/or a wax, preferably with a melting point between 30 and 45, especially between 32 and 35°C, and/or at least one cellulose derivative and/or at least one polymethacrylate acid ester. The quantity of the agent is under 60 and preferably under 10 mg, that of the matrix 1 to 10, preferably 3 to 5 times that of the agent per tablet or dose of granulate. For the treatment of diarrhoea by means of loperamide, the matrix also contains a mixture and quantity of alkaline and/or alkaline earth salts, preferably organic salts, and chlorides which compensate for the loss of electrolyte in the body.

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