Oral pharmaceutical preparation comprising an antiulcer...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 31/4184 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/555 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2307037

It comprises an inert nucleus; and active layer which is soluble or which desintegrates in water and is obtained from a unique aqueous or hydro-alcoholic solution-suspension which comprises: an active principle having an antiulcer activity with formula (I, II or III) and at least one excipient; and a gastroresistant external coating layer obtained from a solution which comprises an enteric covering polymer and at least one excipient. The process is carried out by (1) covering the inert nucleus by nebulisation of the aqueous or hydroalcoholic suspension-solution; (2) drying the active layer formed during the nebulisation of the prior step; and (3) covering the nucleus charged through nebulisation with the solution comprising an enteric coating polymer with at least one excipient to obtain an external gastroresistant coating layer.

L'invention concerne un noyau inerte; une couche active soluble ou à désintégration rapide dans l'eau, obtenue à partir d'une unique solution-suspension aqueuse ou hydro-alcoolique qui renferme: un principe actif à activité anti-ulcéreurse de formule (I, II ou III) et au moins un excipient; et une couche de revêtement externe gastrorésistante obtenue à partir d'une solution qui renferme: un polymère de revêtement intestinal; et au moins un excipient. On met en oeuvre ce procédé en 1) recouvrant les noyaux inertes par une nébulisation de l'unique suspension-solution aqueuse ou hydro-alcoolique; 2) en séchant la couche active formée pendant la nébulisation effectuée à l'étape précédente; et 3) en recouvrant les noyaux chargés par la nébulisation d'une solution qui renferme un polymère de revêtement intestinal avec au moins un excipient pour obtenir une couche de revêtement externe gastrorésistante.

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