Floating microgranules

摘要

Disclosed is a floating granule, formulated to float at the surface of the gastric liquid, having a diameter of less than 3 mm, presenting a core-shell type consisting of a neutral solid core; an internal layer surrounding said core, said layer comprising a mixture formed with i) an active ingredient selected from the group formed by furosemide, tiapride, alfuzosin, captopril, gamma-hydroxybutyric acid (GHB), metformin, nifedipine, buprenorphine, modafinil, methadone, nalbuphine, tetrahydrocannabinol, and ii) an alkaline agent generating a release of gas in the presence of said stomach liquid, an intermediate layer being provided, separating said alkaline agent and said active ingredient when the latter is an acid compound, wherein said alkaline agent is selected from the group consisting of sodium bicarbonate, sodium carbonate, sodium glycine carbonate, potassium bicarbonate, magnesium carbonate and calcium carbonate; and an external coating layer; preferably the neutral core comprises one or more compounds selected from the group consisting of polyols, gums, derivatives of silica, derivatives of calcium or potassium, mineral compounds, saccharose, cellulose derivatives, starch, gluconates, silicates, sugar crystals, and admixtures thereof; and preferably the external coating layer is selected from the group consisting of shellac, polyvinyl pyrrolidone, polyethylene glycol, cellulose derivatives, saccharose, fatty acid glycerides and admixtures thereof. Also disclosed is a method for preparing a floating granule as defined above, the method comprising a step of application, by powdering the active ingredient to the solid core, a step of adding the alkaline agent, and a step of adding an intermediate layer separating said active ingredient from said alkaline agent when said active ingredient is an acid compound, and a step of adding an external coating.