Patent ID: 7767227

Claim:
A sustained-release solid oral galenical form of molsidomine which contains a sustained-release matrix containing a therapeutically effective amount of molsidomine or one active metabolite of molsidomine selected from the group consisting of SIN-1 and SIN-1A, said matrix consisting essentially of: at least 40% by weight of a material selected from the group consisting of: a polymeric material having a high swelling capacity in contact with water or aqueous liquids and gelling properties, and which is a high molecular weight hydroxypropyl methyl cellulose; and a mixture of a polymeric material having a high swelling capacity in contact with water or aqueous liquids selected from the group consisting of crosslinked sodium carboxymethylcellulose, a crosslinked hydroxypropylcellulose, a high molecular weight hydroxymethylpropylcellulose, a polymethylmethacrylate, a crosslinked polyvinylpyrrolidone and a high molecular weight polyvinylalcohol, and a gellable polymeric material selected from the group consisting of methylcellulose, carboxymethylcellulose, a low molecular weight hydroxypropylmethylcellulose, a low molecular weight polyvinylalcohol, a polyethyleneglycol and a non-crosslinked polyvinylpyrrolidone; between 12% and 25% by weight of a lipophilic substance selected from the group consisting of glycerol behenate, an hydrogenated castor oil, glyceryl palmitostearate and glyceryl monooleate; and at least 25% by weight of at least one adjuvant selected from the group consisting of diluents, lubricants, granulating agents, flow improvers and colorants; said galenic form having an in vitro dissolution rate, measured spectrophotometrically at 286 or 311 nm by the method described in the European Pharmacopoeia, 3rd edition or by the method USP XXIV, at 50 rpm, in 500 ml of a 0.1 N HCl medium, at 37° C. of: 15 to 25% of molsidomine released after 1 hour 20 to 35% of molsidomine released after 2 hours 50 to 65% of molsidomine released after 6 hours 75 to 95% of molsidomine released after 12 hours >85% of molsidomine released after 18 hours >90% of molsidomine released after 24 hours, and providing a plasma concentration of at least 5 ng/ml of plasma, over a period of about 24 hours, the plasma peak of molsidomine obtained in vivo occurring 2.5 to 5 hours following the administration of said form, and having a value of between 25 and 40 ng/ml of plasma.