Patent ID: 8420662
Filing Date: 2013-04-16
Classification: A61K,A61P

Abstract:
1. A stable solid preparation comprising as an effective ingredient a 4,5-epoxymorphinan derivative represented by the general formula (I): wherein in formula (I) a double line of a dashed line and a solid line represents a double bond or a single bond; R R R A represents —N(R B represents (i) a valence bond, (ii) straight or branched alkylene having 1 to 14 carbon atoms, which is optionally substituted with at least one or more substituents selected from the group consisting of alkoxy having 1 to 5 carbon atoms, alkanoyloxy having 1 to 5 carbon atoms, hydroxy, fluorine, chlorine, bromine, iodine, amino, nitro, cyano, trifluoromethyl, trifluoromethoxy and phenoxy, wherein 1 to 3 methylene groups in the alkylene (ii) is optionally replaced with carbonyl groups, (iii) straight or branched non-cyclic unsaturated hydrocarbon containing 1 to 3 double bonds and/or triple bonds and having 2 to 14 carbon atoms, which is optionally substituted with at least one or more substituents selected from the group consisting of alkoxy having 1 to 5 carbon atoms, alkanoyloxy having 1 to 5 carbon atoms, hydroxy, fluorine, chlorine, bromine, iodine, amino, nitro, cyano, trifluoromethyl, trifluoromethoxy and phenoxy, wherein 1 to 3 methylene groups in the hydrocarbon (iii) is optionally replaced with carbonyl groups, or (iv) straight or branched saturated or unsaturated hydrocarbon containing 1 to 5 thioether bonds, ether bonds and/or amino bonds and having 1 to 14 carbon atoms, wherein the heteroatom in the hydrocarbon (iv) is not directly bound to A, and 1 to 3 methylene groups in the hydrocarbon (iv) is optionally replaced with carbonyl groups; R R or a pharmacologically acceptable acid addition salt thereof; and further comprising sodium thiosulfate, a sugar or a sugar alcohol, and hydroxypropylcellulose having a low degree of substitution in an amount of 1 to 30% by weight per weight of a unit containing the effective ingredient.