Patent ID: 6346537
Filing Date: 2002-02-12
Classification: A61K,A61P

Abstract:
A solid dispersion comprising a tricyclic compound (I) of the following general formula or a pharmacologically acceptable salt thereof: wherein each of adjacent pairs of R1 and R2, R3 and R4 or R5 and R6 independently (a) are two adjacent hydrogen atoms, or (b) may form another bond formed between the carbon atoms to which they are attached, and further, R2 may be an alkyl group; R7 is a hydrogen atom, a hydroxy group, a protected hydroxy group or an alkoxy group, or an oxo group together with R1, each of R8 and R9 is independently a hydrogen atom or a hydroxy group; R10 is a hydrogen atom, an alkyl group, an alkyl group substituted by one or more hydroxy groups, an alkenyl group, an alkenyl group substituted by one or more hydroxy groups or an alkyl group substituted by an oxo group; X is an oxo group, (a hydrogen atom and a hydroxy group), (a hydrogen atom and a hydrogen atom), or a group represented by the formula â€”CH2Oâ€”; Y is an oxo group, (a hydrogen atom and a hydroxy group), (a hydrogen atom and a hydrogen atom), or a group represented by the formula Nâ€”NR11R12 or Nâ€”OR13; each of R11 and R12 is independently a hydrogen atom, an alkyl group, an aryl group or a tosyl group; each of R13, R14, R15, R16, R17, R18, R19, R22 and R23 is independently a hydrogen atom or an alkyl group; each of R20 and R21 is independently an oxo group or (R20a and a hydrogen atom) or (R21a and a hydrogen atom) in which each of R20a and R21a is independently a hydroxy group, an alkoxy group or a group represented by the formula â€”OCH2OCH2CH2OCH2, or R21a is a protected hydroxy group, or R20a and R21a may together represent an oxygen atom in an epoxide ring; n is an integer of 1 or 2; and in addition to the above definitions, Y, R10 and R23, together with the carbon atoms to which they are attached, may represent a saturated or unsaturated 5- or 6-membered nitrogen, sulfur and/or oxygen containing heterocyclic ring optionally substituted by one or more groups selected from the group consisting of an alkyl, a hydroxy, an alkyl substituted by one or more hydroxy groups, an alkoxy, a benzyl and a group of the formula â€”CH2Se(C6H5); and a pharmaceutically acceptable surfactant selected from the group consisting of polyoxyethylene hydrogenated castor oil, sucrose fatty acid esters, propylene glycol fatty acid mono- or di-esters, and polyoxyethylene sorbitan fatty acid esters, or a combination of two or more of these surfactants; and a pharmaceutically acceptable solid carrier selected from the group consisting of water-soluble polymers, saccharides, and light anhydrous silicic acid, or a combination of two or more of these solid carriers; in which the weight ratio of the tricyclic compound (I), the surfactant and the solid carrier is 1:01Ëœ100:1Ëœ300.