Patent ID: 6586444
Filing Date: 2003-07-01
Classification: A61K,A61P,C07D,Y10S

Abstract:
A pharmaceutical composition in a gel form, which consists essentially of a tricyclic compound, a dissolution/absorption promoter, a pharmaceutical base, a compatibilizing agent and a thickener,wherein said tricyclic compound is the compound of the formula (I): (wherein each of adjacent pairs of R1 and R2, R3 and R4, and R5 and R6 independently (a) is two adjacent hydrogen atoms, but R2 may also be an alkyl group or (b) may form another bond formed between the carbon atoms to which they are attached; R7 is a hydrogen atom, a hydroxy group, a protected hydroxy group, or an alkoxy group, or an oxo group together with R1; R8 and R9 are 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; R11 and R12 are independently a hydrogen atom, an alkyl group, an aryl group or a tosyl group; R13, R14, R15, R16, R17, R18, R19, R22 and R23 are independently a hydrogen atom or an alkyl group; R24 is an optionally substituted ring system which may contain one or more heteroatoms; 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 alkoxy, a benzyl, a group of the formula â€”CH2Se (C6H5), and an alkyl substituted by one or more hydroxy groups); the dissolution/absorption promoter is diethyl sebacate; the pharmaceutical base is a hydrophilic glycol; the compatibilizing agent is diethylene glycol monoethyl ether; and the thickener is cellulose polymer or carboxyvinyl polymer, in which the amount of the dissolution/absorption promotor and the compatibilizing agent to the total composition is about 1-20 wt % (w/w) and about 5-15%(w/w), respectively.