SOLID PHARMACEUTICAL COMPOSITIONS THAT INCLUDE AN S1P RECEIVER AGONIST AND A SUGAR SPIRIT.

摘要

A solid pharmaceutical composition suitable for oral administration, comprising: (a) an S1P receptor agonist; and (b) a sugar alcohol, wherein the S1P receptor agonist is selected from - a compound of the formula I ** see formula ** wherein R1 is a straight or branched (C12-22) carbon chain (C12 -22) - having in the chain a bond or a heteroatom selected from a double bond, a triple bond, O, S, NR6, wherein R 6 is H, alkyl, aralkyl, acyl or alkoxycarbonyl, and carbonyl, and / or - which may have as a substituent alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxyimino, hydroxy or carboxy; or R1 is - a phenylalkyl wherein alkyl is a straight or branched (C6-20) (C6-20) carbon chain; or - a phenylalkyl wherein alkyl is a straight or branched (C 1-30) (C 1-30) carbon chain wherein said phenylalkyl is substituted by - a straight or branched (C 6-20) carbon chain that is optionally substituted by halogen, - a straight or branched (C6-20) alkoxy chain that is optionally substituted by halogen, - a straight or branched (C6-20) alkenyloxy chain. - phenylalkoxy, halophenylalkoxy, phenylalkoxyalkyl, phenoxyalkoxy or phenoxyalkyl, - cycloalkylalkyl substituted by C6-20 alkyl, - heteroarylalkyl substituted by C 6-20 alkyl, - heterocyclic alkyl C6-20 or - heterocyclic alkyl substituted by C 2-20 alkyl, and in where the alkyl functional group may have - In the carbon chain, a bond or a heteroatom selected from a double bond, a triple bond, O, S, sulfinyl, sulfonyl, or NR6, wherein R6 is as defined above, and - as an alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, acyl, alkylamino, alkylthio, acylamino, alkoxycarbonyl, alkoxycarbonylamino, acyloxy, alkylcarbamoyl, nitro, halogen, amino, hydroxy or carboxy substituent, and each of R2, R3, R4 and R5, independently , is H, C1-4 alkyl or acyl; and or its pharmacologically acceptable salt.