Pharmaceutical formulation for intraduodenal administration of apomorphine, 6aR-(-)-N-propyl-norapomorphine and their derivatives and pro-drugs thereof

摘要

Disclosed is a pharmaceutical formulation for the treatment of an affliction selected from the group consisting of Parkinson's disease, restless legs syndrome and erectile dysfunction, which composition comprises at least one member selected from the group consisting of apomorphine, 6aR-(-)-N-propyl-norapomorphine and their derivatives and pro-drugs thereof in the form of the base or the pharmaceutically acceptable salts or solvates thereof as an active ingredient in a pharmaceutical preparation in either the form of an oral formulation having an enteric coating that dissolves in the small intestine or a form suited for administration intraduodenally by intraduodenal catheter through the abdominal wall of a patient or by naso-duodenal catheter, wherein said "derivative" or "pro-drug" is a compound of the formula (I), wherein: R1 and R2 are hydrogen, or one of R1 and R2 is hydrogen or acetyl and the other one is selected from the group consisting of (C2-C20) alkanoyl; halo-(C3-C20) alkanoyl; (C3-C20) alkenoyl; (C4-C7) cycloalkanoyl; (C3-C6)-cycloalkyl(C2-C16)alkanoyl; aroyl which is unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, cyano, trifluoromethanesulphonyloxy, (C1-C3) alkyl and (C1-C3) alkoxy, which latter may in turn be substituted by 1 to 3 halogen atoms; aryl (C2-C16) alkanoyl which is unsubstituted or substituted in the aryl moiety by 1 to 3 substituents selected from the group consisting of halogen, (C1-C3) alkyl and (C1-C3) alkoxy, which latter may in turn be substituted by 1 to 3 halogen atoms; and hetero-arylalkanoyl having one to three heteroatoms selected from O, S and N in the heteroaryl moiety and 2 to 10 carbon atoms in the alkanoyl moiety and which is unsubstituted or substituted in the heteroaryl moiety by 1 to 3 substituents selected from the group consisting of halogen, cyano, trifluoromethane-sulphonyloxy, (C1-C3) alkyl, and (C1-C3) alkoxy, which latter may be in turn be substituted by 1 to 3 halogen atoms; and R3 is selected from the group consisting of methyl and propyl.