Organic acid addition salts of morphine alkaloids and use as transdermal or transmucosal agents

摘要

Transdermal or transmucosal composition for administering morphine alkaloids of formula (I), wherein: R1 is H or a C1-C6 alkyl residue; R2 is H, OH, OC(O)CH3, whereby in this case the fourth valence of the (6) -C atom is occupied by H, or the dyad residues =O, =CH2; R3 is -CH3, cyclopropyl, cyclobutyl or allyl The bond at C7/C8 may be saturated, or a N oxide group may be present at N17 The composition contains the morphine alkaloid as an acid addition salt of an organic acid which is selected from: -monoesters of C3-C16-dicarboxylic acids with monohydric C1-C4-alcohols, -C2-C6 and C8-C16-sulfonic acids, -halogen, p- or m- hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl and/or alkoxy-substituted benzoic acids, which may optionally be alkylated at the N atom, -substituted or non-substituted 5-ring or 6-ring heterocycles comprising at least one N or S atom and having a carboxyl group function, -saturated or unsaturated, optionally substituted, oxocarboxylic acids having 5 to 10 carbon atoms, -phenoxy-substituted saturated C2-C4-carboxylic acids. -aliphatic, aromatic or heterocyclic C2-C12-amino acids, wherein one amino group is substituted with an optionally substituted -benzoyl group The acid addition salt possesses penetration behaviour with a flux of at least 2.34mg.cm2.h. The compositions described above are useful for formulating preparations for pain control or for withdrawal therapy of drug addicts.