Iontophoretic devices
Iontophoretic devices for the delivery of N-phenyl-N-(4-piperidinyl)amide esters are provided. The N-phenyl-N-(4-piperidinyl)amide esters are compounds of the 1. A reservoir comprising a matrix material and, distributed in said matrix material, a pharmaceutically acceptable amount of at least one compound selected from compounds of the formula (I) wherein: X is a member selected from the group consisting of alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxy-carbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl, and mono-, di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl, and lower alkoxy-lower alkyl,; R 1 is a member selected from the group consisting of hydrogen, lower alkoxy-carbonyl; and R 2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof, and the acid addition salts, of said compounds and isomers.
1. An iontophoretic device comprising:
(a) a donor reservoir comprising a matrix material and, distributed in said matrix material, a pharmaceutically acceptable amount of at least one compound selected from compounds of the formula (I)
wherein:
X is a member selected from the group consisting of: alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxy-carbonyl-lower alkyl;
Ar is a member selected from the group consisting of phenyl, and mono-, di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl;
R is a member selected from the group consisting of lower alkyl, OCH 3 and lower alkoxy-lower alkyl;
R 1 is a member selected from the group consisting of hydrogen, and lower alkoxy-carbonyl; and
R 2 is a member selected from the group consisting of hydrogen and methyl, and the optically active and cis-trans isomers thereof, and the acid addition salts of said compounds and isomers;
(b) a current distributing member in electrical communication with the donor reservoir;
(c) an indifferent electrode; and
(d) an electrical power source in electrical connection with the current distributing member and the indifferent electrode.
2. The iontophoretic device of claim 1 wherein X is alkoxy-carbonyl-lower alkyl.
3. The iontophoretic device of claim 1 wherein the at least one compound is the hydrochloride salt of the compound of formula (I) wherein X is CH 2 CH 2 COOCH 3 , R is OCH 3 , R 1 and R 2 are both hydrogen, and Ar is phenyl.
4. The iontophoretic device of claim 1 wherein the matrix material is a polymer gel.
5. The iontophoretic device of claim 1 wherein the matrix material is crosslinked polyvinylpyrrolidone.
6. A method for preparing an iontophoretic reservoir comprising:
distributing in a matrix material an effective amount of at least one compound of the formula (I)
wherein:
X is a member selected from the group consisting of: alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxy-carbonyl-lower alkyl;
Ar is a member selected from the group consisting of phenyl, and mono-, di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl;
R is a member selected from the group consisting of lower alkyl, OCH 3 and lower alkoxy-lower alkyl;
R 1 is a member selected from the group consisting of hydrogen, and lower alkoxy-carbonyl; and
R 2 is a member selected from the group consisting of hydrogen and methyl, and the optically active and cis-trans isomers thereof, and the acid addition salts of said compounds and isomers.
7. The method of claim 6 wherein X is alkoxy-carbonyl-lower alkyl.
8. The method of claim 6 wherein the at least one compound is the hydrochloride salt of the compound of formula (I) wherein X is CH 2 CH 2 COOCH 3 , R is OCH 3 , R 1 and R 2 are both hydrogen, and Ar is phenyl.
9. The method of claim 6 wherein the matrix material is a polymer gel.
10. The method of claim 6 wherein the matrix material is crosslinked polyvinylpyrrolidone.
11. The method of claim 6 , wherein the at least one compound is distributed in the matrix in an amount of from 0.01 milligrams to 1000 milligrams.