Polyamine enhanced formulations for triptan compound iontophoresis
View Patent ↗A patch and compositions for iontophoresis of triptan compounds are described.
1. A method of treating a subject in need thereof, comprising:
administering an effective amount of a triptan compound to a subject using an iontophoretic transdermal patch, wherein the patch comprises an anode reservoir and a cathode reservoir, wherein the anode reservoir comprises a polyamine hydrogel formed from a polyamine salt of a polyacrylate copolymer and an organic acid, and a gel forming amount of water;
wherein the organic acid is a fatty acid, or a dicarboxylic acid, or a combination of both;
wherein the polyamine hydrogel further comprises:
about 3% to about 20% of a triptan compound in intimate mixture with the hydrogel; and
optionally one or more additives,
wherein the effective amount of the triptan compound is delivered to the subject within about one hour at an initial current between about 4 mA and about 5 mA without causing significant erythema.
2. The method of claim 1 , wherein said effective amount is effective to treat a triptan compound responsive state.
3. The method of claim 2 , wherein said triptan compound responsive state is a migraine.
4. The method of claim 1 , wherein the hydrogel comprises at least about 80% water and about 3.0% to about 5.0% triptan compound.
5. The method of claim 1 , wherein the hydrogel comprises between about 3% and about 10% polyamine salt.
6. The method of claim 1 , wherein the hydrogel comprises between about 10% and about 18% polya mine salt.
7. The method of claim 1 , wherein the polyamine salt is a salt of a methacrylate copolymer.
8. The method of claim 1 , wherein the methacrylate co-polymer is an alkylated methacrylate copolymer.
9. The method of claim 1 , wherein the hydrogel comprises about 0.01% to about 1.0% antimicrobial agent.
10. The method of claim 1 , wherein the organic acid comprises lauric acid, which is present in an amount between about 0.5% and about 7.0% .
11. The method of claim 1 , wherein the organic acid comprises adipic acid, which is present in an amount between about 0.1% and about 2.0%.
12. The method of claim 1 , wherein the triptan compound is almotriptan, frovatriptan, eletriptan, zolmitriptan, rizatriptan, sumatriptan, naratriptan, or a pharmaceutically acceptable salt thereof.
13. The method of claim 1 , wherein the triptan compound is sumatriptan or a salt thereof.
14. The method of claim 1 , wherein the triptan compound is sumatriptan succinate or sumatriptan hydrochloride.
15. The method of claim 1 , wherein the patch is capable of administering an effective amount of the triptan compound without substantially affecting skin pH.
16. The method of claim 1 , wherein the patch is capable of administering an effective amount of the triptan compound without substantially affecting skin temperature.
17. The method of claim 1 , wherein the hydrogel has a pH of about 3 to about 8.
18. The method of claim 17 , wherein the hydrogel has a pH of about 5.5 to about 7.
19. The method of claim 18 , wherein the hydrogel has a pH of about 6.
20. The method of claim 1 , wherein the anode reservoir further comprises a solubility enhancer, a permeation enhancer, an antimicrobial agent or any combination thereof.
21. The method of claim 1 , wherein the patch comprises a battery which operates throughout use of the patch.
22. The method of claim 1 , wherein the patch delivers a desired concentration of the triptan compound in less than one hour.
23. The method of claim 1 , wherein the anode reservoir consists essentially of a polyamine hydrogel formed from:
a polyamine salt of a polyacrylate copolymer and adipic acid, and
a gel forming amount of water;
wherein the polyamine hydrogel further comprises:
between about 3% and about 10% of a triptan compound in intimate mixture with the hydrogel, and
between about 0.05% and about 0.75% methyl para-hydroxy benzoate.
24. The method of claim 1 , wherein the organic acid is a fatty acid, a dicarboxylic acid or a mixture thereof.
25. A method of treating a subject in need thereof, comprising administering an effective amount of sumatriptan or a salt thereof to a subject using an iontophoretic transdermal patch, wherein the patch comprises an anode reservoir and a cathode reservoir, wherein said anode reservoir comprises a polyamine hydrogel formed from:
an alkylated methacrylate copolymer,
at least about 80% water,
between about 1.0% and about 5.0% lauric acid, and
between about 0.05% and about 0.75% adipic acid; and
wherein the polyamine hydrogel further comprises:
between about 3% and about 10% sumatriptan or salt thereof in intimate mixture with the hydrogel, and
between about 0.02% and about 0.5% methyl para-hydroxy benzoate; and
wherein the effective amount of the triptan compound is delivered to the subject within about one hour at an initial current between about 4 mA and about 5 mA without causing significant erythema.
26. The method of claim 25 , wherein sumatriptan or a salt thereof is sumatriptan succinate.
27. A method of treating a subject in need thereof, comprising administering an effective amount of sumatriptan succinate to a subject using an iontophoretic transdermal patch, wherein said patch comprises an anode reservoir and a cathode reservoir, wherein said anode reservoir comprises a polyamine hydrogel formed from:
approximately 84% to about 88% water;
approximately 4.0% to about 7.0% alkylated methacrylate co-polymer;
approximately 1.0% to about 5.0% lauric acid; and
approximately 0.05% to about 0.75% adipic acid;
wherein the polyamine hydrogel further comprises:
approximately 3.0% to about 5.0% sumatriptan succinate in intimate mixture with the hydrogel, and
approximately 0.05% to about 0.75% methyl para-hydroxy benzoate; and wherein the effective amount of the triptan compound is delivered to the subject within about one hour at an initial current between about 4 mA and about 5 mA without causing significant erythema.