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Details for Patent: 6,929,801

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Details for Patent: 6,929,801

Title: Transdermal delivery of antiparkinson agents
Abstract:The present invention provides a transdermal drug delivery system which comprises: a therapeutically effective amount of an antiParkinson agent; at least one dermal penetration enhancer, which is a safe skin-tolerant ester sunscreen ester; and at least one volatile liquid. The invention also provides a method for administering at least one systemic acting antiParkinson agent to an animal which comprises applying an effective amount of the antiParkinson agent in the form of the drug delivery system of the present invention.
Inventor(s): Klose; Kathryn Traci-Jane (Chelsea, AU), Tran; Ngan Thi Kim (East Keilor, AU), Morgon; Timothy Matthias (Carlton North, AU), Finnin; Barrie Charles (Glen Iris, AU), Reed; Barry Leonard (Strathmore, AU)
Assignee: Acrux DDS PTY LTD (Victoria, AU)
Filing Date:May 02, 2003
Application Number:10/428,016
Claims:1. A transdermal drug delivery system comprising: (a) a therapeutically effective amount of an antiParkinson agent; (b) at least one dermal penetration enhancer, which is a safe skin-tolerant ester sunscreen of formula (I): ##STR2## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, halide, hydroxy or NR.sup.3 R.sup.4 ; R.sup.2 is a C.sub.8 to C.sub.18 alkyl; R.sup.3 and R.sup.4 are each independently hydrogen, lower alkyl or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a 5- or 6-membered heterocyclic ring; n is 0 or 1, and q is 1 or 2, wherein, when n is 0 and R.sup.1 is NR.sup.3 R.sup.4, then NR.sup.3 R.sup.4 is para-substituted, and wherein said dermal penetration enhancer is present in an amount of from about 10 to about 10,000 wt % based on the weight of the antiParkinson agent; and (c) at least one volatile liquid.

2. The transdermal drug delivery system according to claim 1, wherein the dermal penetration enhancer is octyl salicylate.

3. The transdermal drug delivery system according to claim 1, wherein the volatile liquid selected from the group consisting of ethanol, isopropanol, and a mixture thereof.

4. The transdermal drug delivery system according to claim 1, comprising on a weight basis: (a) from about 1 to about 7% of said antiParkinson agent; (b) from about 1 to about 10% of said at least one dermal penetration enhancer; and (c) from about 83 to about 98% of said volatile liquid.

5. The transdermal drug delivery system according to claim 1, wherein the antiParkinson agent is selected from the group consisting of bornaprine, budipine, entacapone, ethopropazine, lazabemide, memantine, selegiline, tolcapone, trihexyphenidyl, modafinil, talampanel, altinicline, brasofensine, safinamide, droxidopa, rasagline mesylate, cabergoline, pergolide, piribedil, pramipexole, quinagolide, terguride, rotigotine, riluzole, talipexole, piroheptine, bifeprunox, spheramine, sumanirole, lisuride hydrogen maleateor, ropinirole, orphenadrine, and bromocriptine.

6. The transdermal drug delivery system according to claim 5, comprising on a weight basis: (a) from about 1 to about 7% ropinirole; (b) from about 1 to about 10% octyl salicylate; and (c) from about 83 to about 98% Alcohol USP (95% ethanol).

7. The transdermal drug delivery system according to claim 5, comprising on a weight basis: (a) from about 1 to about 5% ropinirole; (b) from about 1 to about 5% octyl salicylate; and (c) from about 45 to about 90% of said volatile liquid; (d) from about 5 to about 45% water; and (e) from about 0.5 to about 5% of a thickening agent.

8. The transdermal drug delivery system according to claim 1, wherein the antiParkinson agent is selected from the group consisting of amantadine, benserazide, carbidopa, levodopa, benztropine, biperiden, benzhexol, and procyclidine.

9. The transdermal drug delivery system according to claim 1, wherein the antiParkinson agent is S(-)-2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetralin (N-0923).

10. A method for administering at least one systemic acting antiParkinson agent to an animal which comprises applying an effective amount of the antiParkinson agent in the form of the drug delivery system according to claim 1.

11. The method according to claim 10, wherein the antiParkinson agent is selected from the group consisting of bornaprine, budipine, entacapone, ethopropazine, lazabemide, memantine, selegiline, tolcapone, trihexyphenidyl, modafinil, talampanel, altinicline, brasofensine, safinamide, droxidopa, rasagline mesylate, cabergoline, pergolide, piribedil, pramipexole, quinagolide, terguride, rotigotine, riluzole, talipexole, piroheptine, bifeprunox, spheramine, sumanirole, lisuride hydrogen maleateor, ropinirole, orphenadrine and bromocriptine.

12. The method according to claim 11, wherein the antiParkinson agent is ropinirole.

13. The method according to claim 10, wherein the antiParkinson agent is selected from the group consisting of amantadine, benserazide, carbidopa, levodopa, benztropine, biperiden, benzhexol, and procyclidine.

14. The method according to claim 10, wherein the antiParkinson agent is S(-)-2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetralin (N-0923).

15. The method according to claim 10, wherein the drug delivery system is applied to the skin of the animal covering a delivery surface area between about 10 and 800 cm.sup.2.

16. The method according to claim 10, wherein the drug delivery system is applied to the skin of the animal covering a delivery surface area between about 10 and 400 cm.sup.2.

17. The method according to claim 10, wherein the drug delivery system is applied to the skin of the animal covering a delivery surface area between about 10 and 200 cm.sup.2.

18. The method according to claim 10, wherein the drug delivery system is applied using a fixed or variable metered dose applicator.
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