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Last Updated: March 28, 2024

Details for Patent: 6,964,777


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Title: Transdermal delivery of antianxiety agents
Abstract:The present invention provides a transdermal drug delivery system which comprises: a therapeutically effective amount of an antianxiety 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 antianxiety agent to an animal which comprises applying an effective amount of the antianxiety agent in the form of the drug delivery system of the present invention.
Inventor(s): Klose; Kathryn Traci-Jane (Chelsea, AU), La Guardia; Ennio (East Coburg, AU), Morgan; 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:10/428,017
Claims:1. A transdermal drug delivery system comprising: (a) a therapeutically effective amount of an antianxiety 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 hormone; 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 0.1 to about 10% of said antianxiety agent; (b) from about 0.1 to about 10% of said at least one dermal penetration enhancer; and (c) from about 80 to about 99.8% of said volatile liquid.

5. The transdermal drug delivery system according to claim 1, wherein the antianxiety agent is selected from the group consisting of azapirones, GABA receptor agonists, 5-HT 1A receptor antagonists and 5-HT 2A/2C antagonists, including salts and derivatives of the aforementioned antianxiety agents.

6. The transdermal drug delivery system according to claim 5, wherein the antianxiety agent is buspirone.

7. The transdermal drug delivery system according to claim 6, comprising on a weight basis: (a) from about 1 to about 6% buspirone; (b) from about 1 to about 10% octyl salicylate; and (c) from about 84 to about 98% Alcohol USP (95% ethanol).

8. The transdermal drug delivery system according to claim 6, comprising on a weight basis: (a) from about 1 to about 5% buspirone; (b) from about 1 to about 5% octyl salicylate; and (c) from about 45 to about 90% of a volatile liquid selected from the group consisting of ethanol, isopropanol, and a mixture thereof; (d) from about 5 to about 45% water; and (e) from about 0.5 to about 5% of a thickening agent.

9. The transdermal drug delivery system according to claim 5, wherein the antianxiety agent is selected from the group consisting of NGD-91-3, DU-125530 amd deramciclane.

10. The transdermal drug delivery system according to claim 1, wherein the antianxiety agent is a benzodiazepine.

11. The transdermal drug delivery system according to claim 10, wherein the benzodiazepine is triazolam.

12. The transdermal drug delivery system according to claim 1, wherein the antianxiety agent is alprazolam.

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

14. The method according to claim 13, wherein the antianxiety agent is selected from the group consisting of azapirones, GABA receptor agonists, 5-HT 1A receptor antagonists and 5-HT 2A/2C antagonists, including salts and derivatives of the aforementioned antianxiety agents.

15. The method according to claim 13, wherein the antianxiety agent is a benzodiazepine.

16. The method according to claim 13, wherein the antianxiety agent is alprazolam.

17. The method according to claim 13, 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.

18. The method according to claim 13, 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.

19. The method according to claim 13, 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.

20. The method according to claim 13, wherein the drug delivery system is applied using a fixed or variable metered dose applicator.

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