Transdermal aerosol compositions

• US 20050186141A1
• Filed: 12/22/2004
• Published: 08/25/2005
• Est. Priority Date: 06/25/2002
• Status: Abandoned Application

• Current Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Original Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Inventors: Wilkins, Nina Frances, Gonda, Igor, Morgan, Timothy Matthias
• Application Number:
  US11/019,121
• Publication Number:
  US 20050186141A1
• Time in Patent Office: Days
• US Class Current: 424/45
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015

Abstract

The present invention provides a pharmaceutical composition for transdermal delivery comprising: one or more physiologically active agents; one or more dermal penetration enhancers; a pharmaceutically acceptable carrier comprising a volatile solvent; and a hydrofluorocarbon propellent; wherein the carrier and penetration enhancers combine to provide a single-phase solution of the one or more physiologically active agents.

Claims

1. A pharmaceutical composition for transdermal delivery comprising;

one or more physiologically active agents;

one or more dermal penetration enhancers;

a pharmaceutically acceptable carrier comprising a volatile solvent; and

a propellent comprising HFC-134a;

wherein the carrier, propellant and penetration enhancer are combined to provide a single-phase solution of the one or more physiologically active agents.

2. A pharmaceutical composition according to claim 1 wherein the volatile solvent has a vapour pressure above 35 mmHg at atmospheric pressure and a temperature of 32°

C.

3. A composition according to claim 1 substantially free of adhesives for forming a film on the skin.

4. A composition according to claim 1 wherein said composition maintains a drying time of less than 2 minutes, more preferably less than 1 minute.

6. A composition according to claim 4 wherein said propellent consists essentially of HFC-134a.

7. A pharmaceutical composition according to claim 1 wherein the propellant is from 15% to 50% by volume of the total pharmaceutical composition.

8. A pharmaceutical composition according to claim 7 wherein the propellant is from 20 to 40% by volume of the composition.

9. A pharmaceutical composition according to claim 1 wherein the penetration enhancer comprises one or more sunscreen esters.

11. A pharmaceutical composition according to claim 9 wherein the one or more sunscreen esters is selected from the group consisting of C₈ to C₁₈ alkylcinnamate, C₈ to C₁₈ alkylmethoxycinnamate, C₈ to C₁₈ alkyl salicylate and mixtures thereof.

12. A pharmaceutical composition according to claim 11 wherein the penetration enhancer is octyl salicylate or padimate-o.

14. A pharmaceutical composition according to claim 9 wherein the composition comprises from 0.1% to 10% by weight of dermal penetration enhancer.

18. A pharmaceutical composition according to claim 1 wherein the solvent comprises ethanol, isopropanol or a mixture thereof, providing a single phase of penetration enhancer and propellent.

19. A pharmaceutical composition according to claim 1 wherein the volatile solvent comprises acetone, chloroform, lower alcohol or mixtures thereof and is present in from 40% to 80% by volume of the total pharmaceutical composition.

20. A pharmaceutical composition according to claim 1 wherein the volatile solvent comprises acetone, chloroform, a lower alcohol or mixtures thereof and is present in from 50% to 70% by volume of the total pharmaceutical composition.

21. A pharmaceutical composition according to claim 1 comprising one or more physiologically active agents selected from the group consisting of steroid, hormone derivative, non-steroidal anti-inflammatory drug, opioid analgesic, antinauseant, antioestrogen, aromatase inhibitor, 5-alpha reductase inhibitor, anxiolytic, prostaglandin, anti-viral drug, anti-migraine compound, antihypertensive agent, anti-malarial compound, bronchodilator anti-depressant, anti-Alzheimer'"'"'s agent, anticholinergic agent, neuroleptic and antipsychotic agent, anti-Parkinson'"'"'s agent, antiandrogen and anoretic agent.

22. A pharmaceutical composition according to claim 21 wherein the one or more physiologically acceptable agents is selected from the group consisting of testosterone, oestradiol, ethinyloestradiol, levonorgestrel, progesterone, norethisterone acetate, ibuprofen, ketoprofen, flurbiprofen, naproxen, diclofenac, fentanyl, buprenorphjne, scopolamine, prochlorperazine, metochlopramide, ondansetron, tamoxifen, epitiostanol, exemestane, darifenacin, 4-hydroxyandrostenedione and it'"'"'s derivatives, finasteride, dutasteride, turosteride, LY191704, MK-386, alprazolam, alprostadil, prostacyclin and it'"'"'s derivatives, melatonin, n-docosanol, tromantadine, lipophilic pro-drugs of acyclovir, low molecular weight heparin, enoxaparin, sumatriptan, amlodipine, nitrendipine, primaquine, minoxidiland it'"'"'s pro-drugs, pilocarpine, salbutamol, terbutaline, sameterol, ibogaine, bupropian, rolipram, tacrine, fluphenazine, haloperidol, N-0923, cyproterone acetate, MENT (7-methyl-19-testosterone), or mazindol or a pharmaceutically acceptable salt or derivative of any one of the aforementioned. More preferably, the physiological agents include apomorphine, oxybutynin, fentanyl, ropinirole, granisetron, rivastigmine, buspirone, rizatriptin, zolmitriptan, lacidipine, tropisetron, olanzapine and methyl phenidate or a pharmaceutically acceptable salt or derivative of any one of the aforementioned.

23. A pharmaceutical composition according to claim 1 wherein the composition is contained in a chamber of a spray applicator device comprising a valve for delivering the composition from the chamber, a nozzle for dispersing the composition as an aerosol and means for providing a metered dose of aerosol from the nozzle said composition being retained under pressure within the chamber so as to maintain said propellent in a liquid form.

5. (canceled)

10. (canceled)

13. (canceled)

15. (canceled)

16. (canceled)

17. (canceled)

24. (canceled)

25. A method of transdermal delivery of a physiologically active agent to a subject forming a composition of the physiologically active agent comprising a dermal penetration enhancer and pharmaceutically acceptable carrier comprising a volatile solvent and HFC-134a propellant to provide a single phase solution under pressure;

applying the composition as an aerosol to the skin of the subject.