Method of treating neuropathic pain

• US 9,012,477 B2
• Filed: 01/05/2010
• Issued: 04/21/2015
• Est. Priority Date: 01/06/2009
• Status: Active Grant

• Current Assignee: Crescita Therapeutics Inc.
• Original Assignee: Nuvo Research AG (Searchlight Pharma, Inc.)
• Inventors: Zhang, Jie, Lippert, Robert
• Primary Examiner(s): RAO, SAVITHA M
• Application Number:
  US12/652,502
• Publication Number:
  US 20110015229A1
• Time in Patent Office: 1,932 Days
• Field of Search: 514/330, 514/535, 514/636
• US Class Current: 514/330
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/24 having an amino or nitro group
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/7015 Drug-containing film-forming compositions, e.g. spray-on
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

A method for treating subjects experiencing neuropathic pain is provided. The method involves the application of a solid-forming local anesthetic formulation to a skin surface of the subject experiencing the neuropathic pain and then maintaining the formulation on the skin surface for a period of time sufficient to allow itself to transdermally deliver the local anesthetic to the subject thereby providing relief from the neuropathic pain within about 45 minutes.

Claims

1. A method of treating neuropathic pain in a subject, comprising:

applying a layer of a solid-forming local anesthetic formulation to a skin surface of a human experiencing neuropathic pain, said solid-forming local anesthetic formulation comprising a local anesthetic agent, water, and at least one polymer selected from the group consisting of polyvinyl alcohol, polyvinylpyrrolidone, ethylcellulose, or combinations thereof, and being in the state of a semi-solid before being applied to said skin surface; and

maintaining said layer of said formulation on said skin surface for a period of time sufficient to allow said layer of said formulation to transdermally deliver the local anesthetic to the subject and to form a layer of a coherent soft solid after a sufficient amount of water is evaporated from said layer of said formulation,

wherein the solid-forming local anesthetic formulation is formulated to deliver the local anesthetic agent to the subject until substantially all of the water present in the formulation has evaporated and delivery of the local anesthetic stops or slows significantly so as to have no therapeutic effect thereafter, and wherein the solid-forming local anesthetic formulation provides relief from said neuropathic pain within about 45 minutes after application to the skin surface.

2. The method of claim 1, wherein the solid-forming local anesthetic formulation is maintained on the skin surface of the subject for a period of time of about 30 minutes to 2 hours.

3. The method of claim 1, wherein the skin surface is directly over the neuropathic pain.

4. The method of claim 1, wherein the method further comprises the step of removing the solid-forming local anesthetic formulation after it forms said layer of coherent soft solid by peeling a coherent soft solid from the skin at from 20 to 120 minutes after application.

5. The method of claim 1, wherein the solid-forming local anesthetic formulation is applied to said skin surface as a layer with a thickness from 0.1 to 3.0 millimeters.

6. The method of claim 1, wherein the solid-forming local anesthetic formulation is applied to said skin surface as a layer with a thickness from 0.2 to 1.5 millimeters.

7. The method of claim 1, wherein said local anesthetic agent includes tetracaine.

8. The method of claim 7, wherein the tetracaine comprises 6 wt % to 8 wt % of the solid-forming local anesthetic formulation before said formulation is applied to said skin surface.

9. The method of claim 1, wherein said local anesthetic agent includes lidocaine.

10. The method of claim 9, wherein the lidocaine comprises 6 wt % to 8 wt % of the solid-forming local anesthetic formulation before said formulation is applied to said skin surface.

11. The method of claim 1, wherein said local anesthetic agent is a eutectic mixture of lidocaine and tetracaine.

12. The method of claim 1, wherein the local anesthetic agent is selected from the group consisting of lidocaine, tetracaine, prilocaine, ropivacaine, bupivacaine, and mixtures thereof.

13. The method of claim 1, wherein the local anesthetic is in base form.

14. The method of claim 1, wherein the solid-forming local anesthetic formulation is formulated to provide relief from said neuropathic pain within about 30 minutes after application to the skin surface.

15. The method of claim 1, wherein the solid-forming local anesthetic formulation is formulated to provide pain relief for at least 9 hours after an application time of at least 45 minutes.

16. The method of claim 1, wherein the solid-forming local anesthetic formulation includes at least about 15 wt % water before being applied to said skin surface.

17. The method of claim 1, wherein the solid-forming local anesthetic formulation includes at least about 22 wt % water before being applied to said skin surface.

18. The method of claim 1, wherein the solid-forming local anesthetic formulation includes at least about 50 wt % water before being applied to said skin surface.

19. The method of claim 1, wherein the polymer includes polyvinyl alcohol.