METHOD OF INDUCING TOPICAL ANESTHESIA AND TRANSDERMAL PATCH

• US 20090123527A1
• Filed: 01/15/2009
• Published: 05/14/2009
• Est. Priority Date: 07/24/2006
• Status: Abandoned Application

• Current Assignee: Akorn Incorporated (Akorn Holdings Topco LLC)
• Original Assignee: Akorn Incorporated (Akorn Holdings Topco LLC)
• Inventors: ALAM, ABU, Reichel, Elias, Busbee, Brandon
• Application Number:
  US12/354,422
• Publication Number:
  US 20090123527A1
• Time in Patent Office: Days
• US Class Current: 424/449
• 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 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system

Abstract

Disclosed is a method of inducing topical anesthesia in a tissue or organ of an animal comprising providing an aqueous gel formulation comprising water, an anesthetic (e.g., lidocaine hydrochloride), a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile and has low particulate count. Also disclosed are a transdermal patch comprising the aqueous gel formulation suitable for applying on the skin of a patient and a method of controlling pain therewith.

Claims

1. A method of inducing topical anesthesia in a tissue or organ of an animal comprising:

a) providing an aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier, wherein the anesthetic is present in an amount of 15 mg per ml to about 50 mg per ml of the formulation, and the gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile having less than about 100 particles of 50 microns particle size or more per ml of the aqueous gel formulation; and

b) topically administering an effective amount of the aqueous gel formulation to the tissue or organ of the animal;

whereby anesthesia is induced on the tissue or organ of the animal,

wherein the aqueous gel formulation is administered prior to, during, or subsequent to a procedure or treatment involving bronchoscopy, colonoscopy, gastro-intestinal procedure, intubation, cannulation, dentistry, dermatology, skin procedures, skin and wound debridement, hair removal, mucosal surfaces, ear, nose, throat, urology, gynecology, herpes, oral mucositis, canker sores, prostate surgery, Botox treatment, plastic surgery, facial surgery, punch biopsy, post-operative analgesia, circumcision, inflammation, neuropathic pain, abrasions, ulcerations, lesions, incisions, trauma, joint spaces, injection sites, venipuncture, vaccination, tooth ache, teething pain, ear piercing, or body orifices.

2. The method of claim 1, wherein the anesthetic is selected from the group consisting of lidocaine, bupivicaine, mepivicaine, proparacaine, and narcaine, and salts thereof.

3. The method of claim 2, wherein the anesthetic is lidocaine hydrochloride.

4. The method of claim 1, wherein the anesthetic is present in an amount of from 15 mg to 38 mg per ml and the aqueous gel formulation is suitable for administration to the eye.

5. The method of claim 1, wherein the viscoelastic polymer comprises a gelling agent.

6. The method of claim 5, wherein the gelling agent is hydroxypropylmethylcellulose.

7. The method of claim 1, wherein the aqueous gel formulation has a pH from about 5.0 to about 7.5.

8. The method of claim 1, wherein the aqueous gel formulation has a viscosity from about 2000 to about 10,000 cps at 25°

C.

9. The method of claim 1, wherein the tonicity modifier is sodium chloride.

12. The method of claim 3, wherein the lidocaine hydrochloride is present in an amount so as to provide a 1.5%, 2.5%, or 3.5% by weight of lidocaine in the aqueous gel formulation.

10-11. -11. (canceled)

13. (canceled)

14. A transdermal patch containing an aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier, wherein the anesthetic is present in an amount of 15 mg per ml to about 50 mg per ml of the formulation, and the gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile having less than about 100 particles of 50 microns particle size or more per ml of the aqueous gel formulation.

15. The transdermal patch of claim 14, which includes a backing layer, an adhesive, a release liner, and a membrane, wherein said membrane and said backing layer forming a drug reservoir containing the aqueous gel formulation.

16. The transdermal patch of claim 15, wherein the adhesive is disposed on the backing layer.

17. The transdermal patch of claim 14, wherein the anesthetic is selected from the group consisting of lidocaine, bupivicaine, mepivicaine, proparacaine, and narcaine, and salts thereof.

18. The transdermal patch of claim 14, wherein the anesthetic is lidocaine hydrochloride.

19. The transdermal patch of claim 14, wherein the anesthetic is present in an amount of from 15 mg to 38 mg per ml of the aqueous gel formulation.

23. The transdermal patch of claim 14, wherein the aqueous formulation has a viscosity from about 2000 to about 10,000 cps at 25°

C.

25. The transdermal patch of claim 18, wherein the lidocaine hydrochloride is present in an amount so as to provide a 1.5%, 2.5%, or 3.5% by weight of lidocaine in the aqueous gel formulation.

26. A method of controlling localized pain of a patient comprising applying to skin of the patient a transdermal patch of claim 14.

27. The method of claim 26, wherein the pain is due to arthritis, lower back or post-herpetic neuralgia.

20-22. -22. (canceled)

24. (canceled)