Topical anesthetic for rapid local anesthesia and method of applying a topical anesthetic

• US 20090048347A1
• Filed: 07/16/2008
• Published: 02/19/2009
• Est. Priority Date: 01/16/2007
• Status: Active Grant

• Current Assignee: Juventio, LLC
• Original Assignee: DermWorx Incorporated
• Inventors: Cooper, Eugene R., Cohen, David M.
• Granted Patent: US 9,283,177 B2
• Time in Patent Office: Days
• US Class Current: 514/626
• CPC Class Codes: A61K 31/164 of a carboxylic acid with an aminoalcohol, e.g. ceramides
• 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 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• 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: A61P 23/02 Local anaesthetics

Abstract

The invention relates to a drug delivery system for the topical administration of anesthetic agents. For example, a topical anesthetic for rapid local anesthesia is provided. The topical anesthetic includes an anesthetic, volatile and non-volatile solvents, and an optional thickener. In addition, a method is taught for applying the topical anesthetic to the face of a patient without occlusion. The anesthetic is applied topically to an area for injection such that the dermatological procedure (cosmetic injections) can be performed in fifteen minutes.

Claims

1. A drug delivery system for topical administration of a local anesthetic agent comprising a local anesthetic agent, an alkane diol, a C₈-C₃₄ fatty acid or corresponding alcohol or ester having a melting point below 40°

C., and a volatile component, wherein the local anesthetic agent is present in an amount such that upon topical application to a surface, evaporation of the volatile component occurs such that the remaining solution is near saturation, at saturation, or above saturation with the local anesthetic agent at the temperature of the surface.

2. The drug delivery system of claim 1, wherein the local anesthetic agent comprises lidocaine.

3. The drug delivery system of claim 1, wherein the local anesthetic agent comprises between 0.001 and 20 percent by weight of the drug delivery system.

4. The drug delivery system of claim 1, wherein the local anesthetic agent comprises less than four percent by weight of the drug delivery system.

5. The drug delivery system of claim 1, wherein the alkane diol is selected from propylene glycol or a butane diol with adjacent hydroxyl groups.

6. The drug delivery system of claim 5, wherein the alkane diol comprises propylene glycol.

7. The drug delivery system of claim 1, wherein the alkane diol comprises between two and 35 percent by weight of the drug delivery system.

8. The drug delivery system of claim 1, wherein the C₈-C₃₄ fatty acid or corresponding alcohol or ester having a melting point below 40°

C. is selected from oleyl alcohol, oleic acid, ester derivatives of oleic acid, a C₁₀ to C₁₄ saturated alcohol or corresponding acid or ester which is a liquid at room temperature, or a C₁₂ to C₂₂ mono- or poly-unsaturated or branched chain alcohol or corresponding acid or ester which is a liquid at room temperature.

9. The drug delivery system of claim 1, wherein the C₈-C₃₄ fatty acid or corresponding alcohol or ester having a melting point below 40°

C. comprises between two and 30 percent by weight of the drug delivery system.

10. The drug delivery system of claim 1, wherein the C₈-C₃₄ fatty acid or corresponding alcohol or ester having a melting point below 40°

C. comprises oleic acid or oleyl alcohol.

11. The drug delivery system of claim 1, wherein the volatile component comprises between 60 and 95 percent by weight of the drug delivery system.

12. The drug delivery system of claim 1, wherein the volatile component comprises one or more short-chain alcohols, volatile silicones, or combinations thereof.

13. The drug delivery system of claim 1, wherein the volatile component comprises ethanol, isopropanol, hexamethyldisiloxane, or a combination thereof.

14. The drug delivery system of claim 1, further comprising a thickener.

15. The drug delivery system of claim 14, wherein the thickener comprises between 0.1 and 3.5 percent by weight of the drug delivery system.

16. The drug delivery system of claim 14, wherein the thickener comprises hydroxypropylcellulose.

18. A method for providing a topical anesthetic effect in an animal, comprising administering to a dermal surface of an animal in need of such treatment a therapeutically effective amount of the drug delivery system of claim 1.

19. The method of claim 18, wherein the animal is a human.

20. A method of applying the drug delivery system of claim 1, comprising applying the drug delivery system to an injection site on skin of a patient.

21. The method of claim 20, further comprising the step of waiting at least fifteen minutes.

22. The method of claim 21, further comprising the step of injecting the patient on the injection site after the waiting step.

23. The method of claim 22, wherein the step of injecting the patient on the injection site occurs no more than about twenty minutes after the applying step.

24. The method of claim 20, wherein the injection site is on a face of the patient.

25. The method of claim 20, wherein the injection site is the site of insertion of an intravenous needle or the site of a needle stick for an IM injection, an innoculation, or a blood drawing.

26. A method of applying the drug delivery system of claim 1, comprising applying the drug delivery system to skin of a patient prior to a dermatological procedure.

27. The method of claim 26, wherein the dermatological procedure is a cosmetic injection, circumcision, a skin biopsy, removal of a pre-cancerous lesion, removal of a wart, removal of a mole, laser hair removal, laser skin resurfacing, or other cutaneous laser procedures.

17. A drug delivery system for topical administration of a local anesthetic agent comprising 4% by weight lidocaine, 4% by weight propylene glycol, 4% by weight oleyl alcohol, 3% by weight hydroxypropylcellulose, 17% by weight polydimethysiloxane, and 68% by weight isopropyl alcohol.