Solid-forming local anesthetic formulations for pain control

• US 10,350,180 B2
• Filed: 06/05/2017
• Issued: 07/16/2019
• Est. Priority Date: 01/14/2010
• Status: Active Grant

• Current Assignee: Crescita Therapeutics Inc.
• Original Assignee: Crescita Therapeutics Inc.
• Inventors: Zhang, Jie
• Primary Examiner(s): Sznaidman, Marcos L
• Application Number:
  US15/613,695
• Publication Number:
  US 20180000757A1
• Time in Patent Office: 771 Days
• Field of Search: 514537
• 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 31/136 having the amino group directly attached to the aromatic ring, e.g. benzeneamine
• 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 47/32 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 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 23/02 Local anaesthetics

Abstract

Solid-forming local anesthetic formulations for pain control can include a lidocaine base and tetracaine base, polyvinyl alcohol, water, and an emulsifier. The formulation can be prepared to be in a semi-solid state prior to application to a skin surface, can form a soft solidified layer after application, and can provide pain relief when applied to a skin surface proximate a pain site.

Claims

1. A solid forming local anesthetic formulation, comprising:

from about 4 wt % to about 10 wt % lidocaine,

from about 4 wt % to about 10 wt % tetracaine,

from about 10 wt % to about 18 wt % polyvinyl alcohol,

from about 25.94 wt % to about 51.87 wt % water,

from about 2 wt % to about 6 wt % of an emulsifying agent selected from sorbitan monopalmitate or sorbitan monostearate,

from about 2 wt % to about 13 wt % petrolatum, and

from about 18 wt % to about 36 wt % dicalcium phosphate,

wherein the water to polyvinyl alcohol weight ratio (w/w) is greater than 2.4.

2. The formulation of claim 1, wherein the lidocaine and tetracaine are each in their base form.

3. The formulation of claim 2, wherein the lidocaine and tetracaine are in the form of a eutectic mixture.

4. The formulation of claim 1, wherein the polyvinyl alcohol has an average mass from about 30,000 Daltons to about 80,000 Daltons.

5. The formulation of claim 1, wherein the emulsifying agent is sorbitan monostearate.

6. The formulation of claim 1, wherein the water to polyvinyl alcohol ratio is greater than 2.5.

7. The formulation of claim 1, wherein the lidocaine and tetracaine is present as a eutectic mixture at a 2:

1 to 1;

2 weight ratio.

8. The formulation of claim 1, wherein the lidocaine and tetracaine is present as a eutectic mixture at about a 1:

1 weight ratio.

9. The formulation of claim 1, wherein the formulation comprises 7 wt % lidocaine and 7 wt % tetracaine.

10. The formulation of claim 1, wherein the formulation is for local anesthesia.

15. The formulation of claim 1, wherein the initial formulation is a cream, ointment, paste, viscous lotion, or gel prior to application to the skin surface.

16. The formulation of claim 1, wherein the polyvinyl alcohol has an average mass from about 20,000 Daltons to about 100,000 Daltons.

17. The formulation of claim 1, wherein the emulsifying agent is sorbitan monopalmitate.

18. The formulation of claim 1, wherein the formulation has an initial viscosity ranging from about 47,800 centipoises to about 828,500 centipoises.

11. A solid forming local anesthetic formulation, comprising:

from about 4 wt % to about 30 wt % of a eutectic mixture of lidocaine and tetracaine,

from about 10 wt % to about 18 wt % polyvinyl alcohol,

from about 25.94 wt % to about 51.87 wt % water,

from about 2 wt % to about 13 wt % petrolatum,

from about 2 wt % to about 6 wt % of an emulsifying agent selected from sorbitan monopalmitate or sorbitan monostearate, and

from about 18 wt % to about 36 wt % dicalcium phosphate,

wherein the water to polyvinyl alcohol weight ratio (w/w) is greater than 2.4.

12. The formulation of claim 11, wherein the water to polyvinyl alcohol ratio is greater than 2.5.

13. The formulation of claim 11, wherein the polyvinyl alcohol has an average mass from about 30,000 Daltons to about 80,000 Daltons.

14. The formulation of claim 11, wherein the formulation is for local anesthesia.

19. The formulation of claim 11, wherein the formulation has an initial viscosity ranging from about 47,800 centipoises to about 828,500 centipoises.