Solid-forming local anesthetic formulations for pain control

• US 9,693,976 B2
• Filed: 01/14/2011
• Issued: 07/04/2017
• 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
• Application Number:
  US13/006,780
• Publication Number:
  US 20120022158A1
• Time in Patent Office: 2,363 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 4 wt % to 10 wt % lidocaine,

from 4 wt % to 10 wt % tetracaine,

from 10 wt % to 18 wt % polyvinyl alcohol,

from 30 wt % to 50 wt % water,

from 2 wt % to 6 wt % of sorbitan monopalmitate or sorbitan monostearate,

from 18 wt % to 32.4 wt % dicalcium phosphate, and

from 2 wt % to 13 wt % petrolatum,

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.

6. The formulation of claim 1, wherein the dicalcium phosphate is present at from 18 wt % to 27 wt %.

8. The formulation of claim 1, wherein the formulation comprises sorbitan monopalmitate.

9. The formulation of claim 1, wherein the formulation comprises sorbitan monostearate.

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

11. 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.

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

1 weight ratio.

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

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

5. A solid-forming local anesthetic formulation, comprising:

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

from 10 wt % to 18 wt % polyvinyl alcohol,

from 30 wt % to 50 wt % water,

from 2 wt % to 13 wt % petrolatum,

from 18 wt % to 32.4 wt % dicalcium phosphate, and

from 2 wt % to 6 wt % sorbitan monostearate,

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

7. The formulation of claim 5, wherein the polyvinyl alcohol has an average mass from about 30,000 Daltons to about 80,000 Daltons.