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Last Updated: May 8, 2024

Claims for Patent: 11,278,623


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Summary for Patent: 11,278,623
Title:Non-aqueous patch
Abstract: Non-aqueous patches comprising lidocaine, which is not dissolved and is present in a crystalline state, have poor permeability to the skin. Therefore, non-aqueous patches have a high concentration of lidocaine. It is pointed out that lidocaine has an adverse effect on the heart. Prolonged use of a high concentration of lidocaine causes side effects, such as shock, rubor, and irritating sensation. External preparations comprising more than 5 mass % of lidocaine are designated as powerful drugs, and cannot be used as household (nonprescription) medicine. Provided is a non-aqueous patch that is effective to relieve muscle pain, the non-aqueous patch comprising lidocaine and/or its reactant, and a dissolving agent composed of an organic acid and a polyalcohol, which are contained in a base.
Inventor(s): Mori; Tatsuya (Saga, JP), Saida; Naoyuki (Saga, JP)
Assignee: ITOCHU CHEMICAL FRONTIER Corporation (Tokyo, JP) OISHI KOSEIDO CO., LTD. (Saga, JP)
Application Number:16/941,429
Patent Claims: 1. A method of treating pain in an individual in need thereof, comprising applying a non-aqueous patch to the skin of the individual in need thereof, wherein the non-aqueous patch comprises a plaster comprising lidocaine, a dissolving agent, and an elastomer, wherein, the plaster comprises 0.5 to 7 mass % lidocaine and 1.435 to 9.1 mass % dissolving agent, the dissolving agent comprises dipropylene glycol and isostearic acid, and the isostearic acid is present in the plaster in an amount of 1.4 to 2.1 mass %.

2. The method of claim 1, wherein the elastomer consists of polyisobutylene and styrene isoprene rubber.

3. The method of claim 1, wherein the plaster comprises 10 mass % to 40 mass % of the elastomer.

4. The method of claim 1, wherein the plaster comprises 20 mass % to 40 mass % of the elastomer.

5. The method of claim 1, wherein the plaster further comprises a terpene resin.

6. The method of claim 1, wherein after application to a human for 12 hours, the amount of lidocaine remaining in the non-aqueous patch is 80% or less than the amount prior to application.

7. The method of claim 1, wherein the amount of lidocaine is 196 mg or less.

8. The method of claim 1, wherein the amount of lidocaine is 0.1 to 1 mg/cm.sup.2 of the plaster.

9. The method of claim 1, wherein the lidocaine is completely dissolved in the dissolving agent.

10. The method of claim 1, wherein the lidocaine is completely dissolved in the plaster.

11. The method of claim 1, wherein the mass of the plaster is from about 60 to 200 g/m.sup.2.

12. The method of claim 1, wherein the mass of the plaster is from 80 to 180 g/m.sup.2.

13. The method of claim 1, wherein the non-aqueous patch further comprises a tackifier resin selected from the group consisting of terpene resin, rosin-based resin, alicyclic petroleum resin, phenolic resin and combinations thereof.

14. The method of claim 1, wherein the non-aqueous patch further comprises liquid paraffin.

15. The method of claim 1, wherein the plaster is held by a substrate selected from the group consisting of nonwoven fabric, woven fabric, knitted fabric or a combination thereof.

16. The method of claim 1, wherein the plaster is adhered to a polyester woven fabric.

17. The method of claim 1, wherein the pain is post-herpetic neuralgia.

18. The method of claim 1, wherein the non-aqueous patch is applied to the individual in need thereof for up to and including 12 hours.

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