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Last Updated: April 17, 2024

Claims for Patent: 9,925,264


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Summary for Patent: 9,925,264
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:15/065,075
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,925,264
Patent Claims: 1. A method of treating pain in a human comprising applying a non-aqueous patch to the human the non-aqueous patch comprising 0.5 to 7 mass % lidocaine, and a dissolving agent consisting essentially of an organic acid and a polyalcohol, which are contained in a plaster, wherein the amount of lidocaine is 0.1 to 1 mg/cm.sup.2 of the plaster, and wherein the proportion of dissolving agent to lidocaine is 0.5 to 5 mass % of dissolving agent relative to 1 mass % of lidocaine.

2. The method of claim 1, wherein the organic acid is isostearic acid.

3. The method of claim 1, wherein the polyalcohol is dipropylene glycol.

4. The method of claim 1, wherein the dissolving agent consists of isostearic acid and dipropylene glycol.

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

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

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

8. The method of claim 7, wherein the mass of the plaster is from 80 to 180 g/m.sup.2.

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

10. The method of claim 1, wherein the non-aqueous patch further comprises an elastomer.

11. The method of claim 10, wherein the elastomer consists of polyisobutylene and styrene isoprene rubber.

12. The method of claim 10, 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.

13. The method of claim 12, wherein the non-aqueous patch further comprises liquid paraffin.

14. 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.

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

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

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