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Last Updated: September 21, 2021

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Claims for Patent: 9,931,403


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Summary for Patent: 9,931,403
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:15/646,744
Patent Claims: 1. A 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/cm2 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 non-aqueous patch according to claim 1, wherein the organic acid is isostearic acid.

3. The non-aqueous patch according to claim 1, wherein the polyalcohol is dipropylene glycol.

4. The non-aqueous patch according to claim 1, wherein the dissolving agent consists essentially of isostearic acid and dipropylene glycol.

5. The non-aqueous patch according to claim 1 wherein the plaster is adhered to a polyester woven fabric.

6. The non-aqueous patch according to claim 1 wherein the lidocaine is completely dissolved in the dissolving agent.

7. The non-aqueous patch of claim 1, wherein the mass of the plaster is from about 60 to 200 g/m2.

8. The non-aqueous patch of claim 7 wherein the mass of the plaster is from 80 to 180 g/m2.

9. The non-aqueous patch according to claim 1 wherein the lidocaine is completely dissolved in the plaster.

10. The non-aqueous patch according to claim 1 further comprising an elastomer.

11. The non-aqueous patch according to claim 10, wherein the elastomer consists of polyisobutylene and styrene isoprene rubber.

12. The non-aqueous patch according to claim 11 further comprising a tackifier resin selected from the group consisting of terpene resin, rosin-based resin, alicyclic petroleum resin, phenolic resin and combinations thereof.

13. The non-aqueous patch according to claim 12, further comprising liquid paraffin.

14. The non-aqueous patch according to 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 non-aqueous patch according to claim 1, wherein the amount of lidocaine is 196 mg or less.

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Serving leading biopharmaceutical companies globally:

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