Claims for Patent: 9,931,403

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 Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,931,403
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.