External preparation for application to the skin containing lidocaine

• US 5,827,529 A
• Filed: 06/10/1994
• Issued: 10/27/1998
• Est. Priority Date: 03/30/1991
• Status: Expired due to Term

• Current Assignee: Teikoku Seiyaku Kabushiki Kaisha
• Original Assignee: Teikoku Seiyaku Kabushiki Kaisha
• Inventors: Ono, Masahiro, Akazawa, Mitsuji, Seki, Michiko, Iwamoto, Kiyomi, Konishi, Ryoji
• Primary Examiner(s): LANE, SALLY GARDNER
• Application Number:
  US08/258,378
• Time in Patent Office: 1,600 Days
• Field of Search: 424/401, 424/78.02, 424/448, 424/485-489, 424/449, 514/817, 514/944
• US Class Current: 424/448
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• 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 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61K 9/7076 the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

An external preparation for application to the skin containing lidocaine which comprises a drug-retaining layer placed on a support, wherein said drug-retaining layer comprises an adhesive gel base and 1 to 10% by weight of lidocaine, said base comprising a water-soluble high molecular weight substance, water and a water-retaining agent, which can release the active lidocaine gradually and constantly so that lidocaine is transdermally absorbed for a long period of time.

Claims

1. An external preparation for application to the skin containing lidocaine which comprises a drug-retaining layer placed on a support, wherein said drug-retaining layer comprises an adhesive gel base and 1 to 10% by weight of lidocaine, said base consisting essentially of 0.5 to 50% by weight of a water-soluble high molecular weight substance selected from the group consisting of gelatin, starch, agar, mannan, alginic acid, polyacrylic acid, a salt of polyacrylic acid, dextrin, methylcellulose, methylcellulose sodium, carboxymethylcellulose, carboxymethylcellulose sodium, polyvinyl alcohol, polyvinyl pyrrolidone, copolymer of methyl vinyl ether and maleic anhydride, gum arabic, tragacanth, karaya gum and locust bean gum, 30 to 70% by weight of water and 1 to 70% by weight of a water-retaining agent selected from the group consisting of ethylene glycol, diethylene glycol, polyethylene glycol, glycerin, sorbitol, martitol, propylene glycol and 1,3-butylene glycol, said lidocaine being dissolved in the base so as to result in a uniform base material.

2. The external preparation of claim 1 wherein said adhesive gel base is capable of controlling the release of drug and has a pH value of 5 to 9.

3. The external preparation of claim 1 wherein the water content of said adhesive gel base is 20 to 50% by weight.

4. The external preparation according to claim 1, wherein said adhesive gel base consists essentially of 0.5 to 50% by weight of a water-soluble high molecular weight substance selected from the group consisting of gelatin, starch, agar, mannan, alginic acid, polyacrylic acid, a salt of polyacrylic acid, dextrin, methylcellulose, methylcellulose sodium, carboxymethylcellulose, carboxymethylcellulose sodium, polyvinyl alcohol, polyvinyl pyrrolidone, copolymer of methyl vinyl ether and maleic anhydride, gum arabic, tragacanth, karaya gum and locust bean gum, 30 to 70% by weight of water and 1 to 70% by weight of a water-retaining agent selected from the group consisting of ethylene glycol, diethylene glycol, polyethylene glycol, glycerin, sorbitol, martitol, propylene glycol and 1,3-butylene glycol;

an absorbing agent and a surfactant, said lidocaine being dissolved in the base so as to result in a uniform base material.

5. The external preparation of claim 4 wherein said absorbing agent is selected from the group consisting of salicylic acid, hyaluronic acid, oleic acid, N,N-diethyl-m-toluamide, n-butyl stearate, benzyl alcohol, isopropyl myristate, isopropyl palmitate, polypropylene glycol, crotamiton, diethyl sebacate, N-methylpyrrolidone, N-ethylpyrrolidone and lauryl alcohol, and said surfactant is selected from the group consisting of polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, sorbitan monooleate and sorbitan monopalmitate.

6. The composition according to claim 1, wherein said water is present in an amount of 34.55% to 70% by weight.