Self-adhesive device for the percutaneous administration of an active ingredient

Claim 2

A self-adhesive matrix for the percutaneous administering of a pharmaceutical active ingredient comprising a)30 to 50 parts by weight of an ethylene/vinyl acetate copolymer material, b) 20 to 45 parts by weight of a higher aliphatic monoalcohol compound, c) 5 to 20 parts by weight of a cellulose derivative material, d) 1 to 20 parts by weight of an ester compound of a polyhydric alcohol with a fatty aliphatic acid, and e) 0.1 to 20 parts by weight of an active ingredient which can be administered percutaneously.

Claim 3

A matrix according to claim 1 wherein the ethylene/vinyl acetate copolymer material has a content of vinyl acetate units of between 35 to 55% by weight, relative to the weight of said copolymer material.

Claim 4

A matrix according to claim 1 wherein the ethylene/vinyl acetate copolymer material has a content of vinyl acetate units of about 45% by weight, relative to the weight of said copolymer material.

Claim 5

A matrix according to claim 1 wherein the higher aliphatic monoalcohol compound is selected from the group consisting of saturated and unsaturated monoalcohol having from 12 to 20 carbon atoms.

Claim 6

A matrix according to claim 1 wherein the cellulose derivative material is selected from the group consisting of alkyl celluloses and hydroxyalkyl celluloses, in particular methyl cellulose, ethyl cellulose, propyl cellulose, methylpropyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose and hydroxypropyl cellulose.

Claim 7

A matrix according to claim 1 wherein the ester compound of a polyhydric alcohol with a fatty aliphatic acid is selected from the group consisting of esters obtained from (i) a glycerol or glycol component and (ii) a fatty aliphatic acid component having from 8 to 18 carbon atoms.

Claim 8

A matrix according to claim 6 wherein the glycol component is selected from the group consisting of ethylene glycol propylene glycol, dipropylene glycol, butylene glycol, triethylene glycol, diethylene glycol, polyethyleneglycol and polypropyleneglycol.

Claim 9

A matrix according to claim 6 wherein the fatty aliphatic acid component is selected from the group consisting of pelargonic acid, stearic acid, isostearic acid, capric acid, caprylic acid, palmitic acid, lauric acid, myristic acid and oleic acid.

Claim 10

A matrix according to claim 1 wherein the active ingredient to be administered percutaneously is an antiinflammatory agent, in particular ibuprofen, ketoprofen, niflumic acid or mefanamic acid.

Claim 11

A matrix according to claim 1 wherein the active ingredient to be administered percutaneously is a calcic antagonist of the dihydropyridine type, such as nifedipine or nicardipine.

Claim 12

A matrix according to claim 1 wherein the active ingredient to be administered percutaneously is a β-blocking agent, such as timolol or propranolol.

Claim 13

A matrix according to claim 1 wherein the active ingredient to be administered percutaneously is a β-stimulating agent, such as procaterol or salbutamol.

Claim 14

A matrix according to claim 1 wherein the weight ratio (a+c)/(b+d) is about 1.

Claim 15

A method for preparing a matrix as claimed in claim 1, coated on a support, said method comprising the following steps : 1) the means a) and part of the means b) are mixed, with stirring, at a temperature greater than or equal to 110° C., and the resulting mixture is homogenized for about 0.5 h, 2) the means c) is incorporated per small portions into the homogenized mixture resulting from stage 1, with stirring, at a temperature greater than or equal to 110° C., then the resulting mixture is homogenized, 3) the remainder of the means b) is incorporated into the homogenized mixture resulting from stage 2, with stirring, at a temperature greater than or equal to 110° C., 4) the resulting mixture thus obtained is homogenized at a temperature greater than or equal to 110° C. and then left to stand for at least 8 hours, 5) the homogenized resulting mixture thus obtained is heated at a temperature of 50°-70° C. for at least 0.25 h, after which the means d) and the active ingredient in a solvent for the said active ingredient, for example ethanol, are incorporated at said temperature of 50°-70° C., said solvent representing from 30 to 100% v/w with respect to the total weight of means a), b), c), d) and e), 6) the resulting mixture thus obtained is homogenized for at least 0.5 h at a temperature of 50°-70° C., 7) the homogenized resulting mixture thus obtained is deposited on a temporary support, at a temperature of the order of 50°-70° C., at a rate of 100 to 300 g/m 2 , for obtaining an assembly consisting of sad temporary support and the matrix deposited thereon, 8) the whole assembly consisting of said temporary support and said matrix is heated at a temperature of the order of 70°-90° C. in order to evaporate the solvent for the active ingredient until the residual proportion is less than 5%, and 9) the resulting dry matrix is transferred onto an appropriate support.