Gel containing pirfenidone

Abstract

The invention relates to a gel composition containing pirfenidone, which is advantageous over other cutaneously administered pharmaceutical forms known in the prior art and which can be used in treatment for the restoration of tissues with fibrotic lesions and for the prevention of fibrotic lesions.

Claims

1. A method for treating fibrotic lesions in a patient in need thereof, the method comprising cutaneous administration to the patient of a Pirfenidone gel consisting of 8% Pirfenidone, 0.5% of a viscous agent, 20% of a solubilizer, 11.5% of a non ionic solubilizer, 0.5% of a conserving agent, 0.5% of a neutralizer agent and 59% of purified water, thereby treating the fibrotic lesions in the patient.

2. The method of claim 1, wherein (a) the viscous agent in the Pirfenidone gel is selected from the group consisting of a Carbomer 940, Carbomer Interpolymer Type A, a cellulose derivative, a gum, and a poloxamer; (b) the solubilizer in the Pirfenidone gel is selected from the group consisting of N-methylpyrrolidone, ethyl alcohol, and propylene glycol; (c) the conserving agent in the Pirfenidone gel is selected from the group consisting of diazolidinyl urea, iodopropynyl butylcarbamate, methylparaben, propylparaben, and mixes of these conserving agents; and (d) the neutralizer agent in the Pirfenidone gel is selected from the group consisting of primary, secondary and tertiary mono-, bi-, and triethanolamine aliphatic amines, and a hydroxide alkaline metal.

3. The method of claim 2, wherein the viscous agent in the Pirfenidone gel is Carbomer 940, the solubilizer is N-methylpyrrolidone, the conserving agent is diazolidinyl urea, and the neutralizer agent is triethanolamine.

4. The method of claim 2, wherein the viscous agent in the Pirfenidone gel is Carbomer 940, the solubilizer is N-methylpyrrolidone, the conserving agent is iodopropynyl butylcarbamate, and the neutralizer agent is triethanolamine.

5. The method of claim 2, wherein the hydroxide alkaline metal in the Pirfenidone gel is sodium hydroxide.

Description

SPECIFICATION OF THE INVENTION

(1) Composition of the Gel

(2) The composition of the gel contains from 2 to 12% of Pirfenidone is elaborated utilizing from 0.4 to 1.2% of a viscous agent, from 10 to 30% of a solubilizer, from 5 to 15% of a non ionic solubilizer, from 0.2 to 1% of a conserving agent, from 0.4 to 1.2% a neutralizer agent and the rest of purified water. The viscous agent is selected from a Carbomer 940; Carbomer Interpolymer Type A, cellulose derivatives; gums; poloxamers, ethyl alcohol and propylene glycol; the conserving agent is selected from a group consisting of Diazolidinyl urea, iodopropynyl butylcarbamate, methylparaben and a mix of these compounds; the neutralizer agent is selected from a group of primary, secondary and tertiary aliphatic amines of the mono-, bi- and triethanolamine type, and of the hydroxide alkaline metals, such as sodium hydroxide.

(3) An example of the composition of the gel is shown in the table 1:

(4) TABLE-US-00001 Component Quantity (g) % Pirfenidone 8 8 Viscous agent 0.5 0.5 Solubilizer 20 20 Non ionic solubilizer 11.5 11.5 Conserving agent 0.5 0.5 Neutralizer 0.5 0.5 Purified water up to 100 59

(5) The gel containing Pirfenidone is manufactured as follows: a) Mix 50% of the total water to be used with the viscous agent, allowing the complete humectation of the viscous agent; b) Mix separately and with constant agitation the Pirfenidone with the solubilizer agent; c) Dissolve separately the non ionic solubilizer agent in the 25% water to be used at 40 C., once dissolved, the 15% of the total water is added; d) Add the solution from part c) to the mix from part b), agitate until the mix is homogenate. e) Dilute the neutralizer agent in 10% of the total water to use, agitate until the mix is homogenate; and f) Add with constant agitation and homogenate in each addition to the mix from part a) the solution from part d); the conservative and the solution from part e).
A prepared composition according to procedure describe is shown in table 2.

(6) TABLE-US-00002 Component Quantity (g) Pirfenidone 8 Carbomer 0.5 N-methylpirrolidone 20 Macrogolglycerol 11.5 Hidroxiestearate 40 Diazolidinilurea and 0.5 Iodopropinil-butilcarbamate Triethanoalamine 0.5 Purified water up to 100
These compositions are shown in an example mode, but they are not limited in any level of the reach of the description of the present invention.