Semi-solid, oil-based pharmaceutical compositions containing pirfenidone for application in tissue repair

1 . A semi-solid pirfenidone pharmaceutical composition comprising:

(a) from 2% to 12% w/w pirfenidone;

(b) from 20% to 60% w/w of propylene glycol;

(c) from 5% to 10% w/w total of one or more of sorbitan stearate, ceteareth-6 and stearyl alcohol, ceteareth-25, and polysorbate 60;

(d) from 2% to 8% w/w total of one or more of cetyl alcohol and stearyl alcohol;

(e) from 0.5% to 3% w/w of one or more dimethicone;

(f) from 0.1% to 2% w/w of sodium methylparaben;

(g) from 0.05% to 0.2% w/w of carbomer;

(h) from 0.05% to 0.2% w/w of triethanolamine;

(i) from 0.05% to 0.2% w/w of sodium propylparaben; and

(j) from 0.0005% to 0.003% w/w of citric acid;

wherein the semi-solid pharmaceutical composition is in the form of a cream.

2 . The semi-solid pirfenidone pharmaceutical composition according to claim 1 , wherein the composition comprises:

(a) from 2% to 12% w/w Pirfenidone;

(b) 50% w/w Propylene Glycol;

(c) 6.382% w/w sorbitan stearate;

(d) 2% w/w Cetyl Alcohol;

(e) 2% w/w Stearyl alcohol;

(f) 1% w/w ceteareth-6 and stearyl alcohol;

(g) 1% w/w ceteareth-25;

(h) 1% w/w Dimethicone;

(i) 0.617% w/w polysorbate 60;

(j) 0.147% w/w Sodium Methylparaben;

(k) 0.1% w/w Carbomer;

(l) 0.1% w/w_Triethanolamine;

(m) 0.066% w/w Sodium Propylparaben;

(n) 0.001% w/w Citric acid; and

(o) Water qs 100%.

3 . The semi-solid pirfenidone pharmaceutical composition of claim 1 further comprising from 0.008% to 0.8% of an antiseptic/preservative.

4 . A method of manufacturing the semi-solid pirfenidone pharmaceutical composition according to claim 1 , the method comprising:

(1) Stirring sorbitan stearate, Cetyl Alcohol, Stearyl Alcohol, ceteareth-6 and stearyl alcohol, ceteareth-25, and Dimethicone and heating at 75-80° C.;

(2) Adding carbomer to 30% of the total water in the composition;

(3) Heating propylene glycol to 75-80° C. and stirring, before gradually adding Pirfenidone while stirring constantly and heating at 75-80° C.;

(4) Maintaining stirring and heating of the reaction of step 3 for 30 min;

(5) Gradually adding Sodium Methylparaben, Sodium Propylparaben, Citric Acid, and Tween 60 (Polysorbate 60 to 30% of the total water in the composition while stirring constantly until completely dissolved;

(6) Gradually adding the contents of step 2 and step 5 to the solution of step 4 while stirring constantly and maintaining heating at 75-80° C.;

(7) Adding the mixture of step 6 to the mixture of step 1 while stirring at 75-80° C. and then maintaining stirring for 20 minutes and lowering the mixture temperature to 40-45° C.;

(8) Gradually adding triethanolamine to the remaining 60% of the total water in the composition while stirring constantly until completely dissolved; and

(9) Adding the solution of step 8 to the mixture of step 7 while stirring for 60 minutes or until reaching a temperature of 30-35° C.

5 . A method of restoring skin imperfections caused by the loss of collagen and other extracellular matrix proteins, the method comprising administering the semi-solid pirfenidone pharmaceutical composition according to claim 1 to the skin of an individual in need of said treatment.

6 . The method of claim 5 , wherein the extracellular matrix proteins are fibronectin and elastin.

7 . A method of treating wrinkles and/or skin thinning comprising administering the semi-solid pirfenidone pharmaceutical composition of claim 1 to the skin of an individual in need of said treatment.