Diclofenac topical formulation
View Patent ↗The present invention provides a gel formulation comprising diclofenac sodium which has superior transdermal flux properties, which may be used for the topical treatment of pain, such as in osteoarthritis.
1. A method for treating pain, said method comprising:
administering a formulation, the formulation comprising:
diclofenac sodium present at 1-5% w/w;
DMSO present at 25% to 60% w/w; and
a viscosity of 500-5000 centipoise, wherein the administration of the formulation is twice daily, to thereby effectively treat pain.
2. The method of claim 1 , wherein the formulation comprises:
(i) 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, or 5.0% w/w and all fractions in between, of diclofenac sodium;
(ii) 30-60% w/w of DMSO;
(iii) 1-15% w/w of propylene glycol;
(iv) 1-30% w/w of ethanol;
(v) optionally glycerine;
(vi) water;
(vii) at least one thickening agent selected from the group consisting of a cellulose polymer, a carbomer polymer, a carbomer derivative, a cellulose derivative, and mixtures thereof.
3. The method of claim 1 , wherein the concentration of diclofenac sodium is a member selected from the group consisting of 1%, 1.5% and 2% w/w, and all fractions in between.
4. The method of claim 2 , wherein the concentration of DMSO is about 40% to about 50% w/w.
5. The method of claim 4 , wherein the concentration of DMSO is a member selected from the group consisting of 40%, 41%, 42%, 43%, 44%, 45%, 46%, 47%, 48%, 49% and 50% w/w, and all fractions in between.
6. The method of claim 2 , wherein the concentration of ethanol is present at 23-29% w/w.
7. The method of claim 2 , wherein the at least one thickening agent is selected from the group consisting of a carbomer polymer, a carbomer derivative and mixtures thereof.
8. The method of claim 7 , wherein the at least one thickening agent is selected from the group consisting of carbopol 971, carbopol 981, carbopol 941, carbopol 1342 and ultrez 10.
9. The method of claim 7 , wherein glycerine is present.
10. The method of claim 2 , wherein the at least one thickening agent is selected from the group consisting of a cellulose polymer, a cellulose derivative, and mixtures thereof.
11. The method of claim 10 , wherein the at least one thickening agent is hydroxypropyl cellulose.
12. The method of claim 11 , wherein the formulation comprises:
(i) 1.5, 2.0, 2.5, 3.0, 3.5, 4.0 or 5.0% w/w, and all fractions in between, of diclofenac sodium;
(ii) 40-50% w/w of DMSO;
(iii) 23-29% w/w of ethanol; and
(iv) 10-12% w/w of propylene glycol.
13. The method of claim 12 , wherein the concentration of diclofenac sodium is a member selected from the group consisting of 1.5% and 2% w/w, and all fractions in between.
14. The method of claim 12 , wherein the concentration of DMSO is a member selected from the group consisting of 40%, 41%, 42%, 43%, 44%, 45%, 46%, 47%, 48%, 49% and 50% w/w, and all fractions in between.
15. The method of claim 12 , wherein the concentration of ethanol is present at 26.5% w/w.
16. The method of claim 1 , wherein the formulation has improved absorption on a per dose basis compared to a comparative liquid composition.
17. The method of claim 1 , wherein the pain is due to osteoarthritis.