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 topical formulation comprising:
diclofenac sodium present at 2% w/w;
dimethyl sulfoxide present at 40% to 50% w/w;
ethanol present at 23% to 29% w/w;
propylene glycol present at 10% to 12% w/w; and
water to make 100% w/w,
wherein the topical formulation has a viscosity of 500 to 5000 centipoise, and wherein the formulation has a pH of 4 to 10.
2. The topical formulation of claim 1 , wherein the concentration of the dimethyl sulfoxide is 45.5% w/w.
3. The topical formulation of claim 1 , wherein the topical formulation comprises at least one thickening agent.
4. The topical formulation of claim 1 , wherein the concentration of the propylene glycol is 10% w/w.
5. The topical formulation of claim 3 , wherein the concentration of the dimethyl sulfoxide is 45.5% w/w.
6. The topical formulation of claim 2 , wherein propylene glycol is present in an amount of 11% w/w.
7. The topical formulation of claim 2 , wherein propylene glycol is present in an amount of 12% w/w.
8. The topical formulation of claim 1 , wherein the viscosity is at least 1000 cp.
9. The topical formulation of claim 2 , wherein the viscosity is at least 1000 cp.
10. The topical formulation of claim 1 , wherein the formulation degrades at less than 1% over 6 months.
11. The topical formulation of claim 2 , wherein the formulation degrades at less than 1% over 6 months.
12. A topical formulation consisting essentially of:
2% w/w diclofenac sodium,
45.5% w/w DMSO,
23-29% w/w ethanol,
10-12% w/w propylene glycol,
at least one thickening agent, and
water,
wherein the topical formulation a viscosity of 500-5000 cp.
13. The topical formulation of claim 12 , wherein the at least one thickening agent comprises hydroxypropyl cellulose.
14. The topical formulation of claim 13 , wherein the hydroxypropyl cellulose is present in an amount of 2.5% w/w.
15. The topical formulation of claim 12 , wherein the pH is 4 to 10.
16. The topical formulation of claim 12 , wherein propylene glycol is present in an amount of 10% w/w.
17. The topical formulation of claim 12 , wherein propylene glycol is present in an amount of 11% w/w.
18. The topical formulation of claim 12 , wherein propylene glycol is present in an amount of 12% w/w.
19. The topical formulation of claim 12 , wherein the formulation degrades at less than 1% over 6 months.
20. A method for treating the pain of osteoarthritis of the knee in a patient in need thereof comprising topically administering to the knee of the patient a formulation of claim 1 .
21. The method of claim 20 , wherein the formulation is topically administered to the knee 2 times per day.
22. A method for treating the pain of osteoarthritis of the knee in a patient in need thereof comprising topically administering to the knee of the patient a formulation of claim 2 .
23. The method of claim 22 , wherein the formulation is topically administered to the knee 2 times per day.
24. A method for treating the pain of osteoarthritis of the knee in a patient in need thereof comprising topically administering to the knee of the patient a formulation of claim 12 .
25. The method of claim 24 , wherein the formulation is topically administered to the knee 2 times per day.