Topical compositions for pain relief, manufacture and use
The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.
1. A topical composition comprising by weight percentage:
i) 0.1-10% capsaicin;
ii) 0.1-0.5% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.3-0.5% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 1-20% ethanol;
v) 0-10% diethylene glycol monomethyl ether,
vi) 0-10% propylene glycol;
vii) 0-15% polysorbate 80;
viii) 0-15% polyoxy 40 hydrogenated castor oil; and
ix) 30-60% water.
2. The topical composition of claim 1 , wherein the capsaicin is in an amount of 0.25-10% by weight.
3. The topical composition of claim 1 , wherein the hyaluronic acid with a molecular weight of about 1,000,000 Daltons is in an amount of 0.1-0.2% by weight; and the hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons is in an amount of 0.3-0.4% by weight.
4. The topical composition of claim 1 , wherein the ethanol is in an amount of 20% by weight.
5. The topical composition of claim 1 , wherein the diethylene glycol monomethyl ether is in an amount of 10% by weight.
6. The topical composition of claim 1 , wherein the propylene glycol is in an amount of 10% by weight.
7. The topical composition of claim 1 , wherein the polysorbate 80 is in an amount of 2-10% by weight.
8. The topical composition of claim 7 , wherein the polysorbate 80 is in an amount of 10% by weight.
9. The topical composition of claim 1 , wherein the polyoxy 40 hydrogenated castor oil is in an amount of 0.5-15% by weight.
10. The topical composition of claim 1 , wherein the polyoxy 40 hydrogenated castor oil is in an amount of 0% by weight.
11. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 0.25% capsaicin;
ii) 0.2% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.3% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
viii) 0.5% polyoxy 40 hydrogenated castor oil; and
ix) water, q.s.
12. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 2% capsaicin;
ii) 0.15% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.35% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
vii) 2% polysorbate 80;
viii) 5% polyoxy 40 hydrogenated castor oil; and
ix) water, q.s.
13. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 2% capsaicin;
ii) 0.1% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.4% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
vii) 2% polysorbate 80;
viii) 5% polyoxy 40 hydrogenated castor oil; and
ix) water, q.s.
14. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 5% capsaicin;
ii) 0.15% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.35% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
viii) 10% polyoxy 40 hydrogenated castor oil; and
ix) water, q.s.
15. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 5% capsaicin;
ii) 0.15% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.35% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
vii) 10% polysorbate 80; and
ix) water, q.s.
16. The topical composition of claim 1 , having the following ingredients by weight percentage:
i) 5% capsaicin;
ii) 0.15% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.35% hyaluronic acid with a molecular weight of about 11,000 or 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
vii) 15% PEG-40 hydrogenated castor oil; and
ix) water, q.s.
17. A topical composition, having the following ingredients by weight percentage:
i) 5% capsaicin;
ii) 0.17% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.33% hyaluronic acid with a molecular weight of about 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
vii) 10% polysorbate 80; and
ix) 44.50% water.
18. A topical composition, having the following ingredients by weight percentage:
i) 0.25% capsaicin;
ii) 0.19% hyaluronic acid with a molecular weight of about 1,000,000 Daltons;
iii) 0.36% hyaluronic acid with a molecular weight of about 20,000 Daltons;
iv) 20% ethanol;
v) 10% diethylene glycol monomethyl ether;
vi) 10% propylene glycol;
viii) 5% polyoxy 40 hydrogenated castor oil; and
ix) 54.2% water.
19. A method of treating pain in a mammal suffering from pain comprising topically administering the topical composition of claim 1 to the mammal.
20. The method of claim 19 , wherein the mammal is a human.
21. The method of claim 20 , wherein the pain is arthritis pain.
22. The method of claim 21 , wherein the arthritis pain is osteoarthritis or rheumatoid arthritis pain.