Topical emulsion composition containing nonsteroidal anti-inflammatory drug
In one aspect, the present invention features an emulsion composition including (i) at least 3%, by weight, of a nonsteroidal anti-inflammatory drug; (ii) at least 15%, by weight, of isopropyl myristate; (iii) at least 25%, by weight, of water; and (iv) one or more emulsifiers; wherein the formulation is substantially free of C1-C4 alcohols.
1. An emulsion composition comprising:
(i) at least 7%, by weight, of a nonsteroidal anti-inflammatory drug;
(ii) at least 15%, by weight, of isopropyl myristate;
(iii) at least 25%, by weight, of water;
(iv) one or more emulsifiers;
(v) one or more pH adjusters; and
(vi) one or more solubilizers,
wherein the one or more pH adjusters comprises diethylamine,
wherein the one or more solubilizers comprises propylene glycol,
wherein said composition contains less than 5% by weight of C1-C16 alcohols, and
wherein said nonsteroidal anti-inflammatory drug is selected from the group consisting of ibuprofen, stereoisomers thereof, and salts thereof.
2. A composition of claim 1 , wherein said composition comprises at least 20%, by weight, of said isopropyl myristate.
3. A composition of claim 1 , wherein said composition comprises at least 40%, by weight, of said water.
4. A compound of claim 1 , wherein said one or more emulsifiers is ethylene glycol stearate.
5. A composition of claim 1 , wherein said composition contains less than 5% by weight of alcohols capable of esterifying said non-steroidal anti-inflammatory drug.
6. A composition of claim 1 , wherein less than 10% of said nonsteroidal anti-inflammatory drug has been converted to an ester following 30 days of storage of the composition in a glass jar with a lid in a laboratory oven maintained at 40° C.
7. A composition of claim 1 , wherein said composition has a plasma area under the curve of at least 5000 ng*hour/mL when an amount of said composition containing 200 mg of said nonsteroidal anti-inflammatory drug is topically applied to a minipig.
8. A composition of claim 1 , wherein said composition has a maximum plasma concentration of at least 200 ng/mL when an amount of the composition containing 200 mg of the nonsteroidal anti-inflammatory drug is topically applied to a minipig.
9. An emulsion composition of claim 1 , wherein:
(i) less than 10% of said nonsteroidal anti-inflammatory drug has been converted to an ester following 30 days of storage of the composition in a glass jar with a lid in a laboratory oven maintained at 40° C.; and
(ii) said composition has a plasma area under the curve of at least 5000 ng*hour/mL and a maximum plasma concentration of at least 200 ng/mL when an amount of said composition containing 200 mg of said nonsteroidal anti-inflammatory drug is topically applied to a minipig.
10. A composition of claim 1 , wherein said one or more pH adjusters further comprises at least one of triethanolamine, octylamine, and diisopropanolamine.
11. A method of treating pain in a subject, said method comprising topically applying to said subject a composition of claim 1 .