Ibuprofen for Topical Administration

Abstract

Set forth herein is a preparation of ibuprofen (2-(4-isobutylphenyl)propionic acid) in the free acid form that is suitable for topical administration. The topical ibuprofen formulation is prepared by dissolving the free acid form of ibuprofen, or preparing a homogeneous suspension of the free acid form of ibuprofen, in the presence of a pharmaceutically acceptable solvent so as to produce a topical drug formulation compatible with the penetration of 2-(4-isobutylphenyl) propionic acid through the skin tissue. Topical formulations of ibuprofen can be based on a pharmaceutically acceptable solvent such as, e.g., a pyrrolidone solvent or dimethylacetamide.

Description

REFERENCE TO RELATED APPLICATION[0001]This application claims benefit of the filing date of U.S. provisional application Ser. No. 61 / 095,672, filed Sep. 10, 2008, hereby incorporated by reference.TECHNICAL FIELD[0002]The present invention relates to topical compositions of ibuprofen and methods for making and using the compositions.BACKGROUND[0003]Ibuprofen, an anti-inflammatory, analgesic, and anti-pyretic agent, is a member of a group of drugs known as non-steroidal anti-inflammatory drugs (NSAIDs). Past formulations of ibuprofen have chiefly made use of the water-based form (salt form) of ibuprofen. Ibuprofen in its salt form forms the basis of such drug products as Advil® (potassium salt form of ibuprofen). Use of ibuprofen in its free acid form has been limited to formulations intended for oral administration, e.g., Motrin® in tablet and oral suspension. IBU® Ibuprofen Tablets USP (Knoll Laboratories, Mount Olive, N.J.) is supplied in tablets for oral administration.[0004]NSAID...

AI Technical Summary

Benefits of technology

[0005]The adverse side effects commonly associated with ibuprofen can be avoided by directly administering ibuprofen to an afflicted site in the form of a topical formulation. The inventive ibuprofen formulations set forth herein provide an alternate, topical, form of delivery to relieve pain and inflammation, e.g., in muscles, joints and soft tissue, while overcoming many difficulties in formulating a therapeutically effective topical pharmacological composition containing ibuprofen, including low solubility of the free acid form of the drug in aqueous solvents, as well as chemical and physical stability and cosmetic appeal.

[0010]In accordance with another embodiment of the invention is a method of preparing a pharmaceutical composition by solubilizing ibuprofen in a pharmaceutically acceptable solvent, creating an active drug-containing solution by combining the solubilized ibuprofen with a skin conditioner and a preservative, creating an aqueous solution containing a conditioner, a pH stabilizer and a preservative, creating an emollient phase by combining an emulsifier, a preservative, an oil and a stabilizer, combining the emollient phase and the aqueous solution, homogenizing to create a homogenized mixture, and adding the active drug containing solution to the homogenized mixture under temperature conditions avoiding degradation of the ibuprofen.

[0011]In related embodiments, the pyrrolidone solvent can be either N-methyl-2-pyrrolidone or 2-pyrrolidone. At least one of the steps of creating an aqueous mixture, creating an emollient phase, combining and homogenizing can include adding a first amount of heat. A second amount of heat can then be removed prior to the adding the active drug containing solution to create the temperature conditions that avoid degradation of the ibuprofen.

Problems solved by technology

Use of ibuprofen in its free acid form has been limited to formulations intended for oral administration, e.g., Motrin® in tablet and oral suspension.

However, some individuals are unable to tolerate oral intake of ibuprofen.

For example, ingestion may result in vomiting, thus leading to ineffective dosing.

Others are able to ingest ibuprofen but, as a result, develop gastric mucosal lesions.

These lesions lead to gastric discomfort and abdominal pain.

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