Non-steroidal anti-inflammatory drug formulations for topical applications to the skin

Abstract

Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain / inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.

Description

FIELD OF INVENTION [0001] This invention relates to topical compositions for transdermal administration of a non-steroidal antiinflammatory drug (NSAID) through the skin of a patient and to the method for transdermally administering the non-steroidal antiinflammatory drug using the topical composition. DISCUSSION OF THE PRIOR ART [0002] All drugs must be administered in such a manner that they reach the intended site in the body in an optimal concentration (amount of drug per unit volume of blood) to achieve the desired effect at the proper time, and for an appropriate length of time. Customarily, drugs are taken orally, injected, inhaled, or applied topically. These conventional routes of administration often fail to meet the stated objectives, however. For example, when drugs are absorbed into the blood stream by whatever route, peaks and valleys in the blood concentration of the drug occur and may cause undesirable effects (e.g., peak levels), or loss of activities (e.g., valleys...

AI Technical Summary

Benefits of technology

"The present invention provides stable topical compositions that can be applied to the skin for the transdermal delivery of ibuprofen or other NSAID compounds. The compositions include a therapeutically effective amount of ibuprofen or other NSAID compound, a skin penetration enhancer, a gelling agent, and optionally a base to provide a pH in the range of from about 6 to about 8. The compositions can be used for the treatment of inflammation and pain. The invention also provides glycol-free topical compositions effective for the transdermal administration of naproxen."

Problems solved by technology

These conventional routes of administration often fail to meet the stated objectives, however.

For example, when drugs are absorbed into the blood stream by whatever route, peaks and valleys in the blood concentration of the drug occur and may cause undesirable effects (e.g., peak levels), or loss of activities (e.g., valleys).

Although these formulations attempt to control the release of drugs from their carriers, the desired effects are often not reproducible, may be subject to patient-to-patient variations, and may not be suitable for prolonged periods of delivery, such as days or even months.

However, present transdermal delivery systems have major drawbacks.

High molecular weight drugs or drugs with too high or low hydrophilic balance often cannot be incorporated into current transdermal systems in concentrations high enough to overcome their impermeability through the stratum corneum.

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