Composition and method for enhanced transdermal absorption of nonsteroidal anti-inflammatory drugs
AssigneeUniversity of Georgia Research Foundation, Inc.
InventorsH. Won Jun, Lisheng Kang
Life of this patent
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Abstract
A novel topical formulation for delivery of nonsteroidal anti-inflammatory drugs (NSAIDs) is characterized by enhanced transdermal absorption and efficacy. A two phase liquid composition has aqueous and oil phases, the oil phase having a relatively high concentration of the NSAID to enhance transdermal absorption and efficacy when incorporated into the topical anti-inflammatory formulation. The two phase liquid composition preferably contains, in addition to an NSAID, at least one melting point depressing agent. A preferred topical anti-inflammatory composition includes S(+)-ibuprofen, thymol, and ethyl alcohol or isopropyl alcohol.
Claims40
A composition comprising:
- at least one nonsteroidal anti-inflammatory drug (NSAID):
- at least one alcohol selected from the group consisting of isopropyl alcohol, ethyl alcohol and propylene glycol;
- at least one melting point depressing agent selected from the group consisting of thymol, menthol, eucalyptol, eugenol, methyl salicylate, phenyl salicylate, capsaicin, butylated hydroxytoluene, a local anesthetic agent and any combination thereof, said melting point depressing agent present in the composition in an amount of less than about ¼ of the weight of the NSAID;
- said composition having spontaneously equilibrated aqueous and oil phases, wherein the NSAID is in substantially melted form at 25° C. and wherein the concentration of the NSAID in the oil phase is, by weight, at least about 40% of the weight of the oil phase.
A composition having spontaneously equilibrated aqueous and oil phases at 25° C., said composition comprising:
- S(+)-ibuprofen;
- at least one alcohol selected from the group consisting of isopropyl alcohol, ethyl alcohol and propylene glycol;
- at least one melting point depressing agent selected from the group consisting of thymol, menthol, eucalyptol, eugenol, methyl salicylate, phenyl salicylate, capsaicin, butylated hydroxytoluene, a local anesthetic agent and any combination thereof, said melting point depressing agent present in the composition in an amount of less than about ¼ of the weight of the S(+)-ibuprofen;
- and
- water;
- wherein the S(+) ibuprofen is present in the composition in substantially melted form at 25° C. and wherein the concentration of the S(+)-ibuprofen in the equilibrated oil phase is, by weight, at least about 40% of the weight of the oil phase.
A method for making a two phase liquid composition comprising:
- mixing at least one NSAID, at least one alcohol selected from the group consisting of isopropyl alcohol, ethyl alcohol and propylene glycol, at least one melting point depressing agent selected from the group consisting of thymol, menthol, eucalyptol, eugenol, methyl salicylate, phenyl salicylate, capsaicin, butylated hydroxytoluene, a local anesthetic agent and any combination thereof, wherein the amount of said melting point depressing agent is less than about ¼ of the weight of the NSAID, and water;
- to form a composition in which the NSAID is present in the composition in substantially melted form at 25° C., said composition having spontaneously equilibrated aqueous and oil phases at 25° C., said oil phase comprising at least a portion of the NSAID, wherein the concentration of the NSAID in the oil phase is, by weight, at least about 40% of the weight of the oil phase.
A composition made by the method comprising:
- mixing at least one NSAID;
- at least one alcohol selected from the group consisting of isopropyl alcohol, ethyl alcohol and propylene glycol;
- a melting point depressing agent selected from the group consisting of thymol, menthol, eucalyptol, eugenol, methyl salicylate, phenyl salicylate, capsaicin, butylated hydroxytoluene, a local anesthetic agent and any combination thereof, wherein the amount of said melting point depressing agent is less than about ¼ of the weight of the NSAID;
- and water;
- to cause the spontaneous formation of a composition in which the NSAID is present in substantially melted form at 25° C., said composition having equilibrated aqueous and oil phases at 25° C., said oil phase comprising at least a portion of the NSAID, wherein the concentration of the NSAID in the oil phase is, by weight, at least about 40% of the weight of the oil phase.
Dependencies are inferred from the claim text.