초록 ▼

Topical pharmaceutical compositions comprising a pharmaceutically-active agent and a novel, penetration-enhancing vehicle or carrier are disclosed. The vehicle or carrier comprises a binary combination of N-(2-Hydroxyethyl) pyrrolidone and a "cell-envelope disordering compound". The compositions pro

Topical pharmaceutical compositions comprising a pharmaceutically-active agent and a novel, penetration-enhancing vehicle or carrier are disclosed. The vehicle or carrier comprises a binary combination of N-(2-Hydroxyethyl) pyrrolidone and a "cell-envelope disordering compound". The compositions provide marked transepidermal and percutaneous delivery of the active selected. A method of treating certain pathologies and conditions responsive to the selected active, systemically or locally, is also disclosed.

대표청구항 ▼

1. A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) a safe and effective amount of a non-steroidal anti-inflammatory agent selected from the group consisting of salicylic acid, acetyl salicylic acid, methyl salicylate, glycol salicylate, salicylmides, be

1. A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) a safe and effective amount of a non-steroidal anti-inflammatory agent selected from the group consisting of salicylic acid, acetyl salicylic acid, methyl salicylate, glycol salicylate, salicylmides, benzyl-2,5-diacetoxybenzoic acid, ibuprofen, fulindac, naproxen, ketoprofen, etofenamate, phenylbutazone, indomethacin, piroxicam, and mixtures thereof; (b) 0% to about 80% by weight of a solvent selected from ethanol or 2-propanol; (c) 0% to about 80% by weight water; and (d) about 10% to about 99.9% by weight of a penetration-enhancing vehicle consisting essentially of (i) N-(2-hydroxyethyl)pyrrolidone, and (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, oleyl alcohol, monoolein, myristyl alcohol, and mixtures thereof; wherein component (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 1:5 to about 500:1 by weight. 2. A composition according to claim 1 wherein component (d) is present at a level of about 15% to about 99.9% by weight. 3. A compound according to claim 2 wherein component (d) is present at a level of about 25% to about 99.9% by weight. 4. A composition according to claim 1 wherein components (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 5:1 to about 100:1 by weight. 5. A composition according to claim 4 wherein components (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 10:1 to about 100:1 by weight. 6. A composition according to claim 5 wherein components (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 15:1 to about 100:1 by weight. 7. A composition according to claim 1 wherein component (b) is present at a level of about 0% to about 70% by weight. 8. A composition according to claim 1 wherein component (d)(ii) is selected from the group consisting of methyl laurate, oleic acid, myristyl alcohol, and mixtures thereof. 9. A composition according to claim 8 wherein component (d)(ii) is methyl laurate. 10. A composition according to claim 8 wherein component (d)(ii) is oleic acid. 11. A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) about 0.01% to about 10%, by weight, of a non-steroidal anti-inflammatory agent selected from the group consisting of salicylic acid, acetyl salicylic acid, methyl salicylate, glycol salicylate, salicylmides, benzyl-2,5-diacetoxybenzoic acid, ibuprofen, fulindac, naproxen, ketoprofen, etofenamate, phenylbutazone, indomethacin, piroxicam, and mixtures thereof; (b) 0% to about 80% by weight of a solvent selected from ethanol and 2-propanol; (c) 0% to about 80% by weight water; (d) about 10% to about 99.9% by weight of a penetration-enhancing vehicle consisting essentially of (i) N-(2-hydroxyethyl)pyrrolidone, and (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, oleyl alcohol, monoolein, myristyl alcohol, and mixtures thereof; wherein component (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 5:1 to about 100:1 by weight. 12. A composition according to claim 11 wherein component (d) is present at a level of about 15% to about 99.9% by weight. 13. A compound according to claim 12 wherein component (d) is present at a level of about 25% to about 99.9% by weight. 14. A composition according to claim 11 wherein components (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 10:1 to about 100:1 by weight. 15. A composition according to claim 14 wherein components (d)(i) and (d)(ii) are present in a ratio of (d)(i):(d)(ii) of about 15:1 to about 100:1 by weight. 16. A composition according to claim 11 wherein component (b) is present at a level of about 0% to about 70% by weight. 17. A composition according to claim 11 wherein component (d)(ii) is selected from the group consisting of methyl laurate, oleic acid, myristyl alcohol, and mixtures thereof. 18. A composition according to claim 17 wherein component (d)(ii) is methyl laurate. 19. A composition according to claim 17 wherein component (d)(ii) is oleic acid. 20. A composition according to claim 1 wherein the non-steroidal anti-inflammatory agent is present at a level of about 0.05% to about 10% by weight. 21. A composition according to claim 1 wherein said composition is substantially free of any single member of the saturated straight chain C 16 -C 20 normal fatty alcohols or saturated straight chain C 4 -C 20 mono- or dicarboxylic acids. 22. A composition according to claim 21 wherein said composition contains less than 3.5%, by weight, of any single saturated straight chain C 16 -C 20 normal fatty alcohols or saturated straight chain C 4 -C 20 mono- and dicarboxylic acids.