Penetrating topical pharmaceutical compositions containing N-(2-hydroxyethyl) pyrrolidone
AssigneeThe Procter & Gamble Company
InventorEugene R. Cooper
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Abstract
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.
Claims22
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.
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.
Dependencies are inferred from the claim text.