《穿透含有N-（2 - 羟乙基）吡咯烷酮局部药物组合物》.docVIP

Penetrating topical pharmaceutical compositions containing N-(2-hydroxyethyl) pyrrolidone 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. 图片(19) ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? 权利要求(22) What is claimed is: 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 prese