Composition for external application comprising aripiprazole and organic acid as active ingredients

摘要

[Summary] An external preparation formulation superior in the transdermal absorbability has been desired as a new administration route of aripiprazole. Transdermal absorption of aripiprazole has been enabled for the first time by appropriately combining aripiprazole and an organic acid (particularly fatty acid with low lipophilicity). That is, it has been found that more superior transdermal absorbability can be achieved by forming a salt by using a compound showing lipophilicity within the range of −1.5-2, such as fatty acid and the like. It has been further found that the transdermal absorbability is remarkable improved by appropriately selecting the solvent composition. As a result, since a new dosage form of aripiprazole other than oral preparation has been developed, a new transdermal absorption preparation of aripiprazole can be provided.

主权项

1. A transdermal absorption preparation comprising a single active agent, an ester solvent, and an amide solvent,
wherein the single active agent is a lactic acid salt of aripiprazole, wherein the molar ratio of the lactic acid to aripiprazole is from 0.5:1 to 3:1, wherein the weight ratio of the ester solvent to the amide solvent is from 1:1 to 1:4; wherein the amide solvent is selected from the group consisting of N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, and combinations thereof, and wherein the ester solvent is selected from the group consisting of isopropyl myristate, diethyl sebacate, medium-chain triglyceride, propylene carbonate, and combinations thereof.