The present invention is intended to achieve a good solubility in the percutaneous absorption control agent under mild conditions of water soluble effective components and in a short time.The present invention relates toA method of preparing a solution comprising a water-soluble active ingredient and a percutaneous absorption control agent(step 1) the water soluble active component is dissolved in short chain alcohol to obtain a short chain alcohol solution；(step 2) the transdermal absorption control agent is added to the short chain alcohol solution obtained in stepObtaining a mixture；(step 3) from the mixed solution obtained in stepPreparation method comprising the step of removing said short chain alcohol；Solution comprising water soluble active component and percutaneous absorption control agent obtained in said preparation methodAlso containing a fat soluble mediumPercutaneous absorption composition；The present invention relates to a method for controlling release of water soluble active components including the above process in the skin.本発明は、水溶性有効成分が緩和な条件でかつ短時間で経皮吸収制御剤への良好な溶解性を達成することを目的とする。 本発明は、水溶性有効成分及び経皮吸収制御剤を含む溶液の調製方法であって、（工程１）前記水溶性有効成分を短鎖アルコールに溶解させて短鎖アルコール溶液を得る工程；（工程２）工程１で得られた短鎖アルコール溶液に前記経皮吸収制御剤を加えて、混合液を得る工程；（工程３）工程２で得られた混合液から、前記短鎖アルコールを除去する工程を含む調製方法；前記調製方法で得られる水溶性有効成分及び経皮吸収制御剤を含む溶液、ならびに脂溶性媒体を含む、経皮吸収組成物；ならびに前記工程を含む水溶性有効成分の皮膚中での放出を制御する方法に関する。
