Abstract: It has been demanded to develop a formulation for a novel external preparation having excellent transdermal absorption of a basic pharmacologically active component contained therein. It is found that the lipid solubility (log P values) of a basic pharmacologically active component and an organic acid (particularly a fatty acid) contribute significantly to the transdermal absorption of the basic pharmacologically active component in the selection of proper combinations of the basic pharmacologically active component and the organic acid. Namely, it is found that superior transdermal absorption of a basic pharmacologically active component having a lipid solubility level of 0.5 to 5 can be achieved by forming a salt of the component with a fatty acid having a lipid solubility level of ?1 to 4. Thus, it becomes possible to provide a novel external preparation having excellent transdermal absorption properties.

Abstract: [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.

Abstract: [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.

Abstract: It has been demanded to develop a formulation for a novel external preparation having excellent transdermal absorption of a basic pharmacologically active component contained therein. It is found that the lipid solubility (logP values) of a basic pharmacologically active component and an organic acid (particularly a fatty acid) contribute significantly to the transdermal absorption of the basic pharmacologically active component in the selection of proper combinations of the basic pharmacologically active component and the organic acid. Namely, it is found that superior transdermal absorption of a basic pharmacologically active component having a lipid solubility level of 0.5 to 5 can be achieved by forming a salt of the component with a fatty acid having a lipid solubility level of ?1 to 4. Thus, it becomes possible to provide a novel external preparation having excellent transdermal absorption properties.

Abstract: The invention provides a salt, particularly an ionic liquid, of a non-steroidal anti-inflammatory drug (NSAID) comprising a carboxylic acid and an organic amine compound, as well as a method of producing such a salt.

Abstract: An optically active imidazolylpropanol compound of the formula: ##STR1## wherein n is an integer of 3 or 4, and its acid addition salts, which is useful as an antifungal agent, prepared by reacting an imidazolylthiol of the formula: ##STR2## with an alkylating agent of the formula:CH.sub.3 --(CH.sub.2).sub.n --X (III)wherein n is as defined above and X is a halogen atom, an alkylsulfonyloxy group or an arylsulfonyloxy group.

Abstract: A process for producing a compound of the formula (I) ##SPC1##wherein R.sub.2 is a hydrogen atom or an ester protective group, which is useful as a precursor for the production of cephalosporin derivatives, comprising reacting a phosphoramide derivative of cephalosporin of the formula (II) ##SPC2##wherein R.sub.1 is a lower alkyl group and R.sub.2 is as defined above, with a phosphorus acid. A further embodiment includes preparing the phosphoramide derivative of cephalosporin of the formula (II) by reactng a compound of the formula (III) ##SPC3##wherein R.sub.1 and R.sub.2 are as defined above, with an acid compound.