Nippon Zoki Pharmaceutical Co., Ltd.

Nihon University

Toa Eiyo Ltd.

Takayuki Furuishi

Kunihiro Minami

Koji Kunimasu

Kazuo Tomono

Toyofumi Suzuki

Toshiro Fukami

Takayuki Minowa

Miho Komine

Kunihiko Kimura

A pharmaceutical composition for external use which is an organogel containing a fatty acid ester and a glycerolglycerin fatty acid ester, in particular, a novel transdermally absorbabedle pharmaceutical composition for external use which has a drug such as non-narcotic analgesics as an active ingredient made in organogel form containing a drug such as non-narcotic analgesics as an active ingredient, a fatty acid ester and a glycerolglycerin fatty acid ester, and a method for producing the composition. The pharmaceutical composition significantly improves skin permeability of drugs such as non-narcotic analgesics and allows a sufficient amount of drug to permeate the skin sustainably. Moreover, since the pharmaceutical composition is in organogel form, it can be easily applied to a preparation in practice. In addition, the pharmaceutical composition can provide efficient use and the like of drugs due to a high drug release rate and therefore is highly useful.

Pharmaceutical composition for external use

A proline ester represented by the following formula (I): wherein Rrepresents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.

Proline ester and preparation containing the same for percutaneous administration

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Tokyo, Japan

Takayuki Furuishi