Pola Pharma Inc.

Nihon Nohyaku Co., Ltd.

Takaaki Masuda

Hirokazu Kobayashi

Hiroshi Yamaguchi

Hideo Kaneda

Naoko Kobayashi

Hideaki Sasagawa

Makoto Gotoh

Nobuo Kubota

Naoto Nishida

Kahori Fujii

Yoshiyuki Miyata

Tetsuya Endo

Compositions having an increased amount of an effective component retained in the composition for a pump foamer are provided. A composition for external use is described which contains: 1) an N-alkyl-2-pyrrolidone and/or a diester carbonate; and 2) a surfactant. The composition is in a foam state upon use.

External-use composition producing foamed state upon use

Provided is a product exhibiting good bubbles even from a screen foamer composition using a non-ionic surfactant. This foam contains a non-ionic surfactant and is composed of an air layer and a bubble shell encapsulating the air layer. The bubble shell has a high light transmission region which is optically transparent and a low light transmission region which is less optically transparent than the highlight transmission region, both regions being disposed so as to spread across a surface of the bubble shell in such a manner as to form an identifiable boundary therebetween; and when the foam is allowed to stand at 25&#xb0; C., an area of the low light transmission region occupying the surface area of the bubble shell expands over time, and thus the entire surface of the bubble shell becomes occupied by the low light transmission region.

Foam, screen foamer composition, and evaluation method for same

The present invention addresses the issue of providing an external composition for screen foamers such as pump foamers, that can be safely used even when not removed after application. Provided is an external composition for screen foamers, including a non-ionic surfactant as a foaming component and, ideally, being in a soluble state.

External composition for screen foamers

Disclosed is a pharmaceutical composition for antifungal use, comprising: 1) one or more compounds selected from compounds represented by the general formula (1) below and physiologically acceptable salts thereof; 2) one or more compounds selected from polypropylene glycol, diesters of dibasic acids, triacetin, 2-ethyl-1,3-hexanediol, lauromacrogol, and polyoxyethylene-polyoxypropylene glycol; and 3) one or more compounds selected from glucono-&#x3b4;-lactone, propylene glycol, glycerin, and lactic acid. General formula (1) (In the formula, X represents a halogen or hydrogen). wherein X represents a halogen or hydrogen.

Antifungal composition

An object is to provide a crystal having a new crystal habit of luliconazole and expand the possibility of application to pharmaceuticals. Disclosed is a crystal of luliconazole having such a crystal habit that (020) plane is a specific crystal growth surface. 

Crystal having specific crystal habit and pharmaceutical composition containing the crystal as active ingredient

Disclosed is an antifungal agent for external use, which is characterized by containing a compound represented by the general formula (1), 50 to 95 mass % of an alcohol such as ethanol, 0.1 to 35 mass % of water or the like, and 0.01 to 5 mass % of a cellulose thickening agent. X is a halogen or H. 

Antifungal pharmaceutical composition

Means for improving the solubility of luliconazole is provided. A crystal of luliconazole represented by the following formula is provided, wherein the crystal has such a crystal habit that (011) plane is a specific crystal growth plane. The crystal is characterized in that Iwith respect to a sum total of I, I, I, I, I, I, I, I, I, I, I, I, I, I, and Iis not less than 25%, provided that integrated intensities of diffraction peaks, which correspond to the (001), (100), (10-1), (011), (110), (11-1), (10-2), (11-2), (020), (021), (20-2), (121), (013), (11-3), and (221) planes, are designated as I, I, I, I, I, I, I, I, I, I, I, I, I, I, and Irespectively in relation to the diffraction peaks detected in a range of 2&#x3b8;=5 to 35&#xb0; in a powder X-ray diffractometry using CuK&#x3b1; radiation. 

Crystalline form having specific crystal habit and pharmaceutical composition containing this crystalline form as active ingredient

An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal of luliconazole wherein the crystal has such a crystal habit that (021) plane is a specific crystal growth plane.

Crystal having crystal habits and pharmaceutical composition obtained by processing the crystal

An object is to establish an index to prepare a stable pharmaceutical formulation by specifying a related substance of luliconazole which appears depending on the type of a selected solvent in the luliconazole pharmaceutical formulation and which is different from the SE form and the Z form. Disclosed is an amide derivative of luliconazole.

Amide derivative and use of the same as stability index of a luliconazole pharmaceutical formulation

Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole. 

Method of evaluating pharmaceutical preparation containing luliconazole and index substance

An object is to provide means for suppressing the formation of any isomer of luliconazole on account of any influence of, for example, the humidity and the light and improving the stability. Disclosed is a method for differential evaluating a crystal of luliconazole, comprising differential evaluating the crystal by using, as indexes, surface free energy of the crystal of luliconazole and a ratio of a polar component of the surface free energy, wherein the crystal is evaluated to be stable on condition that the surface free energy is smaller and the ratio of the polar component is lower.

Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal

An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal consisting of luliconazole and short chain alcohol having a number of carbon atom or atoms of 1 to 4.

Crystal and pharmaceutical preparation containing the same crystal

An object is to provide a medicament preparation which is excellent in the solubilization stability in relation to a compound represented by the general formula (1) during the storage in a low temperature region and a high temperature region. The present invention resides in a pharmaceutical composition comprising 1) the compound represented by the general formula (1) and/or a salt thereof and 2) a polyhydric alcohol derivative. General formula (1) (In the formula, R, Rindependently represent hydrogen atom or halogen atom respectively, and at least one of R, Ris halogen atom.) 

Antimycotic pharmaceutical composition

Disclosed is an antifungal agent for external use, which is characterized by containing a compound represented by the general formula (1) below, 50-95% by mass of an alcohol, and 0.1-35% by mass of water and/or an anionic surfactant. 

Growing community of inventors

Kanagawa, Japan

Takaaki Masuda