Otsuka Pharmaceutical Company, Limited

Yuso Tomohira

Takakuni Matsuda

Keigo Yamada

Yusuke Kato

Kazumi Kondo

Shin Miyamura

Yasuhiro Menjo

Takahiro Tomoyasu

Tadashi Mukai

Shogo Hiraoka

Shinichi Ishikawa

Yoshikazu Oka

Minoru Kashimoto

Daisuke Kuribayashi

Tetsuroh Ichiba

Masakazu Nagasawa

Yasuo Yamaguchi

Hajime Toguchi

Masafumi Toda

Tetsuroh 59-15 Aza Sumiyoshikaitaku Ichiba

The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral so weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.

Aqueous ophthalmic suspension of crystalline rebamipide

The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral to weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.

The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein Rrepresents a &#x2014;CO&#x2014;(CH)&#x2014;CORgroup (wherein n is an integer of 1 to 4, and Ris (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5 -methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Benzazepine derivatives useful as vasopressin antagonists

The present invention provides a pharmaceutical composition that can efficiently achieve its medicinal action by having excellent basic pharmacologically active substance absorbency, even the basic pharmacologically active substance is poorly soluble, the pharmaceutical composition being prepared by adding (i) a basic pharmacologically active substance together with (ii) a fatty acid and organic acid glycerol ester and/or fatty acid and organic acid polyglycerol ester.

Pharmaceutical composition achieving excellent absorbency of pharmacologically active substance

The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein Rrepresents a &#x2014;CO&#x2014;(CH)&#x2014;CORgroup (wherein n is an integer of 1 to 4, and Ris (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

The present invention provides theophylline sustained release particles which contain a polyglycerol fatty acid ester as a matrix base material, which have a homogenous nucleus particle structure, which can effectively mask the unpleasant taste of medicaments, and which exhibit an excellent sustained medicament releasability (dissolvability) and outstanding storage stability. In particular, the present invention provides, among other things, a method for preparing theophylline sustained release particles comprising the steps of heating a matrix base material containing a polyglycerol fatty acid ester, theophylline and ethyl cellulose to give a molten mixture; spray-cooling the molten mixture to obtain spherical core particles having an average particle diameter of 250 &#x3bc;m or less; and applying fine particles to the core particles by fusion coating.

Medicament sustained-release particles and method for preparing the same

The present invention provides a medicinal composition that exhibits excellent storage stability and, even over long-term storage, little change in the release rate of the pharmacologically active substance contained therein. The medicinal composition of the invention prepared by dissolving or dispersing a pharmacologically active substance and a pH-independent water-insoluble polymer in a molten low-melting substance, and which can be prepared by spraying a liquid substance, obtained by dissolving or dispersing the pharmacologically active substance in a molten mixture comprising the low-melting substance and the pH-independent water-insoluble polymer, and then cooling the liquid substance.

Medicinal composition

The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein Rrepresents a &#x2014;CO&#x2014;(CH)&#x2014;CORgroup (wherein n is an integer of 1 to 4, and Ris (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Disclosed is a method for stabilizing a solid pharmaceutical preparation containing a pharmacological substance and sodium lauryl sulfate, the method comprising incorporating into the preparation at least one member selected from the group consisting of neutral salts, basic salts and basic substances. The preparation containing sodium lauryl sulfate prepared by the method of the invention has superior performance, including high storage stability, suppression of discoloration and deterioration, and prevention of change in its properties, such as the dissolution rate of pharmacological substance from the preparation.

Method for stabilizing preparation

Provided is a cilostazol preparation which comprises incorporating a fine powder of cilostazol into a dispersing and/or solubilizing agent thereby to enhance the dispersibility and/or solubility. Further, provided is a process for improving absorbability of a slightly soluble drug such as cilostazol even at the lower portion of the digestive tract, wherein said drug is hard to be absorbed at the lower portion of the digestive tract when a conventional method is used. According to the present invention, cilostazol is absorbed enough even at the lower portion of the digestive tract to have an effect as thrombolytic drug, cerebral circulation improving drug or the like.

Growing community of inventors

Tokushima, Japan

Yuso Tomohira