Otsuka Pharmaceutical Company, Limited

I. Otsuka Pharmaceutical Co., Ltd.

Takakuni Matsuda

Yoshito Masuda

Yuso Tomohira

Yusuke Kato

Vijay H Naringrekar

Yasuhiro Menjo

Manoj Nerurkar

Keigo Yamada

Janusz W Kostanski

Daiki Kaneko

Shogo Hiraoka

Yusuke Hoshika

Kazumi Kondo

Shin Miyamura

Takahiro Tomoyasu

Shinichi Ishikawa

Makoto Komatsu

Fumitaka Goto

Kai Suzuki

Miki Aihara

Hiroyuki Fujiki

Shizuo Kinoshita

Kenichi Miyata

Koji Ohmoto

Junichi Hatanaka

Yasuo Yamaguchi

An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 send having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1.000 s, as measured.

Injectable preparation

An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 sand having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1,000 s, as measured.

The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof,wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., Rrepresents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Water-soluble benzoazepine compound and its pharmaceutical composition

A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle thereof, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.

Controlled release sterile injectable aripiprazole formulation and method

This invention provides an injectable formulation to be administered intramuscularly or subcutaneously that is used for the prevention or treatment of polycystic kidney disease, and that can maintain a therapeutically effective blood concentration of tolvaptan for a long period of time; and a process for producing the same. More specifically, this invention relates to an injectable depot formulation comprising (1) a particle containing optically active tolvaptan as an active ingredient and (2) a pharmaceutically acceptable carrier for injection, and a process for producing the same.

Injectable depot formulation comprising optically active tolvaptan and process of producing the same

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

Disclosed are a method for producing an aripiprazole suspension, wherein the aripiprazole has a mean particle size of 1 to 10 &#x3bc;m, the method comprising the steps of: (a) combining bulk aripiprazole and a vehicle to form a primary suspension; (b) subjecting the primary suspension to first pulverization using e.g., a high shear pulverizing machine, a dispersion machine that applies shear force to a material to be processed, a colloid mill, an ultrasonic dispersion machine, or a high-pressure jet type emulsifying dispersion machine to form a secondary suspension; and (c) subjecting the secondary suspension to second pulverization using e.g., a high-pressure jet type emulsifying dispersion machine to form a sterile final suspension; and a method for producing a freeze-dried formulation from the aripiprazole suspension.

Methods for producing aripiprazole suspension and freeze-dried formulation

The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof,

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

A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.

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.

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Tokushima, Japan

Takakuni Matsuda