Shin-etsu Chemical Co., Ltd.

Shin-etsu Chemical C O., Ltd.

Aichi-prefectural Government

Ichinomy Fashion Design Center Foundation

Naosuke Maruyama

Kazuki Kikuchi

Hiroshi Umezawa

Takuya Yokosawa

Mitsuhiro Yoshida

Junichi Matsubara

Fumie Kusaki

Hiroyasu Kokubo

Sakae Obara

Akira Kitamura

Kazuhisa Hayakawa

Yuichi Nishiyama

Yasuyuki Hirama

Shogo Warashina

Tatsuya Yamashita

Ikuo Fukui

Soji Tanioka

Takafumi Hoshino

Miyuki Fukasawa

Shin-Ichiro Nakamura

Mitsuo Narita

Yoshiaki Kawashima

Fumie Tanno

Hidenori Tsuduki

Tsuyoshi Shikano

Hiroshi Kawamura

Tsuneo Hayata

Provided is a rapid release tablet excellent in binding capability and disintegrability and also excellent in storage stability and the like. More specifically, provided are a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight and D-mannitol, wherein the D-mannitol contains 0.9% by weight or less of D-sorbitol; a rapid release tablet comprising the granulated composite and a drug; and a method for producing a granulated composite comprising the steps of: mixing low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, first D-mannitol, and water to obtain an aqueous dispersion, and granulating while adding the aqueous dispersion to second D-mannitol, wherein the first D-mannitol and the second D-mannitol contain 0.9% by weight or less of D-sorbitol in total.

Granulated composite, rapid release tablet and method for producing same

Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa&#xb7;s.

Hypromellose acetate succinate powder excellent in dissolved state and production method thereof, and production methods for composition for solid dispersion, coating composition, drug-containing particle, and solid

A composition for an enteric hard capsule by taking advantage of conventionally unknown thermal gelation characteristics of a neutralized aqueous solution of an enteric polymer, so as to obtain an enteric capsule having sufficient water and acid resistances. More specifically, the composition has hypromellose acetate succinate having a molar substitution with an acetyl group per anhydroglucose unit of 0.6 to 0.8 and a ratio of the molar substitution with an acetyl group to a molar substitution with a succinyl group per anhydroglucose unit of 2.0 to 4.0, a neutralizer, and water method produces an enteric hard capsule having the steps of: immersing a core pin heated at 50 to 80&#xb0; C. in the composition, taking the immersed core pin out of the composition, and drying a gel layer of the hypromellose acetate succinate formed on the taken-out core pin.

Composition for enteric hard capsule and method for producing enteric hard capsule

Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm; and a hot-melt extrusion composition comprising the HPMCAS and a drug. Also provided is a method for producing a hot-melt extrudate including the steps of: hot-melting the hot-melt extrusion composition at a hot-melt temperature equal to or higher than a melting temperature of the HPMCAS, or at a hot-melt temperature equal to or higher than a temperature at which both of the HPMCAS and the drug become melt; and extruding the hot-melted composition.

Hypromellose acetate succinate for use as hot-melt extrusion carrier, hot-melt extrusion composition, and method for producing hot-melt extrudate

Provided are a drug-containing particle capable of suppressing dissolution of a drug in the oral cavity to suppress an unpleasant taste thereof and having excellent dissolution of the drug in the digestive tract after passing through the oral cavity; a method for preparing the drug-containing particle; a coating composition used for preparing the drug-containing particle; and a solid preparation having the drug-containing particle. More specifically, provided are a coating composition having 100 parts by weight of a cellulose-based enteric base and 50 parts by weight or less of a water-soluble cellulose ether; a drug-containing particle having a drug-containing core and a coat portion obtained by coating the core with the coating composition; a solid preparation having the drug-containing particle; and a method for preparing a drug-containing particle having a step of coating the drug-containing core with the coating composition.

Coating composition, drug-containing particle, solid preparation and method for preparing drug-containing particle

Regarding coating of fine particles or the like, provided are a coating composition containing methyl cellulose having small adhesiveness, resistance to generation of lumps, ability to form uniform coating, and ability to form a coating composition easily with water of normal temperature; a method for producing the coating composition; and a solid preparation. More specifically provided are a coating composition including methyl cellulose having such a viscosity that a viscosity at 20&#xb0; C. of a 2% by weight aqueous solution of the methyl cellulose is 1 to 15 mPa&#xb7;s and having such a dissolution start temperature that a dissolution start temperature of a 12% by weight aqueous liquid of the methyl cellulose is 10 to 25&#xb0; C. and a solvent; a solid preparation obtained by coating of the coating composition; and the like.

Coating composition containing methyl cellulose, method for producing the same, and solid preparation

Provided is low-substituted hydroxypropyl cellulose from which a granulation product having an adequate particle size can be obtained in a wet granulation method and a tablet having excellent compactibility and disintegrability can be obtained. More specifically, provided is low-substituted hydroxypropyl cellulose having a hydroxypropoxyl content of from 5 to 16% by weight and a water-soluble content of less than 2% by weight, wherein a weight ratio of water to the low-substituted hydroxypropyl cellulose giving a maximum torque is from 3 to 5 as determined while adding one part by weight of water per minute to one part by weight of the low-substituted hydroxypropyl cellulose under mixing with biaxial mixing blades. Also provided are a solid preparation including the low-substituted hydroxypropyl cellulose, and the like.

Low-substituted hydroxypropyl cellulose and solid preparation

There are provided HPMCAS (hypromellose acetate succinate) having such a property that a solution of the HPMCAS in a solvent has a controlled viscosity; and a method for producing the HPMCAS. More specifically, provided are HPMCAS having such property that a solution of 10 parts by weight of the HPMCAS in 100 parts by weight of a mixed solvent having a weight ratio of methylene chloride to methanol of 1:1 has a viscosity at 20&#xb0; C. of 135 mPa&#xb7;s or less; and a method for producing the HPMCAS including an esterification step of adding acetic anhydride and succinic anhydride to a solution of hypromellose in glacial acetic acid in the presence of sodium acetate to obtain a reaction product mixture, wherein the succinic anhydride is added intermittently, and a precipitation step of mixing the reaction product mixture with water to precipitate the HPMCAS.

Hypromellose acetate succinate and method for producing the same

Hypromellose acetate succinate powder excellent in dissolved state and production method thereof, and production methods for composition for solid dispersion, coating composition, drug-containing particle, and solid preparation

Provided are a solid preparation comprising an alkyl cellulose which provides excellent moldability and disintegrability even in a small amount of the alkyl cellulose, and a production method therefor. Specifically, provided are a solid preparation having an alkyl cellulose having a specific surface area by BET method of 0.5 to 10.0 m/g and a dissolution start temperature of 5 to 27&#xb0; C.; and a method for producing a solid preparation having the steps of: mixing a cellulose pulp and a first alkali metal hydroxide solution with stirring to obtain alkali cellulose, reacting the alkali cellulose with an alkylating agent to obtain a first reaction mixture, mixing the first reaction mixture and a second alkali metal hydroxide solution with stirring and without further addition of any alkylating agent to obtain a second reaction mixture, and pulverizing an alkyl cellulose isolated from the second reaction mixture to obtain an alkyl cellulose.

Solid preparation containing alkyl cellulose and method for producing the same

Provided is a composition for hot melt extrusion including a drug and hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more and a mole ratio of an acetyl group to a succinyl group of less than 1.6. Further, provided is a method for producing a hot melt extrudate including the step of hot melt-extruding a composition for hot melt extrusion including a drug and hypromellose acetate succinate having a molar hydroxypropoxy substitution of 0.40 or more and a mole ratio of an acetyl group to a succinyl group of less than 1.6, at a hot melt temperature of not lower than a melting temperature of the hypromellose acetate succinate or of not lower than a temperature at which both the hypromellose acetate succinate and the drug are melted.

Composition for hot melt extrusion and method for producing hot melt extrudate by using same

Provided are an alkyl cellulose excellent in formability when added even in a small amount and not causing marked delay in disintegration; a solid preparation comprising it; and a method for producing the solid preparation. More specifically, provided are an alkyl cellulose for use in tableting, the alkyl cellulose having a specific surface area of from 0.5 to 10.0 m/g as measured by BET method and a solid preparation comprising the alkyl cellulose. Also provided is a method for producing the alkyl cellulose, comprising the steps of: bringing pulp into contact with an alkali metal hydroxide solution to obtain alkali cellulose, reacting the alkali cellulose with an etherifying agent to obtain a first alkyl cellulose, pulverizing the first alkyl cellulose, and depolymerizing the pulverized first alkyl cellulose through hydrolysis with an acid catalyst or through oxidative decomposition with an oxidant to obtain a second alkyl cellulose.

Alkyl cellulose for use in tableting and solid preparation comprising same

There are provided a solution for spray drying having a high transmittance and markedly reduced generation of undissolved matter; and a method for producing a solid dispersion by using the solution for spray drying so that clogging with the undissolved matter is reduced and dissolution is improved. More specifically, there is provided a solution for spray drying comprising hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more, a solvent, and a drug. There is also provided a method for producing a solid dispersion comprising the step of removing the solvent from the spray drying solution.

Solution for spray drying comprising hypromellose acetate succinate and method for producing solid dispersion

Provided is a base material for dry direct tableting, the material being excellent in a binding property and disintegrability. More specifically, provided is a method of preparing a composite granule comprising at least a step of granulating a second sugar or sugar alcohol while adding thereto an aqueous dispersion comprising at least low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of 5 to 16% by weight, polyvinyl alcohol, a first sugar or sugar alcohol, and water.

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Joetsu, Japan

Naosuke Maruyama