Shin-Etsu Chemical Co., Ltd.

Yasuyuki Hirama

Naosuke Maruyama

Akira Kitamura

Takuya Yokosawa

Taishi Kitaguchi

Shogo Warashina

Akiko Tsuchida

Kentaro Miki

Aya Tsuchiya

Tsubasa Oguro

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

There are provided an enteric coating composition having an excellent film-forming property, being capable of forming a film at a lower temperature than conventional compositions, and/or being capable of avoiding decomposition of a drug due to a high temperature and operational troubles due to or nozzle clogging; and others. More specifically, there are provided an enteric coating composition containing hypromellose acetate succinate having a molar substitution of hydroxypropoxy groups of 0.40 or more, and water; a method for producing a solid preparation including steps of coating a drug-containing core with the enteric coating composition to obtain a coating layer, and drying the coating layer; and a solid preparation containing a drug-containing core, and a coating layer directly or indirectly on the core, the coating layer containing a hypromellose acetate succinate having a molar substitution of hydroxypropoxy groups of 0.40 or more.

Enteric coating composition, solid preparation and method for producing solid preparation

There is provides a method for producing sieved low-substituted hydroxypropyl cellulose (L-HPC) at improved yield, while maintaining flowability and tablet properties. More specifically, there is provided a method for producing sieved L-HPC including a first sieving step of sieving L-HPC having a hydroxypropoxy group content of 5 to 16% by mass with a sieving shaker with horizontal movement of a sieve surface to obtain first sieve-residual L-HPC and first sieve-passed L-HPC, a second sieving step of sieving the first sieve-residual L-HPC with a sieving shaker with vertical movement of a sieve surface to obtain second sieve-residual L-HPC and second sieve-passed L-HPC, and a step of combining the first sieve-passed L-HPC and the second sieve-residual L-HPC to obtain the sieved L-HPC.

Method for producing sieved low-substituted hydroxypropyl cellulose

There is provided low-substituted hydroxypropyl cellulose (L-HPC) having good bindability, anti-capping performance and disintegratability. More specifically, there are provided L-HPC having a hydroxypropoxy group content of 5 to 16% by mass and a volume fraction of long fibrous particles of more than 50.0% relative to all of L-HPC particles which are classified, on a basis of dynamic image analysis, into fine particles, spherical particles, the long fibrous particles and short fibrous particles; and a solid preparation containing the L-HPC.

Low-substituted hydroxypropyl cellulose 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.

There are provided low-substituted hydroxypropyl cellulose (L-HPC) having good compressibility and capping-prevention performance, and others. Specifically, provided are L-HPC having a hydroxypropoxy content of 5 to 16% by weight, a volume fraction of long fibrous particles of 20 to 40% and a volume fraction of short fibrous particles of 26 to 60% with the proviso that the latter is greater than the former; and a solid preparation containing the L-HPC. Also provided is a method for producing the L-HPC including the steps of: bringing powdery pulp having a length-weighted mean width of 10 to 25 &#x3bc;m into contact with an alkali metal hydroxide solution, reacting the alkali cellulose with propylene oxide, and neutralizing the alkali metal hydroxide present in the reaction product with an acid to precipitate crude low-substituted hydroxypropyl cellulose in the absence of a step of dissolving a portion or all of the reaction product.

Low-substituted hydroxypropyl cellulose, production method thereof, and solid preparation

There is provided is a hydroxyalkyl alkyl cellulose exhibiting good flowability and high compressibility. More specifically, provided are a hydroxyalkyl alkyl cellulose having a volume-based average particle diameter, determined by dry laser diffractometry, of 50 to 100 &#x3bc;m, and having, on a basis of a dynamic image analysis to divide all particles into fine particles, spherical particles and fibrous particles, a volume fraction of the fibrous particles consisting of long and short fibrous particles relative to all of the particles of 45 to 70%, and a volume fraction of the fine particles relative to all of the particles of less than 2.0%; a solid preparation including the hydroxyalkyl alkyl cellulose; and others.

Hydroxyalkyl alkyl cellulose, method for producing the same, and solid preparation

Provided are low-substituted hydroxypropyl cellulose (L-HPC) having a hydroxypropoxy content of from 5 to 16% by weight, and having, on a basis of a dynamic image analysis to divide all particles into fine, spherical, and fibrous particles consisting of long and short fibrous particles, a volume fraction of the long fibrous particles of from 15 to 50% and a volume fraction of the short fibrous particles of from 23 to 60%; and a solid preparation containing the L-HPC. Also provided is a method for producing the L-HPC including the steps: bringing sheet-like or chip-like pulp having a length-weighted average fiber length of from 2.40 to 3.50 mm into contact with an alkali metal hydroxide solution, reacting the resulting alkali cellulose with propylene oxide, and dispersing the resulting reaction product in water containing an acid to partially dissolve it therein, followed by neutralization with an acid to precipitate crude L-HPC.

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.

Method of preparing composite granule comprising low-substituted hydroxypropyl cellulose and rapid release preparation

Provided is a hydroxyalkyl alkyl cellulose exhibiting good flowability and high compressibility. More specifically, there are provided a hydroxyalkyl alkyl cellulose having a volume-based average particle size, determined by dry laser diffractometry, of more than 100 &#x3bc;m and not more than 150 &#x3bc;m; and after dividing all particles into fine particles, spherical particles and fibrous particles by a dynamic image analysis, a volume fraction of the fibrous particles relative to all of the particles of more than 40% and not more than 50%, and a volume fraction of the fine particles relative to all of the particles of less than 2.0%; a solid preparation including the hydroxyalkyl alkyl cellulose; and others.

Provided is nonionic and excellently stable low-substituted hydroxypropylcellulose having improved compressibility and flowability, and further having improved disintegration and texture in oral cavity. More specifically provided is low-substituted hydroxypropylcellulose having a crystallinity of 60% or less, a degree of hydroxypropoxyl substitution of 5 to 9% by weight, and an aspect ratio of less than 2.5, wherein the crystallinity is calculated based on a diffraction intensity by wide-angle X-ray diffraction measurement according to the following formula (1):Crystallinity(%)={()/}&#xd7;100&#x2003;&#x2003;(1)wherein Ic means a diffraction intensity at a diffraction angle 2&#x3b8; of 22.5&#xb0; and Ia means a diffraction intensity at a diffraction angle 2&#x3b8; of 18.5&#xb0;.

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Joetsu, Japan

Yasuyuki Hirama