Abstract: Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D50) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm3; 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.

Abstract: 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.

Abstract: 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.

Abstract: Provided are a composition for hot-melt extrusion which can be hot-melt extruded at a temperature lower than a conventional temperature and therefore free of heat-induced deactivation of a drug; and a method for producing a hot-melt extrusion product which is simpler than a spray-drying method. More specifically, 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. Also provided is a method for producing a hot-melt extrusion product including a step of hot-melt extruding a composition for hot-melt extrusion including a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 or more at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.

Abstract: 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.

Abstract: 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.

Abstract: A composition comprising 10-80% by weight of a cellulose ether and a solvent selected from a water-soluble polyhydric alcohol, polyhydric alcohol ether, polyhydric alcohol ester, and ethanolamine is effective for purging extrusion and injection molding machines. The purging composition exerts a satisfactory purging or cleaning effect, but little abrasion effect, thus avoiding any abrasion of machine internal components by purging. Even if part of the purging composition is left within the machine after the composition is discharged out, the residue can be readily removed.

Abstract: Provided are a solid preparation comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without impairing the dissolution of the solid preparation, and a method for producing the same. More specifically, provided are a solid preparation comprising a poorly soluble drug, an enteric polymer, an excipient and a disintegrator, a mixed powder comprising at least the excipient and the disintegrator is partly or entirely covered with a solid dispersion comprising the poorly soluble dug and the enteric polymer; and a method for producing a solid preparation, comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder comprising an excipient and a disintegrator; and granulating and drying a resultant.

Abstract: Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D50) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm3; 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.

Abstract: Provided are a composition for hot-melt extrusion which can be hot-melt extruded at a temperature lower than a conventional temperature and therefore free of heat-induced deactivation of a drug; and a method for producing a hot-melt extrusion product which is simpler than a spray-drying method. More specifically, 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. Also provided is a method for producing a hot-melt extrusion product including a step of hot-melt extruding a composition for hot-melt extrusion including a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 or more at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.

Abstract: A composition comprising 10-80% by weight of a cellulose ether and a solvent selected from a water-soluble polyhydric alcohol, polyhydric alcohol ether, polyhydric alcohol ester, and ethanolamine is effective for purging extrusion and injection molding machines. The purging composition exerts a satisfactory purging or cleaning effect, but little abrasion effect, thus avoiding any abrasion of machine internal components by purging. Even if part of the purging composition is left within the machine after the composition is discharged out, the residue can be readily removed.

Abstract: A granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing dissolving of the solid dispersion, and a method for producing same is composed of 1 to 10% by weight of a poorly soluble drug, a water-soluble polymer, an excipient and 15 to 50% by weight if a disintegrator; a tablet of a solid dispersion composed of a poorly soluble drug, 1 to 5% by weight of a water-soluble polymer, an excipient and 15 to 50% by weight of a disintegrator; and a method for producing a granule or tablet of a solid dispersion comprising spraying a water-soluble polymer solution, in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder of an excipient and a disintegrator, and granulating and drying a resultant.

Abstract: A granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing dissolving of the solid dispersion, and a method for producing same is composed of 1 to 10% by weight of a poorly soluble drug, a water-soluble polymer, an excipient and 15 to 50% by weight if a disintegrator; a tablet of a solid dispersion composed of a poorly soluble drug, 1 to 5% by weight of a water-soluble polymer, an excipient and 15 to 50% by weight of a disintegrator; and a method for producing a granule or tablet of a solid dispersion comprising spraying a water-soluble polymer solution, in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder of an excipient and a disintegrator, and granulating and drying a resultant.

Abstract: Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same.

Abstract: Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.

Abstract: Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.

Abstract: Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.

Abstract: Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 ?m and a specific surface area measured by BET method of at least 1.

Abstract: Provided are a solid preparation comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without impairing the dissolution of the solid preparation, and a method for producing the same. More specifically, provided are a solid preparation comprising a poorly soluble drug, an enteric polymer, an excipient and a disintegrator, a mixed powder comprising at least the excipient and the disintegratior is partly or entirely covered with a solid dispersion comprising the poorly soluble dug and the enteric polymer; and a method for producing a solid preparation, comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder comprising an excipient and a disintegrator; and granulating and drying a resultant.

Abstract: Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same.