Abstract: This invention provides a suspension for oral administration comprising particles containing amorphous tolvaptan that can inhibit or delay crystallization of amorphous tolvaptan over time in the suspension, and stably maintain high solubility of tolvaptan and excellent absorbability of tolvaptan from the gastrointestinal tract; and a solid formulation for oral administration that can be suspended to prepare the suspension for oral administration at the time of use. This invention relates to a suspension for oral administration, in particular, a syrup, comprising (a) particles containing amorphous tolvaptan, (b) hydroxypropyl methylcellulose (HPMC), and (c) a solvent, wherein the amount of the HPMC (b) is 0.1 to 25% by weight based on the total weight of the suspension for oral administration.

Abstract: This invention provides a suspension for oral administration comprising particles containing amorphous tolvaptan that can inhibit or delay crystallization of amorphous tolvaptan over time in the suspension, and stably maintain high solubility of tolvaptan and excellent absorbability of tolvaptan from the gastrointestinal tract; and a solid formulation for oral administration that can be suspended to prepare the suspension for oral administration at the time of use. This invention relates to a suspension for oral administration, in particular, a syrup, comprising (a) particles containing amorphous tolvaptan, (b) hydroxypropyl methylcellulose (HPMC), and (c) a solvent, wherein the amount of the HPMC (b) is 0.1 to 25% by weight based on the total weight of the suspension for oral administration.

Abstract: This invention provides a suspension for oral administration comprising particles containing amorphous tolvaptan that can inhibit or delay crystallization of amorphous tolvaptan over time in the suspension, and stably maintain high solubility of tolvaptan and excellent absorbability of tolvaptan from the gastrointestinal tract; and a solid formulation for oral administration that can be suspended to prepare the suspension for oral administration at the time of use. This invention relates to a suspension for oral administration, in particular, a syrup, comprising (a) particles containing amorphous tolvaptan, (b) hydroxypropyl methylcellulose (HPMC), and (c) a solvent, wherein the amount of the HPMC (b) is 0.1 to 25% by weight based on the total weight of the suspension for oral administration.

Abstract: This invention provides a suspension for oral administration comprising particles containing amorphous tolvaptan that can inhibit or delay crystallization of amorphous tolvaptan over time in the suspension, and stably maintain high solubility of tolvaptan and excellent absorbability of tolvaptan from the gastrointestinal tract; and a solid formulation for oral administration that can be suspended to prepare the suspension for oral administration at the time of use. This invention relates to a suspension for oral administration, in particular, a syrup, comprising (a) particles containing amorphous tolvaptan, (b) hydroxypropyl methylcellulose (HPMC), and (c) a solvent, wherein the amount of the HPMC (b) is 0.1 to 25% by weight based on the total weight of the suspension for oral administration.

Abstract: A dry powder inhalation system suitable for transpulmonary administration characterized by using a combination of: (1) A vessel housing a freeze-dried composition that contains a single dose of an active ingredient, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.015 or more, and (iii) a property of becoming fine particles having a mean particle diameter of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) A device capable of applying said air impact to the freeze-dried composition in said vessel and for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system of the invention characterized by using a combination of: (1) a vessel housing a freeze-dried composition that contains a single dose of an active ingredient, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.015 or more, and (iii) a property of becoming fine particles having a mean particle diameter of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising means capable of applying said air impact to the freeze-dried composition in said vessel, and means for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: A dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system is characterized by using a combination of: (1) a vessel housing a freeze-dried composition prepared by freeze-drying a composition liquid containing ingredients in a non-dissolved form, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.05 or more, and (iii) a property of becoming fine particles having a mean particle diameter (mass median aerodynamic diameter) of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising a member capable of applying the air impact to the freeze-dried composition in said vessel, and a member for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: An inhalation device for transpulmonary administration comprises: a chamber (16) for containing a pharmaceutical composition which is pulverized into fine particles by an air-generated impact for dispersal in air; an air inlet flow path (2) for introducing to the chamber (16) outside air to apply the air-generated impact to the pharmaceutical composition and for injecting the outside air toward the pharmaceutical composition; an inhalation flow path (1) for inhaling the pulverized pharmaceutical composition; a housing (9) for accommodating the chamber (16), the air inlet flow path (2), and the inhalation flow path (1); a mouthpiece (10) provided at one end of the housing (9), the mouthpiece (9) being provided with a mouth-side flow path (11) which communicates with the inhalation flow path (1), and an auxiliary flow path (12).

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system of the invention characterized by using a combination of: (1) a vessel housing a freeze-dried composition that contains a single dose of an active ingredient, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.015 or more, and (iii) a property of becoming fine particles having a mean particle diameter of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising means capable of applying said air impact to the freeze-dried composition in said vessel, and means for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system of the invention characterized by using a combination of: (1) a vessel housing a freeze-dried composition that contains a single dose of an active ingredient, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.015 or more, and (iii) a property of becoming fine particles having a mean particle diameter of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising means capable of applying said air impact to the freeze-dried composition in said vessel, and means for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: A non-powder-form freeze-dried composition for transpulmonary administration has a disintegration index greater than or equal to 0.015 and contains at least one active ingredient. The composition becomes fine particles upon receiving air impact at an air speed greater than or equal to 1 meter/second and an air flow rate greater than or equal to 17 milliliters/second. The fine particles have a mean particle diameter less than or equal to 1×10?5 meters and/or a fine particle fraction greater than or equal to 10%. A method of making the composition, a vessel containing the composition, a method of administering the composition, a dry powder inhalation system for transpulmonary administration, and a method of transpulmonary administration are also disclosed.

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system of the present invention characterized by using a combination of: (1) a vessel housing a freeze-dried composition prepared by freeze-drying a composition liquid containing ingredients in a non-dissolved form, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.05 or more, and (iii) a property of becoming fine particles having a mean particle diameter (mass median aerodynamic diameter) of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising a member capable of applying said air impact to the freeze-dried composition in said vessel, and a member for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: An inhalation device for transpulmonary administration comprises: a chamber (16) for containing a pharmaceutical composition which is pulverized into fine particles by an air-generated impact for dispersal in air; an air inlet flow path (2) for introducing to the chamber (16) outside air to apply the air-generated impact to the pharmaceutical composition and for injecting the outside air toward the pharmaceutical composition; an inhalation flow path (1) for inhaling the pulverized pharmaceutical composition; a housing (9) for accommodating the chamber (16), the air inlet flow path (2), and the inhalation flow path (1); a mouthpiece (10) provided at one end of the housing (9), the mouthpiece (9) being provided with a mouth-side flow path (11) which communicates with the inhalation flow path (1), and an auxiliary flow path (12).

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration. The dry powder inhalation system of the present invention characterized by using a combination of: (1) a vessel housing a freeze-dried composition prepared by freeze-drying a composition liquid containing ingredients in a non-dissolved form, and has: (i) a non-powder cake-like form, (ii) a disintegration index of 0.05 or more, and (iii) a property of becoming fine particles having a mean particle diameter (mass median aerodynamic diameter) of 10 microns or less or a fine particle fraction of 10% or more upon receipt of an air impact having an air speed of at least 1 m/sec and an air flow rate of at least 17 ml/sec; and (2) a device comprising a member capable of applying said air impact to the freeze-dried composition in said vessel, and a member for discharging the powder-form freeze-dried composition that has been made into fine particles.

Abstract: The present invention provides a novel dry powder inhalation system suitable for transpulmonary administration.