An embodiment of the present invention provides a sitagliptin preparation in which the production of nitrosamines is suppressed. Alternatively, an embodiment of the present invention provides a method of storage of a sitagliptin preparation to suppress the production of nitrosamines. According to an embodiment of the present invention, a sitagliptin preparation is provided comprising a sitagliptin containing tablet, and a case or a packing sealing the sitagliptin containing tablet, wherein an equilibrium relative humidity of the sitagliptin containing tablet as converted at 24° C. is 0.3% or less when the sitagliptin preparation is stored for one month under a condition of 25° C. and a relative humidity of 60%.
B65D 75/36 - Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents one sheet or blank being recessed and the other formed of relatively stiff flat sheet material, e.g. blister packages
B65D 77/04 - Articles or materials enclosed in two or more containers disposed one within another
B65D 81/26 - Adaptations for preventing deterioration or decay of contentsApplications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants with provision for draining away, or absorbing, fluids, e.g. exuded by contentsApplications of corrosion inhibitors or desiccators
2.
GRANULES, GRANULE-CONTAINING PHARMACEUTICAL PREPARATION, AND GRANULE-CONTAINING FOOD
One of the purposes of the present invention is to provide granules which can be applied to a granular or tablet preparation containing a fat-soluble or oily drug or food or a water- or oxygen-labile drug or food. In one embodiment, one of the purposes of the present invention is to provide granules containing a solidified liquid oil and applicable to a granular or tablet preparation containing a fat-soluble or oily drug or food or a water- or oxygen-labile drug or food. According to one embodiment of the present invention, granules are provided, each granule comprising: a gel particle containing a liquid oil and stearic acid, calcium stearate or magnesium stearate; and a powder additive layer disposed on the surface of the gel particle. In the gel particle, the mass ratio of the amount of stearic acid, calcium stearate or magnesium stearate to the amount of the liquid oil may be 1:1 or greater.
A23L 33/115 - Fatty acids or derivatives thereofFats or oils
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
One embodiment of the present invention provides a prasugrel hydrochloride-containing formulation in which the production of similar substances is suppressed. According to one embodiment of the present invention, provided is a prasugrel hydrochloride-containing formulation comprising prasugrel hydrochloride and at least one disintegrant selected from the group consisting of carmellose calcium, croscarmellose sodium, and sodium carboxymethyl starch. An uncoated tablet containing prasugrel hydrochloride and the disintegrant may contain 1-20 mass% of the disintegrant.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
One embodiment of the present invention provides an enzalutamide solid dispersion that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides an enzalutamide-containing preparation that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides a method for producing an enzalutamide solid dispersion that maintains the amorphous state of enzalutamide and has improved dissolution properties. Alternatively, one embodiment of the present invention provides a method for producing an enzalutamide-containing preparation that maintains the amorphous state of enzalutamide and has improved dissolution properties. According to one embodiment of the present invention, an enzalutamide solid dispersion which includes enzalutamide in an amorphous state and hydroxypropyl cellulose that serves as an amorphousness-maintaining polymer is provided.
One problem addressed by one embodiment of the present invention is to provide a teneligliptin-containing preparation in which an amorphous form of teneligliptin is maintained and an increase in related substances is suppressed after storage under open conditions susceptible to humidity. According to one embodiment of the present invention, provided is a teneligliptin-containing preparation comprising porous silica, amorphous teneligliptin supported on the porous silica, an organic acid, and propyl gallate. The teneligliptin-containing preparation may comprise particles comprising porous silica, amorphous teneligliptin supported on the porous silica, and an organic acid.
JAPAN AS REPRESENTED BY DIRECTOR-GENERAL OF NATIONAL INSTITUTE OF INFECTIOUS DISEASES (Japan)
SAWAI PHARMACEUTICAL Co., Ltd. (Japan)
Inventor
Watashi, Koichi
Saso, Wakana
Terashima, Toru
Abstract
In an embodiment, a Stephania cepharantha-derived alkaloid-containing preparation for treatment of a novel coronavirus infection is provided. According to an embodiment of the present invention, a preparation for treatment of a novel coronavirus infection comprises Cepharanthine, Isotetrandrine, Cycleanine, and Berbamine. A preparation for treatment of a novel coronavirus infection is for treatment of an infection caused by the novel coronavirus mutant strain. According to an embodiment of the present invention, a Stephania cepharantha-derived alkaloid-containing preparation for treatment of a novel coronavirus infection is provided.
A61K 36/71 - Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
One problem to be addressed by an embodiment of the present invention is to provide teneligliptin-containing particles that maintain the amorphous form of teneligliptin after storage in an opened condition susceptible to the effects of humidity. Moreover, another problem to be addressed by an embodiment of the present invention is to provide teneligliptin-containing particles where generation of analog substances during production is suppressed. An additional problem to be addressed by an embodiment of the present invention is to provide a formulation comprising such teneligliptin-containing particles. According to an embodiment of the present invention, teneligliptin-containing particles comprising porous silica and amorphous teneligliptin supported on the porous silica are provided.
One embodiment of the present invention provides a method for quantifying reactive NOx, which is an NOx source that could contribute to the generation of nitroso compounds. Another embodiment of the present invention provides a formulation for suppressing the generation of nitroso compounds, the formulation being designed on the basis of the method for quantifying reactive NOx, which could contribute to the generation of nitroso compounds. A method for quantifying reactive NOx according to one embodiment includes adding an amine source to a sample and generating nitroso compounds. According to this embodiment, it is permissible to carry out heating under hermetic conditions to generate the nitroso compounds.
G01N 31/00 - Investigating or analysing non-biological materials by the use of the chemical methods specified in the subgroupsApparatus specially adapted for such methods
A61K 47/16 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen
One embodiment of the present invention provides a method for selecting an additive capable of inhibiting a nitrosation reaction. Another embodiment of the present invention provides a preparation prevented from the generation of a nitroso compound, the preparation containing an additive selected by a method for selecting an additive capable of inhibiting a nitrosation reaction. The method for selecting an additive capable of inhibiting a nitrosation reaction according to one embodiment comprises: adding an amine source and an NOx source to an additive to generate a nitroso compound, quantifying the amount of the generated nitroso compound, and evaluating about the nitrosation reaction inhibition effect of the additive on the basis of the amount of the generated nitroso compound.
G01N 31/00 - Investigating or analysing non-biological materials by the use of the chemical methods specified in the subgroupsApparatus specially adapted for such methods
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
A preparation containing saxagliptin having improved stability and a method for producing the same are provided. According to an embodiment of the present invention, a preparation containing saxagliptin including a plain tablet part containing one or more first additive agent selected from a group consisting of D-mannitol, lactose, anhydrous lactose, and anhydrous dibasic calcium phosphate, the plain tablet part containing less than 35% by weight of crystalline cellulose with respect to 100% by weight of the plain tablet part, and a film coating part in contact with the plain tablet part and containing saxagliptin, a salt thereof, or a hydrate thereof, and a method for producing the same are provided.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
11.
METHOD FOR PRODUCING FESOTERODINE FUMARATE-CONTAINING FORMULATION
One embodiment of the present invention provides a method for producing a stable fesoterodine fumarate-containing formulation. In said method the generation of related substances is suppressed by using an easy-to-handle general-purpose additive and a simple method. One embodiment of the present invention provides a method for producing a fesoterodine fumarate-containing formulation, the method comprising dry-granulating fesoterodine fumarate, lactose, crystalline cellulose, and a lubricant to obtain an agglomerated material. Further, one embodiment of the present invention provides a method for producing a fesoterodine fumarate-containing formulation, the method comprising mixing and tableting fesoterodine fumarate, lactose, crystalline cellulose, hypromellose, and a lubricant. In the method, the fesoterodine fumarate, the lactose, the crystalline cellulose, the hypromellose, and the lubricant are each rendered as a dry powder and mixed.
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A medicinal preparation containing an apremilast hydrate is provided in which the apremilast hydrate is inhibited from undergoing crystal transition or dissolution delay. The medicinal preparation containing an apremilast hydrate according to an embodiment of the present invention is characterized by including an apremilast hydrate and a lubricant having a melting point of 220°C or higher. In the medicinal preparation containing an apremilast hydrate, the lubricant may be sodium stearyl fumarate or talc. The lubricant may be sodium stearyl fumarate.
JAPAN AS REPRESENTED BY DIRECTOR-GENERAL OF NATIONAL INSTITUTE OF INFECTIOUS DISEASES (Japan)
SAWAI PHARMACEUTICAL CO., LTD. (Japan)
Inventor
Watashi Koichi
Saso Wakana
Terashima Toru
Abstract
In one embodiment, provided is a Stephania cephalantha-derived alkaloid-containing preparation for treating SARS-CoV-2 infection. According to one embodiment of the present invention, the preparation for treating SARS-CoV-2 infection contains cepharanthine, isotetrandrine, cycleanine and berbamine. This preparation for treating SARS-CoV-2 infection is for treating infection caused by a SARS-CoV-2 variant. According to one embodiment of the present invention, provided is a Stephania cephalantha-derived alkaloid-containing preparation for treating SARS-CoV-2 infection.
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
A61K 36/59 - Menispermaceae (Moonseed family), e.g. hyperbaena or coralbead
One of the problems of one embodiment of the present invention is to provide film-coated granules which have a new film constitution. Alternatively, one of the problems of one embodiment of the present invention is to provide a pharmaceutical preparation containing the film-coated granules which have a new film constitution. Alternatively, one of the problems of one embodiment of the present invention is to provide a new dry manufacturing method of the film-coated granules. Alternatively, one of the problems of one embodiment of the present invention is to provide a new dry manufacturing method of the pharmaceutical preparation containing the film-coated granules. According to one embodiment of the present invention, a film-coated granule is provided that comprises a core particle having a melt component, and a film arranged on a surface of the core particle, wherein the film includes a porous substance, a plasticizer and a polymer.
Provided is a melt granulated product with a high particle size homogeneity. Alternatively, provided is a pharmaceutical composition using said melt granulated product. Alternatively, provided is a melt granulated product with a high drug content. Alternatively, provided is a pharmaceutical composition using the melt granulated product. According to one embodiment of the present invention, a granule is provided that comprises an active ingredient, a melt component, and a polymer, wherein the active ingredient, the melt component and the polymer are bound. In addition, the melt component may be solid at room temperature, and have a melting point of 100° C. or less. The polymer may be solid at room temperature, and have a glass transition point of 100° C. or less.
According to one embodiment of the present invention, granules having a high content of an active ingredient and a high uniformity of particle size are provided. Alternatively, according to one embodiment of the present invention, a preparation containing granules having a high content of an active ingredient and a high uniformity of particle size is provided. According to one embodiment of the present invention, a granule is provided that comprises a nuclear material, a melt component layer arranged on a surface of the nuclear material, and an active ingredient-containing layer arranged on a surface of the melt component layer, wherein the melt component layer contains a first melt component and the active ingredient-containing layer contains an active ingredient and a second melt component or a polymer having compatibility with the first melt component.
A solid preparation containing tafamidis includes tafamidis, and a carrier containing one or more selected from a group consisting of magnesium aluminometasilicate, microcrystalline cellulose, low substituted hydroxypropyl cellulose, crospovidone and calcium silicate, and a method for producing the same are provided.
The present invention provides: a linagliptin-containing orally disintegrating tablet which is capable of sufficiently masking bitterness; and a method for producing the same. According to an embodiment of the present invention, provided is a linagliptin-containing orally disintegrating tablet containing: linagliptin; and an additive including at least one selected from the group consisting of carmellose calcium, crosscarmellose sodium, carmellose, and sodium starch glycolic acid. The additive may also include at least one selected from the group consisting of carmellose calcium, crosscalmellose sodium, and carmellose.
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07D 473/06 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
19.
METHOD FOR MANUFACTURING ORALLY DISINTEGRATING TABLET, AND ORALLY DISINTEGRATING TABLET
A method for manufacturing an orally disintegrating tablet, in which adequate hardness for preventing breakage of the tablet during transport or handling by a medical practitioner or a patient is provided while rapid disintegration is maintained. The method for manufacturing an orally disintegrating tablet according to an embodiment of the present invention comprises spraying or dropping a liquid including hydroxypropyl cellulose having a viscosity in a 2% aqueous solution at 20° C. of 150 mPa·s or more and 400 mPa·s on additives, and performing fluid bed granulation. The liquid including hydroxypropyl cellulose may be sprayed or dropped on the additives so that the content of the hydroxypropyl cellulose with respect to 100 wt % of the orally disintegrating tablet is 0.2 wt % to 5 wt %.
One of the objects of the present invention is to provide a granule capable of sufficiently masking bitterness. Alternatively, one of the objects of the present invention is to provide a preparation containing a granule capable of sufficiently masking bitterness. According to an embodiment of the present invention, a granule is provided including a core substance on which a melt component and an active ingredient are disposed, a gelling substance-containing layer disposed on a surface where the melt component and the active ingredient are disposed, and a hydrophobic polymer-containing layer disposed on a surface of the gelling substance-containing layer.
The present invention provides a film coating composition for a solid preparation that is easy to take. The present invention also provides a solid preparation that is easy to take. A film coating composition according to an embodiment of the present invention contains a polyvinyl alcohol-polyethylene glycol graft copolymer and a thickening agent. The thickening agent may be composed of one or more substances that are selected from the group consisting of xanthan gum, locust bean gum, pectin, carrageenan, guar gum, gellan gum, and carboxy vinyl polymer.
A preparation containing saxagliptin having improved stability and a method for producing the same are provided. According to an embodiment of the present invention, a preparation containing saxagliptin including a plain tablet part containing one or more first additive agent selected from a group consisting of D-mannitol, lactose, anhydrous lactose, and anhydrous dibasic calcium phosphate, the plain tablet part containing less than 35% by weight of crystalline cellulose with respect to 100% by weight of the plain tablet part, and a film coating part in contact with the plain tablet part and containing saxagliptin, a salt thereof, or a hydrate thereof, and a method for producing the same are provided.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
Provided is a melt granulated substance with a high grain size homogeneity. Furthermore, provided is a pharmaceutical composition using said melt granulated substance. Furthermore, provided is a melt granulated substance that has high content of active pharmaceutical ingredient. Furthermore, provided is a pharmaceutical composition using said melt granulated substance. An embodiment of the present invention provides granules that contain: an active pharmaceutical ingredient, a melt component, and a polymer, wherein the active pharmaceutical ingredient, the melt component and the polymer are bound together. Furthermore, the melt component is solid at ordinary temperature, and may have a melting point of 100℃ or less. The polymer is solid at ordinary temperature, and may have a glass transition point of 100℃ or less.
An embodiment of the present invention provides granules with a high content of active pharmaceutical ingredient and with a high degree of grain size homogeneity. Another embodiment of the present invention provides a preparation containing granules with high content of active pharmaceutical ingredient and with a high degree of grain size homogeneity. Another embodiment of the present invention provides granules containing: a core substance, a melt component layer disposed on the surface of the core substance, and an active pharmaceutical ingredient-containing layer disposed on the surface of the melt component layer, wherein the melt component layer contains a first melt component, and the active pharmaceutical ingredient-containing layer contains an active pharmaceutical ingredient and a second melt component or a polymer exhibiting compatibility with the first melt component.
METHOD FOR PRODUCING GRANULES CONTAINING A CORE PARTICLE, GRANULES CONTAINING A CORE PARTICLE, PHARMACEUTICAL COMPOSITION CONTAINING THE GRANULES CONTAINING THE CORE PARTICLE, AND PREPARATION CONTAINING THE PHARMACEUTICAL COMPOSITION
A method for producing granules containing a core particle by using a general granulation method is provided. Granules containing a core particle produced by the method are provided. In addition, a pharmaceutical composition and preparation containing the granules containing the core particle are provided. The granulation method according to an embodiment of the present invention granulates by splaying granulation liquid having a mist diameter (D50) not more than the particle size (D50) of the core particle on a mixture containing a drug substance and a core particle. The granulation liquid may be water. The particle size of the core particle (D50) may be larger than the particle size (D50) of the drug substance.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
Provided are a vildagliptin-containing dry granulated powder, a vildagliptin-containing tablet, and methods for producing these, with which the generation of vildagliptin analogs during storage is inhibited. An embodiment of the present invention provides a vildagliptin-containing dry granulated powder that contains at least 50% by weight of vildagliptin. An embodiment of the present invention also provides a vildagliptin-containing tablet that is produced by tableting a mixture that contains the vildagliptin-containing dry granulated powder. The present invention provides a vildagliptin-containing dry granulated powder, a vildagliptin-containing tablet, and methods for producing these, with which the generation of vildagliptin analogs during storage is inhibited.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
27.
METHOD FOR MANUFACTURING ORALLY DISINTEGRATING TABLET, AND ORALLY DISINTEGRATING TABLET
Provided is a method for manufacturing an orally disintegrating tablet, in which adequate hardness for preventing breakage of the tablet during transport or handling by a medical practitioner or a patient is provided while rapid disintegration is maintained. A method for manufacturing an orally disintegrating tablet according to an embodiment of the present invention comprises spraying or dropping a liquid including hydroxypropyl cellulose having a viscosity in a 2% aqueous solution at 20°C of 150 mPa∙s to 400 mPa∙s into an additive, and performing fluid bed granulation. The liquid including hydroxypropyl cellulose may be sprayed or dropped into the additive so that the content of the hydroxypropyl cellulose with respect to 100 wt% of the orally disintegrating tablet is 0.2 wt% to 5 wt%.
An anhydrous dasatinib-containing preparation comprising an anhydrous dasatinib and a titanium oxide or colorant or antioxidant is provided. In one embodiment, the anhydrous dasatinib-containing preparation improves photostability upon storage. The weight ratio of the titanium oxide per the anhydrous dasatinib may be more than 0 and 2 or less, or the weight ratio of the colorant per the anhydrous dasatinib may be more than 0 and 1 or less, or the weight ratio of the antioxidant per the anhydrous dasatinib may be more than 0 and 0.5 or less.
The present invention provides a film coating composition for a solid preparation that is easy to take. The present invention also provides a solid preparation which is easy to take. A film coating composition according to one embodiment of the present invention contains a polyvinyl alcohol-polyethylene glycol graft copolymer and a thickening agent. The thickening agent may be composed of one or more substances that are selected from the group consisting of xanthane gum, locust bean gum, pectin, carrageenan, guar gum, gellan gum and carboxy vinyl polymers.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
C09D 171/00 - Coating compositions based on polyethers obtained by reactions forming an ether link in the main chainCoating compositions based on derivatives of such polymers
30.
Sustained-release preparation containing pseudoephedrine or a pharmaceutically acceptable salt thereof
A sustained-release preparation containing pseudoephedrine is provided comprising pseudoephedrine or a pharmaceutically acceptable salt thereof, and a hardened oil or stearic acid. The sustained-release preparation containing pseudoephedrine may contain a hardened oil or stearic acid in an amount of 100% by mass to 500% by mass with respect to the content of the pseudoephedrine or a pharmaceutically acceptable salt thereof. In addition, the sustained-release preparation containing pseudoephedrine may have a first part and a second part, the first part may contain the pseudoephedrine or a pharmaceutically acceptable salt thereof, and the first part or the second part may contain an optional active ingredient.
Provided is an orally disintegrating tablet film-coated with a composition for film coating containing hypromellose and hydroxypropyl cellulose but not containing a plasticizer.
Provided is a novel additive for an orally disintegrating tablet providing quick disintegrability and tablet hardness to the orally disintegrating tablet, and a producing method therefor. According to an embodiment of the present invention, there is provided an additive for an orally disintegrating tablet characterized by including D-mannitol, low-substituted hydroxypropyl cellulose (however, excluding the low-substituted hydroxypropyl cellulose having a mean particle size of 20 μm or less and a substitution degree of hydroxypropoxy groups of 11%, a mean particle size of 45 μm or less and a substitution degree of hydroxypropoxy groups of 14%, and a mean particle size of 45 μm or less and a substitution degree of hydroxypropoxy groups of 11% and a 90% cumulated particle size of 100 μm or less), crospovidone, and microcrystalline cellulose, wherein the low-substituted hydroxypropyl cellulose and the crospovidone are included in a ratio of 5:4.
Provided is an anhydrous dasatinib-containing preparation which is characterized by containing anhydrous dasatinib, titanium oxide or a coloring agent or an antioxidant. In one embodiment, the anhydrous dasatinib-containing preparation has improved photostability during storage. When the content of the anhydrous dasatinib is taken as 1, the weight ratio of the titanium oxide may be more than 0 and not more than 2. When the content of the anhydrous dasatinib is taken as 1, the weight ratio of the coloring agent may be more than 0 and not more than 1. When the content of the anhydrous dasatinib is taken as 1, the weight ratio of the antioxidant may be more than 0 and not more than 0.5.
A mouthfeel evaluation method for an orally disintegrating test object is provided, the method including, by a measurement apparatus, giving a predetermined distortion with a predetermine cycle as applying a predetermined pressure to the orally disintegrating test object, adding a predetermined amount of a test liquid to the test object, and measuring a loss tangent of the test object with time.
Provided is a novel additive for an orally disintegrating tablet which imparts a rapid disintegration property and a tablet hardness to the orally disintegrating tablet and a method for producing the same. An additive for an orally disintegrating tablet according to one embodiment of the present invention includes a D-mannitol, a low-substituted hydroxypropyl cellulose (excluding those having a mean particle size of 20 μm or less and a substitution degree of the hydroxypropoxy groups of 11%, having a mean particle size of 45 μm or less and a substitution degree of the hydroxypropoxy groups of 14% and having a mean particle size of 45 μm or less and a substitution degree of the hydroxypropoxy groups of 11% together with a 90% cumulated particle size of 100 μm or less), a crospovidone and a crystalline cellulose.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
water absorption rate of tablet=(mass of tablet after measurement of time for solution to penetrate−mass of tablet before measurement of time for solution to penetrate)/(time for solution to penetrate from one end to other end) (1).
G01N 5/02 - Analysing materials by weighing, e.g. weighing small particles separated from a gas or liquid by absorbing or adsorbing components of a material and determining change of weight of the adsorbent, e.g. determining moisture content
G01N 15/08 - Investigating permeability, pore volume, or surface area of porous materials
A61K 9/00 - Medicinal preparations characterised by special physical form
G01N 33/00 - Investigating or analysing materials by specific methods not covered by groups
37.
Mirabegron-containing tablet, method for producing mirabegron-containing pharmaceutical preparation, and method for producing mirabegron-containing granulated product
To provide a mirabegron-containing tablet that maintains the amorphous form of mirabegron even after long-term storage. Also, to provide a mirabegron-containing pharmaceutical preparation that can maintain the purity of mirabegron while preventing the generation of related substances at the time of storage, a method for producing a mirabegron-containing pharmaceutical preparation, and a method for producing a mirabegron-containing granulated product. According to an embodiment of the present invention, there is provided a mirabegron-containing pharmaceutical preparation containing mirabegron, hypromellose, and polyvinylpyrrolidone. The mirabegron-containing pharmaceutical preparation may contain a spray-dried granulated product containing the mirabegron, the hypromellose, and the polyvinylpyrrolidone.
Provided are: a novel orally disintegrating tablet additive composition that provides orally disintegrating tablets with high disintegrability and tablet hardness; and a method for producing the same. An orally disintegrating tablet additive composition according to an embodiment of the present invention is characterized by including: D-mannitol; a low degree-of-substitution hydroxypropylcellulose (excluding: those having the average particle diameter of 20 μm or less, and having the degree of substitution of hydroxypropoxy group of 11%; those having the average particle diameter of 45 μm or less, and having the degree of substitution of hydroxypropoxy group of 14%; and those having the average particle diameter of 45 μm or less, and having the degree of substitution of hydroxypropoxy group of 11%, and having 90% cumulative particle diameter of 100 μm or less); crospovidone; and crystalline cellulose. The content ratio of the low degree-of-substitution hydroxypropylcellulose to the crospovidone is 5:4.
Provided is an evaluation method for evaluating the texture of food or a medicine disintegrable in the oral cavity, such as an orally disintegrable tablet or tablet candy, by imitating the environment in the oral cavity. Further provided is an evaluation apparatus for evaluating the texture of food or a medicine disintegrable in the oral cavity, such as an orally disintegrable tablet or tablet candy, by imitating the environment in the oral cavity. The texture evaluation method for an orally disintegrable test object according to one embodiment of the present invention is characterized in that a measurement device gives prescribed distortion at a prescribed cycle to the orally disintegrable test object while applying prescribed pressure to the test object, and measures the loss tangent of the test object over time by adding a prescribed amount of a test liquid to the test object.
Provided are: a novel additive which is for an orally disintegrating tablet and imparts rapid disintegratability and tablet hardness to the orally disintegrating tablet; and a method for producing the additive. An additive for an orally disintegrating tablet according to one embodiment of the present invention is characterized by comprising D-mannitol, low-substituted hydroxypropyl celluloses (excluding those in which the average particle size is 20 μm or less and the degree of substitution of hydroxypropoxy groups is 11%, those in which the average particle size is 45 μm or less and the degree of substitution of hydroxypropoxy groups is 14%, and those in which the average particle size is 45 μm or less, the degree of substitution of hydroxypropoxy groups is 11%, and the particle diameter at 90% of the cumulative particle size distribution is 100 μm or less), crospovidone, and crystalline cellulose.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
Provided is an intraorally disintegrable tablet containing olmesartan medoxomil, said tablet having improved mechanical strength of the tablet. Also provided is an intraorally disintegrable tablet containing olmesartan medoxomil, said tablet maintaining the chemical stability of the drug. The intraorally disintegrable tablet according to the present invention containing olmesartan medoxomil contains olmesartan medoxomil and a mixture in which magnesium metasilicate aluminates of multiple grades are combined together. The intraorally disintegrable tablet according to the present invention containing olmesartan medoxomil may contain the mixture, in which magnesium metasilicate aluminates of multiple grades are combined together, in an amount of 1-3 wt% inclusive relative to the total tablet weight.
Provided is an evaluating method capable of appropriately evaluating a degree of disintegration of an orally disintegrating tablet irrespective of the prescription system. Also provided is an evaluating device capable of appropriately evaluating a degree of disintegration of an orally disintegrating tablet irrespective of the prescription system. The method of evaluating an orally disintegrating tablet according to one mode of embodiment of the present invention includes: measuring the mass of the orally disintegrating tablet; placing the orally disintegrating tablet on a preparation placement surface of a test solution supply unit; measuring a water absorption time for a test solution to penetrate from one end of the orally disintegrating tablet in contact with the preparation placement surface to the other end of the orally disintegrating tablet; measuring the mass of the orally disintegrating tablet for which the time for the test solution to penetrate has been measured; and calculating a water absorption rate of the orally disintegrating tablet from the following formula (1); wherein the water absorption rate of the orally disintegrating tablet is evaluated relative to a water absorption rate of 0.004 g/sec. [Formula 1] Water absorption rate of orally disintegrating tablet = (mass of orally disintegrating tablet after measurement of time for test solution to be absorbed - mass of orally disintegrating tablet before measurement of time for test solution to be absorbed) / time for test solution to penetrate from one end to other end of orally disintegrating tablet (1)
The purpose of the present invention is to provide a gefinitib-containing tablet that has an improved supersaturation-maintaining capacity and an improved tablet stability. The gefinitib-containing tablet according to the present invention is characterized by comprising a plain tablet containing gefinitib and a coating part containing a graft copolymer of polyvinyl alcohol with polyethylene glycol. The tablet may contain 0.5-8.0 wt% inclusive of the graft copolymer of polyvinyl alcohol with polyethylene glycol per 100 wt% of gefinitib.
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 43/00 - Drugs for specific purposes, not provided for in groups
44.
MIRABEGRON-CONTAINING TABLET, METHOD FOR PRODUCING MIRABEGRON-CONTAINING PHARMACEUTICAL PREPARATION AND METHOD FOR PRODUCING MIRABEGRON-CONTAINING GRANULATED PRODUCT
[Problem] To provide a mirabegron-containing tablet which retains the amorphous state of mirabegron after long-term storage; a mirabegron-containing pharmaceutical preparation capable of retaining mirabegron purity by preventing analog formation during storage; a method for producing a mirabegron-containing pharmaceutical preparation; and a method for producing a mirabegron-containing granulated product. [Solution] According to one embodiment of the present invention, provided is a mirabegron-containing pharmaceutical preparation, characterized in comprising mirabegron, and hypromellose and polyvinyl pyrrolidone. The mirabegron-containing pharmaceutical preparation may comprise a spray-dried granulated product comprising the mirabegron and the hypromellose and the polyvinyl pyrrolidone.
Provided is an orally disintegrating tablet coated with film that allows the time elapsed before a film thereof dissolves to be shorter, has a good feel when the tablet is taken, and is capable of being easily mass-produced. The orally disintegrating tablet coated with film is coated with a film coating composition, the film coating composition comprises a water-soluble and ethanol-insoluble film coating base; and at least one plasticizer selected from the group consisting of propylene glycol and polyethylene glycol in a liquid or semisolid state at room temperature. The orally disintegrating tablet coated with film is coated with a film coating composition, the film coating composition comprises a water-soluble and ethanol-insoluble film coating base; and at least one plasticizer selected from the group consisting of propylene glycol and polyethylene glycol in a liquid or semisolid state at room temperature, and contains the plasticizer in 10% by weight or more with respect to a weight of the film coating base.
The present invention addresses the main problem of providing a novel method for producing a freeze-dried preparation (combination drug) for injection that comprises tazobactam sodium and piperacillin sodium. An example of the production method according to the present invention is as follows. A method for producing a freeze-dried preparation for injection, said method being characterized by comprising: (a) a step for blowing carbon dioxide gas into an aqueous sodium hydroxide solution; and (b) a step for dissolving tazobactam and piperacillin in the solution obtained in step (a). According to the present invention, a freeze-dried preparation showing good defoaming performance after redissolution can be obtained.
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 9/19 - Particulate form, e.g. powders lyophilised
A candesartan cilexetil-containing preparation contains candesartan cilexetil and lauromacrogol. The lauromacrogol may be contained at a ratio of 2.4 parts by weight or less with respect to 100 parts by weight of the candesartan cilexetil-containing preparation. The candesartan cilexetil-containing preparation may further contain at least one kind of pharmacologically acceptable additives among a diluent, a disintegrant and a binder.
Provided is an orally disintegrating tablet coated with a film, in which the time required for dissolving the film is short, and which has good feeling upon ingestion and can be produced readily in a large quantity. The orally disintegrating tablet according to the present invention is coated with a composition for film coating purposes, wherein the composition comprises a water-soluble and ethanol-insoluble coating film base material and at least one plasticizer selected from the group consisting of propylene glycol and polyethylene glycol that has a liquid or semisolid form at room temperature. Alternatively, the orally disintegrating tablet according to the present invention is coated with a composition for film coating purposes, wherein the composition comprises a water-soluble and ethanol-insoluble coating film base material and at least one plasticizer selected from the group consisting of propylene glycol and polyethylene glycol that has a liquid or semisolid form at room temperature, and wherein the amount of the plasticizer contained is larger by 10% by weight or more than the amount of the coating film base material.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention provides a pharmaceutical composition containing candesartan cilexetil, which is produced by wet granulation using a dispersion liquid of candesartan cilexetil together with a powder of an additive. The dispersion liquid may contain a water-soluble polymer, a sugar alcohol or a stabilizer. The water-soluble polymer may be hydroxypropyl cellulose. The sugar alcohol may be mannitol. The stabilizer may be lauromacrogol.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
Provided is a stable multilayer tablet containing telmisartan and hydrochlorothiazide, which is suppressed in decomposition of hydrochlorothiazide during storage, or the like. Provided is a multilayer tablet which comprises: a first layer that contains telmisartan, meglumine and a moisture-absorbing substance; and a second layer that contains hydrochlorothiazide. The moisture-absorbing substance may be a porous moisture-absorbing substance. The porous moisture-absorbing substance may be selected from among light anhydrous silicic acid, synthetic aluminum silicate, natural aluminum silicate, calcium silicate, magnesium silicate, magnesium aluminosilicate, magnesium aluminometasilicate, hydrated silicon dioxide and silicon dioxide.
A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
A candesartan cilexetil-containing preparation contains candesartan cilexetil and lauromacrogol. The lauromacrogol may be contained at a ratio of 2.4 parts by weight or less with respect to 100 parts by weight of the candesartan cilexetil-containing preparation. The candesartan cilexetil-containing preparation may further contain at least one kind of pharmacologically acceptable additives among a diluent, a disintegrant and a binder.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention provides: a pitavastatin-containing preparation containing pitavastatin or a pharmacologically acceptable salt thereof and at least one kind of a basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds, and an aqueous solution or an aqueous dispersion of the pitavastatin-containing preparation having a pH of more than 8 and 10 or less; and a method for producing a pitavastatin-containing preparation, including blending at least one kind of a basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds with pitavastatin or a pharmacologically acceptable salt thereof, to make an aqueous solution or an aqueous dispersion of the pitavastatin-containing preparation have a pH of more than 8 and 10 or less.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
The present invention provides: a pitavastatin-containing preparation, which is characterized by containing pitavastatin or a pharmacologically acceptable salt thereof and at least one basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds, and which is also characterized in that an aqueous solution or aqueous dispersion thereof has a pH of more than 8 but 10 or less; and a method for producing a pitavastatin-containing preparation, which is characterized in that the above-described specific basic additive is blended with pitavastatin or a pharmacologically acceptable salt thereof so that an aqueous solution or aqueous dispersion thereof has a pH of more than 8 but 10 or less.
An atrovastatin-containing coated preparation characterized by comprising a solid material comprising atrovastatin, a pharmacologically acceptable salt thereof or a solvate of atrovastatin or the pharmacologically acceptable salt and a coating agent comprising a poly(vinyl alcohol) copolymer, wherein the solid material is coated with the coating agent; and a method for preventing the production of an analogue of atrovastatin, a pharmacologically acceptable salt thereof or a solvate of atrovastatin or the pharmacologically acceptable salt and a method for stabilizing atrovastatin, a pharmacologically acceptable salt thereof or a solvate of atrovastatin or the pharmacologically acceptable salt, each of which is characterized by coating the solid material with a coating agent comprising a poly(vinyl alcohol) copolymer.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
The invention provides an orally disintegrating tablet containing (a) one or more saccharides or sugar alcohols selected from the group consisting of mannitol, lactose, xylitol, sucrose, erythritol and glucose and (b) low substituted hydroxypropylcellulose and substantially free of a starch disintegrant, which tablet is produced by steps of granulating a composition containing the above-mentioned components (a) and (b) by an agitation granulation method, and compression-molding the obtained granulation product. The invention also provides a method of producing an orally disintegrating tablet substantially free of a starch disintegrant, including steps of granulating a composition containing the above-mentioned components by an agitation granulation method, and compression-molding the obtained granulation product.
Disclosed are: a process for producing spherical microparticles comprising tamsulosin hydrochloride; spherical microparticles produced by the process; coated microparticles produced by coating the spherical microparticles; and an orally disintegrating tablet comprising the coated microparticles. The process comprises the following steps (1) to (3): (1) mixing/stirring tamsulosin hydrochloride (a), microcrystalline cellulose (b) and water together until water is penetrated into the mixture of the components (a) and (b) homogeneously; (2) granulating the mixture produced in step (1) into granules by using a rotating granulator in which the peripheral speed is set to 5.5 to 9.0 m/s; and (3) drying the granules produced in step (2).
The purpose of this object is to provide an oral cavity disintegrating tablet which quickly disintegrates in the oral cavity, can be easily produced, has a desired appropriate hardness and is excellent in storage stability, and a method of producing the same. An oral cavity disintegrating tablet which contains (a) one or more sugars or sugar alcohols selected from the group consisting of mannitol, lactose, xylitol, sucrose, erythritol and glucose and (b) a hydroxypropyl cellulose having a low substitution degree and is produced by a process comprising the steps of granulating a composition containing the components (a) and (b) as described above by the agitation granulation method and then compression-molding the granular product thus obtained, wherein the oral cavity disintegrating tablet is substantially free from a starch-based disintegrating agent. A method of producing an oral cavity disintegrating tablet which is substantially free from a starch-based disintegrating agent, comprising the steps of granulating a composition containing the components as described above by agitating and then compression-molding the granular product thus obtained.
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