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WO2012001977A1 - Composition se désagrégeant et article moulé par compression se désagrégeant facilement - Google Patents

Composition se désagrégeant et article moulé par compression se désagrégeant facilement Download PDF

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Publication number
WO2012001977A1
WO2012001977A1 PCT/JP2011/003743 JP2011003743W WO2012001977A1 WO 2012001977 A1 WO2012001977 A1 WO 2012001977A1 JP 2011003743 W JP2011003743 W JP 2011003743W WO 2012001977 A1 WO2012001977 A1 WO 2012001977A1
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WIPO (PCT)
Prior art keywords
disintegrating
weight
parts
starches
starch
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
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PCT/JP2011/003743
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English (en)
Japanese (ja)
Inventor
晴佳 小泉
忠司 深美
淑郎 長井
田中　伸和
町村　等
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FUJI CHMICAL INDUSTRY CO LTD
Original Assignee
FUJI CHMICAL INDUSTRY CO LTD
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Priority to JP2012522471A priority Critical patent/JPWO2012001977A1/ja
Publication of WO2012001977A1 publication Critical patent/WO2012001977A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
    • A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
    • A23G3/346—Finished or semi-finished products in the form of powders, paste or liquids
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
    • A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
    • A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
    • A23L29/212—Starch; Modified starch; Starch derivatives, e.g. esters or ethers
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
    • A23P10/00—Shaping or working of foodstuffs characterised by the products
    • A23P10/20—Agglomerating; Granulating; Tabletting
    • A23P10/28—Tabletting; Making food bars by compression of a dry powdered mixture
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • the present invention relates to starches, which are components that can be used in foods without any restriction on ingestion, as needed, disintegrating compositions for foods made of crystalline cellulose or inorganic substances, and tablet-type compression-molded foods made of these ingredients About.
  • Health foods in the form of tablets are ingested by so-called super disintegrants such as polyvinylpyrrolidone, croscarmellose sodium and sodium carboxymethyl starch used in pharmaceutical tablets, and disintegrants such as carmellose calcium and low-substituted hydroxypropylcellulose. Because of the limitations, most disintegrants cannot be used, and even if they can be used, the amount is so small that a disintegrant having sufficient disintegration is required. In addition, since tablet-shaped health foods contain naturally derived powders and the like, the compounding amount of the utility component is often 40% or more, and an excellent disintegrant is required without compounding much.
  • super disintegrants such as polyvinylpyrrolidone, croscarmellose sodium and sodium carboxymethyl starch used in pharmaceutical tablets
  • disintegrants such as carmellose calcium and low-substituted hydroxypropylcellulose. Because of the limitations, most disintegrants cannot be used, and even if they can be used, the amount is so small that
  • chewable and orally disintegrating tablet-shaped health foods are desired as forms that can be easily taken by elderly people, children, patients who have difficulty in swallowing drugs, and can be easily taken without water.
  • Health foods of these shapes need to be disintegrated only with saliva in the oral cavity, and an excellent disintegrant is required. Moreover, since it disintegrates in the oral cavity, it is also important that the food texture is good.
  • the present inventors have proposed a composite particle composition obtained by spray-drying D-mannitol / erythritol, a super disintegrant, an inorganic substance, etc. as an excipient for an orally rapidly disintegrating compression molded product of a pharmaceutical (patent) References 1, 2).
  • Super disintegrants such as crospovidone and croscarmellose sodium
  • disintegrants such as low-substituted hydroxypropylcellulose have limited amounts that can be used in foods and restrictions on their use, making them difficult to use in foods .
  • An effervescent intraoral quick disintegrating tablet comprising a network maintaining agent such as corn starch and a coloring preventing agent such as xylitol or lactose in an organic acid and carbonate is known (Patent Document 3).
  • a network maintaining agent such as corn starch
  • a coloring preventing agent such as xylitol or lactose in an organic acid and carbonate
  • Patent Document 3 An effervescent intraoral quick disintegrating tablet comprising a network maintaining agent such as corn starch and a coloring preventing agent such as xylitol or lactose in an organic acid and carbonate.
  • An immediate-release compression molding product in which an active ingredient, lactose, corn starch, crystalline cellulose, silicon dioxide, and other pharmaceutical additives are dry-mixed and kneaded and granulated, and then compression-molded (Patent Document 4).
  • Patent Document 4 There is a description about the release of the active ingredient, but there is no description about the disintegration property in the oral cavity.
  • Tablets with compression-molded rice starch, celluloses, D-mannitol, etc. with a moisture content of 6-14% by weight (Patent Document 5), starch such as rice starch and cellulose are granulated at a ratio of 90: 10-50: 50
  • a solid preparation having a practical hardness and disintegration time in which the amount thereof is 60% or more of a tablet is known (Patent Document 6).
  • comment starch is used as a binder, and there is a description of the general tablet formability and disintegration, pharmacopeia disintegration time. There is no description which has the outstanding performance of an orally quick disintegrating tablet using a specific starch.
  • JP 2005-139168 A International Publication WO2007 / 29376 Pamphlet Japanese Patent Laid-Open No. 11-310539 JP 2000-026292 A JP 2006-176696 A JP 2007-332074 A
  • Easy-disintegrating compression-molded product that does not contain highly disintegrating disintegrants, has good hardness, disintegration, and texture and can be widely used in the field of foods and pharmaceuticals, and for foods required for its production
  • An object is to provide a disintegrating compressed composition.
  • starches with a small particle size and low amylose content, and compression molded products containing crystalline cellulose and inorganic substances as required have excellent disintegration. It has been found that an easily disintegrating compression-molded product having sufficient properties, sufficient hardness that does not cause problems during production and transportation, and having a mouthfeel and taste without problems in the oral cavity. Further, it has been found that a composition obtained by granulating starch having a small particle size and a low amylose content has good performance for producing a compression-molded product for food.
  • the compression molded product of the present invention and containing starches with a low amylose content has sufficient hardness that does not cause sticking or capping during compression molding, does not cause problems during production and transportation, and has a good fast disintegration time.
  • the intraoral rapidly disintegrating tablet of the present invention is composed of components that are not particularly restricted, it can be used in a wide range of foods and pharmaceuticals.
  • Example 2 is an SEM photograph (1 memory: 10 ⁇ m) of spray-dried particles of Example 1.
  • the present invention is a starch having a small particle size and a low amylose content (starch of the present invention), a particulate disintegrating composition composed of crystalline cellulose or an inorganic substance, if necessary, and a small particle size, and It is an orally disintegrating compression-molded product containing starches having a low amylose content and, if necessary, crystalline cellulose and inorganic substances.
  • the particulate disintegrating composition of the present invention has a spherical particulate structure in which starches having a small particle diameter and a low amylose content are aggregated and bonded to each other.
  • the average particle size of the particulate disintegrating composition of the present invention may be 10 to 500 ⁇ m, preferably 20 to 300 ⁇ m, more preferably 30 to 200 ⁇ m from the viewpoint of preventing roughness in the oral cavity and disintegration.
  • An average particle diameter is D50 of the integrated diameter calculated
  • the particle shape is preferably spherical, and the sphericity is 0.7 or more, preferably 0.8 or more. The sphericity is obtained by dividing the minor axis of the particle by the major axis from the SEM photograph. From these, since it is the particle
  • the static specific volume of the particle composition of the present invention is preferably 1.0 to 4.0 ml / g, more preferably 1.5 to 3.5 ml / g, still more preferably 1.5 to 3.0 ml / g. It is. Since the particle composition child has such a static specific volume, it can be easily filled into a mortar when it is formed into a tablet, so that the formulation process proceeds smoothly, and the tablet is uniformly compressed and excellent tableting. Can show gender.
  • the static specific volume can be measured according to standard methods.
  • the average particle size of the starch is large, the compression moldability is poor, and it is 1 to 15 ⁇ m, preferably 2 to 10 ⁇ m, more preferably 3 to 8 ⁇ m.
  • Starch is divided into amylose and amylopectin depending on its structure. Starches with a low amylose content contain a large amount of amylopectin. Amylopectin has a structure in which sugar chains are separated, and the more amylopectin, the stronger the aggregation of starch particles. Furthermore, the compression moldability is improved by using starches having a small average particle diameter. After drying, since the starch particles contained in the disintegrating composition have many intergranular voids, the effect of water introduction into the composition is high, and the composition disintegrates with a slight amount of water in the oral cavity. In the present invention, low amylose starches have the same meaning as high amylopectin starches.
  • Starch having a small particle size and low amylose content is starch derived from rice, and most preferably starch derived from glutinous rice. Any of the glutinous rice varieties may be used. Starch derived from glutinous rice contains almost no amylose. Within the range of the amylose content and average particle diameter of the starches of the present invention, glutinous rice and other starches may be mixed. As starches to be mixed, rice starch and waxy corn starch are suitable.
  • the crystalline cellulose used in the disintegrating composition of the present invention those having excellent compression moldability can be used.
  • the average particle size is 10 to 100 ⁇ m
  • the bulk density is 0.1 to 0.5 g / ml
  • the shape is A fibrous or nearly spherical particle can be used.
  • the inorganic substance is a fine inorganic substance having an average particle size of 0.1 to 300 ⁇ m and a high specific surface area.
  • an inorganic substance By including an inorganic substance, there are effects such as a reduction in molding pressure during compression molding of the granulated particles of the present invention, a water-conducting effect in the oral cavity, and an improvement in yield during the production of granulated particles.
  • It is at least one selected from talcite, aluminum silicate, calcium phosphate, calcium carbonate, calcium silicate, magnesium silicate, talc, magnesium oxide, magnesium hydroxide, magnesium alumina hydroxide, dry aluminum hydroxide gel, and the like.
  • it is at least one selected from magnesium carbonate, calcium carbonate, calcium hydrogen phosphate, anhydrous calcium hydrogen phosphate, anhydrous silicic acid, calcium silicate, and talc. More preferably, it is at least one selected from calcium hydrogen phosphate, anhydrous calcium hydrogen phosphate, anhydrous silicic acid, calcium silicate, and talc.
  • the particulate disintegrating composition of the present invention can be mixed with sugars to adjust the taste and disintegration.
  • the saccharide is a saccharide and / or a sugar alcohol, and includes one or more of these.
  • Examples of the saccharide include one or more of mannitol, xylitol, sorbitol, erythritol, maltitol, lactose, sucrose, glucose, fructose, maltose, trehalose, palatinit, and palatinose.
  • Preferred are erythritol, xylitol, maltitol, and mannitol.
  • the particulate disintegrating composition particle composition of the present invention two or more kinds of effective components described later at the time of production and other components that can be combined within a range not impairing the disintegrating property described later can be blended.
  • the compounding amount of the components is 0.1 to 1000 parts by weight, preferably 0.1 to 1000 parts by weight with respect to 100 parts by weight of starches or a total of 100 parts by weight of crystalline cellulose and inorganic substances as necessary. 200 parts by weight, most preferably 0.1 to 100 parts by weight.
  • the particle composition of the present invention can be produced by a wet method capable of obtaining desired physical properties.
  • Commonly used methods such as spray drying, fluidized bed granulation drying, stirring granulation, wet extrusion It can be produced by a wet granulation method such as a granulation method.
  • a method of instantly drying the dispersion using a spray nozzle is preferred, and fluidized bed granulation, stirring granulation, tumbling is performed by spraying the dispersion solution onto the core particles.
  • layer drying and spray drying in which granulation is performed only by the spraying step of the dispersion solution are preferable. Spray drying is most preferred from the standpoint of ease of production and ease of obtaining desired physical properties.
  • each component such as crystalline cellulose and inorganic substance is uniformly dispersed in the solvent, and the particle composition is obtained by quickly removing the solvent. Obtainable. What is necessary is just to set conditions according to the characteristic of each wet granulation apparatus.
  • a production method of the spray drying method it can be produced by dispersing starches, if necessary, crystalline cellulose and inorganic substances in a water-soluble solvent, and spray-drying the dispersion according to a conventional method. More specifically, a dispersion is prepared by adding a water-soluble binder, starches, a molding agent and an inorganic substance to a water-soluble solvent, but there is no particular order of administration, and there is something that you want to completely dissolve. In particular, it is preferable to prepare a dispersion obtained by dissolving or dispersing a water-soluble binder in an aqueous solvent in advance and then uniformly dispersing hardly soluble substances such as starches, molding agents and inorganic substances.
  • the dispersion can be produced by spray drying. Moreover, it can manufacture by spray-drying the dispersion liquid which added 1 or more types of the other component which can be mix
  • the solvent may be any solvent that does not affect the properties of the particle composition and is acceptable for pharmaceuticals and foods. Examples thereof include water and ethanol, and two or more of them may be used in combination.
  • the dispersion can be prepared by a known method, for example, ordinary stirring, colloid mill, high-pressure homogenizer, ultrasonic irradiation, etc., but any method capable of highly dispersing particles in an aqueous dispersion. That's fine.
  • the concentration in the dispersion may be in a range that can be spray-dried depending on the viscosity of the dispersion, that is, 5 to 50% by weight, preferably 10 to 45% by weight.
  • the spray drying conditions are not particularly limited, it is preferable to use a disk-type or nozzle-type spray dryer as the spray dryer.
  • the inlet temperature is preferably about 120 to 300 ° C.
  • the outlet temperature is preferably about 80 to 130 ° C.
  • the particle size of the particle composition can be appropriately adjusted depending on the concentration of the aqueous solution or aqueous dispersion, the spray drying method, the drying conditions, and the like.
  • the production methods of fluidized bed granulation, stirring granulation, and rolling bed granulation can be obtained by spraying a solution in which other components are dispersed using starches, crystalline cellulose, and inorganic substances as core particles. Some insoluble components may also be suspended in the dispersion and sprayed.
  • the production conditions may be set so as to have the structure of the particle composition of the present invention described above.
  • the spraying solvent can be increased, the drying rate can be slowed down, for example, the temperature can be lowered, and the suspension can be easily and uniformly dispersed with the core particles.
  • the collapsible compression molded product of the present invention will be described below.
  • the “easily disintegrating compression molding” in the present invention can rapidly disintegrate in the oral cavity, for example, within 180 seconds, preferably within 60 seconds, more preferably within 40 seconds, and most preferably within 30 seconds.
  • the orally disintegrating time here is the time obtained by the conditions of the orally disintegrating tablets described later and the methods of the examples.
  • the disintegration time in the oral cavity varies depending on the tablet size and tablet shape, and this is also included in the present invention.
  • “texture” that does not cause discomfort in the oral cavity means that it does not feel powdery, mud smell, or the mossiness that increases when the blended raw material absorbs moisture.
  • “Taste” that does not produce a pleasant feeling means that there is no sourness, bitterness, astringency, etc. derived from the raw materials.
  • the easily disintegrating compression molded product of the present invention has a good texture, whereas the compression molded product containing starches having a large amount of amylose and starches having an average particle size of 20 ⁇ m or more absorbs moisture and increases. It is difficult to drink without water when multiple tablets are included in the oral cavity.
  • the collapsible compression-molded product of the present invention comprises an active ingredient, starches with low amylose, and if necessary, crystalline cellulose, an inorganic material, and a lubricant.
  • starch, crystalline cellulose, and inorganic substance having a small amount of amylose those of the aforementioned disintegrating particle composition can be used.
  • the proportion of starches in the disintegrating compression molded product of the present invention is 1 to 90 parts by weight, preferably 5 to 80 parts by weight, more preferably 20 to 70 parts by weight, based on 100 parts by weight of the entire disintegrating compression molded product. It is.
  • the active ingredient is 0.1 to 500 parts by weight and the lubricant is 0.1 to 20 parts by weight with respect to 100 parts by weight of starches, crystalline cellulose, and inorganic substances in total.
  • the active ingredient is 0.1 to 300 parts by weight and the lubricant is 0.5 to 20 parts by weight with respect to 100 parts by weight of the starches, crystalline cellulose and inorganic substances in total.
  • the disintegrating compression molded product of the present invention may contain the particulate disintegrating composition irrespective of the blending ratio in the previous stage.
  • the disintegrating compression-molded product comprises the particulate disintegrating composition of the present invention, an active ingredient, a lubricant, and a pharmaceutical additive described later.
  • starches, crystalline cellulose, and inorganic substances can be added to adjust the moldability and disintegrating property.
  • the active ingredient is 0.1 to 500 parts by weight and the lubricant is 0.1 to 20 parts by weight with respect to 100 parts by weight of the particulate disintegrating composition of the present invention.
  • the active ingredient is 5 to 300 parts by weight and the lubricant is 0.5 to 20 parts by weight with respect to 100 parts by weight of the particulate disintegrating composition of the present invention.
  • the active ingredient, the coating of the active ingredient or the granulated product of the active ingredient can be added to the collapsible compression molded product of the present invention. Since these moldability and disintegration properties change due to their inherent properties, excipients and binders can be added to adjust the moldability and disintegration properties, and these can be added to the particle composition. You may add to a disintegrating compression molding.
  • the addition to the collapsible compression molded product is mixing and compression molding together with the particle composition and active ingredients.
  • filler and a binder are contained in the other component which can be mix
  • the collapsible compression-molded product of the present invention contains pharmaceutical additives such as active ingredients, excipients, binders, surfactants, acidulants, sweeteners, corrigents, fragrances, colorants, stabilizers as necessary. One or more of these are blended. Each blending ratio is 100 parts by weight of starch, crystalline cellulose, and inorganic substance or 100 parts by weight of the particle composition.
  • lubricants such as the aforementioned starches
  • excipients such as the aforementioned starches are preferably mixed in advance in order to improve the formulation process such as fluidity of the particle composition of the present invention.
  • Examples of the lubricant used in the present invention include gum arabic powder, cacao butter, carnauba wax, carmellose calcium, carmellose sodium, caropeptide, hydrous silicon dioxide, dry aluminum hydroxide gel, glycerin, magnesium silicate, light anhydrous silica.
  • Acid light liquid paraffin, crystalline cellulose, hydrogenated oil, synthetic aluminum silicate, sesame oil, wheat starch, white beeswax, magnesium oxide, dimethylpolysiloxane, potassium sodium tartrate, sucrose fatty acid ester, glycerin fatty acid ester, silicone resin, hydroxylated Aluminum gel, stearyl alcohol, stearic acid, aluminum stearate, calcium stearate, polyoxyl stearate, magnesium stearate, cetanol, gelatin, tar , Magnesium carbonate, precipitated calcium carbonate, corn starch (corn starch), lactose, hard fat, sucrose, potato tempun, hydroxypropyl cellulose, fumaric acid, sodium stearyl fumarate, polyethylene glycol, polyoxyethylene polyoxypropylene glycol, polysorbate, Examples include beeswax, magnesium aluminate metasilicate, methyl cellulose, mole, glyceryl monostearate, sodium lauryl
  • excipient in the present invention examples include the aforementioned starches, adipic acid, pregelatinized starch, erythritol, sodium carboxymethyl starch, carmellose, carmellose calcium, carmellose sodium, hydrous silicon dioxide, agar, xylitol, guar gum, Starch acrylate, L-aspartic acid, aminoethylsulfonic acid, aminoacetic acid, candy (powder), gum arabic, gum arabic powder, alginic acid, sodium alginate, pregelatinized starch, inositol, ethylcellulose, ethylene vinyl acetate copolymer, erythritol, chloride Sodium, olive oil, kaolin, cacao butter, casein, fructose, pumice grains, carmellose, carmellose sodium, hydrous silicon dioxide, dry yeast, dry aluminum hydroxide , Dry sodium sulfate, dry magnesium sulfate, agar, agar powder,
  • crystalline cellulose croscarmellose sodium, magnesium aluminate metasilicate, magnesium aluminate silicate, calcium hydrogen phosphate, anhydrous calcium hydrogen phosphate, anhydrous calcium hydrogen phosphate granulated product, calcium silicate, aluminum silicate Silica, magnesium carbonate.
  • binder in the present invention examples include alginic acid, ethyl acrylate / methyl methacrylate copolymer emulsion, acetylglycerin fatty acid ester, aminoalkyl methacrylate copolymer E, aminoalkyl methacrylate copolymer RS, aminoethylsulfonic acid, candy ( Powder), gum arabic, gum arabic powder, sodium alginate, propylene glycol alginate, pregelatinized starch, ester gum H, ethyl cellulose, alum powder, hydrolyzed gelatin powder, sodium caseinate, fructose, caramel, karaya gum powder, carboxyvinyl polymer, Carboxymethylethylcellulose, sodium carboxymethyl starch, carmellose, carmellose sodium, hydrous silicon dioxide, agar, garlic powder, xanthan Oil, beef tallow oil, guar gum, glycerin, synthetic aluminum silicate, light anhydrous silicic
  • the active ingredient is not particularly limited, but it is a nutritional ingredient, so-called health food material, vitamins, peripheral nerve agent, antipyretic analgesic / anti-inflammatory agent, hypnotic sedative, neuropsychiatric agent, etc .; skeletal muscle relaxant Drugs for peripheral nerves such as cardiotonic agents, cardiovascular agents such as cardiotonic agents, arrhythmic agents, diuretics, and vasodilators; drugs for respiratory organs such as bronchodilators and antitussives; digestive agents, intestinal regulating agents, antacids, etc. Gastrointestinal drugs; metabolic drugs such as hormones and antihistamines; anti-ulcer agents; antibiotics; chemotherapeutic agents; herbal extracts;
  • Nutritional ingredients include proteins, carbohydrates, lipids, vitamins, minerals and other beneficial ingredients.
  • vitamins include carotenoids such as astaxanthin, vitamin A, ⁇ -carotene, lutein, zeaxanthin, fursultiamine, fursultiamine hydrochloride, prosultiamine, octothiamine, thiamine disulfide, bisbutyamine, bisbuthiamine Vitamin B1 such as bisibutiamine, benfotiamine, cetotiamine hydrochloride or a derivative thereof or a salt thereof, riboflavin, sodium riboflavin phosphate, sodium flavin adenine dinucleotide, a riboflavin vitamin B2 or a derivative thereof, or a salt thereof, Vitamin C derivatives such as ascorbic acid, ascorbic acid glucoside, L-ascorbyl palmitate, L-ascorbic acid phosphate, tocopherol, tocopherol acetate, co Click tocop
  • Examples of so-called health food materials include deoxyribonucleic acid and salts thereof, adenylic acid derivatives such as adenosine triphosphate and adenosine monophosphate and salts thereof, ribonucleic acid and salts thereof, guanine, xanthine and derivatives thereof and Nucleic acid-related substances such as salt; Serum deproteinized extract, spleen extract, placenta extract, chicken crown extract, royal jelly extract, etc .; yeast extract, lactic acid bacteria extract, bifidobacteria extract, ganoderma extract Extracts from microorganisms such as foods; extracts from plants such as carrot extract, assembly extract, rosemary extract, buckwheat extract, garlic extract, hinokitiol, cephalanthin; ⁇ - or ⁇ -linolenic acid, Eicosapentaenoic acid and derivatives thereof, succinic acid and derivatives thereof, and salts thereof, estradio And derivatives thereof, and salts
  • those having a bitter taste or those that cause release in the digestive tract can be processed by a known method such as coating.
  • a known method such as coating.
  • the method described in JP-A No. 11-263723 that is, an active ingredient, a readily soluble substance such as xylitol, sorbitol, and sucrose, and a water-soluble binder such as polyvinylpyrrolidone, pullulan, hydroxypropylcellulose, hydroxypropylmethylcellulose, gum arabic, and gelatin , And mannitol, lactose, and mannose can be coated with an active ingredient by spray drying, fluidized bed granulation, stirring granulation, kneading granulation, or the like.
  • flavoring and flavoring As long as the astringency, sourness, and bitterness derived from the ingredients can be suppressed by flavoring and flavoring, acidulants (for example, citric acid, tartaric acid, malic acid, ascorbic acid, etc.), sweeteners (sodium saccharin, diglycyrrhizic acid) Potassium, aspartame, stevia, thaumatin, etc.), flavoring agents, flavors (for example, various fruit flavors including lemon oil, orange oil, strawberry and yogurt, mint, menthol, etc.). These flavoring agents and flavoring agents can be blended in an amount of 0.01 to 0.5 parts by weight with respect to 100 parts by weight of the whole tablet.
  • acidulants for example, citric acid, tartaric acid, malic acid, ascorbic acid, etc.
  • sweeteners sodium saccharin, diglycyrrhizic acid
  • Potassium sodium saccharin, diglycyrrhizic acid
  • aspartame ste
  • the disintegrating compression molded product of the present invention can be blended with other ingredients that can be blended in foods as long as the disintegrating property is not impaired.
  • surfactant for example, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene glycol, sorbitan fatty acid ester, polysorbate, glycerin fatty acid
  • Esters sodium lauryl sulfate, etc.
  • foaming agents eg, sodium bicarbonate, sodium carbonate, etc.
  • colorants eg, edible red No. 2, edible blue No. 2, edible yellow No. 5, edible lake pigment, iron sesquioxide, carmine, etc.
  • Stabilizers for example, sodium edetate, tocopherol, cyclodextrin, etc.
  • the collapsible compression-molded product of the present invention comprises an active ingredient, starches, lubricants, at least one selected from crystalline cellulose, inorganic substances, and other additives, and an active ingredient and other ingredients that can be blended with other pharmaceuticals. After mixing, it can be manufactured by compression molding.
  • the starches, if necessary, crystalline cellulose, and inorganic substances can be added after producing the rare particles composition as described above. Since uniformity, texture, disintegration, and compression moldability are more excellent, it is preferable to granulate in advance rather than dry mixing.
  • the compression molding is preferably performed by the direct tableting method, and the molding pressure at that time varies depending on the size of the tablet, but is usually 200 to 2000 kgf, preferably 250 to 1600 kgf, more preferably 250 to 1200 kgf. is there.
  • the collapsible compression molded product of the present invention usually has a hardness of 20 to 150 N, preferably 30 to 120 N, more preferably 40 to 100 N.
  • the disintegrating compression molded product of the present invention is also characterized by good moldability, and does not cause tableting troubles such as sticking and capping during compression molding of tablets.
  • a compression molded product comprising starches having a large amount of amylose or starches having an average particle diameter of 20 ⁇ m or more has poor moldability.
  • a molding pressure of 1500 kg or more is required to set a hardness of 50 N, Prone to sticking and capping.
  • active ingredients starches, crystalline cellulose, and inorganic substances may be wet granulated and then compression molded.
  • wet granulation method include a spray drying method, a fluidized bed granulation drying method, a stirring granulation method, and a wet extrusion granulation method.
  • aging such as heating and humidification can be performed according to a conventional method to impart desired hardness and disintegration.
  • the lubricant may be mixed with other components and then mixed with other compounding components and then compression molded. It is possible to manufacture by compression method (external lubrication method) and apply desired hardness and disintegration to the surface of the punch and the surface of the mortar of the compression molding machine. Can do.
  • the method of applying the lubricant to the mortar can be performed by a conventionally known method or machine.
  • the disintegrating compression-molded product of the present invention can be used as other solid preparations such as those that are not intended for disintegrating tablets in the mouth, such as chewable tablets or tablets that disintegrate in the digestive tract. Can do. In the case of a chewable tablet type or a general tablet, the hardness may be higher than the above-mentioned hardness.
  • the disintegrating compression-molded product of the present invention can be used for foods that disintegrate in the oral cavity because it disintegrates immediately with a small amount of water.
  • Example 2 Production of Particle Disintegrating Composition 80 parts by weight of waxy rice starch, 15 parts by weight of crystalline cellulose, and 5 parts by weight of magnesium carbonate (magnesium carbonate light (food additive): manufactured by Kamishima Chemical Co., Ltd.) are uniformly added to water. After the dispersion, spray drying was performed using a spray dryer at an outlet temperature of 90 to 100 ° C. to obtain a white spherical particle composition having good fluidity.
  • magnesium carbonate magnesium carbonate
  • Example 4 Production of Particle Composition Erythritol (erythritol: manufactured by Mitsubishi Chemical Foods) 5 parts by weight, waxy rice starch 77 parts by weight, crystalline cellulose 15 parts by weight, anhydrous calcium hydrogen phosphate 3 parts by weight uniformly in water After the dispersion, spray drying was performed using a spray dryer at an outlet temperature of 90 to 100 ° C. to obtain a white spherical particle composition having good fluidity.
  • Erythritol erythritol: manufactured by Mitsubishi Chemical Foods
  • Example 5 Production of Particle Composition Maltose (Sanmalto S, Hayashibara Co., Ltd.) 10 parts by weight, waxy rice starch (72 parts by weight, microcrystalline cellulose 15 parts by weight, anhydrous calcium hydrogen phosphate 3 parts by weight in water Then, the mixture was spray-dried at an outlet temperature of 90 to 100 ° C. using a spray dryer to obtain a white spherical particle composition having good fluidity.
  • Example 6 Manufacture of disintegrating compression molded product After mixing 99 parts by weight of the granulated product prepared in Example 1 and 1 part by weight of sucrose stearate (Ryoto Sugar Ester S370, manufactured by Mitsubishi Chemical Foods) Then, the tablet was tableted with a set hardness of 50 N using a rotary tableting machine to obtain tablets having a weight of 200 mg, a diameter of 8 mm, and 9R.
  • Example 7 Manufacture of disintegrating compression-molded product After mixing 99 parts by weight of the granulated product prepared in Example 2 and 1 part by weight of sucrose stearate, tableting was performed with a rotary tableting machine at a set hardness of 50 N. A tablet having a weight of 200 mg, a diameter of 8 mm, and 9R was obtained.
  • Example 8 Production of disintegrating compression molded product After mixing 99 parts by weight of the granulated product produced in Example 3 and 1 part by weight of sucrose stearate, tableting was performed using a rotary tableting machine with a set hardness of 50 N. A tablet having a weight of 200 mg, a diameter of 8 mm, and 9R was obtained.
  • Example 9 Manufacture of disintegrating compression-molded product After mixing 99 parts by weight of the granulated product prepared in Example 4 and 1 part by weight of sucrose stearate, tableting was performed with a rotary tableting machine at a set hardness of 50N. A tablet having a weight of 200 mg, a diameter of 8 mm, and 9R was obtained.
  • Example 10 Manufacture of disintegrating compression-molded product After mixing 99 parts by weight of the granulated product prepared in Example 5 and 1 part by weight of sucrose stearate, tableting was performed with a rotary tableting machine at a set hardness of 50N. A tablet having a weight of 200 mg, a diameter of 8 mm, and 9R was obtained.
  • the tablet was tableted with a set hardness of 50 N using a rotary tableting machine to obtain tablets having a weight of 200 mg, a diameter of 8 mm, and 9R.
  • the compression-molded product containing the low amylose starches of the present invention is excellent in moldability, disintegration time, and texture, and is excellent as an intraoral quick disintegrating tablet.
  • the compression-molded product containing the high amylose starches of Comparative Example 1 causes sticking due to high molding pressure and the like, and because it has a powdery property derived from starch in the oral cavity, as an orally disintegrating tablet Is not suitable.
  • Example 11 to 15 and Comparative Example 1 Effect of blending amount
  • the granulated product produced in Example 1 is lactose blending amount shown in Table 2, citric acid 2 parts by weight, aspartame 0.9 part by weight, lemon flavor 1
  • tableting was performed with a rotary tableting machine with a set hardness of 50 N, and tablets with a weight of 200 mg, a diameter of 8 mm, and 9R were obtained.
  • the disintegration time of the tablet mainly composed of lactose of Comparative Example 1 was 300 seconds or more.
  • the compression-molded product containing the low amylose starches of the present invention has an extremely excellent disintegration property with a disintegration time of 30 seconds or less regardless of the blending amount between 10 and 95.2 parts by weight. ing.
  • Example 16 20 parts by weight of the granulated product produced in Example 1, 21.1 parts by weight of lactose, 5 parts by weight of crystalline cellulose, 50 parts by weight of N-acetylglucosamine, 2 parts by weight of citric acid, 0.9 part by weight of aspartame, orange flavor 1 After mixing 4 parts by weight and 0.7 parts by weight of calcium stearate, the tablet was tableted with a setting hardness of 50 N using a rotary tableting machine to obtain tablets having a weight of 200 mg, a diameter of 8 mm, and 9R. The decay time was 22 seconds.
  • Example 17 82 parts by weight of waxy rice starch, 3 parts by weight of crystalline cellulose and anhydrous calcium hydrogen phosphate were placed in a mortar, and water was added and kneaded to such an extent that the powder became wet. The mixture was sieved with a 150 mesh sieve and dried overnight at 80 ° C. to obtain a white powder. After 99 parts by weight of this powder was mixed with 1 part by weight of sucrose stearate, the tablet was tableted with a set hardness of 50 N using a rotary tableting machine to obtain tablets having a weight of 200 mg, a diameter of 8 mm, and 9R. The decay time was 38 seconds.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Veterinary Medicine (AREA)
  • Nutrition Science (AREA)
  • Animal Behavior & Ethology (AREA)
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Abstract

L'invention concerne un article moulé par compression qui se désagrège et présente une sensation en bouche et un goût favorables dans la cavité buccale, une excellente capacité au formage en comprimé, une dureté suffisante pour éviter des problèmes tels que la transformation en poudre ou l'ébréchure durant le procédé de formulation ou durant la distribution, et une désagrégation favorable dans la cavité buccale, et qui ne contient pas de délitant haute performance pour lequel des restrictions s'appliquent à la consommation. L'article comprimé présentant d'excellentes propriétés de désagrégation peut être produit par inclusion d'un amidon et, en fonction des besoins, d'une cellulose cristalline ou d'une poudre inorganique, avec ensuite un moulage par compression. En utilisant cet article moulé par compression, on peut obtenir un article moulé par compression qui se désagrège et présente une sensation en bouche, un goût, une dureté et des propriétés de désagrégation qui sont excellents, dont la consommation n'est pas limitée, et qui est utilisé dans des applications alimentaires.
PCT/JP2011/003743 2010-06-29 2011-06-29 Composition se désagrégeant et article moulé par compression se désagrégeant facilement Ceased WO2012001977A1 (fr)

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JP2014218447A (ja) * 2013-05-02 2014-11-20 旭化成ケミカルズ株式会社 結晶セルロースの複合組成物
WO2015008825A1 (fr) * 2013-07-19 2015-01-22 株式会社三和化学研究所 Comprimé à désintégration orale
JP2016124856A (ja) * 2014-12-29 2016-07-11 沢井製薬株式会社 ナフトピジル含有口腔内崩壊錠
WO2018003762A1 (fr) * 2016-06-28 2018-01-04 株式会社日本抗菌総合研究所 Excipient et pastille associée
JP2018154573A (ja) * 2017-03-16 2018-10-04 株式会社ファンケル プロテオグリカン含有易崩壊性錠剤

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014218447A (ja) * 2013-05-02 2014-11-20 旭化成ケミカルズ株式会社 結晶セルロースの複合組成物
WO2015008825A1 (fr) * 2013-07-19 2015-01-22 株式会社三和化学研究所 Comprimé à désintégration orale
JP2016124856A (ja) * 2014-12-29 2016-07-11 沢井製薬株式会社 ナフトピジル含有口腔内崩壊錠
WO2018003762A1 (fr) * 2016-06-28 2018-01-04 株式会社日本抗菌総合研究所 Excipient et pastille associée
CN109414051A (zh) * 2016-06-28 2019-03-01 株式会社日本抗菌总和研究所 赋形剂和片剂
JPWO2018003762A1 (ja) * 2016-06-28 2019-04-18 株式会社日本抗菌総合研究所 賦形剤及び錠剤
JP7020688B2 (ja) 2016-06-28 2022-02-16 株式会社日本抗菌総合研究所 賦形剤及び錠剤
JP2022051776A (ja) * 2016-06-28 2022-04-01 株式会社日本抗菌総合研究所 賦形剤及び錠剤
JP7239119B2 (ja) 2016-06-28 2023-03-14 株式会社日本抗菌総合研究所 賦形剤及び錠剤
JP2018154573A (ja) * 2017-03-16 2018-10-04 株式会社ファンケル プロテオグリカン含有易崩壊性錠剤

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