WO2017002803A1 - 固形製剤の外層用組成物及び該外層用組成物を含む易服用性固形製剤 - Google Patents
固形製剤の外層用組成物及び該外層用組成物を含む易服用性固形製剤 Download PDFInfo
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- WO2017002803A1 WO2017002803A1 PCT/JP2016/069132 JP2016069132W WO2017002803A1 WO 2017002803 A1 WO2017002803 A1 WO 2017002803A1 JP 2016069132 W JP2016069132 W JP 2016069132W WO 2017002803 A1 WO2017002803 A1 WO 2017002803A1
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
-
- 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
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
Definitions
- the present invention relates to a particle composition comprising a sugar alcohol and a water-insoluble polymer, an outer layer composition such as an easy-to-take solid preparation containing a gelling agent that exhibits slipperiness upon contact with the particle composition, and water,
- an outer layer composition such as an easy-to-take solid preparation containing a gelling agent that exhibits slipperiness upon contact with the particle composition, and water
- the present invention relates to a solid preparation containing an outer layer composition.
- the formulation is a dosage form such as a liquid or jelly.
- the active ingredient is high, masking of the taste is difficult, and the active ingredient such as the drug is unstable in water. Therefore, it is difficult to obtain such a dosage form.
- the surface of tablets is coated with a gelling agent, and when exposed to moisture in the oral cavity, it exhibits slipperiness, improving mucosal sliding, and easy to drink Tablets have been developed.
- a gel is freeze-dried to form a tablet; 2) a film having a drug layer sandwiched between gelled layers is punched into a circle; and 3) a tablet is sandwiched between gelled layer films. 4) Processes such as spraying a coating liquid for gelling on tablets are used.
- Patent Document 1 includes a first thickener, a polyvalent metal compound, and a second thickener which are metal cross-linking thickeners as a coating composition used for an easy-to-take solid preparation.
- COATING COMPOSITION, AND METHOD FOR PRODUCING ORAL COMPOSITION BY SPRAY COATING ON A DRUG CORE CONTAINING ACTIVE INGREDIENT, AND ALCOHOLIC COMPOSITION PRODUCED IN THOSE Is described.
- Patent Document 2 describes a method capable of forming a molded product having a core using a molding material such as a granular material as a raw material, and a rotary cored tablet machine (compression molding means) therefor.
- a molding material such as a granular material as a raw material
- a rotary cored tablet machine compression molding means
- Patent Document 3 aims to provide spherical granules of 100% erythritol, and granulate and dry 100% erythritol ultrafine powder having an average particle size in the range of 0.4 ⁇ m to 23 ⁇ m under the spray of ethanol.
- erythrocyte spherical granules for direct hitting which are obtained by sizing, are described.
- Patent Document 4 as a method for producing excipients used for compression processing for pharmaceuticals and foods, an aqueous sugar alcohol solution is sprayed with a fluidized bed granulation coating apparatus without blending a binder. And a method for producing a sugar alcohol granule aggregate obtained by granulation.
- composition for an outer layer of a solid preparation containing a particle composition containing a sugar alcohol and a water-insoluble polymer, a gelling agent that exhibits slipperiness upon contact with water, and the particle composition, and The invention relating to easy-to-take solid preparations containing the composition for the outer layer is not described.
- the object of the present invention is to solve such problems in the prior art, and to be useful for solid preparations, a particle composition having excellent moldability, the particle composition, and a gel that exhibits slipperiness upon contact with water. It is providing the composition for easy-to-take solid preparations containing an agent, and the solid preparation containing this composition. “Easy to take” generally means that it is easy to swallow (easy to swallow) as a property / characteristic of a solid preparation or the like.
- the objective of this invention is providing the manufacturing method of this easily takeable solid formulation etc. which include only the process of compression-molding by dry type using this composition.
- the present invention provides the following aspects.
- a particle composition comprising a sugar alcohol and a water-insoluble polymer.
- the water-insoluble polymer is microfibrillar cellulose.
- the average fiber length is 0.01 to 2 mm and the average fiber diameter is 0.001 to 1 ⁇ m in the microfibrous cellulose.
- the water-insoluble polymer is crystalline cellulose.
- Aspect 5 The particle composition according to any one of aspects 1 to 4, wherein the sugar alcohol comprises one or more selected from the group consisting of erythritol, xylitol, mannitol, sorbitol, lactitol, isomalt, and maltitol.
- a composition for an easy-to-use solid preparation comprising the particle composition according to any one of Embodiments 1 to 5 and a gelling agent that exhibits slipperiness upon contact with water.
- the gelling agent comprises at least one water-soluble polymer.
- Embodiment 8 Embodiment 8.
- composition according to embodiment 7 wherein the water soluble polymer is selected from the group consisting of carmellose sodium, xanthan gum, sodium alginate, carrageenan, and gelatin.
- the composition according to aspect 6 comprising carmellose sodium, erythritol or xylitol, and microfibrous cellulose.
- a solid preparation comprising the particle composition according to embodiments 1 to 5.
- An easy-to-use solid preparation comprising the composition according to embodiments 6 to 10.
- the easily takeable solid preparation according to aspect 12 which is a granule for food or medicine.
- a ready-to-use solid preparation for food or medicine comprising an inner core coated with the composition for an outer layer according to aspect 10.
- Aspect 15 The method for producing an easily takeable solid preparation according to any one of aspects 12 to 14, comprising only a dry compression molding step.
- a particle composition having excellent moldability which is useful as a composition for an outer layer such as a solid preparation, particularly an easy-to-take solid preparation, is provided.
- an inner layer (inner core) and an outer layer are provided.
- the first aspect of the present invention relates to a particle composition comprising a sugar alcohol and a water-insoluble polymer. As shown in the examples of the present specification, the particle composition has excellent moldability.
- any substance known to those skilled in the art can be used as long as the moldability of the composition can be effectively improved, and it may be a natural product or a synthetic product.
- the water-insoluble polymer examples include microfibrous cellulose, crystalline cellulose, powdered cellulose and various cellulose derivatives known to those skilled in the art. Among these, microfibrous cellulose is particularly preferable.
- Microfibrous cellulose is a cellulose that is generally produced from plant fibers and has a fiber diameter (short diameter) or thickness of several nanometers to 1 ⁇ m. This means that the surface area is remarkably increased, the hydrophilicity that is inherent in cellulose is remarkably increased, and a three-dimensional network structure is formed by entanglement of microfibers. To do.
- Such a dried product of fine fibrous cellulose can be obtained directly in a dry state by any conventionally known technique, for example, by directly pulverizing a cellulose fiber in a dry state with a ball mill (Patent Document 5).
- the water-suspended microfibrous cellulose composed of the microfibrous cellulose microfibrillated with a high-pressure homogenizer in the aqueous dispersion of cellulose fibers is subjected to solvent substitution in the substitution step, and then the solvent is removed by the drying step.
- a dried product of fine fibrous cellulose can be obtained by pulverizing in the pulverizing step (Patent Document 6).
- a preferred example of the microfibrous cellulose is a fiber aggregate having an average fiber length of about 0.01 to 2 mm and an average fiber diameter of about 0.001 to 1 ⁇ m, preferably an average fiber diameter of about 0.01 to 0.00.
- a microfibrous cellulose having a thickness of 1 ⁇ m can be given (Patent Document 2).
- such a microfibrous cellulose (with a water content of 10 to 35% solids) is a product name “CELISH” series (average fiber diameter of about 0.01 to 0.1 ⁇ m), Daicel Finechem Co., Ltd.
- CELISH average fiber diameter of about 0.01 to 0.1 ⁇ m
- crystalline cellulose As typical examples of crystalline cellulose, commercially available products such as Avicel (FMC Corporation), Theolas (Asahi Kasei Chemicals Co., Ltd.), and Viva Poor (Retttenmeier) can be mentioned. As a representative example of powdered cellulose, KC Flock (Nippon Paper Industries) Chemical), ARBOCEL (Letttenmeier), Solka Flock (Kimura Sangyo).
- the sugar alcohol can include any sugar alcohol known to those skilled in the art, for example, one or more selected from the group consisting of erythritol, xylitol, mannitol, sorbitol, lactitol, isomalt, and maltitol.
- the mixing ratio of the sugar alcohol and the water-insoluble polymer in the particle composition can be appropriately selected by those skilled in the art, but is usually preferably in the range of 99: 1 to 80:20 by weight ratio.
- the particle composition can be produced by any granulation method and means known to those skilled in the art. For example, as described in the examples of the present specification, it can be produced by spraying a water-insoluble polymer suspension onto a sugar alcohol.
- the particle composition preferably has the following physical properties. (1) Average particle size: 50 to 500 microns, (2) Water content: 0.1 to 2.0% by weight.
- the second aspect of the present invention is a composition for an easily takeable solid preparation containing the particle composition and a gelling agent that exhibits slipperiness upon contact with water, for example, an outer layer composition of the easily takeable solid preparation.
- the composition also has excellent moldability.
- the “gelling agent that exhibits slipperiness upon contact with water” refers to moisture in the oral cavity when the tablet is taken without water, as described in the examples of the present specification. It means a substance that forms a slippery film on the surface of a solid tablet in the environment, and as a result, can promote the slipperiness of the tablet itself. In addition, the promotion of slipperiness facilitates swallowing of the tablet even when taking with water.
- gelling agents include water-soluble polymers such as those selected from the group consisting of sodium carboxymethylcellulose (also referred to as “carmellose sodium”), sodium alginate, carrageenan, xanthan gum and gelatin. I can do it.
- the water-soluble polymer may be a natural product or a synthetic product.
- the composition include a composition containing carmellose sodium, erythritol or xylitol, and microfibrous cellulose.
- a person skilled in the art can appropriately select the mixing ratio of the particle composition and the gelling agent that exhibits slipperiness when in contact with water, but the weight ratio is preferably in the range of 10:90 to 99: 1.
- Other components can be included as appropriate.
- the composition can be produced by any method and means known to those skilled in the art as described in the examples of the present specification.
- the third aspect of the present invention relates to a solid preparation containing the particle composition of the present invention.
- the particle composition of the present invention can be contained in any constituent or form in a solid preparation.
- an easy-to-use solid preparation containing the ready-to-use solid preparation composition according to the second aspect of the present invention as the outer layer composition can be exemplified.
- ready-to-use solid preparation of the present invention include a ready-to-use solid preparation for food or medicine, which is formed by coating the inner core with the composition for outer layer.
- the granule for foodstuffs or a medicine containing the composition for easy-to-take solid preparations of this invention can be mentioned.
- Such easy-to-take solid preparations are preferably produced using the production methods described below, in addition to any method / means known to those skilled in the art.
- the inner surface of the mortar, the lower end surface of the upper punch, and the upper end surface of the lower punch are filled with the powder composed of the composition for the outer layer containing the gelling agent that exhibits slipperiness upon contact with water and the core tablet separately or simultaneously after compression.
- molding can be mentioned.
- the inner core tablet can be produced by using any method and means known to those skilled in the art using the core molding material, but is preferably obtained by dry-molding the core molding material.
- a lubricant may be applied in advance before applying the powder made of the composition for the outer layer to the inner surface of the mortar, the upper and lower end surfaces, and the lower and upper end surfaces.
- powder means an aggregate of fine solids, and includes, for example, a powder having a size and shape finer than granules or granules. Therefore, the powdery outer layer composition and the core molding material may be used as they are, or any of those known to those skilled in the art such as dry granulation method and wet granulation method. It can be manufactured by the method and means.
- Examples of the dry granulation method include a crushing granulation method and a roll compression method, and include, for example, a step of compressing each component in a powder state into a small lump and appropriately pulverizing and granulating it.
- the wet granulation method is a method of forming a composite by dispersing and drying each component in the presence of water.
- Specific examples of the wet granulation method include spray drying, rolling granulation, and stirring granulation. Examples thereof include spraying methods such as granulation and fluidized bed granulation, freeze-drying methods, and kneading granulation, and these can be produced by any method known to those skilled in the art.
- “mortar”, “upper arm” and “lower arm” mean that the outer layer forming agent and the inner core tablet are compressed from four directions, and as a result, the compressed inner core tablet is It is a member for molding easy-to-use solid preparations coated with the outer layer composition, and as long as it has substantially such functions and characteristics, it has a different name in each powder compression molding machine / device. Also included are members that are called.
- each step such as filling the inner surface of the mortar, the lower end surface of the upper punch, and the upper end surface of the lower punch with the powder made of the composition for the outer layer and the inner core tablet is arbitrary known to those skilled in the art depending on the manufacturing apparatus used. It can be implemented by means / methods.
- the powder comprising the outer layer composition and the inner core tablet can be filled into the inner surface of the die, the upper and lower end surfaces, and the lower upper end surface of the lower core using appropriate means.
- the powder composed of the composition for the outer layer may be divided into a plurality of times. For example, it can be carried out by filling the inner core tablet after filling the powder composed of the outer layer composition and further filling the powder composed of the outer layer composition. It is also possible to perform compression molding of the inner core tablet and compression molding of the powder composed of the outer layer composition at a time.
- the solid preparation of the present invention is an oral preparation also referred to as “nucleated tablet”.
- various functional foods such as nutritional functional foods and health foods, and as a pharmaceutical product Have the uses.
- the “nuclear molding material” can contain various components known to those skilled in the art depending on the respective uses.
- various nutritional components such as proteins, sugars, lipids and minerals; various vitamins and their derivatives; health food materials such as various extracts derived from microorganisms, plants or animals; and sourness
- Various types based on Article 10 of the Food Sanitation Law such as fragrances, sweeteners, excipients, surfactants, lubricants, adjuvants, acidulants, sweeteners, corrigents, fragrances, colorants, and stabilizers It can contain other optional ingredients acceptable as food ingredients (food additives) listed in the list of specified additives or existing additives, and general food and beverage additives
- Examples of the use and types of the above-mentioned medicinal ingredients include, for example, central nervous system drugs, peripheral nervous system drugs, sensory organ drugs, vaginal cardiovascular drugs, respiratory organ drugs, digestive organ drugs, hormone drugs, urine Reproductive organ drugs, other individual organ system drugs, vitamins, nourishing tonics, blood and body fluid drugs, other metabolic drugs, cell utilization drugs, oncology drugs, radiopharmaceuticals, allergy drugs, other Drugs for tissue cell function, herbal medicines, Kampo medicines, other herbal medicines and medicines based on Kampo medicines, antibiotic drugs, chemotherapeutic agents, biological drugs, drugs against parasites, drugs against other pathogenic organisms, antiseptic drugs, Diagnostic drugs, public health drugs, in-vitro diagnostic drugs, and the like.
- the tableting pressure at the time of compression molding is usually in the range of 2 to 100 kN.
- the size, shape, etc. of the solid preparation of the present invention is usually in the range of 3 to 20 mm in diameter and 15 to 2000 mg in weight, and the inner core tablet is usually 1.8 to 18 mm in diameter and weight. It is in the range of 10-1800 mg.
- These all have arbitrary shapes known to those skilled in the art, such as corner flat locks and true flat locks. These can be measured by any method known to those skilled in the art.
- the thickness of the coating layer (outer layer) made of the outer layer composition is about 0.1 to 5 mm.
- Average particle size 2 g of the particle composition is measured using a ⁇ 75 mm automatic shaking sieve (M-2 type, Tsutsui Riken Kikai Co., Ltd.).
- Hardness was measured using a digital Kiya-type hardness meter (Fujiwara Manufacturing Co., Ltd.). The hardness was measured 6 times, and the average value was taken as the measurement result.
- Thickness of outer layer The thickness of the outer layer was determined by measuring the average value of the outer layer of the cross section by using a magnifier with a scale of 10 times (one scale 0.1 mm) after breaking the tablet. When it was difficult to distinguish between the core tablet and the outer layer, food dye was added to the core tablet and measured.
- Slipperiness Three adult men and women took tablets without water and evaluated the slipperiness according to the following four-level evaluation criteria. 4: Long slipperiness and easy to swallow 3: Slippery and easy to swallow 2: Slightly slippery but difficult to swallow 1: Slippery and difficult to swallow
- Ease of peeling Five tablets were put in a PE bag and stored for 1 week, and the number of tablets peeled off when held by hand was counted.
- Taste masking effect The average value of the time required for 5 adult men and women to take the tablets without water and feel the taste of the core tablet was taken as the measurement result.
- the obtained particle composition 1 was tableted using a simple tableting machine (HANDTAB-100, Ichihashi Seiki Co., Ltd.) at a tableting compression force of 8 kN, and a tablet having a diameter of 8.0 mm, a corner flat tablet and a weight of 250 mg Obtained.
- HANDTAB-100 Ichihashi Seiki Co., Ltd.
- Particle Composition 4 384 g of maltitol fine powder (Resis, Mitsubishi Chemical Foods) is put into a fluidized bed granulator (FL-LABO, Freund Sangyo Co., Ltd.), and a wet product of microfibrous cellulose (Serish, Daicel Finechem Co., Ltd.) Granulation was carried out by spraying 320 g of a serisch suspension diluted with water to 5% at a rate of 12 g / min to obtain a particle composition 4 of the present invention.
- the obtained particle composition 4 had the following physical property values. (1) Average particle size: 251 microns, (2) Water: 0.62% by weight.
- the obtained particle composition was tableted in the same manner as in Example 1 to obtain a tablet having a diameter of 8.0 mm, a corner flat tablet, and a weight of 250 mg.
- Table 1 shows the hardness measurement results for the tablets obtained in the above Examples and Comparative Examples.
- Example 1 From the results shown in Table 1, in Examples 1, 2, and 4, a particle composition produced by a method including a wet granulation process using a microfibrous slurry, and addition of crystalline cellulose in Example 3
- the tablet obtained using the particle composition produced by the method including the wet granulation step uses the particle composition (Comparative Example 1) obtained in the same granulation method using only the sugar alcohol. Compared with the tablet obtained in this way, it was demonstrated that it has excellent moldability to obtain high tablet hardness.
- Example 1 4.0 g of the particle composition ⁇ obtained in Example 1 and 1.0 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) ⁇ were mixed to obtain the composition of the present invention.
- the obtained composition was compressed at a compression force of 8 kN using a simple tableting machine (HANDTAB-100, Ichihashi Seiki Co., Ltd.) in which a small amount of calcium stearate (Taihei Chemical Industry Co., Ltd.) was applied in advance to the surfaces of the mortar and upper and lower punches. Tableting was performed to obtain a tablet having a diameter of 8.0 mm, a corner flat tablet, and a weight of 250 mg.
- the composition of the present invention was obtained by mixing 4.0 g of the particle composition obtained in Example 2 and 1.0 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.). The obtained composition was tableted in the same manner as in Example 5 to obtain a tablet having a diameter of 8.0 mm, a corner flat tablet, and a weight of 250 mg.
- the composition of the present invention was obtained by mixing 4.0 g of the particle composition obtained in Example 4 and 1.0 g of carmellose sodium (CMC Daicel, Daicel Finechem Co., Ltd.).
- the obtained composition was tableted in the same manner as in Example 5 to obtain a tablet having a diameter of 8.0 mm, a corner flat tablet, and a weight of 250 mg.
- Table 2 shows the hardness measurement results for the tablets obtained in Examples 5 to 7 and Comparative Examples 2 and 3.
- the composition of the present invention comprising a sugar alcohol (particle composition) obtained by spraying and granulating a water-insoluble polymer and a water-soluble polymer.
- the tablet obtained using the product obtained a high tablet hardness with a low compression force as compared with the tablet obtained using a mixture containing a sugar alcohol and a water-soluble polymer (Comparative Examples 2 and 3). It has been demonstrated that it has excellent formability.
- a tablet obtained by using a mixture containing a sugar alcohol and a water-soluble polymer (Comparative Example 2), it is obtained using a mixture containing crystalline cellulose in addition to the sugar alcohol and the water-soluble polymer.
- the tablet tablet (Comparative Example 4) had a tableting compression force of 8 kN and a hardness of 23 N, and although the moldability was improved by adding crystalline cellulose, sufficient moldability could not be obtained by simply adding it. .
- the composition of the present invention is used as an outer layer of an easy-to-use solid preparation, when the cellulose content in the outer layer increases, the amount of moisture absorbed by the cellulose increases, and the time until the slipperiness is developed is delayed. Since a lot of moisture may be required, it is not preferable to increase the amount of cellulose in order to improve moldability.
- Example 1 4.5 g of the particle composition obtained in Example 1 and 0.5 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) were mixed to obtain the composition for the outer layer of the present invention.
- CMC Daicel Daicel Finechem Co., Ltd.
- a simple tablet molding machine (HANDTAB-100, Ichihashi Seiki Co., Ltd.), in which 210 mg of the inner core tablet and 40 mg of the composition for the outer layer were applied in advance to a surface of the mortar and upper and lower heels with a small amount of calcium stearate (Taihei Chemical Industry Co., Ltd.). Tableting was performed at a tablet compression force of 12 kN to obtain a dry-coated tablet having a diameter of 8.0 mm, a straight tablet, and a weight of 250 mg.
- Example 6 is the same as Example 6 except that 4.5 g of the particle composition obtained in Example 2 and 0.5 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) are mixed to obtain the composition for the outer layer of the present invention.
- CMC Daicel Daicel Finechem Co., Ltd.
- a dry-coated tablet having a diameter of 8.0 mm, a true flat tablet and a weight of 250 mg was obtained.
- Example 8 is the same as Example 8 except that 4.5 g of the particle composition obtained in Example 4 and 0.5 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) are mixed to obtain the outer layer composition of the present invention.
- CMC Daicel Daicel Finechem Co., Ltd.
- a dry-coated tablet having a diameter of 8.0 mm, a true flat tablet and a weight of 250 mg was obtained.
- Lactose cake (FlowLac90, Megre Japan Co., Ltd.) 17.9g, Hydroxypropylcellulose candy (HPC-SSL-SFP, Nippon Soda Co., Ltd.) 2.0g, Calcium stearate (Taihei Chemical Industry Co., Ltd.) g 0.1g are mixed. Obtained.
- the obtained mixture was tableted using a simple tablet molding machine (HANDTAB-100, Ichibashi Seiki Co., Ltd.) at a tableting compression force of 5 kN to obtain an inner core tablet having a diameter of 10.0 mm, R14 tablets, and a weight of 400 mg.
- Example 1 4.5 g of the particle composition obtained in Example 1 and 0.5 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) were mixed to obtain the outer layer composition of the present invention.
- carmellose sodium candy CMC Daicel, Daicel Finechem Co., Ltd.
- Example 11 is the same as Example 11 except that 4.5 g of the particle composition obtained in Example 2 and 0.5 g of carmellose sodium candy (CMC Daicel, Daicel Finechem Co., Ltd.) are mixed to obtain the outer layer composition of the present invention.
- a dry-coated tablet having a diameter of 12.0 mm, R14 tablets, and a weight of 600 mg was obtained.
- the outer layer of the present invention comprising a sugar alcohol (particle composition) obtained by spraying and granulating a water-insoluble polymer and a water-soluble polymer.
- a sugar alcohol particle composition
- the dry coated tablet coated with the composition for the outer layer does not impair the slipperiness. It has been demonstrated that it has excellent properties with suppressed ease of peeling.
- Lactose cake (FlowLac90, Megre Japan Co., Ltd.) 13.7g, Hydroxypropylcellulose candy (HPC-SSL-SFP, Nippon Soda Co., Ltd.) g 2.0g, Vitamin C ⁇ ⁇ ⁇ ⁇ (Vitamin C, Iwaki Pharmaceutical Co., Ltd.) 4.0g, Sucralose candy (Sucralose) , Saneigen FFI Co., Ltd.) 0.2 g and magnesium stearate (Taihei Chemical Industry Co., Ltd.) 0.1 g were mixed to obtain a mixture.
- the obtained mixture was tableted using a simple tableting machine (HANDTAB-100, Ichibashi Seiki Co., Ltd.) at a tableting compression force of 2 kN to obtain an inner core tablet having a diameter of 10.0 mm, R14 tablets, and a weight of 400 mg.
- HANDTAB-100 Ichibashi Seiki Co., Ltd.
- a dry-coated tablet having a diameter of 12.0 mm, an R14 tablet, and a weight of 800 mg was obtained in the same manner as in Example 13 except that tableting was performed using 400 mg of the composition for outer layer.
- the outer layer of the present invention containing a sugar alcohol (particle composition) obtained by spraying and granulating a water-insoluble polymer and a water-soluble polymer. It was demonstrated that the coated tablet coated with the composition for use has excellent properties in which the ease of peeling of the outer layer is suppressed without impairing the slipperiness and the taste of the tablet is masked. . It was also demonstrated that the taste masking time can be controlled by changing the thickness of the outer layer.
- Formulation 1 was prepared by mixing 267 g of the particle composition obtained in Example 1, 30 g of carmellose sodium (CMC Daicel, Daicel Finechem Co., Ltd.), and 3 g of calcium stearate (Taihei Chemical Industry Co., Ltd.). Formulation 1 was dry granulated (TF-LABO, Freund Sangyo Co., Ltd.) and then pulverized to obtain a gelled granule. The obtained gelled granules were measured for the following characteristics.
- Moldability The moldability of the granules was evaluated according to the following three evaluation criteria. 3: A granulated product with sufficient strength can be obtained. 2: The granulated product collapses when touched by hand. 1: Cannot be granulated.
- Slippery Three adult men and women took the granule without water, and evaluated the slipperiness according to the following three evaluation criteria. 3: Slippery and easy to swallow 2: Slightly slippery but difficult to swallow 1: Hard to slip and difficult to swallow
- Adhesiveness Three adult men and women took the granule without water, and the adhesiveness was evaluated according to the following three evaluation criteria. 3: Does not adhere to the oral cavity 2: Slightly adheres to the oral cavity 1: Strong sense of adhesion to the oral cavity
- Example 15 From the results shown in Table 5, in Example 15, a granule excellent in moldability, slipperiness, and adhesiveness was obtained by using a sugar alcohol obtained by spraying and granulating a water-insoluble polymer. I was able to get it.
- the present invention greatly contributes to research and development related to compositions for outer layers of easily takeable solid preparations.
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Abstract
Description
糖アルコール及び水不溶性高分子を含む粒子組成物。
[態様2]
水不溶性高分子が微小繊維状セルロースである態様1記載の粒子組成物。
[態様3]
微小繊維状セルロースにおける平均繊維長0.01~2mm及び平均繊維径0.001~1μmである、態様2記載の粒子組成物。
[態様4]
水不溶性高分子が結晶セルロースである態様1記載の粒子組成物。
[態様5]
糖アルコールがエリスリトール、キシリトール、マンニトール、ソルビトール、ラクチトール、イソマルト、及びマルチトールから成る群から選択される一つ以上を含む、態様1~4のいずれか一項に記載の粒子組成物。
[態様6]
態様1~5のいずれか一項に記載の粒子組成物及び水に触れると滑り性を示すゲル化剤を含む易服用性固形製剤用組成物。
[態様7]
ゲル化剤が少なくとも1種の水溶性高分子を含む、態様6記載の組成物。
[態様8]
水溶性高分子がカルメロースナトリウム、キサンタンガム、アルギン酸ナトリウム、カラギーナン、及びゼラチンから成る群から選択される、態様7に記載の組成物。
[態様9]
カルメロースナトリウム、エリスリトール又はキシリトール、及び、微小繊維状セルロースを含む、態様6に記載の組成物。
[態様10]
易服用性固形製剤の外層用である態様6~9のいずれか一項に記載の組成物。
[態様11]
態様1~5に記載の粒子組成物を含む固形製剤。
[態様12]
態様6~10に記載の組成物を含む易服用性固形製剤。
[態様13]
食品用又は医薬用の顆粒剤である、態様12に記載の易服用性固形製剤。
[態様14]
態様10に記載の外層用組成物で内核を被覆して成る、食品用又は医薬用の易服用性固形製剤。
[態様15]
乾式で圧縮成形する工程のみを含む、態様12~14に記載のいずれか一項に記載の易服用性固形製剤の製造方法。
(1)平均粒子径:50~500ミクロン、(2)水分:0.1~2.0重量%。
以下の実施例及び比較例で得た各錠剤について、以下の方法によって、組成物の平均粒子径及び水分、並びに、硬度、外層の厚さ、滑りやすさ、外層のはがれやすさ、味マスキング効果を以下の条件・方法で測定した。
水分:粒子組成物5gをハロゲン水分測定器(HB43型、メトラートレド株式会社)を用いて測定する。
4: 滑りやすさが持続しさらに飲み込みやすい
3: 滑りやすく飲み込みやすい
2: わずかに滑りやすいが飲み込みにくい
1: 滑りづらく飲み込みにくい
エリスリトール(エリスリトールT、三菱化学フーズ株式会社)368gを流動層造粒機(FL-LABO、フロイント産業株式会社)に投入し、微小繊維状セルロースの湿潤体(セリッシュ、ダイセルファインケム株式会社)を水で希釈し5%にしたセリッシュ懸濁液 640gを12g/minの速度で噴霧することによって造粒し、本発明の粒子組成物1を得た。尚、得られた粒子組成物1は以下の物性値を有していた。(1)平均粒子径:171ミクロン、(2)水分:0.40重量%。
得られた粒子組成物1を簡易錠剤成形機(HANDTAB-100、市橋精機株式会社)を用い、打錠圧縮力8kNにおいて打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
キシリトール粉砕品(キシリット、三菱化学フーズ株式会社)384gを流動層造粒機(FL-LABO、フロイント産業株式会社)に投入し、微小繊維状セルロースの湿潤体(セリッシュ、ダイセルファインケム株式会社)を水で希釈し5%にしたセリッシュ懸濁液 320gを12g/minの速度で噴霧することによって造粒し、本発明の粒子組成物2を得た。尚、得られた粒子組成物2は以下の物性値を有していた。(1)平均粒子径:296ミクロン、(2)水分:0.28重量%。
得られた粒子組成物2を実施例1と同様に打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
キシリトール粉砕品(キシリット、三菱化学フーズ株式会社)380g、結晶セルロース(セオラス、旭化成ケミカルズ) 20gを流動層造粒機(FL-LABO、フロイント産業株式会社)に投入し、水 320gを12g/minの速度で噴霧することによって造粒し、本発明の粒子組成物3を得た。尚、得られた粒子組成物3は以下の物性値を有していた。(1)平均粒子径:207ミクロン、(2)水分:0.50重量%。
[粒子組成物の評価3]
得られた粒子組成物3を実施例1と同様に打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
マルチトール微粉品(レシス、三菱化学フーズ株式会社)384gを流動層造粒機(FL-LABO、フロイント産業株式会社)に投入し、微小繊維状セルロースの湿潤体(セリッシュ、ダイセルファインケム株式会社)を水で希釈し5%にしたセリッシュ懸濁液 320gを12g/minの速度で噴霧することによって造粒し、本発明の粒子組成物4を得た。尚、得られた粒子組成物4は以下の物性値を有していた。(1)平均粒子径:251ミクロン、(2)水分:0.62重量%。
得られた粒子組成物4を実施例1と同様に打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
エリスリトール(エリスリトールT、三菱化学フーズ株式会社)304gを流動層造粒機(FL-LABO、フロイント産業株式会社)に投入し、30%エリスリトール水溶液320gを12g/minの速度で噴霧することによって造粒し、粒子組成物を得た。尚、得られた粒子組成物は以下の物性値を有していた。(1)平均粒子径:452ミクロン、(2)水分:1.64重量%。
以上の実施例および比較例で得た各錠剤について、硬度の測定結果を表1に示す。
エリスリトール (エリスリトールT微粉、三菱化学フーズ株式会社) 4.0g、カルメロースナトリウム (CMCダイセル、ダイセルファインケム株式会社) 1.0gを混合し、混合物を得た。得られた混合物を、打錠圧縮力14kNにおいて打錠した以外は実施例5と同様にして打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
キシリトール (キシリット微粉、三菱化学フーズ株式会社) 4.0g、カルメロースナトリウム (CMCダイセル、ダイセルファインケム株式会社) 1.0gを混合し、混合物を得た。得られた混合物を、比較例2と同様にして打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
エリスリトール (エリスリトールT微粉、三菱化学フーズ株式会社) 3.5g、カルメロースナトリウム (CMCダイセル、ダイセルファインケム株式会社) 1.0g、結晶セルロース (セオラス、旭化成ケミカルズ) 0.5gを混合し、混合物を得た。得られた混合物を、比較例2と同様にして打錠し、直径8.0mm、隅角平錠、重量250mgの錠剤を得た。
実施例5~7および比較例2、3で得た各錠剤について、硬度の測定結果を表2に示す。
エリスリトール (エリスリトールT微粉、三菱化学フーズ株式会社) 4.5g、カルメロースナトリウム (CMCダイセル、ダイセルファインケム株式会社) 0.5gを混合し、外層用組成物を得た以外は実施例6と同様にして、直径8.0mm、真平錠、重量250mgの有核錠を得た。
実施例8~12および比較例5で得た各錠剤について、硬度、表面のはがれやすさ、滑りやすさを測定した。測定結果を表3に示す。
実施例13及び14で得た各錠剤について、硬度、外層の厚さ、表面のはがれやすさ、滑りやすさ、味マスキング効果を測定した。測定結果を表4に示す。
3:十分な強度の造粒物が得られる
2:手で触ると造粒物が崩れる
1:造粒できない
3: 滑りやすく飲み込みやすい
2: わずかに滑りやすいが飲み込みにくい
1: 滑りづらく飲み込みにくい
3: 口腔内に付着しない
2: 口腔内にわずかに付着する
1: 口腔内への付着感が強い
Claims (15)
- 糖アルコール及び水不溶性高分子を含む粒子組成物。
- 水不溶性高分子が微小繊維状セルロースである請求項1記載の粒子組成物。
- 微小繊維状セルロースにおける平均繊維長0.01~2mm及び平均繊維径0.001~1μmである、請求項2記載の粒子組成物。
- 水不溶性高分子が結晶セルロースである請求項1記載の粒子組成物。
- 糖アルコールがエリスリトール、キシリトール、マンニトール、ソルビトール、ラクチトール、イソマルト、及びマルチトールから成る群から選択される一つ以上を含む、請求項1~4のいずれか一項に記載の粒子組成物。
- 請求項1~5に記載の粒子組成物及び水に触れると滑り性を示すゲル化剤を含む易服用性固形製剤用組成物。
- ゲル化剤が少なくとも1種の水溶性高分子を含む、請求項6記載の組成物。
- 水溶性高分子がカルメロースナトリウム、キサンタンガム、アルギン酸ナトリウム、カラギーナン、及びゼラチンから成る群から選択される、請求項7に記載の組成物。
- カルメロースナトリウム、エリスリトール又はキシリトール、及び、微小繊維状セルロースを含む、請求項6に記載の組成物。
- 易服用性固形製剤の外層用である請求項6~9のいずれか一項に記載の組成物。
- 請求項1~5に記載の粒子組成物を含む固形製剤。
- 請求項6~10に記載の組成物を含む易服用性固形製剤。
- 食品用又は医薬用の顆粒剤である、請求項12に記載の易服用性固形製剤。
- 請求項10に記載の外層用組成物で内核を被覆して成る、食品用又は医薬用の易服用性固形製剤。
- 乾式で圧縮成形する工程のみを含む、請求項12~14に記載のいずれか一項に記載の易服用性固形製剤の製造方法。
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Also Published As
Publication number | Publication date |
---|---|
EP3315137A1 (en) | 2018-05-02 |
KR20180021057A (ko) | 2018-02-28 |
US20180243221A1 (en) | 2018-08-30 |
US11058643B2 (en) | 2021-07-13 |
CN107708737A (zh) | 2018-02-16 |
TW201717915A (zh) | 2017-06-01 |
JPWO2017002803A1 (ja) | 2018-04-19 |
CN107708737B (zh) | 2021-02-05 |
TWI695722B (zh) | 2020-06-11 |
JP6776234B2 (ja) | 2020-10-28 |
EP3315137B1 (en) | 2020-12-30 |
EP3315137A4 (en) | 2019-02-27 |
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