WO2020179736A1 - フィルムコーティング組成物及び固形製剤 - Google Patents

フィルムコーティング組成物及び固形製剤 Download PDF

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Publication number
WO2020179736A1
WO2020179736A1 PCT/JP2020/008709 JP2020008709W WO2020179736A1 WO 2020179736 A1 WO2020179736 A1 WO 2020179736A1 JP 2020008709 W JP2020008709 W JP 2020008709W WO 2020179736 A1 WO2020179736 A1 WO 2020179736A1
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Prior art keywords
film coating
coating composition
solid preparation
tablet
tablets
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Ceased
Application number
PCT/JP2020/008709
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English (en)
French (fr)
Japanese (ja)
Inventor
航 伊豆井
克樹 中道
卓也 松川
菊岡　広晃
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Sawai Pharmaceutical Co Ltd
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Sawai Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sawai Pharmaceutical Co Ltd filed Critical Sawai Pharmaceutical Co Ltd
Priority to KR1020217027236A priority Critical patent/KR102692871B1/ko
Priority to EP20766738.7A priority patent/EP3936581A4/en
Priority to JP2021504082A priority patent/JP7317940B2/ja
Priority to CN202080016684.8A priority patent/CN113508165A/zh
Publication of WO2020179736A1 publication Critical patent/WO2020179736A1/ja
Priority to US17/464,473 priority patent/US20210393534A1/en
Anticipated expiration legal-status Critical
Priority to US19/228,026 priority patent/US20250295595A1/en
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D7/00—Features of coating compositions, not provided for in group C09D5/00; Processes for incorporating ingredients in coating compositions
    • C09D7/40—Additives
    • C09D7/65—Additives macromolecular
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/34—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
    • 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
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D129/00—Coating compositions based on homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal, or ketal radical; Coating compositions based on hydrolysed polymers of esters of unsaturated alcohols with saturated carboxylic acids; Coating compositions based on derivatives of such polymers
    • C09D129/02—Homopolymers or copolymers of unsaturated alcohols
    • C09D129/04—Polyvinyl alcohol; Partially hydrolysed homopolymers or copolymers of esters of unsaturated alcohols with saturated carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D151/00—Coating compositions based on graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Coating compositions based on derivatives of such polymers
    • C09D151/08—Coating compositions based on graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Coating compositions based on derivatives of such polymers grafted on to macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D171/00—Coating compositions based on polyethers obtained by reactions forming an ether link in the main chain; Coating compositions based on derivatives of such polymers
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D7/00—Features of coating compositions, not provided for in group C09D5/00; Processes for incorporating ingredients in coating compositions
    • C09D7/40—Additives
    • C09D7/43—Thickening agents
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
    • C09D7/00—Features of coating compositions, not provided for in group C09D5/00; Processes for incorporating ingredients in coating compositions
    • C09D7/40—Additives
    • C09D7/60—Additives non-macromolecular
    • C09D7/63—Additives non-macromolecular organic

Definitions

  • the present invention relates to film coating compositions and solid formulations.
  • Patent Document 1 states that as a technique for improving the cohesiveness of tablets in the oral cavity and facilitating swallowing, a) a first thickener selected from the group consisting of carboxyvinyl polymer and sodium alginate; b) many. A valent metal compound; c) at least one second thickener selected from the group consisting of xanthan gum, guar gum, and sodium alginate in an amount of 10 to 40% by mass based on all components except the solvent (provided that the first If the thickening agent is sodium alginate, the second thickening agent is not sodium alginate); d) 5-35% by weight of hydroxypropyl methylcellulose in all ingredients excluding solvent; and e) excluding solvent.
  • a first thickener selected from the group consisting of carboxyvinyl polymer and sodium alginate
  • a valent metal compound c) at least one second thickener selected from the group consisting of xanthan gum, guar gum, and sodium alginate in an amount of 10 to 40% by
  • Patent Document 2 contains a sugar alcohol and a gelling agent that exhibits slipperiness when in contact with water in order to impart excellent moldability (hardness), slipperiness and the like useful to a solid preparation. Described are particle compositions for easy-to-use solid formulations, characterized in that part or all of the surface of the particle composition is coated with a gelling agent.
  • Patent Document 3 in order to improve swallowability, a water-soluble polymer and guar gum are contained, and guar gum is dispersed in water at a concentration of 1% w/w for 2 hours, and a Brookfield RVT is used at 25°C.
  • guar gum With a minimum viscosity of about 700 cP when measured, guar gum imparts a weight gain of at least about 0.25 wt% to the uncoated tablets coated with an aqueous dispersion containing the film coating composition, a) less than about 3.
  • a powdered film coating composition having a coefficient of static friction; or b) at least one of a coefficient of kinetic friction of less than 5 is described.
  • One embodiment of the present invention provides a film coating composition for a solid dosage form that is easy to take. Also, one embodiment of the present invention provides a solid formulation that is easy to take.
  • a film coating composition containing a polyvinyl alcohol, polyethylene glycol, graft copolymer and a thickener is provided.
  • the thickening agent may be one or more selected from the group consisting of xanthan gum, locust bean gum, pectin, carrageenan, guar gum, gellan gum, and carboxyvinyl polymer.
  • a solid preparation containing an uncoated tablet containing a main agent and a coating layer arranged outside the uncoated tablet and composed of the film coating composition according to claim 1. Provided.
  • a film coating composition for a solid dosage form that is easy to take can be provided. Moreover, according to one embodiment of the present invention, it is possible to provide a solid preparation that is easy to take.
  • the film coating composition according to one embodiment of the present invention contains a polyvinyl alcohol / polyethylene glycol / graft copolymer and a thickener.
  • the thickener include, but are not limited to, xanthan gum, locust bean gum, pectin, carrageenan, guar gum, gellan gum, and carboxyvinyl polymer.
  • the thickening agent may be one or more selected from the group consisting of xanthan gum, carrageenan, and carboxyvinyl polymer.
  • the film coating composition can be used to coat the outer surface of the uncoated tablet containing the active agent. That is, a coating layer in which the film coating composition is solidified is arranged on the outside of the uncoated tablet.
  • the uncoated tablet to be coated is not particularly limited, and is not limited to a circular tablet, and may be an elliptical or polygonal deformed tablet.
  • a tablet having a general size or a mini tablet may be used.
  • tablets of general size can have, for example, a diameter or major axis of 5 mm or more and 20 mm or less.
  • the mini-tablet has a diameter or major axis of less than 5 mm and can be, for example, 1 mm or more and 4 mm or less.
  • the smaller the size of a tablet the easier it is to swallow, and it is said that if the diameter exceeds 8 mm, it becomes difficult to swallow.
  • the tablet size suitable for administration of elderly people with impaired swallowing function is 7 to 8 mm in diameter in the case of a circular tablet. Even if the size of the solid preparation coated with the film coating composition of the present invention exceeds this size, when it gets wet with water such as saliva, the surface becomes gelled and slippery, and the resistance when passing through the throat is reduced. In addition to making it easier to swallow, it is possible to mask tastes such as bitterness derived from drugs.
  • the film coating composition of the present invention can be applied not only to tablets having a size generally used for general purposes but also to mini-tablets having a diameter of about 1 to 4 mm. Mini-tablets have recently attracted attention as a dosage form that can be easily dosed and swallowed by children and the elderly.
  • the mini-tablet coated with the film coating composition of the present invention does not stick to the oral cavity, and a plurality of tablets can be taken together.
  • the film coating composition of the present invention has a simple formulation structure, but adjusts the pharmaceutical properties such as the disintegration property of the solid preparation, the dissolution rate of the film coating layer, or the degree of masking the taste. The desired solid preparation can be easily produced.
  • the film coating composition according to one embodiment of the present invention can be produced by a known production method.
  • the film coating composition is prepared by, for example, dissolving or dispersing polyvinyl alcohol/polyethylene glycol/graft copolymer, a thickener, and optionally a pharmaceutically acceptable additive in a solvent. You may prepare a thing.
  • the solvent used may be any solvent commonly used for film coating, and includes, for example, alcohols such as ethanol and isopropanol, water, or a mixture thereof.
  • the amount of thickener used can be appropriately increased or decreased depending on the type of thickener.
  • the appropriate amount of the thickener varies depending on the type, but it is preferable that the amount is less than that of the polyvinyl alcohol/polyethylene glycol/graft copolymer. % Or less, 1% by weight or more and 10% by weight or less, or 2% by weight or more and 7% by weight or less.
  • a solid preparation having a coating layer can be manufactured by a known manufacturing method.
  • a coating device may be used to spray a film coating composition on a plain tablet for coating, and the solvent may be removed to produce a solid preparation having a coating layer.
  • Examples 1 to 15 In Examples 1 to 15 of the present invention, polyvinyl alcohol/polyethylene glycol/graft copolymer (Kollicoat (registered trademark) IR, BASF), a thickener and other additives were dissolved in a water/ethanol mixed solution (8:2). Dispersed to prepare a film coating composition.
  • a thickener selected from xanthan gum, iota carrageenan, kappa carrageenan, locust bean gum, LM pectin, HM pectin, guar gum, gellan gum and carboxyvinyl polymer was examined.
  • the compositions of the film coating compositions of Examples 1 to 15 are shown in Tables 1 to 3.
  • compositions of the film coating compositions of Examples 1 to 15 are shown in Tables 1 to 3.
  • Comparative Examples 2 to 7 As Comparative Example 2, a film coating composition was prepared without using a thickener and using only polyvinyl alcohol/polyethylene glycol/graft copolymer. As Comparative Example 3, a film coating composition was produced using the same amount of polyvinyl alcohol / polyethylene glycol / graft copolymer and thickener. In Comparative Examples 4 to 7, hypromellose (hereinafter, also referred to as HPMC) or hydroxypropyl cellulose (hereinafter, also referred to as HPC) was used instead of the polyvinyl alcohol/polyethylene glycol/graft copolymer used in Examples 1 to 15. To produce a film coating composition.
  • HPMC hypromellose
  • HPC hydroxypropyl cellulose
  • the polyvinyl alcohol/polyethylene glycol/graft copolymer used in Examples 1 to 15 was used as HPMC (TC-5 (registered trademark) M, Shin-Etsu Chemical Co., Ltd.) or HPC (SSL). , Shin-Etsu Chemical Co., Ltd.), and other additives were added, and the same manufacturing method as in Examples 1 to 15 was used.
  • HPMC TC-5 (registered trademark) M, Shin-Etsu Chemical Co., Ltd.
  • HPC HPC
  • the compositions of the film coating compositions of Comparative Examples 2 to 7 are shown in Tables 4 to 5.
  • the film coating compositions of Comparative Examples 3 to 5 had extremely high viscosity and were difficult to prepare, and it was impossible to produce a solid preparation.
  • a coating device (LABO, Freund Sangyo Co., Ltd.) was used to spray the uncoated tablet ( ⁇ 9 mm) obtained in Comparative Example 1 so that the film coating composition had a solid content of 3 w/w% per tablet. Solid formulations 2, 6 and 7 were obtained.
  • Comparative Example 8 As Comparative Example 8, a film coating composition was produced according to Example 1 described in Patent Document 1. Specifically, HPMC, HPC, carboxyvinyl polymer, calcium chloride dihydrate, jet mill ground xanthan gum and jet mill ground erythritol were dispersed in ethanol to prepare a film coating composition of Comparative Example 8. The composition of the film coating composition of Comparative Example 8 is shown in Table 6. With a coating device (LABO, Freund Sangyo Co., Ltd.), the film coating composition was sprayed onto a plain tablet ( ⁇ 9 mm) as a solid content so that 3 w/w% per tablet was obtained to obtain a solid preparation of Comparative Example 8. ..
  • compositions of the film coating compositions of Comparative Examples 2 to 8 are shown in Tables 4 to 6.
  • FIG. 1 is a schematic view showing a method for measuring maximum stress according to an embodiment of the present invention.
  • a small bench tester (SHIMADZU EZ-LX) manufactured by Shimadzu Corporation was used to measure the maximum stress.
  • the silicon tube 101 (9 mm in diameter) was filled with 3 tablets of uncoated tablets or solid preparation 103 having a diameter of 9 mm and soaked in water for 2 seconds, and was extruded from above the silicon tube 101 using a cylindrical plunger 105 having a diameter of 5 mm.
  • the lower part of the silicon tube 101 is fixed by a stainless steel plate 107 having a hole of the same size as the outer diameter of the silicon tube 101, and the maximum stress when passing through the fixed portion was measured.
  • the maximum stress was obtained as an average value of three measurements.
  • the maximum stresses of the measured uncoated tablets or solid preparations of Examples and Comparative Examples are shown in Tables 1 to 6, respectively.
  • the solid preparations of Examples 1 to 15 using the film coating composition of the present invention had a maximum stress of about 4 N or less.
  • Comparative Example 1 of an uncoated tablet which had a strong resistance to the throat in the sensory test and was difficult to swallow
  • Comparative Examples 6 and 7 of the solid preparation coated with a general film which caused a feeling of sticking in the oral cavity. was good.
  • Tables 1 to 6 show the disintegration time of the uncoated tablets or solid preparations of the measured examples and comparative examples, and the dissolution time of the film coating layer, respectively.
  • the disintegration time is preferably 60 minutes or less, more preferably 30 minutes or less, because it is not preferable that the disintegration time is extremely extended by applying the film coating.
  • the dissolution time of the film coating layer is preferably 20 seconds or more in consideration of the time required for swallowing by the recipient, and is preferably 30 seconds or more in consideration of a patient whose swallowing function is deteriorated. ..
  • the dissolution time of the film coating layer of Comparative Example 2 was only 11 seconds, which was in agreement with the result of the sensory test. Further, it was found that, unlike the mini tablet described in Patent Document 1, Comparative Example 8 was applied to a tablet having a general size ( ⁇ 9 mm), and the disintegration time was extremely delayed.
  • Example 16 Polyvinyl alcohol, polyethylene glycol, graft copolymer (Kollicaat (registered trademark) IR, BASF), xanthan gum, titanium oxide and talc as thickeners are dissolved and dispersed in a water / ethanol mixed solution (8: 2) to prepare a film coating composition. Prepared. In the coating apparatus (LABO, Freund Sangyo Co., Ltd.), the film coating composition was sprayed on the uncoated tablets of the mini-tablet obtained in Comparative Example 9 as a solid content so as to be equivalent to 13 w / w% per tablet, and the examples were carried out. 16 solid formulations were obtained.
  • Comparative Example 10 As Comparative Example 10, a film coating composition was prepared without using the xanthan gum used in Example 16. In a coating device (LABO, Freund Sangyo Co., Ltd.), the uncoated tablets of the mini-tablets obtained in Comparative Example 9 were sprayed with the film coating composition so that the solid content was equivalent to 13 w/w% per tablet, and Comparative Example 10 solid formulations were obtained.
  • a coating device LABO, Freund Sangyo Co., Ltd.
  • compositions of the film coating compositions of Example 16 and Comparative Example 10 are shown in Table 7.
  • Example 16 With respect to the plain tablets or solid preparations of Example 16 and Comparative Examples 9 to 10 described above, three test subjects (adult male) took 84 tablets each to confirm the feeling of ingestion. In Example 16, when it was taken, it took 20 to 30 seconds until the bitterness due to the drug was felt, but in Comparative Examples 9 to 10, the bitterness was felt immediately after taking the drug.
  • Example 16 when taken, the tablets did not stick to each other in the oral cavity, and the tablets adhered easily to each other, but in Comparative Examples 9 to 10, the tablets were not collected together and it was difficult to take.
  • the maximum stress in the case of using the solid preparation of ⁇ 2 mm is larger than that in the case of using the solid preparation of ⁇ 9 mm, because the larger surface area causes the frictional force with the silicon tube to increase.
  • the solid preparation of Example 16 using the film coating composition of the present invention was compared to the plain tablet Comparative Example 9 in which the tablets were hard to be taken in the sensory test without being cohesive. The result was that the slipperiness was also good.

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PCT/JP2020/008709 2019-03-04 2020-03-02 フィルムコーティング組成物及び固形製剤 Ceased WO2020179736A1 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1020217027236A KR102692871B1 (ko) 2019-03-04 2020-03-02 필름 코팅 조성물 및 고형 제제
EP20766738.7A EP3936581A4 (en) 2019-03-04 2020-03-02 FILM COATING COMPOSITION AND SOLID PREPARATION
JP2021504082A JP7317940B2 (ja) 2019-03-04 2020-03-02 フィルムコーティング組成物及び固形製剤
CN202080016684.8A CN113508165A (zh) 2019-03-04 2020-03-02 薄膜包衣组合物和固体制剂
US17/464,473 US20210393534A1 (en) 2019-03-04 2021-09-01 Film coating composition and solid preparation
US19/228,026 US20250295595A1 (en) 2019-03-04 2025-06-04 Film coating composition and solid preparation

Applications Claiming Priority (2)

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JP2019-038589 2019-03-04
JP2019038589 2019-03-04

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US17/464,473 Continuation US20210393534A1 (en) 2019-03-04 2021-09-01 Film coating composition and solid preparation

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US (2) US20210393534A1 (https=)
EP (1) EP3936581A4 (https=)
JP (1) JP7317940B2 (https=)
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CN (1) CN113508165A (https=)
TW (1) TWI791142B (https=)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020189824A (ja) * 2019-05-20 2020-11-26 キョーリンリメディオ株式会社 レベチラセタムを含有する錠剤とその製造方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5426018B2 (https=) 1974-05-01 1979-09-01
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CN113508165A (zh) 2021-10-15
KR20210118164A (ko) 2021-09-29
US20210393534A1 (en) 2021-12-23
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