WO2021182467A1 - 顆粒及びそれを用いた製剤 - Google Patents
顆粒及びそれを用いた製剤 Download PDFInfo
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- WO2021182467A1 WO2021182467A1 PCT/JP2021/009284 JP2021009284W WO2021182467A1 WO 2021182467 A1 WO2021182467 A1 WO 2021182467A1 JP 2021009284 W JP2021009284 W JP 2021009284W WO 2021182467 A1 WO2021182467 A1 WO 2021182467A1
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- Prior art keywords
- polymer
- drug substance
- component
- granules
- molten component
- Prior art date
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- 239000008187 granular material Substances 0.000 title claims abstract description 53
- 238000002360 preparation method Methods 0.000 title claims description 6
- 229920000642 polymer Polymers 0.000 claims abstract description 54
- 239000008186 active pharmaceutical agent Substances 0.000 claims abstract description 47
- 238000002844 melting Methods 0.000 claims abstract description 9
- 230000008018 melting Effects 0.000 claims abstract description 9
- 239000007787 solid Substances 0.000 claims abstract description 9
- 230000009477 glass transition Effects 0.000 claims abstract description 6
- 229940088679 drug related substance Drugs 0.000 claims description 34
- 239000000654 additive Substances 0.000 claims description 20
- 229920003144 amino alkyl methacrylate copolymer Polymers 0.000 claims description 12
- 235000021355 Stearic acid Nutrition 0.000 claims description 10
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical group CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 10
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 10
- 239000008117 stearic acid Substances 0.000 claims description 10
- 229920003147 ammonioalkyl methacrylate copolymer Polymers 0.000 claims description 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 229920002884 Laureth 4 Polymers 0.000 claims description 6
- 230000000996 additive effect Effects 0.000 claims description 6
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 229960003943 hypromellose Drugs 0.000 claims description 4
- IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical class CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 claims description 3
- 239000007884 disintegrant Substances 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 3
- 239000000155 melt Substances 0.000 abstract description 17
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 9
- 239000000126 substance Substances 0.000 abstract description 9
- 238000007909 melt granulation Methods 0.000 description 15
- 238000000034 method Methods 0.000 description 14
- 239000002245 particle Substances 0.000 description 11
- 229920003134 Eudragit® polymer Polymers 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 5
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 229940117841 methacrylic acid copolymer Drugs 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000007908 dry granulation Methods 0.000 description 3
- 239000000825 pharmaceutical preparation Substances 0.000 description 3
- 239000002775 capsule Substances 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 229940127557 pharmaceutical product Drugs 0.000 description 2
- 238000005096 rolling process Methods 0.000 description 2
- 229960004115 sitagliptin phosphate Drugs 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- RTZRUVMEWWPNRR-UHFFFAOYSA-N tert-butyl n-(3-iodo-1h-pyrrolo[2,3-b]pyridin-5-yl)carbamate Chemical compound CC(C)(C)OC(=O)NC1=CN=C2NC=C(I)C2=C1 RTZRUVMEWWPNRR-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 0 C(C1)C2C1C1*C2C1 Chemical compound C(C1)C2C1C1*C2C1 0.000 description 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000011361 granulated particle Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- -1 hypromellose acetate succinate ester Chemical class 0.000 description 1
- 238000007561 laser diffraction method Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000006191 orally-disintegrating tablet Substances 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000000790 scattering method Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Images
Classifications
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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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
Definitions
- the present invention relates to granules having a high content, a drug substance, and a uniform particle size, and a preparation using the same.
- the drug substance is granulated with various additives.
- the granulation method is divided into wet granulation and dry granulation depending on the presence or absence of a solvent.
- a dry granulation method that does not use a solvent is selected.
- the melt granulation method in which the additive is melted by heat and used as a binder is used.
- Patent Document 1 describes drug-containing particles produced by the melt granulation method.
- the particles described in Patent Document 1 have not been studied at all for the control of granulated particles.
- one object of the present invention is to provide a molten granulated product having a high drug content.
- Another object of the present invention is to provide a pharmaceutical composition using the molten granulated product.
- a granule containing a drug substance, a molten component, and a polymer, to which the drug substance, the molten component, and the polymer are bound.
- the polymer may be solid at room temperature and have a glass transition point of 100 ° C. or lower.
- the polymer may be selected from the group consisting of aminoalkyl methacrylate copolymers, ammonioalkyl methacrylate copolymers, methacrylic acid copolymers, hypromellose acetate succinates, or polyvinylpyrrolidone. good.
- the drug substance, the molten component, and the polymer may have a structure in which they are melted and mixed with each other.
- It may have a structure in which a part of the drug substance, the molten component, and the polymer is melted and bonded to each other.
- 50% by mass or more of the drug substance may be contained with respect to the total mass of the drug substance, the molten component and the polymer.
- a pharmaceutical product containing any of the above granules and one or more pharmaceutically acceptable additives is provided.
- the additive may be a disintegrant.
- granules having a high content of API and a uniform particle size are provided.
- a preparation containing granules having a high content of a drug substance and a uniform particle size is provided.
- FIG. 1 is a schematic view (cross-sectional view) showing the granules 10 according to the embodiment of the present invention.
- Granule 10 contains drug substance 11, melt component 13, and polymer 15.
- the granule 10 is a particle formed by binding the drug substance 11, the molten component 13, and the polymer 15 by melt granulation.
- the API 11 is not particularly limited.
- a solvent, particularly water is not used, so that a water-unstable API can be preferably used.
- the melt component 13 constituting the granule 10 is selected from oil-based additives applicable to melt granulation. Further, the molten component 13 is preferably selected from additives in which the API 11 is not denatured or a significant increase in related substances is observed due to contact with the API 11. Since the granules 10 are formed by the melt granulation method, the melt component 13 is selected from additives that are solid at room temperature. Considering the temperature range generally used in the melt granulation method, the melt component 13 is preferably selected from the additives having a melting point of 100 ° C. or lower, and the drug substance 11 is denatured and a remarkable increase in related substances is observed. It is preferable to select from additives having a melting point in a temperature range that does not cause damage. Further, the molten component 13 is selected in consideration of the combination with the polymer 15.
- the polymer 15 is compatible with the molten component and is selected from additives applicable to melt granulation.
- the polymer is "compatible" with respect to the molten component, it means that the molten component and the polymer are not separated from each other. Alternatively, it indicates a state in which the polymer is dispersed in the molten component, or a state in which the molten component is dispersed in the polymer. In one embodiment, the state in which the molten component and the polymer are not separated is confirmed by an increase in the viscosity of the mixture (liquid or semi-solid having fluidity) when the molten component and the polymer are mixed and the molten component is melted. can do.
- the polymer 15 is preferably selected from additives in which the API 11 is not denatured by contact with the API 11 or a significant increase in related substances is observed.
- the polymer 15 is selected from additives that are solid at room temperature. Considering the temperature range generally used in the melt granulation method, the polymer 15 is preferably selected from additives having a glass transition point of 100 ° C. or lower, and the drug substance 11 is modified or a significant increase in related substances is observed. It is preferable to select from additives having a glass transition point in a temperature range that is not recognized. Further, the polymer 15 is selected in consideration of the combination with the molten component 13.
- the polymer 15 is an aminoalkyl methacrylate copolymer, an ammonioalkyl methacrylate copolymer, a methacrylic acid copolymer, or hypromellose.
- Acetate ester succinate or polyvinylpyrrolidone can be combined.
- stearic acid can be combined as the melt component 13
- aminoalkyl methacrylate copolymer, ammonioalkyl methacrylate copolymer, or polyvinylpyrrolidone can be combined as the polymer 15.
- lauromacrogol as the molten component 13 and aminoalkyl methacrylate copolymer, ammonioalkyl methacrylate copolymer, methacrylic acid copolymer, or hypromellose acetate succinate ester can be combined as the polymer 15.
- the drug substance 11, the melt component 13, and the polymer 15 need only form granules, and the drug substance 11, the melt component 13, and the polymer 15 are melted and mixed with each other. It may have a structure in which a part of the drug substance 11, the molten component 13, and the polymer 15 are melted and bonded to each other.
- FIG. 2 is a flow chart illustrating a method for producing granules according to an embodiment of the present invention.
- the drug substance 11, the melt component 13 and the polymer 15 are mixed, and the drug substance 11, the melt component 13 and the polymer 15 are melted and granulated by a melt granulation method to form granules 10 (S101).
- the temperature of these additives is heated to a temperature equal to or higher than the melting point of the molten component 13 and equal to or higher than the glass transition point of the polymer 15.
- the heating temperature is 100 ° C. or lower. It is preferable to perform melt granulation in a temperature range in which the API 11 is not denatured or a significant increase in related substances is observed.
- the drug substance 11, the molten component 13, and the polymer 15 can be bound to each other to produce the granules 10.
- the granules 10 can be easily produced by the melt granulation method.
- a preparation using the granule 10 can be produced.
- granules 10 and a pharmaceutically acceptable known additive may be mixed to prepare a pharmaceutical composition.
- the pharmaceutical composition may be tableted into tablets.
- the pharmaceutical composition to which the disintegrant is added may be tableted to obtain an orally disintegrating tablet.
- the pharmaceutical composition may be encapsulated in a capsule to form a capsule tablet.
- aminoalkyl methacrylate copolymer E (Evonik, Eudragit (registered trademark) EPO), ammonioalkyl methacrylate copolymer RL (Evonik, Eudragit (registered trademark) RLPO), methacrylate copolymer L (Evonik, Eudragit (registered trademark)) L100-55), hypromellose acetate succinate (Shin-Etsu Chemical Co., Ltd., Shin-Etsu AQOAT® HPMC AS LF), or polyvinylpyrrolidone (BASF, K30) was used.
- Example 1 310.2 g of sitagliptin phosphate as a drug substance, 37.5 g of stearic acid (Nichiyu Co., Ltd.) as a melting component, and 37.5 g of aminoalkyl methacrylate copolymer E (Ebonic, Eudragit® EPO) as a polymer. It was put into a dynamic granulator (Paurec Co., Ltd., MP-01), and the rotor rotation speed was 400 rpm, the supply air volume was 0.24 L / min to 0.37 L / min, and the supply air temperature was 82.9 ° C to 89.6 ° C. Granulation was performed for 100 minutes. At this time, the temperature of the additive was 55.4 ° C to 68.1 ° C.
- SEM scanning electron microscope
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
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- Molecular Biology (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
図2は、本発明の一実施形態に係る顆粒の製造方法を説明するフロー図である。原薬11、溶融成分13及びポリマー15を混合し、溶融造粒法により、原薬11、溶融成分13及びポリマー15を溶融させて造粒し、顆粒10を形成する(S101)。このとき、これらの添加剤の温度を、溶融成分13の融点以上、且つポリマー15のガラス転移点以上の温度に加熱する。溶融造粒法に一般に用いられる温度範囲を考慮すると、加熱温度は100℃以下である。なお、原薬11が変性したり類縁物質の顕著な増加が認められたりしない温度範囲で溶融造粒することが好ましい。
顆粒10を用いた製剤を製造することができる。例えば、顆粒10と医薬的に許容された公知の添加剤とを混合して医薬組成物としてもよい。また、医薬組成物を打錠して錠剤としてもよい。また、崩壊剤を添加した医薬組成物を打錠して口腔内崩壊錠としてもよい。また、医薬組成物をカプセルに封入してカプセル錠としてもよい。
溶融成分1g、ポリマー1gを混合後、80℃で2時間加熱した。また、第1の溶融成分2gも同様に80℃、2時間加熱し、溶融成分のみとポリマーを混合した溶融成分の粘度の比較を手触りで評価した。溶融成分としてラウロマクロゴール(日本サーファクタント工業株式会社)、ステアリン酸(日油株式会社)又は硬化油(フロイント産業、ラブリワックス)を用いた。また、ポリマーとして、アミノアルキルメタクリレートコポリマーE(エボニック社、オイドラギット(登録商標)EPO)、アンモニオアルキルメタクリレートコポリマーRL(エボニック社、オイドラギット(登録商標)RLPO)、メタクリル酸コポリマーL(エボニック社、オイドラギット(登録商標)L100-55)、ヒプロメロース酢酸エステルコハク酸エステル(信越化学工業株式会社、Shin-Etsu AQOAT(登録商標)HPMC AS LF)、又はポリビニルピロリドン(BASF社、K30)を用いた。
原薬としてシタグリプチンリン酸塩310.2gと、溶融成分としてステアリン酸(日油株式会社)37.5g、ポリマーとしてアミノアルキルメタクリレートコポリマーE(エボニック社、オイドラギット(登録商標)EPO)37.5gを転動造粒機(株式会社パウレック、MP-01)に投入し、ロータ回転数400rpm、給気風量 0.24L/min~0.37L/min、給気温度82.9℃~89.6℃で100分間造粒した。このとき、添加剤の温度は55.4℃~68.1℃であった。
原薬としてシタグリプチンリン酸塩310.2gと、溶融成分として硬化油(フロイント産業株式会社、ラブリワックス)37.5g、ポリマーとしてアミノアルキルメタクリレートコポリマーE(エボニック社、オイドラギット(登録商標)EPO)37.5gを転動造粒機(株式会社パウレック、MP-01)に投入し、ロータ回転数400rpm、給気風量 0.24L/min~0.37L/min、給気温度82.9℃~89.6℃で100分間造粒した。このとき、添加剤の温度は55.4℃~68.1℃であった。硬化油とアミノアルキルメタクリレートコポリマーEの相溶性が良くないため、造粒工程後も各成分は造粒されておらず粉末の混合物のままであった。
Claims (9)
- 原薬と、溶融成分と、ポリマーと、を含み、
前記原薬と、前記溶融成分と、前記ポリマーとが結着している、顆粒。 - 前記溶融成分は、常温で固体であり、且つ100℃以下の融点を有する、請求項1に記載の顆粒。
- 前記ポリマーは、常温で固体であり、且つ100℃以下のガラス転移点を有する、請求項1に記載の顆粒。
- 前記溶融成分がステアリン酸又はラウロマクロゴールである場合に、前記ポリマーは、アミノアルキルメタクリレートコポリマー、アンモニオアルキルメタクリレートコポリマー、メタクリル酸コポリマー、ヒプロメロース酢酸エステルコハク酸エステル、若しくはポリビニルピロリドンからなる群から選択される、請求項1に記載の顆粒。
- 前記原薬と、前記溶融成分と、前記ポリマーとが溶融して互いに混合した構造を有する、請求項1に記載の顆粒。
- 前記原薬と、前記溶融成分と、前記ポリマーとの一部が溶融して互いに結着した構造を有する、請求項1に記載の顆粒。
- 前記原薬、前記溶融成分及び前記ポリマーの質量の合計に対して、50質量%以上の前記原薬が含まれる、請求項1に記載の顆粒。
- 請求項1乃至7の何れか一に記載の顆粒と、
医薬的に許容された1つ以上の添加剤と、を含む、製剤。 - 前記添加剤は、崩壊剤である、請求項8に記載の製剤。
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
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CN202180017989.5A CN115209876A (zh) | 2020-03-11 | 2021-03-09 | 颗粒和使用该颗粒的制剂 |
EP21766854.0A EP4119129A4 (en) | 2020-03-11 | 2021-03-09 | GRANULES AND THEIR USE |
KR1020227026916A KR20220123689A (ko) | 2020-03-11 | 2021-03-09 | 과립 및 그것을 이용한 제제 |
JP2022507218A JPWO2021182467A1 (ja) | 2020-03-11 | 2021-03-09 | |
US17/942,333 US20230014578A1 (en) | 2020-03-11 | 2022-09-12 | Granules and preparation using same |
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US202062988083P | 2020-03-11 | 2020-03-11 | |
US62/988,083 | 2020-03-11 |
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US17/942,333 Continuation US20230014578A1 (en) | 2020-03-11 | 2022-09-12 | Granules and preparation using same |
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US (1) | US20230014578A1 (ja) |
EP (1) | EP4119129A4 (ja) |
JP (1) | JPWO2021182467A1 (ja) |
KR (1) | KR20220123689A (ja) |
CN (1) | CN115209876A (ja) |
TW (1) | TW202200118A (ja) |
WO (1) | WO2021182467A1 (ja) |
Citations (3)
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JPH05194193A (ja) * | 1991-11-14 | 1993-08-03 | Dai Ichi Seiyaku Co Ltd | マスクされた粒状物 |
JPH06116138A (ja) * | 1992-03-12 | 1994-04-26 | Taisho Pharmaceut Co Ltd | 経口製剤用組成物 |
JP2016511223A (ja) | 2012-12-21 | 2016-04-14 | サノフイ | フェキソフェナジン高含有固形単位およびその製造法 |
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US5965161A (en) * | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
UA80393C2 (uk) * | 2000-12-07 | 2007-09-25 | Алтана Фарма Аг | Фармацевтична композиція, яка містить інгібітор фде 4, диспергований в матриці |
JP4310605B2 (ja) * | 2001-05-25 | 2009-08-12 | 大塚製薬株式会社 | 医薬用組成物 |
CA2475441C (en) * | 2002-02-21 | 2011-07-05 | Otsuka Pharmaceutical Co., Ltd. | Sustained release preparations and process for producing the same |
EP1757277A4 (en) * | 2004-06-03 | 2012-11-21 | Taisho Pharmaceutical Co Ltd | ORAL PREPARATIONS AND METHOD FOR THEIR MANUFACTURE |
AU2011236548A1 (en) * | 2010-04-07 | 2012-11-01 | Lupin Limited | Controlled release pharmaceutical compositions of tapentadol |
JP2015054822A (ja) * | 2013-09-10 | 2015-03-23 | ニプロ株式会社 | クロピドグレル含有錠剤およびその製造方法 |
EP3454847A4 (en) * | 2016-05-09 | 2019-12-18 | Dispersol Technologies, LLC | IMPROVED DRUG FORMULATIONS |
JP2018083809A (ja) * | 2016-11-16 | 2018-05-31 | 沢井製薬株式会社 | シロドシン含有粒子の製造方法及びシロドシン含有口腔内崩壊錠の製造方法 |
JP6895779B2 (ja) * | 2017-03-17 | 2021-06-30 | 東和薬品株式会社 | アジルサルタン含有固形医薬組成物 |
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2021
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- 2021-03-09 EP EP21766854.0A patent/EP4119129A4/en active Pending
- 2021-03-09 WO PCT/JP2021/009284 patent/WO2021182467A1/ja unknown
- 2021-03-09 KR KR1020227026916A patent/KR20220123689A/ko active Search and Examination
- 2021-03-09 CN CN202180017989.5A patent/CN115209876A/zh active Pending
- 2021-03-10 TW TW110108516A patent/TW202200118A/zh unknown
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Patent Citations (3)
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JPH05194193A (ja) * | 1991-11-14 | 1993-08-03 | Dai Ichi Seiyaku Co Ltd | マスクされた粒状物 |
JPH06116138A (ja) * | 1992-03-12 | 1994-04-26 | Taisho Pharmaceut Co Ltd | 経口製剤用組成物 |
JP2016511223A (ja) | 2012-12-21 | 2016-04-14 | サノフイ | フェキソフェナジン高含有固形単位およびその製造法 |
Non-Patent Citations (2)
Title |
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PAWAR, A. H. ET AL.: "Development and evaluation of taste masked granular formulation of satranidazole by melt granulation technique", JOURNAL OF PHARMACEUTICS, vol. 2014, 789676, 12 February 2014 (2014-02-12), pages 1 - 7, XP055856729 * |
See also references of EP4119129A4 |
Also Published As
Publication number | Publication date |
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KR20220123689A (ko) | 2022-09-08 |
EP4119129A4 (en) | 2024-01-24 |
TW202200118A (zh) | 2022-01-01 |
CN115209876A (zh) | 2022-10-18 |
JPWO2021182467A1 (ja) | 2021-09-16 |
US20230014578A1 (en) | 2023-01-19 |
EP4119129A1 (en) | 2023-01-18 |
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