TWI455732B - 經口粉粒狀抗腫瘤劑 - Google Patents

經口粉粒狀抗腫瘤劑 Download PDF

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Publication number
TWI455732B
TWI455732B TW097151038A TW97151038A TWI455732B TW I455732 B TWI455732 B TW I455732B TW 097151038 A TW097151038 A TW 097151038A TW 97151038 A TW97151038 A TW 97151038A TW I455732 B TWI455732 B TW I455732B
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TW
Taiwan
Prior art keywords
antitumor agent
oral
agent according
tegafur
coated
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TW097151038A
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English (en)
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TW200932286A (en
Inventor
Yoshito Ohnishi
Tetsuo Ogata
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Taiho Pharmaceutical Co Ltd
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Publication of TW200932286A publication Critical patent/TW200932286A/zh
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Publication of TWI455732B publication Critical patent/TWI455732B/zh

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; 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
    • A61K9/14—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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (7)

  1. 一種經口粉粒狀抗腫瘤劑，其特徵在於：利用含有甘露醇且不含纖維素衍生物的糖類對含有抗腫瘤劑之粉粒狀組合物進行包衣，該抗腫瘤劑含有(a)替加氟、(b)吉莫斯特及(c)氧酸鉀。
  2. 如請求項1之經口粉粒狀抗腫瘤劑，其中劑型為顆粒劑。
  3. 如請求項1之經口粉粒狀抗腫瘤劑，其以莫耳比為1：0.4：1之比例含有(a)替加氟、(b)吉莫斯特及(c)氧酸鉀。
  4. 如請求項1至3中任一項之經口粉粒狀抗腫瘤劑，其中以包衣膜包覆之粉粒狀物中包含0.5~15質量%之替加氟。
  5. 如請求項1至3中任一項之經口粉粒狀抗腫瘤劑，其中以包衣膜包覆之粉粒狀物中包含5~10質量%之替加氟。
  6. 如請求項1之經口粉粒狀抗腫瘤劑，其中使用甘露醇進行包衣之比例為總包衣量之90~100質量%。
  7. 如請求項1之經口粉粒狀抗腫瘤劑，其中包衣僅以甘露醇進行包衣。
TW097151038A 2007-12-27 2008-12-26 經口粉粒狀抗腫瘤劑 TWI455732B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2007335754 2007-12-27

Publications (2)

Publication Number Publication Date
TW200932286A TW200932286A (en) 2009-08-01
TWI455732B true TWI455732B (zh) 2014-10-11

Family

ID=40823952

Family Applications (1)

Application Number Title Priority Date Filing Date
TW097151038A TWI455732B (zh) 2007-12-27 2008-12-26 經口粉粒狀抗腫瘤劑

Country Status (10)

Country Link
US (3) US20100266706A1 (zh)
EP (1) EP2223683B1 (zh)
JP (3) JP5356255B2 (zh)
KR (1) KR101503559B1 (zh)
CN (1) CN101909602B (zh)
ES (1) ES2476259T3 (zh)
HK (1) HK1148206A1 (zh)
MY (1) MY151207A (zh)
TW (1) TWI455732B (zh)
WO (1) WO2009084216A1 (zh)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5356255B2 (ja) * 2007-12-27 2013-12-04 大鵬薬品工業株式会社 経口粉粒状抗腫瘍剤
SG10201505503WA (en) * 2011-05-25 2015-09-29 Taiho Pharmaceutical Co Ltd Dry-coated tablet containing tegafur, gimeracil and oteracil potassium
EA026665B1 (ru) * 2011-11-24 2017-05-31 Имунекс Фарма Илак Санайи Ве Тикарет А.С. Твердые формы препаратов иматиниба, ресуспензируемые непосредственно перед применением
TWI608849B (zh) * 2014-06-16 2017-12-21 國邑藥品科技股份有限公司 可調控釋放度之高載藥量之醫藥組合物及其製備方法
CN107865871B (zh) * 2016-09-23 2021-09-03 江苏恒瑞医药股份有限公司 一种替吉奥组合物及其制备方法
CN106619689B (zh) * 2016-12-30 2018-05-01 陈晓华 一种用于治疗癌症的药物组合物、试剂盒及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05194200A (ja) * 1991-10-01 1993-08-03 Takeda Chem Ind Ltd 凝集防止剤をコーティングした徐放性微粒子製剤
WO2004087126A1 (en) * 2003-03-31 2004-10-14 Pliva-Lachema A.S. Pharmaceutical composition containing platinum complex as active substance and method of manufacturing thereof
EP1757283A1 (en) * 2004-06-09 2007-02-28 Taiho Pharmaceutical Co., Ltd. Antitumor effect fortifier, antitumor agent and method of therapy for cancer

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JPH0436237A (ja) 1990-06-01 1992-02-06 Taiho Yakuhin Kogyo Kk 抗腫瘍性複合製剤
CA2079509C (en) * 1991-10-01 2002-05-14 Shigeyuki Takada Prolonged release microparticle preparation and production of the same
US6613360B1 (en) * 1998-10-01 2003-09-02 Powderject Research Limited Particle formation
JP5046463B2 (ja) * 2001-05-16 2012-10-10 大塚製薬株式会社 徐放性医薬組成物
ES2739023T3 (es) * 2001-07-06 2020-01-28 Veloxis Pharmaceuticals As Aglomeración controlada
EP1423092A2 (en) * 2001-09-05 2004-06-02 Vectura Limited Functional powders for oral delivery
FR2850576B1 (fr) * 2003-02-05 2007-03-23 Ethypharm Sa Composition comprenant un melange de principes actifs, et procede de preparation
JP4803969B2 (ja) * 2004-03-31 2011-10-26 小林製薬株式会社 植物抽出物を含有する粒剤の製造方法
CN100333726C (zh) * 2004-12-23 2007-08-29 鲁南制药集团股份有限公司 含有替加氟、吉莫斯特和氧嗪酸钾的口腔崩解片
JP4994618B2 (ja) * 2005-08-11 2012-08-08 学校法人北里研究所 Ｔｓ−１／カンプトテシン類による化学放射線療法
JP5356255B2 (ja) * 2007-12-27 2013-12-04 大鵬薬品工業株式会社 経口粉粒状抗腫瘍剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05194200A (ja) * 1991-10-01 1993-08-03 Takeda Chem Ind Ltd 凝集防止剤をコーティングした徐放性微粒子製剤
WO2004087126A1 (en) * 2003-03-31 2004-10-14 Pliva-Lachema A.S. Pharmaceutical composition containing platinum complex as active substance and method of manufacturing thereof
EP1757283A1 (en) * 2004-06-09 2007-02-28 Taiho Pharmaceutical Co., Ltd. Antitumor effect fortifier, antitumor agent and method of therapy for cancer

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Publication number Publication date
JP5356255B2 (ja) 2013-12-04
JP5611403B2 (ja) 2014-10-22
EP2223683B1 (en) 2014-06-18
US20160151295A1 (en) 2016-06-02
HK1148206A1 (en) 2011-09-02
ES2476259T3 (es) 2014-07-14
JP2014012705A (ja) 2014-01-23
CN101909602A (zh) 2010-12-08
EP2223683A1 (en) 2010-09-01
JP2013155184A (ja) 2013-08-15
US20130078309A1 (en) 2013-03-28
TW200932286A (en) 2009-08-01
KR20100101112A (ko) 2010-09-16
KR101503559B1 (ko) 2015-03-17
JPWO2009084216A1 (ja) 2011-05-12
EP2223683A4 (en) 2011-01-19
MY151207A (en) 2014-04-30
JP5722967B2 (ja) 2015-05-27
CN101909602B (zh) 2012-06-13
WO2009084216A1 (ja) 2009-07-09
US20100266706A1 (en) 2010-10-21

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