WO2019108021A3 - 토파시티닙을 포함하는 약제학적 조성물 - Google Patents

토파시티닙을 포함하는 약제학적 조성물 Download PDF

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Publication number
WO2019108021A3
WO2019108021A3 PCT/KR2018/015103 KR2018015103W WO2019108021A3 WO 2019108021 A3 WO2019108021 A3 WO 2019108021A3 KR 2018015103 W KR2018015103 W KR 2018015103W WO 2019108021 A3 WO2019108021 A3 WO 2019108021A3
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WO
WIPO (PCT)
Prior art keywords
tofacitinib
pharmaceutical composition
provides
present
water
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PCT/KR2018/015103
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English (en)
French (fr)
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WO2019108021A2 (ko
Inventor
김진환
신동철
황용연
Original Assignee
보령제약 주식회사
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Application filed by 보령제약 주식회사 filed Critical 보령제약 주식회사
Publication of WO2019108021A2 publication Critical patent/WO2019108021A2/ko
Publication of WO2019108021A3 publication Critical patent/WO2019108021A3/ko

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone

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  • Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 토파시티닙 또는 이의 약학적으로 허용되는 염을 함유하는 코어; 및 상기 코어 상에 수불용성 코팅기제 및 수용성 코팅기제를 함유하는 코팅층을 포함하는 약제학적 조성물에 대한 것이다. 본 발명은 토파시티닙의 초기 방출이 억제되고, 초반 지연 시간(Lag time)을 가지는 약제학적 조성물을 제공하며, 토파시티닙의 유효 혈중농도를 유지시켜 1일 1회 복용이 가능한 약제학적 조성물을 제공한다. 또한, 본 발명은 토파시티닙의 함량균일성, 가용성, 안정성 및 생체이용률이 우수한 약제학적 조성물을 제공한다.
PCT/KR2018/015103 2017-11-30 2018-11-30 토파시티닙을 포함하는 약제학적 조성물 WO2019108021A2 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2017-0163608 2017-11-30
KR1020170163608A KR102078805B1 (ko) 2017-11-30 2017-11-30 토파시티닙을 포함하는 약제학적 조성물

Publications (2)

Publication Number Publication Date
WO2019108021A2 WO2019108021A2 (ko) 2019-06-06
WO2019108021A3 true WO2019108021A3 (ko) 2019-07-25

Family

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Application Number Title Priority Date Filing Date
PCT/KR2018/015103 WO2019108021A2 (ko) 2017-11-30 2018-11-30 토파시티닙을 포함하는 약제학적 조성물

Country Status (2)

Country Link
KR (1) KR102078805B1 (ko)
WO (1) WO2019108021A2 (ko)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220401446A1 (en) * 2019-08-29 2022-12-22 Synthon B.V. Controlled release tofacitinib compositions
CN110787145B (zh) * 2019-12-17 2022-03-29 南京康川济医药科技有限公司 一种枸橼酸托法替布缓释片及其制备方法
CN111184696A (zh) * 2020-02-26 2020-05-22 江苏艾立康药业股份有限公司 一种枸橼酸托法替布缓释片及其制备方法
CN112755000A (zh) * 2021-01-21 2021-05-07 石药集团欧意药业有限公司 一种枸橼酸托法替布缓释片

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20130132630A (ko) * 2011-04-08 2013-12-04 화이자 인코포레이티드 토파시티닙의 결정질 형태 및 비결정질 형태, 및 토파시티닙 및 침투 증진제를 포함하는 제약 조성물
KR20130142168A (ko) * 2011-01-27 2013-12-27 라티오팜 게엠베하 조정된 방출을 위한 타소시티닙 함유 경구투여용 제제
KR20150131238A (ko) * 2013-03-16 2015-11-24 화이자 인코포레이티드 토파시티닙 경구용 지속 방출 투여 형태

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20130142168A (ko) * 2011-01-27 2013-12-27 라티오팜 게엠베하 조정된 방출을 위한 타소시티닙 함유 경구투여용 제제
KR20130132630A (ko) * 2011-04-08 2013-12-04 화이자 인코포레이티드 토파시티닙의 결정질 형태 및 비결정질 형태, 및 토파시티닙 및 침투 증진제를 포함하는 제약 조성물
KR20150131238A (ko) * 2013-03-16 2015-11-24 화이자 인코포레이티드 토파시티닙 경구용 지속 방출 투여 형태

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BURMESTER, G. R.: "Tofacitinib (CP-690,550) in combination with methotrexate in patients with active rheumatoid arthritis with an inadequate response to tumour necrosis factor inhibitors: a randomised phase 3 trial", THE LANCET, vol. 381, 2013, pages 451 - 460, XP002727328, doi:10.1016/S0140-6736(12)61424-X *
CADA, D. J.: "Tofacitinib", HOSPITAL PHARMACY, vol. 48, no. 5, 2013, pages 413 - 424 *

Also Published As

Publication number Publication date
KR20190064215A (ko) 2019-06-10
WO2019108021A2 (ko) 2019-06-06
KR102078805B1 (ko) 2020-02-19

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