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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
Authority
WO
WIPO (PCT)
Prior art keywords
tofacitinib
pharmaceutical composition
provides
present
water
Prior art date
Application number
PCT/KR2018/015103
Other languages
English (en)
French (fr)
Other versions
WO2019108021A2 (ko
Inventor
김진환
신동철
황용연
Original Assignee
보령제약 주식회사
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 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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Classifications

    • 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
KR1020170163608A KR102078805B1 (ko) 2017-11-30 2017-11-30 토파시티닙을 포함하는 약제학적 조성물
KR10-2017-0163608 2017-11-30

Publications (2)

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

Family

ID=66664069

Family Applications (1)

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
EP4021451A1 (en) * 2019-08-29 2022-07-06 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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