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1. WO2013008981 - SPHERICAL PARTICLES OF CLOPIDOGREL BISULFATE, PHARMACEUTICAL COMPOSITION INCLUDING SAME, AND METHOD FOR MANUFACTURING SAME

Publication Number WO/2013/008981
Publication Date 17.01.2013
International Application No. PCT/KR2011/008071
International Filing Date 27.10.2011
IPC
A61K 9/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
16Agglomerates; Granulates; Microbeadlets
A61K 9/20 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, lozenges or tablets
C07D 495/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/4365 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4365the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
CPC
A61K 31/4365
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4365the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 9/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
A61K 9/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
A61K 9/2018
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
2004Excipients; Inactive ingredients
2013Organic compounds, e.g. phospholipids, fats
2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
A61K 9/2054
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
2004Excipients; Inactive ingredients
2022Organic macromolecular compounds
205Polysaccharides, e.g. alginate, gums; Cyclodextrin
2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
A61K 9/2095
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
Applicants
  • 삼진제약 주식회사 SAMJIN PHARMACEUTICAL CO., LTD. [KR]/[KR] (AllExceptUS)
  • (주)에이에스텍 ASTECH. CO., LTD. [KR]/[KR] (AllExceptUS)
  • 조의환 CHO, Eui Hwan (UsOnly)
  • 신희종 SHIN, Hee Jong (UsOnly)
  • 송우헌 SONG, Woo Heon (UsOnly)
  • 이순환 LEE, Sun Hwan (UsOnly)
  • 윤종배 YOON, Jong Bae (UsOnly)
  • 박종성 PARK, Jong Sung (UsOnly)
Inventors
  • 조의환 CHO, Eui Hwan
  • 신희종 SHIN, Hee Jong
  • 송우헌 SONG, Woo Heon
  • 이순환 LEE, Sun Hwan
  • 윤종배 YOON, Jong Bae
  • 박종성 PARK, Jong Sung
Agents
  • 김현진 KIM, Hyun Jin
Priority Data
10-2011-006903912.07.2011KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) SPHERICAL PARTICLES OF CLOPIDOGREL BISULFATE, PHARMACEUTICAL COMPOSITION INCLUDING SAME, AND METHOD FOR MANUFACTURING SAME
(FR) PARTICULES SPHÉRIQUES DE CLOPIDOGREL BISULFATE, COMPOSITION PHARMACEUTIQUE COMPRENANT CELLES-CI ET PROCÉDÉ DE FABRICATION CORRESPONDANT
(KO) 클로피도그렐 황산수소염의 구형 입자, 이를 포함하는 약학적 조성물 및 이의 제조방법
Abstract
(EN)
The present invention relates to spherical particles of clopidogrel bisulfate having a 10% volume particle diameter (d0.1) of 30 μm or more and a 50% volume particle diameter (d0.5) in the range of 50 to 200 μm, and to a pharmaceutical composition including same. The spherical particles of the present invention not only significantly improve unfavorable properties in a conventional pharmaceutical preparation of clopidogrel bisulfate, i.e. defective compression and flow and a strong surface electrostatic force, but can also significantly reduce tableting impediments such as weight deviations and sticking during preparation by means of a direct powder compression technique, and the danger of crystalline conversion. Thus, the composition has improved physiochemical stability and, due to anti-clotting effects of the composition, can be effectively used as a therapeutic agent for arteriosclerosis, stroke, myocardial infarction, and atherosclerosis.
(FR)
L'invention concerne des particules sphériques de clopidogrel bisulfate qui présentent un diamètre de particules en volume à 10% (d0.1) supérieur ou égal à 30 μm, et un diamètre de particules en volume à 50% (d0.5) compris entre 50 et 200 μm, et une composition pharmaceutique comprenant ces particules. Les particules sphériques de l'invention permettent non seulement d'améliorer considérablement des propriétés défavorables d'une préparation pharmaceutique classique de clopidogrel bisulfate, telles que de mauvaises caractéristiques de compression et d'écoulement et une force électrostatique superficielle élevée, mais aussi de réduire considérablement des inconvénients liés à la fabrication de comprimés, tels que des écarts de poids et une adhérence pendant une préparation utilisant une technique de compression directe de poudre, ainsi que le risque d'une transformation cristalline. Cette composition possède ainsi une stabilité physiochimique améliorée, et, grâce à ses effets anticoagulants, peut être utilisée efficacement comme agent thérapeutique pour traiter l'artériosclérose, l'accident vasculaire cérébral, l'infarctus du myocarde et l'athérosclérose.
(KO)
본 발명은 30 μm 이상의 10% 체적 입경(d0.1) 및 50 내지 200 μm 범위의 50% 체적 입경(d0.5)을 가지는 클로피도그렐 황산수소염의 구형 입자 및 이를 포함하는 약학적 조성물에 관한 것으로서 본 발명의 구형 입자는 종래 클로피도그렐 황산수소염의 제제화하기 어려운 특성, 즉 불량한 압축성, 흐름성 및 강력한 표면 정전기력을 현저히 개선할 뿐만 아니라, 직접분말압축법에 의한 정제의 제조시 중량편차, 스티킹(sticking) 등의 타정 장애와 결정형 전환의 위험성을 현저히 줄일 수 있고, 물리화학적 안정성을 개선할 수 있는바, 항 혈전 효과에 의한 동맥경화증, 뇌졸중, 심근경색 및 죽상동맥경화증을 위한 치료제로 유용하게 사용될 수 있다.
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