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WO2019199135A1 - Procédé de préparation d'une formulation solide administrée par voie orale comprenant du lénalidomide - Google Patents

Procédé de préparation d'une formulation solide administrée par voie orale comprenant du lénalidomide Download PDF

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Publication number
WO2019199135A1
WO2019199135A1 PCT/KR2019/004475 KR2019004475W WO2019199135A1 WO 2019199135 A1 WO2019199135 A1 WO 2019199135A1 KR 2019004475 W KR2019004475 W KR 2019004475W WO 2019199135 A1 WO2019199135 A1 WO 2019199135A1
Authority
WO
WIPO (PCT)
Prior art keywords
lenalidomide
mixture
additive
mixing
drug
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/KR2019/004475
Other languages
English (en)
Korean (ko)
Inventor
박상엽
임혜정
이사원
서민효
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Samyang Biopharmaceuticals Corp
Original Assignee
Samyang Biopharmaceuticals Corp
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
Priority claimed from KR1020190043377A external-priority patent/KR102286500B1/ko
Application filed by Samyang Biopharmaceuticals Corp filed Critical Samyang Biopharmaceuticals Corp
Publication of WO2019199135A1 publication Critical patent/WO2019199135A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • the present invention relates to the preparation of lenalidomide. Specifically, it relates to a solid preparation for oral administration of lenalidomide.
  • capsules are also a problem when the capsule is taken with water, the capsule is stuck to the throat or esophagus during swallowing.
  • the capsule is prepared by filling the granules in the capsule, the tablet has a problem of inferior content uniformity as compared to the capsule.
  • the lenalidomide in addition, in the present invention, further comprising the step of sieving the mixture of the first step and lenalidomide before mixing in the second step, the lenalidomide can be mixed inside the mixture of the first step when sieving It is desirable to.
  • Lenalidomide may have a D50 greater than 2 ⁇ m.
  • the tablet may have a biological initial equivalence with a conventional capsule by having an appropriate initial dissolution amount and a disintegration time, and may prevent a process disorder during tableting.
  • Lenalidomide preferably has a D50 of 2.5-50 ⁇ m, more preferably 3-40 ⁇ m, even more preferably 5-30 ⁇ m, even more preferably 7-20, most preferably 10-15 ⁇ m.
  • D10 refers to the diameter of the particles corresponding to the lower 10% in terms of volume distribution
  • D50 and D90 refer to the diameters of the particles corresponding to 50% and 90%, respectively.
  • D [4,3] means the volume average diameter. This can be measured using an optical diffraction particle size analyzer.
  • Step 1 Mixing the Additives Except Glidants (e.g. at least one of Diluents, Binders and Disintegrants)
  • Glidants e.g. at least one of Diluents, Binders and Disintegrants
  • the coating base is 1 to 30 parts by weight, preferably 2 to 25 parts by weight, more preferably 3 to 20 parts by weight, even more preferably 4 to 15 parts by weight, even more preferably based on 100 parts by weight of uncoated tablet. 5 to 15 parts by weight, most preferably 6 to 15 parts by weight, can be used. If less than the above range, the total uncoated tablet may not be sufficiently coated, on the contrary, if a large amount may cause a delay in dissolution rate.
  • lenalidomide 125 g was divided into three portions. As lenalidomide, micronized raw materials corresponding to D10 3 ⁇ m, D50 13 ⁇ m, D90 44 ⁇ m, and D [4, 3] 19 ⁇ m were used.
  • the additive mixture was divided into about 4 portions, the first quarter of the amount spread over a 40mesh sieve and a network, and 1/3 of the drug was scattered over the additive mixture. On top of that, about a quarter of the additive mixture was further removed so that the initially scattered drug was covered. Again about 1/3 of the drug was scattered over the additive mixture and sprinkled. Approximately one quarter of the additive mixture was further reduced to cover the scattered drug. Finally, the entire remaining volume of the drug was scattered over the additive mixture, and then the drug was scattered with the remaining amount of the additive mixture, and then sieved. The sieved mixture was placed in a double cone mixer and mixed at 20 rpm for 25 minutes.
  • the mixture was tableted with a rectangular punch based on 400 mg weight per tablet, which was compressed while feeding the mixture to an open feeder while rotating the disk at a speed of 4 rpm.
  • the prepared uncoated tablet was coated with the uncoated tablet of Example 1.

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un procédé de préparation d'un comprimé de lénalidomide pour une administration orale, comprenant : une première étape pour mélanger un additif pharmaceutiquement acceptable; une deuxième étape pour mélanger le mélange de la première étape et du lénalidomide; une troisième étape de mélange du mélange de la deuxième étape et d'un lubrifiant; et une quatrième étape de compression directe du mélange à partir de la troisième étape.
PCT/KR2019/004475 2018-04-13 2019-04-13 Procédé de préparation d'une formulation solide administrée par voie orale comprenant du lénalidomide Ceased WO2019199135A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR20180043595 2018-04-13
KR10-2018-0043595 2018-04-13
KR10-2019-0043377 2019-04-12
KR1020190043377A KR102286500B1 (ko) 2018-04-13 2019-04-12 레날리도마이드를 포함하는 경구용 고형제제의 제조방법

Publications (1)

Publication Number Publication Date
WO2019199135A1 true WO2019199135A1 (fr) 2019-10-17

Family

ID=68164325

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2019/004475 Ceased WO2019199135A1 (fr) 2018-04-13 2019-04-13 Procédé de préparation d'une formulation solide administrée par voie orale comprenant du lénalidomide

Country Status (1)

Country Link
WO (1) WO2019199135A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120046315A1 (en) * 2008-11-14 2012-02-23 Katrin Rimkus Intermediate and oral administrative formats containing lenalidomide
KR20150091165A (ko) * 2012-12-07 2015-08-07 사노피 항-cd38 항체 및 레날리도마이드를 포함하는 조성물
CN105534981A (zh) * 2016-03-04 2016-05-04 四川美大康华康药业有限公司 一种来那度胺组合物片剂及其制备方法
KR20160146770A (ko) * 2014-05-01 2016-12-21 테바 파마슈티컬즈 오스트레일리아 피티와이 엘티디 레날리도마이드 또는 포말리도마이드 및 ｃｄ38 항체-감쇠 인터페론-알파 구성체의 조합, 및 이의 용도
WO2017032870A1 (fr) * 2015-08-27 2017-03-02 Grindeks, A Joint Stock Company Composition pharmaceutique pouvant incorporer la lénalidomine sous diverses variantes cristallines

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120046315A1 (en) * 2008-11-14 2012-02-23 Katrin Rimkus Intermediate and oral administrative formats containing lenalidomide
KR20150091165A (ko) * 2012-12-07 2015-08-07 사노피 항-cd38 항체 및 레날리도마이드를 포함하는 조성물
KR20160146770A (ko) * 2014-05-01 2016-12-21 테바 파마슈티컬즈 오스트레일리아 피티와이 엘티디 레날리도마이드 또는 포말리도마이드 및 ｃｄ38 항체-감쇠 인터페론-알파 구성체의 조합, 및 이의 용도
WO2017032870A1 (fr) * 2015-08-27 2017-03-02 Grindeks, A Joint Stock Company Composition pharmaceutique pouvant incorporer la lénalidomine sous diverses variantes cristallines
CN105534981A (zh) * 2016-03-04 2016-05-04 四川美大康华康药业有限公司 一种来那度胺组合物片剂及其制备方法

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