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WO2025136341A1 - Comprimé comprenant du brexpiprazole - Google Patents

Comprimé comprenant du brexpiprazole Download PDF

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Publication number
WO2025136341A1
WO2025136341A1 PCT/TR2024/051657 TR2024051657W WO2025136341A1 WO 2025136341 A1 WO2025136341 A1 WO 2025136341A1 TR 2024051657 W TR2024051657 W TR 2024051657W WO 2025136341 A1 WO2025136341 A1 WO 2025136341A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
tablet according
sodium
cellulose
brexpiprazole
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.)
Pending
Application number
PCT/TR2024/051657
Other languages
English (en)
Inventor
Fatih Sunel
Fadime Bilgehan ATAK
Seval Ataman
Onder SARP
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.)
Sanovel Ilac Sanayi ve Ticaret AS
Original Assignee
Sanovel Ilac Sanayi ve Ticaret AS
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 TR2023/018022 external-priority patent/TR2023018022A1/tr
Application filed by Sanovel Ilac Sanayi ve Ticaret AS filed Critical Sanovel Ilac Sanayi ve Ticaret AS
Publication of WO2025136341A1 publication Critical patent/WO2025136341A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

  • the present invention relates to a tablet comprises brexpiprazole or a salt thereof and at least one pharmaceutically acceptable excipient wherein sodium stearyl fumarate is present as lubricant. Further, the present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient process.
  • the main object of the present invention is to provide a tablet comprising brexpiprazole with content uniformity and high stability.
  • Another object of the present invention is to provide a tablet comprising brexpiprazole having desired level of dissolution profile.
  • Another object of the present invention is to provide a process for preparing a tablet comprising brexpiprazole which is simple and rapid, cost effective, time-saving and industrially convenient process.
  • a tablet comprises brexpiprazole or a salt thereof and at least one pharmaceutically acceptable excipient wherein sodium stearyl fumarate is present as lubricant.
  • the amount of lubricant in the tablet is 0.1% to 3.0% by weight of the total composition.
  • the amount of brexpiprazole or a salt thereof is between 0.1% and 10.0% by weight of the total composition.
  • brexpiprazole or a salt thereof having the following particle sizes is very important for formulation. Especially, it positively affects the dissolution properties.
  • the obtained tablets have the desired dissolution profile.
  • 'particle size means the cumulative volume size distrubition as tested by any conventionally accepted method such as the laser diffraction method (i.e. Malvern Mastersizer 2000 analysis).
  • d (0.9) means the size at which %90 by volume of the particles are finer.
  • brexpiprazole or a salt thereof has a d (0.9) particle size between 1 pm and 35 pm, more preferably between 3 pm and 27 pm.
  • the tablet comprises at least one pharmaceutically acceptable excipient which is selected from the group comprising fillers, binders, disintegrants, lubricants or mixtures thereof.
  • Suitable fillers are selected from group comprising lactose monohydrate, microcrystalline cellulose, mannitol, pregelatinized starch, ammonium alginate, calcium carbonate, lactose anhydrous, calcium phosphate, calcium phosphate dehydrate, neutral pellets, calcium sulfate, cellulose, ethylcellulose, fructose, glyceryl palmitostearate, magnesium carbonate, magnesium oxide, maltodextrin, maltose, medium chain triglycerides, polydextrose, polymethacrylates, sodium alginate, sodium chloride, sorbitol, starch, sucrose, sugar sphericals , polysorbate 80, xylitol or mixtures thereof.
  • filler is lactose monohydrate, microcrystalline cellulose, lactose anhydrous or mixtures thereof. According to this embodiment of the present invention, filler is lactose monohydrate and microcrystalline cellulose.
  • filler is lactose anhydrous and microcrystalline cellulose.
  • the amount of filler in the tablet is 80.0% to 95.0% by weight of the total composition. Preferably, it is 86.0% to 92.0% by weight of the total composition.
  • a process for preparing a tablet comprising brexpiprazole or a salt thereof comprises the below following steps; a) Mixing used fillers, b) Mixing brexpiprazole, at least one binder and at least one disintegrant, c) Mixing the mixture at step (a) and the mixture at step (b) with geometric dilution d) Sieving the mixture and then mixing, e) Adding sodium stearyl fumarate and then mixing, f) Compressing the total mixture into tablet.
  • Example 1 Tablet

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material 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)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un comprimé comprenant du brexpiprazole ou un sel de celui-ci et au moins un excipient pharmaceutiquement acceptable, le fumarate de stéaryle sodique étant présent en tant que lubrifiant. En outre, la présente invention concerne également un procédé simple, rapide, économique, économe en temps et industriellement pratique.
PCT/TR2024/051657 2023-12-22 2024-12-20 Comprimé comprenant du brexpiprazole Pending WO2025136341A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2023018022 2023-12-22
TR2023/018022 TR2023018022A1 (tr) 2023-12-22 Brekspi̇prazol i̇çeren bi̇r tablet

Publications (1)

Publication Number Publication Date
WO2025136341A1 true WO2025136341A1 (fr) 2025-06-26

Family

ID=96137835

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/TR2024/051657 Pending WO2025136341A1 (fr) 2023-12-22 2024-12-20 Comprimé comprenant du brexpiprazole

Country Status (1)

Country Link
WO (1) WO2025136341A1 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012137971A1 (fr) * 2011-04-05 2012-10-11 Otsuka Pharmaceutical Co., Ltd. Combinaisons comprenant du brexpiprazole ou un sel de celui-ci et un second médicament en vue d'une utilisation dans le traitement d'un trouble du système nerveux central
WO2018033481A1 (fr) * 2016-08-16 2018-02-22 H E X A L Aktiengesellschaft Comprimé à libération immédiate d'un composé benzothiophène
EP3501506A1 (fr) * 2017-12-19 2019-06-26 Alfred E. Tiefenbacher (GmbH & Co. KG) Composition de comprimé pharmaceutique comprenant du brexpiprazole

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012137971A1 (fr) * 2011-04-05 2012-10-11 Otsuka Pharmaceutical Co., Ltd. Combinaisons comprenant du brexpiprazole ou un sel de celui-ci et un second médicament en vue d'une utilisation dans le traitement d'un trouble du système nerveux central
WO2018033481A1 (fr) * 2016-08-16 2018-02-22 H E X A L Aktiengesellschaft Comprimé à libération immédiate d'un composé benzothiophène
EP3501506A1 (fr) * 2017-12-19 2019-06-26 Alfred E. Tiefenbacher (GmbH & Co. KG) Composition de comprimé pharmaceutique comprenant du brexpiprazole

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