EP2758030A1 - Forme posologique orale comprimée de maléate d'asénapine - Google Patents

Forme posologique orale comprimée de maléate d'asénapine

Info

Publication number
EP2758030A1
EP2758030A1 EP12761718.1A EP12761718A EP2758030A1 EP 2758030 A1 EP2758030 A1 EP 2758030A1 EP 12761718 A EP12761718 A EP 12761718A EP 2758030 A1 EP2758030 A1 EP 2758030A1
Authority
EP
European Patent Office
Prior art keywords
dosage form
asenapine maleate
pharmaceutical dosage
monoclinic
compressed pharmaceutical
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.)
Withdrawn
Application number
EP12761718.1A
Other languages
German (de)
English (en)
Inventor
Max Born
Diana Fischer
Ina Otto
Yvonne Fischer
Carsten BRÄUER
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.)
Hexal AG
Original Assignee
Hexal AG
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 Hexal AG filed Critical Hexal AG
Priority to EP12761718.1A priority Critical patent/EP2758030A1/fr
Publication of EP2758030A1 publication Critical patent/EP2758030A1/fr
Withdrawn legal-status Critical Current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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

  • a further embodiment of the present invention relates to a container comprising a compressed pharmaceutical dosage form as described herein or according to any of claims 1 to 10, wherein the container is prepared from a material having a permeability for water vapor as measured according to DIN 53122 of from 1,0 g * m "2 * d to 5000 g * m "2 * d "1 .
  • FIGURE LEGENDS The accompanying drawings, which are incorporated and form part of the specification, merely illustrate certain embodiments of the present invention. They are meant to serve to explain specific modes of the present invention to those skilled in the art.
  • Figure 1 XRPD pattern of monoclinic asenapine maleate in the form of crystalline material having a particle size distribution characterized by a d95 of 34.9 ⁇ obtained from example 2c).
  • compressed dosage form denotes solid preparations (e.g., tablets) each containing a single dose of one or more active substances.
  • compressed dosage forms include uncoated tablets; coated tablets; effervescent tablets; soluble tablets; dispersible tablets; orodispersible tablets; and tablets for use in the mouth.
  • Such compressed dosage forms can be prepared by compressing uniform volumes of particles or particle aggregates produced by granulation methods.
  • the particles consist of one or more active substances with or without excipients such as diluents, binders, disintegrating agents, glidants, lubricants, substances capable of modifying the behaviour of the preparation in the digestive tract, colouring matter authorised by the competent authority and flavouring substances.
  • means are taken to ensure that they possess a suitable mechanical strength to avoid crumbling or breaking on handling or subsequent processing.
  • the process of providing compressed dosage forms is well known to the skilled person.
  • micronized denotes the process of mechanically reducing the average diameter of a solid material's particles.
  • Traditional micronization techniques are based on friction to reduce particle size. Such methods include milling, bashing and grinding.
  • a typical industrial mill is composed of a cylindrical metallic drum that usually contains steel spheres. As the drum rotates the spheres inside collide with the particles of the solid, thus crushing them towards smaller diameters. In the case of grinding, the solid particles are formed when the grinding units of the device rub against each other while particles of the solid are trapped in between. Methods like crushing and cutting are also used for reducing particle diameter, but produce more coarse particles compared to the two previous techniques (and are therefore the early stages of the micronization process).
  • Crushing employs hammer-like tools to break the solid into smaller particles by means of impact. Cutting uses sharp blades to cut the coarse solid pieces into smaller ones. All these techniques are well known to the skilled person.
  • the disintegrant is selected from the group consisting of cross-linked carboxymethylcellulose sodium, cross-linked polyvinylpyrrolidone, pregelatinized starch, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium alginate, sodium starch glycolate, crospovidone, croscarmellose sodium and low substituted hydroxyl propyl cellulose.
  • the disintegrant is cross-linked carboxymethylcellulose (also known as carboxymethylcellulose).
  • filler is a mixture of microcrystalline cellulose and mannitol.
  • other fillers such as calcium carbonate, dibasic calcium phosphate etc can be added, microcrystalline cellulose is most preferred. Microcrystalline cellulose in the range of from 5 % to 50 % (w/w) is found suitable.
  • the microcrystalline cellulose is present in an amount of from 5 % to 30 % (w/w) of total filler, preferably of from 10 % to 20 % (w/w) of total filler.
  • microcrystalline cellulose is present in the inventive dosage form in an amount of from 10 % to 20 % (w/w) of total filler
  • mannitol is present in the inventive dosage form in an amount of from 80 % to 90 % (w/w) of total filler.
  • the inventive dosage form comprises 40.0 % to 90.0 % (w/w), 60.0 % to 90.0 % (w/w), 70.0 % to 90.0 % (w/w) or 75 % to 85 % (w/w) of total filler (i.e. one or more fillers).
  • the inventive dosage form comprises a mixture of microcrystalline cellulose and mannitol
  • a further embodiment of the present invention is directed to a compressed dosage form obtainable by this method.
  • a further embodiment of the present invention is directed to a method for the preparation of the compressed pharmaceutical dosage form as described herein above, the method comprising:
  • Another embodiment of the present invention relates to the above-described dosage form for use in the treatment of acute schizophrenia, bipolar disorder or manic episodes in bipolar I disorders, the dosage form comprising microcrystalline monoclinic asenapine maleate as active ingredient.
  • the specific nature of the products and compositions of the present invention e. g. the nature of the additional components, the relative proportions of the components and the physical nature of the composition
  • the above invention has been described with respect to some of its preferred embodiments, this is in no way to limit the scope of the invention.
  • the person skilled in the art is clearly aware of further embodiments and alterations to the previously described embodiments that are still within the scope of the present invention.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une forme posologique pharmaceutique comprimée destinée à une administration sublinguale ou buccale et pouvant se déliter rapidement, la forme posologique pharmaceutique comprimée contenant du maléate d'asénapine sous une forme monoclinique microcristalline. La présente invention concerne en outre un procédé de préparation de ladite forme posologique et un récipient comprenant ladite forme posologique.
EP12761718.1A 2011-09-21 2012-09-13 Forme posologique orale comprimée de maléate d'asénapine Withdrawn EP2758030A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP12761718.1A EP2758030A1 (fr) 2011-09-21 2012-09-13 Forme posologique orale comprimée de maléate d'asénapine

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11182256A EP2572703A1 (fr) 2011-09-21 2011-09-21 Forme pharmaceutique orale compressée pour maléate d'asénapine
PCT/EP2012/067920 WO2013041435A1 (fr) 2011-09-21 2012-09-13 Forme posologique orale comprimée de maléate d'asénapine
EP12761718.1A EP2758030A1 (fr) 2011-09-21 2012-09-13 Forme posologique orale comprimée de maléate d'asénapine

Publications (1)

Publication Number Publication Date
EP2758030A1 true EP2758030A1 (fr) 2014-07-30

Family

ID=46881046

Family Applications (2)

Application Number Title Priority Date Filing Date
EP11182256A Ceased EP2572703A1 (fr) 2011-09-21 2011-09-21 Forme pharmaceutique orale compressée pour maléate d'asénapine
EP12761718.1A Withdrawn EP2758030A1 (fr) 2011-09-21 2012-09-13 Forme posologique orale comprimée de maléate d'asénapine

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP11182256A Ceased EP2572703A1 (fr) 2011-09-21 2011-09-21 Forme pharmaceutique orale compressée pour maléate d'asénapine

Country Status (2)

Country Link
EP (2) EP2572703A1 (fr)
WO (1) WO2013041435A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR201509009A1 (en) * 2014-12-11 2017-02-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi THIN FILM STRIP OF ASENAPINE
ES2769286T3 (es) 2016-12-20 2020-06-25 Lts Lohmann Therapie Systeme Ag Sistema terapéutico transdérmico que contiene asenapina
WO2018115010A1 (fr) 2016-12-20 2018-06-28 Lts Lohmann Therapie-Systeme Ag Système thérapeutique transdermique contenant de l'asénapine et un polysiloxane ou un polyisobutylène
ES2881783T3 (es) 2017-06-26 2021-11-30 Lts Lohmann Therapie Systeme Ag Sistema terapéutico transdérmico que contiene asenapina y polímero de acrílico y silicona
CA3101420A1 (fr) 2018-06-20 2019-12-26 Lts Lohmann Therapie-Systeme Ag Systeme therapeutique transdermique contenant de l'asenapine
CN112533593A (zh) 2018-06-20 2021-03-19 罗曼治疗系统股份公司 含有阿塞那平的透皮治疗系统
KR20230027201A (ko) * 2020-06-19 2023-02-27 아세르타 파마. 비.브이. 아칼라브루티닙 말레산염 투약 형태

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7605526A (nl) 1976-05-24 1977-11-28 Akzo Nv Nieuwe tetracyclische derivaten.
JP4099224B2 (ja) 1994-03-02 2008-06-11 ナームローゼ・フエンノートチヤツプ・オルガノン 舌下又はバッカル医薬組成物
DE602006000080T2 (de) 2005-04-07 2008-05-15 N.V. Organon Kristallform von Asenapinmaleat
TW200817414A (en) 2006-07-05 2008-04-16 Organon Nv Process for the preparation of asenapine and intermediate products used in said process
WO2011159903A2 (fr) * 2010-06-18 2011-12-22 Dr. Reddy's Laboratories Ltd. Maléate d'asénapine

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
None *
See also references of WO2013041435A1 *

Also Published As

Publication number Publication date
WO2013041435A1 (fr) 2013-03-28
EP2572703A1 (fr) 2013-03-27

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