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WO2018192590A2 - Composition pharmaceutique orale stable et procédé de préparation associé - Google Patents

Composition pharmaceutique orale stable et procédé de préparation associé Download PDF

Info

Publication number
WO2018192590A2
WO2018192590A2 PCT/CN2018/091940 CN2018091940W WO2018192590A2 WO 2018192590 A2 WO2018192590 A2 WO 2018192590A2 CN 2018091940 W CN2018091940 W CN 2018091940W WO 2018192590 A2 WO2018192590 A2 WO 2018192590A2
Authority
WO
WIPO (PCT)
Prior art keywords
polymer
pharmaceutically acceptable
composition
compound
formula
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/CN2018/091940
Other languages
English (en)
Chinese (zh)
Other versions
WO2018192590A3 (fr
Inventor
高慧燕
张利锋
陈见阳
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.)
Zhejiang Jingxin Pharmaceutical Co Ltd
Original Assignee
Zhejiang Jingxin Pharmaceutical Co Ltd
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 Zhejiang Jingxin Pharmaceutical Co Ltd filed Critical Zhejiang Jingxin Pharmaceutical Co Ltd
Publication of WO2018192590A2 publication Critical patent/WO2018192590A2/fr
Publication of WO2018192590A3 publication Critical patent/WO2018192590A3/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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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

  • an oral pharmaceutical composition comprising an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, said pharmaceutically
  • the acceptable carrier includes a polymer having a melting point or a glass transition temperature or a softening temperature of less than 180 ° C, and the mass ratio of the polymer to the compound of the formula I or a pharmaceutically acceptable salt thereof is 1 the above;
  • the polymer is one or more selected from the group consisting of hydroxyalkylalkylcellulose, N-vinylpyrrolidone, and vinyl acetate copolymer and poloxamer.
  • the present invention provides an oral pharmaceutical composition
  • a compound of formula I which exhibits good stability under accelerated conditions or at least satisfies the above ICH requirements.
  • the premix a is added to the jacketed vessel, mixed with the polymer melted therein, and stirred to obtain uniform particles, which are cooled and sieved;
  • the solution a' and the diluent are mixed, stirred and granulated;
  • the obtained granules are sieved, mixed with a lubricant, and then filled into a capsule or tablet.
  • the solution a" in the first step above is obtained by mixing a compound of the formula I or a pharmaceutically acceptable salt thereof, a polymer with a suitable solvent.
  • the solution a" of the above first step may further contain other excipients such as a surfactant, an antioxidant, and the like.
  • Compound I lactose, corn starch, sodium carboxymethylcellulose and povidone are mixed, wet granulated and dried to obtain dry granule 1, and talc powder, magnesium stearate and dry granule 2 are mixed, and then tableted.
  • the tablet weighs 300 mg.
  • the compound I is dissolved in ethanol to obtain a solution 1; the poloxamer 188 is further heated and melted in a water bath at 70-80 ° C to obtain a solution 2; the solution 1 is added to the solution 2, and the solution is stirred to obtain a solution 3; To a mixture of lactose and microcrystalline cellulose, followed by granulation and drying to obtain dry granules 4, magnesium stearate and dry granules 4 were mixed, and then filled into capsules, and the capsule contents were 50 mg, 150 mg and 300 mg, respectively.
  • the granulating pot body is heated by temperature control in a 50-70 ° C water bath, and then sequentially added microcrystalline cellulose, lactose, when the temperature of the material reaches 50-55 ° C, adding solution 2 granulation, drying to obtain dry granules 3;
  • Compound 1 is dissolved in isopropanol to obtain solution 1; poloxamer 188 is further heated and melted in a 70-80 ° C water bath to obtain solution 2; the solution 1 is added to the solution 2, and stirred to obtain a solution 3; 3 is added to the microcrystalline cellulose, then granulated and dried to obtain dry granules 4, and magnesium stearate and dry granules 4 are mixed, and then filled into capsules, and the capsule contents are 80 mg, 80 mg and 240 mg, respectively.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une composition pharmaceutique orale stable et un procédé de préparation associé. La composition contient une quantité efficace d'un composé ayant la structure représentée par la formule I ou un sel pharmaceutiquement acceptable de celui-ci et un support pharmaceutiquement acceptable, le support pharmaceutiquement acceptable comprenant un polymère ayant un point de fusion, une température de transition vitreuse et une température de ramollissement inférieure à 180 °C, le rapport en masse du polymère relativement au composé ayant la structure représentée par la formule I ou son sel pharmaceutiquement acceptable étant supérieur à 1.
PCT/CN2018/091940 2017-04-21 2018-06-20 Composition pharmaceutique orale stable et procédé de préparation associé Ceased WO2018192590A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201710264635.6A CN107007559B (zh) 2017-04-21 2017-04-21 一种稳定的口服药物组合物及其制备方法
CN201710264635.6 2017-04-21

Publications (2)

Publication Number Publication Date
WO2018192590A2 true WO2018192590A2 (fr) 2018-10-25
WO2018192590A3 WO2018192590A3 (fr) 2018-12-20

Family

ID=59446978

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2018/091940 Ceased WO2018192590A2 (fr) 2017-04-21 2018-06-20 Composition pharmaceutique orale stable et procédé de préparation associé

Country Status (2)

Country Link
CN (1) CN107007559B (fr)
WO (1) WO2018192590A2 (fr)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR5278A (es) * 1995-03-24 1996-07-04 Lilly Co Eli Formulacion oral de 2-metil-tieno-benzodiacepina
TR199900651T2 (xx) * 1996-09-24 1999-07-21 Eli Lilly And Company Kaplanm�� par�ac�k form�lasyonu.
CA2372040C (fr) * 1999-05-12 2008-12-02 Francois Jenck Derive d'imidazodiazepine
EP2332524A1 (fr) * 2005-02-15 2011-06-15 Elan Pharma International Limited Aérosol et composition injéctable de benzodiazépine nanoparticulaire
US20090054412A1 (en) * 2007-08-20 2009-02-26 John Alan Kemp Treatment of Sleep Disorders
CN101827597B (zh) * 2007-08-20 2013-03-13 伊沃泰克国际有限责任公司 睡眠障碍的治疗

Also Published As

Publication number Publication date
WO2018192590A3 (fr) 2018-12-20
CN107007559B (zh) 2020-05-15
CN107007559A (zh) 2017-08-04

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