CN113473988A - 无定形固体分散体 - Google Patents

无定形固体分散体 Download PDF

Info

Publication number
CN113473988A
CN113473988A CN201980092118.2A CN201980092118A CN113473988A CN 113473988 A CN113473988 A CN 113473988A CN 201980092118 A CN201980092118 A CN 201980092118A CN 113473988 A CN113473988 A CN 113473988A
Authority
CN
China
Prior art keywords
dispersion
iti
dioxane
methanol
solvent
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
CN201980092118.2A
Other languages
English (en)
Chinese (zh)
Inventor
李鹏
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.)
Intra Cellular Therapies Inc
Original Assignee
Intra Cellular Therapies Inc
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 Intra Cellular Therapies Inc filed Critical Intra Cellular Therapies Inc
Publication of CN113473988A publication Critical patent/CN113473988A/zh
Pending legal-status Critical Current

Links

Images

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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/16—Peri-condensed systems
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980092118.2A 2018-12-14 2019-12-13 无定形固体分散体 Pending CN113473988A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862779930P 2018-12-14 2018-12-14
US62/779,930 2018-12-14
PCT/US2019/066247 WO2020123952A1 (en) 2018-12-14 2019-12-13 Amorphous solid dispersions

Publications (1)

Publication Number Publication Date
CN113473988A true CN113473988A (zh) 2021-10-01

Family

ID=71077112

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980092118.2A Pending CN113473988A (zh) 2018-12-14 2019-12-13 无定形固体分散体

Country Status (9)

Country Link
EP (1) EP3893878A4 (https=)
JP (1) JP7523440B2 (https=)
KR (1) KR20210103501A (https=)
CN (1) CN113473988A (https=)
AU (1) AU2019398451B2 (https=)
CA (1) CA3123085A1 (https=)
IL (1) IL283927A (https=)
MX (1) MX2021006886A (https=)
WO (1) WO2020123952A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024083026A1 (zh) 2022-10-19 2024-04-25 四川科伦药物研究院有限公司 一种卢美哌隆药物组合物、长效微球缓释制剂及其制备方法
CN118566395A (zh) * 2024-08-02 2024-08-30 则正(济南)生物科技有限公司 测定甲苯磺酸卢美哌隆口崩片中杂质含量的方法、应用和系统

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112584837A (zh) * 2018-08-31 2021-03-30 细胞内治疗公司 新方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018031535A1 (en) * 2016-08-09 2018-02-15 Assia Chemical Industries Ltd. Solid state forms of lumateperone ditosylate salt
WO2018071233A1 (en) * 2016-10-12 2018-04-19 Intra-Cellular Therapies, Inc. Amorphous solid dispersions
WO2018189646A1 (en) * 2017-04-10 2018-10-18 Dr. Reddy's Laboratories Limited AMORPHOUS FORM AND SOLID DISPERSIONS OF LUMATEPERONE p-TOSYLATE

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11655251B2 (en) * 2017-11-27 2023-05-23 Egis Gyogyszergyar Zrt. Method for the production of lumateperone and its salts
CN112584837A (zh) * 2018-08-31 2021-03-30 细胞内治疗公司 新方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018031535A1 (en) * 2016-08-09 2018-02-15 Assia Chemical Industries Ltd. Solid state forms of lumateperone ditosylate salt
WO2018071233A1 (en) * 2016-10-12 2018-04-19 Intra-Cellular Therapies, Inc. Amorphous solid dispersions
WO2018189646A1 (en) * 2017-04-10 2018-10-18 Dr. Reddy's Laboratories Limited AMORPHOUS FORM AND SOLID DISPERSIONS OF LUMATEPERONE p-TOSYLATE

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024083026A1 (zh) 2022-10-19 2024-04-25 四川科伦药物研究院有限公司 一种卢美哌隆药物组合物、长效微球缓释制剂及其制备方法
CN118566395A (zh) * 2024-08-02 2024-08-30 则正(济南)生物科技有限公司 测定甲苯磺酸卢美哌隆口崩片中杂质含量的方法、应用和系统

Also Published As

Publication number Publication date
EP3893878A1 (en) 2021-10-20
IL283927A (en) 2021-07-29
JP7523440B2 (ja) 2024-07-26
JP2022512239A (ja) 2022-02-02
AU2019398451B2 (en) 2024-12-05
MX2021006886A (es) 2021-09-14
CA3123085A1 (en) 2020-06-18
EP3893878A4 (en) 2022-08-17
KR20210103501A (ko) 2021-08-23
WO2020123952A1 (en) 2020-06-18
AU2019398451A1 (en) 2021-07-15

Similar Documents

Publication Publication Date Title
US12472178B2 (en) Amorphous solid dispersions
TWI810243B (zh) 用於治療囊腫纖化症之醫藥組合物
WO2020242935A1 (en) Methods of treatment for cystic fibrosis
AU2018351533A1 (en) Crystalline forms and compositions of CFTR modulators
CN113473988A (zh) 无定形固体分散体
HRP20020777A2 (en) Hydrophilic molecular disperse solutions of carvedilol
EA017553B1 (ru) Гидробромид ивабрадина
KR101288001B1 (ko) 모사프라이드를 유효성분으로 함유하는 서방성 제제
HK40060531A (zh) 无定形固体分散体
WO2016169534A1 (en) Solid forms of amorphous empagliflozin
US9211290B2 (en) Solid dispersions of amorphous paroxetine mesylate
HK40011133A (en) Amorphous solid dispersions
HK40011133B (zh) 无定形固体分散体
Jung et al. Enhanced Dissolution Rate of Dronedarone Hydrochloride via Preparation of Solid Dispersion using Vinylpyrrolidone‐Vinyl Acetate Copolymer (Kollidone® VA 64)
WO2016165676A1 (en) Amorphous forms of vemurafenib

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40060531

Country of ref document: HK