BR112020005421A8 - Composição farmacêutica, método para solucionar baixa solubilidade aquosa de uma formulação de roflumilaste e método para inibir fosfodiesterase 4 em um paciente - Google Patents

Composição farmacêutica, método para solucionar baixa solubilidade aquosa de uma formulação de roflumilaste e método para inibir fosfodiesterase 4 em um paciente

Info

Publication number
BR112020005421A8
BR112020005421A8 BR112020005421A BR112020005421A BR112020005421A8 BR 112020005421 A8 BR112020005421 A8 BR 112020005421A8 BR 112020005421 A BR112020005421 A BR 112020005421A BR 112020005421 A BR112020005421 A BR 112020005421A BR 112020005421 A8 BR112020005421 A8 BR 112020005421A8
Authority
BR
Brazil
Prior art keywords
roflumilast
patient
water
pharmaceutical composition
aqueous solubility
Prior art date
Application number
BR112020005421A
Other languages
English (en)
Other versions
BR112020005421A2 (pt
Inventor
W Osborne David
Original Assignee
Arcutis Inc
Arcutis Biotherapeutics 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 Arcutis Inc, Arcutis Biotherapeutics Inc filed Critical Arcutis Inc
Publication of BR112020005421A2 publication Critical patent/BR112020005421A2/pt
Publication of BR112020005421A8 publication Critical patent/BR112020005421A8/pt

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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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A61K9/122—Foams; Dry foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A baixa solubilidade aquosa de roflumilaste em preparações parenterais e emulsões tópicas, suspensões, géis ou soluções pode ser melhorada incluindo-se uma mescla de solventes miscíveis em água na composição farmacêutica. A mescla de solventes miscíveis em água pode incluir éter monoetílico de dietileno glicol (Nome comercial Transcutol®; abreviado DEGEE) e água. A razão de éter monoetílico de dietileno glicol para água é de 1:10 a 20:1. A composição resultante melhorou a biodisponibilidade e eficácia e pode ser usada para inibir fosfodiesterase 4 em um paciente que precisa de tal tratamento.
BR112020005421A 2017-09-22 2018-09-19 Composição farmacêutica, método para solucionar baixa solubilidade aquosa de uma formulação de roflumilaste e método para inibir fosfodiesterase 4 em um paciente BR112020005421A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15/712,900 US11534493B2 (en) 2017-09-22 2017-09-22 Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents
US15/712,900 2017-09-22
PCT/US2018/051691 WO2019060379A1 (en) 2017-09-22 2018-09-19 PHARMACEUTICAL COMPOSITIONS OF ROFLUMILAST IN AQUEOUS MIXTURES OF PHARMACEUTICALLY ACCEPTABLE SOLVENTS MISCIBLE TO WATER

Publications (2)

Publication Number Publication Date
BR112020005421A2 BR112020005421A2 (pt) 2020-09-29
BR112020005421A8 true BR112020005421A8 (pt) 2022-12-13

Family

ID=63794682

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020005421A BR112020005421A8 (pt) 2017-09-22 2018-09-19 Composição farmacêutica, método para solucionar baixa solubilidade aquosa de uma formulação de roflumilaste e método para inibir fosfodiesterase 4 em um paciente

Country Status (13)

Country Link
US (2) US11534493B2 (pt)
EP (2) EP4316590A3 (pt)
JP (3) JP7191944B2 (pt)
KR (1) KR102681877B1 (pt)
CN (1) CN111107836A (pt)
AU (1) AU2018337752B2 (pt)
BR (1) BR112020005421A8 (pt)
CA (1) CA3076002A1 (pt)
EA (1) EA202090813A1 (pt)
ES (1) ES2972843T3 (pt)
IL (1) IL273376B2 (pt)
MX (2) MX2020003001A (pt)
WO (1) WO2019060379A1 (pt)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11129818B2 (en) 2017-06-07 2021-09-28 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having improved delivery and plasma half life
US12042487B2 (en) 2018-11-16 2024-07-23 Arcutis Biotherapeutics, Inc. Method for reducing side effects from administration of phosphodiesterase-4 inhibitors
US20200155524A1 (en) 2018-11-16 2020-05-21 Arcutis, Inc. Method for reducing side effects from administration of phosphodiesterase-4 inhibitors
US12011437B1 (en) 2017-06-07 2024-06-18 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
US9895359B1 (en) * 2017-06-07 2018-02-20 Arcutis, Inc. Inhibition of crystal growth of roflumilast
US20210161870A1 (en) * 2017-06-07 2021-06-03 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
KR20210044191A (ko) 2018-06-04 2021-04-22 아큐티스, 인크. 로플루밀라스트 피부 침투 지연 시간의 개선 방법 및 제형
CN114828840A (zh) * 2019-10-11 2022-07-29 泽威恩制药有限责任公司 秋水仙碱的改进的局部用组合物
EP4096630A1 (en) * 2020-01-31 2022-12-07 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having improved delivery and plasma half-life
WO2022169615A1 (en) * 2021-02-05 2022-08-11 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile

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Also Published As

Publication number Publication date
CN111107836A (zh) 2020-05-05
US20190091333A1 (en) 2019-03-28
AU2018337752A1 (en) 2020-04-09
EA202090813A1 (ru) 2020-08-14
EP3684334A1 (en) 2020-07-29
BR112020005421A2 (pt) 2020-09-29
JP2020534303A (ja) 2020-11-26
EP3684334C0 (en) 2023-12-06
MX2023011557A (es) 2023-10-09
EP4316590A3 (en) 2024-05-01
ES2972843T3 (es) 2024-06-17
CA3076002A1 (en) 2019-03-28
JP2023027195A (ja) 2023-03-01
IL273376A (en) 2020-05-31
WO2019060379A1 (en) 2019-03-28
IL273376B2 (en) 2024-07-01
US11534493B2 (en) 2022-12-27
JP7191944B2 (ja) 2022-12-19
KR20200058402A (ko) 2020-05-27
JP2024028911A (ja) 2024-03-05
EP4316590A2 (en) 2024-02-07
US20230091358A1 (en) 2023-03-23
KR102681877B1 (ko) 2024-07-04
EP3684334B1 (en) 2023-12-06
AU2018337752B2 (en) 2024-03-28
IL273376B1 (en) 2024-03-01
MX2020003001A (es) 2020-09-28
JP7402301B2 (ja) 2023-12-20

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Legal Events

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07G Grant request does not fulfill article 229-c lpi (prior consent of anvisa) [chapter 7.7 patent gazette]

Free format text: NOTIFICACAO DE DEVOLUCAO DO PEDIDO EM FUNCAO DA REVOGACAO DO ART. 229-C DA LEI NO 9.279, DE 1996, POR FORCA DA LEI NO 14.195, DE 2021

B350 Update of information on the portal [chapter 15.35 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B25D Requested change of name of applicant approved

Owner name: ARCUTIS BIOTHERAPEUTICS, INC. (US)

B25G Requested change of headquarter approved

Owner name: ARCUTIS BIOTHERAPEUTICS, INC. (US)

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]