BR112019025748A8 - Método para inibir o crescimento de cristal de roflumilast ou mudanças no tamanho de partícula em uma composição, composição farmacêutica e método de inibição de fosfodiesterase 4 em um paciente - Google Patents
Método para inibir o crescimento de cristal de roflumilast ou mudanças no tamanho de partícula em uma composição, composição farmacêutica e método de inibição de fosfodiesterase 4 em um pacienteInfo
- Publication number
- BR112019025748A8 BR112019025748A8 BR112019025748A BR112019025748A BR112019025748A8 BR 112019025748 A8 BR112019025748 A8 BR 112019025748A8 BR 112019025748 A BR112019025748 A BR 112019025748A BR 112019025748 A BR112019025748 A BR 112019025748A BR 112019025748 A8 BR112019025748 A8 BR 112019025748A8
- Authority
- BR
- Brazil
- Prior art keywords
- inhibiting
- composition
- patient
- crystal growth
- pharmaceutical composition
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 4
- MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical compound FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 title abstract 4
- 229960002586 roflumilast Drugs 0.000 title abstract 4
- 239000000203 mixture Substances 0.000 title abstract 3
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 title abstract 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 title abstract 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 2
- 239000002245 particle Substances 0.000 title 1
- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-methylpentane-2,4-diol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 abstract 2
- 229940051250 hexylene glycol Drugs 0.000 abstract 1
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Abstract
Os cristais de roflumilast foram mostrados para aumentar em tamanho durante o armazenamento. O tamanho dos cristais de roflumilast pode afetar a biodisponibilidade e a eficácia de uma composição farmacêutica. O crescimento de cristais de roflumilast pode ser inibido durante o armazenamento incluindo hexilenoglicol na composição. A composição resultante tem uma melhor biodisponibilidade e eficácia e pode ser usada para inibir a fosfodiesterase 4 em um paciente com necessidade de tal tratamento.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15/616,409 US9895359B1 (en) | 2017-06-07 | 2017-06-07 | Inhibition of crystal growth of roflumilast |
| US15/616,409 | 2017-06-07 | ||
| US15/676,373 US9907788B1 (en) | 2017-06-07 | 2017-08-14 | Inhibition of crystal growth of roflumilast |
| US15/676,356 US9884050B1 (en) | 2017-06-07 | 2017-08-14 | Inhibition of crystal growth of roflumilast |
| US15/676,356 | 2017-08-14 | ||
| US15/676,373 | 2017-08-14 | ||
| PCT/US2018/035854 WO2018226584A1 (en) | 2017-06-07 | 2018-06-04 | Inhibition of crystal growth of roflumilast |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112019025748A2 BR112019025748A2 (pt) | 2020-06-23 |
| BR112019025748A8 true BR112019025748A8 (pt) | 2022-12-13 |
Family
ID=61027004
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112019025748A BR112019025748A8 (pt) | 2017-06-07 | 2018-06-04 | Método para inibir o crescimento de cristal de roflumilast ou mudanças no tamanho de partícula em uma composição, composição farmacêutica e método de inibição de fosfodiesterase 4 em um paciente |
Country Status (13)
| Country | Link |
|---|---|
| US (8) | US9895359B1 (pt) |
| EP (1) | EP3634380B1 (pt) |
| JP (2) | JP6401884B1 (pt) |
| KR (1) | KR102607917B1 (pt) |
| CN (2) | CN112263577A (pt) |
| AU (1) | AU2018282098B2 (pt) |
| BR (1) | BR112019025748A8 (pt) |
| CA (1) | CA3006836C (pt) |
| EA (1) | EA039942B1 (pt) |
| IL (1) | IL271028B2 (pt) |
| MX (2) | MX2019014741A (pt) |
| NZ (2) | NZ759871A (pt) |
| WO (1) | WO2018226584A1 (pt) |
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| US11129818B2 (en) | 2017-06-07 | 2021-09-28 | Arcutis Biotherapeutics, Inc. | Topical roflumilast formulation having improved delivery and plasma half life |
| 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 |
| US10821075B1 (en) * | 2017-07-12 | 2020-11-03 | James Blanchard | Compositions for topical application of a medicaments onto a mammalian body surface |
| US11534493B2 (en) * | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
| BR112020024768A8 (pt) * | 2018-06-04 | 2022-12-13 | Arcutis Inc | Método para reduzir o intervalo de penetração cutânea de roflumilaste em um paciente, composição farmacêutica compreendendo roflumilaste e uma mistura emulsificante e composição farmacêutica compreendendo roflumilaste e pelo menos um emulsificante |
| US20200155524A1 (en) * | 2018-11-16 | 2020-05-21 | Arcutis, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| DE102019201034B4 (de) | 2019-01-28 | 2023-10-12 | Ford Global Technologies, Llc | Abgassystem für einen Verbrennungsmotor mit SCR-Kühlung sowie Kraftfahrzeug |
| IL295172A (en) | 2020-01-31 | 2022-09-01 | Arcutis Biotherapeutics Inc | Composition of topical roflumilest with improved administration and half-life in plasma |
| US20230134782A1 (en) * | 2020-05-07 | 2023-05-04 | Arcutis Biotherapeutics, Inc. | Treatment of skin conditions using high krafft temperature anionic surfactants |
| IL303379A (en) | 2020-12-04 | 2023-08-01 | Arcutis Biotherapeutics Inc | A topical formulation of ROFLUMILAST with antifungal activity |
| WO2022169615A1 (en) | 2021-02-05 | 2022-08-11 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| CN116867480A (zh) * | 2021-02-10 | 2023-10-10 | 洛利克斯治疗有限公司 | 眼部递送罗氟司特的方法 |
| US20230190651A1 (en) * | 2021-12-17 | 2023-06-22 | Arcutis Biotherapeutics, Inc. | Topical Aerosol Foams |
| WO2023177416A1 (en) | 2022-03-14 | 2023-09-21 | Arcutis Biotherapeutics, Inc. | Self-preserving topical pharmaceutical compositions comprising diethylene glycol monoethyl ether |
| US20240108609A1 (en) * | 2022-09-15 | 2024-04-04 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast and solvents capable of dissolving high amounts of the drug |
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