MX2020003001A - Composiciones farmacéuticas de roflumilast en mezclas acuosas de solventes miscibles en agua, farmacéuticamente aceptables. - Google Patents
Composiciones farmacéuticas de roflumilast en mezclas acuosas de solventes miscibles en agua, farmacéuticamente aceptables.Info
- Publication number
- MX2020003001A MX2020003001A MX2020003001A MX2020003001A MX2020003001A MX 2020003001 A MX2020003001 A MX 2020003001A MX 2020003001 A MX2020003001 A MX 2020003001A MX 2020003001 A MX2020003001 A MX 2020003001A MX 2020003001 A MX2020003001 A MX 2020003001A
- Authority
- MX
- Mexico
- Prior art keywords
- water
- roflumilast
- miscible
- pharmaceutically acceptable
- pharmaceutical compositions
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 4
- 239000002904 solvent Substances 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical group FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 title abstract 2
- 229960002586 roflumilast Drugs 0.000 title abstract 2
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 abstract 3
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 2
- 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 abstract 1
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 abstract 1
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 abstract 1
- 239000000839 emulsion Substances 0.000 abstract 1
- 239000000499 gel Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000000243 solution Substances 0.000 abstract 1
- 239000000725 suspension Substances 0.000 abstract 1
- 230000000699 topical effect Effects 0.000 abstract 1
Classifications
-
- 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
- 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
- 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
- A61K9/06—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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
- Dispersion Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La baja solubilidad acuosa de roflumilast en preparaciones parenterales y emulsiones tópicas, suspensiones, geles o soluciones se puede mejorar al incluir una mezcla de solventes miscibles en agua en la composición farmacéutica; la mezcla de solventes miscibles en agua puede incluir dietilen glicol monoetil éter (Nombre comercial Transcutol(r); abreviado DEGEE) y agua; la relación de dietilen glicol monoetil éter a agua es de 1:10 a 20:1; la composición resultante tiene biodisponibilidad y eficacia mejoradas y se puede utilizar para inhibir la fosfodiesterasa 4 en un paciente en necesidad de dicho tratamiento.
Applications Claiming Priority (2)
| 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 |
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| MX2020003001A true MX2020003001A (es) | 2020-09-28 |
Family
ID=63794682
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020003001A MX2020003001A (es) | 2017-09-22 | 2018-09-19 | Composiciones farmacéuticas de roflumilast en mezclas acuosas de solventes miscibles en agua, farmacéuticamente aceptables. |
| MX2023011557A MX2023011557A (es) | 2017-09-22 | 2020-03-18 | Composiciones farmaceuticas de roflumilast en mezclas acuosas de solventes miscibles en agua, farmaceuticamente aceptables. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2023011557A MX2023011557A (es) | 2017-09-22 | 2020-03-18 | Composiciones farmaceuticas de roflumilast en mezclas acuosas de solventes miscibles en agua, farmaceuticamente aceptables. |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US11534493B2 (es) |
| EP (2) | EP4316590A3 (es) |
| JP (3) | JP7191944B2 (es) |
| KR (1) | KR102681877B1 (es) |
| CN (2) | CN119386013A (es) |
| AU (1) | AU2018337752B2 (es) |
| CA (1) | CA3076002A1 (es) |
| EA (1) | EA202090813A1 (es) |
| ES (1) | ES2972843T3 (es) |
| IL (1) | IL273376B2 (es) |
| MX (2) | MX2020003001A (es) |
| WO (1) | WO2019060379A1 (es) |
Families Citing this family (17)
| 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 |
| US20200155524A1 (en) | 2018-11-16 | 2020-05-21 | Arcutis, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| US12042487B2 (en) | 2018-11-16 | 2024-07-23 | Arcutis Biotherapeutics, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| 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 |
| US12011437B1 (en) | 2017-06-07 | 2024-06-18 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| US11534493B2 (en) * | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
| AU2019281888B2 (en) | 2018-06-04 | 2024-05-02 | Arcutis Biotherapeutics, Inc. | Method and formulation for improving roflumilast skin penetration lag time |
| EP4041211A4 (en) * | 2019-10-11 | 2023-09-06 | Zenvision Pharma LLP | IMPROVED TOPICAL COMPOSITION OF COLCHICINE |
| BR112022015104A2 (pt) * | 2020-01-31 | 2022-09-27 | Arcutis Biotherapeutics Inc | Método para melhorar a distribuição e estender a meia-vida plasmática de uma composição de roflumilaste e uso de uma composição |
| MX2023006602A (es) | 2020-12-04 | 2023-08-07 | Arcutis Biotherapeutics Inc | Formulación tópica de roflumilast que tiene propiedades antimicoticas. |
| WO2022169615A1 (en) * | 2021-02-05 | 2022-08-11 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| WO2023129215A1 (en) | 2021-12-28 | 2023-07-06 | Arcutis Biotherapeutics, Inc. | Topical roflumilast aerosol foams |
| KR20250057103A (ko) | 2022-09-15 | 2025-04-28 | 아큐티스 바이오테라퓨틱스, 인크. | 로플루밀라스트 및 많은 양의 약물을 용해시킬 수 있는 용매의 약학 조성물 |
| WO2025054483A1 (en) | 2023-09-07 | 2025-03-13 | Arcutis Biotherapeutics, Inc. | Dosing regimens using topical roflumilast compositions |
| US20250090509A1 (en) * | 2023-09-15 | 2025-03-20 | Arcutis Biotherapeutics, Inc. | Methods of reducing itch using topical roflumilast compositions |
| CN117462487A (zh) * | 2023-11-29 | 2024-01-30 | 沈阳药科大学 | 一种罗氟司特油凝胶及其制备方法 |
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| AU2259692A (en) * | 1991-07-03 | 1993-02-11 | Sano Corporation | Composition and method for transdermal delivery of diclofenac |
| SI0706513T1 (en) | 1993-07-02 | 2002-10-31 | Altana Pharma Ag | Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors |
| GB9618974D0 (en) * | 1996-09-11 | 1996-10-23 | Glaxo Group Ltd | Medicaments |
| FR2758459B1 (fr) | 1997-01-17 | 1999-05-07 | Pharma Pass | Composition pharmaceutique de fenofibrate presentant une biodisponibilite elevee et son procede de preparation |
| UA80393C2 (uk) | 2000-12-07 | 2007-09-25 | Алтана Фарма Аг | Фармацевтична композиція, яка містить інгібітор фде 4, диспергований в матриці |
| MY140561A (en) | 2002-02-20 | 2009-12-31 | Nycomed Gmbh | Dosage form containing pde 4 inhibitor as active ingredient |
| DK2020243T3 (en) * | 2002-05-28 | 2018-11-19 | Astrazeneca Ab | Pharmaceutical composition which can be applied topically |
| DE602004023921D1 (de) | 2003-03-10 | 2009-12-17 | Nycomed Gmbh | Neues verfahren zur herstellung vonroflumilast |
| US20060204526A1 (en) * | 2003-08-13 | 2006-09-14 | Lathrop Robert W | Emulsive composition containing Dapsone |
| EP1670433B1 (en) * | 2003-10-10 | 2011-11-23 | Antares Pharma IPL AG | Transdermal pharmaceutical formulation for minimizing skin residues |
| DE102004046235A1 (de) | 2004-09-22 | 2006-03-30 | Altana Pharma Ag | Arzneimittelzubereitung |
| JPWO2006041121A1 (ja) * | 2004-10-13 | 2008-05-15 | 協和醗酵工業株式会社 | 慢性皮膚疾患の治療および/または予防剤 |
| FR2898499B1 (fr) * | 2006-03-15 | 2008-11-28 | Galderma Sa | Nouvelles compositions topiques sous forme d'emulsion h/e comprenant un glycol pro-penetrant |
| WO2007127158A2 (en) * | 2006-04-25 | 2007-11-08 | Croda, Inc | Modification of percutaneous absorption of topically active materials |
| CN101541321A (zh) * | 2006-09-06 | 2009-09-23 | Isw集团公司 | 局部用组合物 |
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| WO2013030789A1 (en) | 2011-08-30 | 2013-03-07 | Ranbaxy Laboratories Limited | Pharmaceutical oral solid dosage form containing a poorly water soluble pde - iv inhibitor |
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| CN110403922A (zh) | 2013-01-28 | 2019-11-05 | 理森制药股份公司 | 通过吸入罗氟司特n-氧化物治疗自身免疫、呼吸和/或炎性病症的方法 |
| MX2013001279A (es) * | 2013-01-31 | 2013-08-26 | Miguel Angel Garcia Perez | Composicion farmaceutica con un inhibidor selectivo de la enzima fosfodiesterasa en forma de gel oral. |
| US20140275265A1 (en) * | 2013-03-12 | 2014-09-18 | Core Products International, Inc. | Therapeutic cream for application to skin |
| UA119324C2 (uk) * | 2013-04-02 | 2019-06-10 | Теміс Медікер Лімітед | Композиції фармацевтично активних речовин, що містять моноетиловий ефір діетиленгліколю або інші алкільні похідні |
| WO2015132708A1 (en) | 2014-03-07 | 2015-09-11 | Torrent Pharmaceuticals Limited | Pharmaceutical composition of roflumilast |
| JP2017529334A (ja) * | 2014-08-27 | 2017-10-05 | アッヴィ・インコーポレイテッド | 局所製剤 |
| PL3383363T3 (pl) | 2015-11-30 | 2021-05-31 | Anacor Pharmaceuticals, Inc. | Preparaty farmaceutyczne do stosowania miejscowego do leczenia stanów związanych z zapaleniem |
| BR112018076114A2 (pt) * | 2016-06-15 | 2019-03-26 | Torrent Pharmaceuticals Limited | composições tópicas de apremilast |
| US9895359B1 (en) * | 2017-06-07 | 2018-02-20 | Arcutis, Inc. | Inhibition of crystal growth of roflumilast |
| US11534493B2 (en) | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
-
2017
- 2017-09-22 US US15/712,900 patent/US11534493B2/en active Active
-
2018
- 2018-09-19 WO PCT/US2018/051691 patent/WO2019060379A1/en not_active Ceased
- 2018-09-19 ES ES18783250T patent/ES2972843T3/es active Active
- 2018-09-19 JP JP2020516414A patent/JP7191944B2/ja active Active
- 2018-09-19 AU AU2018337752A patent/AU2018337752B2/en active Active
- 2018-09-19 IL IL273376A patent/IL273376B2/en unknown
- 2018-09-19 EA EA202090813A patent/EA202090813A1/ru unknown
- 2018-09-19 CA CA3076002A patent/CA3076002A1/en active Pending
- 2018-09-19 KR KR1020207008018A patent/KR102681877B1/ko active Active
- 2018-09-19 MX MX2020003001A patent/MX2020003001A/es unknown
- 2018-09-19 CN CN202411489846.6A patent/CN119386013A/zh active Pending
- 2018-09-19 EP EP23214185.3A patent/EP4316590A3/en active Pending
- 2018-09-19 EP EP18783250.6A patent/EP3684334B1/en active Active
- 2018-09-19 CN CN201880060842.2A patent/CN111107836A/zh active Pending
-
2020
- 2020-03-18 MX MX2023011557A patent/MX2023011557A/es unknown
-
2022
- 2022-11-22 US US18/057,777 patent/US20230091358A1/en not_active Abandoned
- 2022-12-07 JP JP2022195731A patent/JP7402301B2/ja active Active
-
2023
- 2023-12-07 JP JP2023207175A patent/JP7664358B2/ja active Active
-
2025
- 2025-06-18 US US19/242,164 patent/US20250312457A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP4316590A2 (en) | 2024-02-07 |
| KR20200058402A (ko) | 2020-05-27 |
| IL273376B1 (en) | 2024-03-01 |
| US11534493B2 (en) | 2022-12-27 |
| JP7402301B2 (ja) | 2023-12-20 |
| JP2024028911A (ja) | 2024-03-05 |
| EP3684334A1 (en) | 2020-07-29 |
| KR102681877B1 (ko) | 2024-07-04 |
| CN119386013A (zh) | 2025-02-07 |
| JP2023027195A (ja) | 2023-03-01 |
| WO2019060379A1 (en) | 2019-03-28 |
| JP7664358B2 (ja) | 2025-04-17 |
| BR112020005421A2 (pt) | 2020-09-29 |
| EP3684334B1 (en) | 2023-12-06 |
| AU2018337752A1 (en) | 2020-04-09 |
| EA202090813A1 (ru) | 2020-08-14 |
| US20250312457A1 (en) | 2025-10-09 |
| IL273376A (en) | 2020-05-31 |
| BR112020005421A8 (pt) | 2022-12-13 |
| CN111107836A (zh) | 2020-05-05 |
| EP3684334C0 (en) | 2023-12-06 |
| EP4316590A3 (en) | 2024-05-01 |
| IL273376B2 (en) | 2024-07-01 |
| US20230091358A1 (en) | 2023-03-23 |
| MX2023011557A (es) | 2023-10-09 |
| ES2972843T3 (es) | 2024-06-17 |
| AU2018337752B2 (en) | 2024-03-28 |
| JP7191944B2 (ja) | 2022-12-19 |
| JP2020534303A (ja) | 2020-11-26 |
| CA3076002A1 (en) | 2019-03-28 |
| US20190091333A1 (en) | 2019-03-28 |
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