CA3166300A1 - Topical roflumilast formulation having improved delivery and plasma half-life - Google Patents
Topical roflumilast formulation having improved delivery and plasma half-life Download PDFInfo
- Publication number
- CA3166300A1 CA3166300A1 CA3166300A CA3166300A CA3166300A1 CA 3166300 A1 CA3166300 A1 CA 3166300A1 CA 3166300 A CA3166300 A CA 3166300A CA 3166300 A CA3166300 A CA 3166300A CA 3166300 A1 CA3166300 A1 CA 3166300A1
- Authority
- CA
- Canada
- Prior art keywords
- roflumilast
- phosphate
- formulation
- ceteth
- topical
- 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
Links
- 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 claims abstract description 181
- 239000000203 mixture Substances 0.000 title claims abstract description 179
- 229960002586 roflumilast Drugs 0.000 title claims abstract description 172
- 238000009472 formulation Methods 0.000 title description 90
- 230000000699 topical effect Effects 0.000 title description 33
- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-methylpentane-2,4-diol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 claims abstract description 80
- 229910019142 PO4 Inorganic materials 0.000 claims abstract description 44
- 239000010452 phosphate Substances 0.000 claims abstract description 44
- 229940051250 hexylene glycol Drugs 0.000 claims abstract description 39
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims abstract description 30
- 238000011282 treatment Methods 0.000 claims abstract description 29
- RNPXCFINMKSQPQ-UHFFFAOYSA-N dicetyl hydrogen phosphate Chemical compound CCCCCCCCCCCCCCCCOP(O)(=O)OCCCCCCCCCCCCCCCC RNPXCFINMKSQPQ-UHFFFAOYSA-N 0.000 claims abstract description 28
- 229940093541 dicetylphosphate Drugs 0.000 claims abstract description 28
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims abstract description 28
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims abstract description 25
- 238000000034 method Methods 0.000 claims abstract description 17
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 68
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- 238000011200 topical administration Methods 0.000 claims description 12
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- NEOZOXKVMDBOSG-UHFFFAOYSA-N propan-2-yl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OC(C)C NEOZOXKVMDBOSG-UHFFFAOYSA-N 0.000 description 1
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- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 1
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- QUCDWLYKDRVKMI-UHFFFAOYSA-M sodium;3,4-dimethylbenzenesulfonate Chemical compound [Na+].CC1=CC=C(S([O-])(=O)=O)C=C1C QUCDWLYKDRVKMI-UHFFFAOYSA-M 0.000 description 1
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- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
- 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
- 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
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- 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
- A61P17/04—Antipruritics
-
- 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]
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dispersion Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16/778,845 US11129818B2 (en) | 2017-06-07 | 2020-01-31 | Topical roflumilast formulation having improved delivery and plasma half life |
| US16/778,845 | 2020-01-31 | ||
| PCT/US2021/015740 WO2021155173A1 (en) | 2020-01-31 | 2021-01-29 | Topical roflumilast formulation having improved delivery and plasma half-life |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3166300A1 true CA3166300A1 (en) | 2021-08-05 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3166300A Pending CA3166300A1 (en) | 2020-01-31 | 2021-01-29 | Topical roflumilast formulation having improved delivery and plasma half-life |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP4096630A1 (ja) |
| JP (1) | JP2023513092A (ja) |
| KR (1) | KR20220134617A (ja) |
| CN (1) | CN115551478A (ja) |
| AU (1) | AU2021214399A1 (ja) |
| BR (1) | BR112022015104A2 (ja) |
| CA (1) | CA3166300A1 (ja) |
| IL (1) | IL295172A (ja) |
| MX (1) | MX2022009399A (ja) |
| WO (1) | WO2021155173A1 (ja) |
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| WO2024058848A1 (en) * | 2022-09-15 | 2024-03-21 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast and solvents capable of dissolving high amounts of the drug |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
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| PT706513E (pt) | 1993-07-02 | 2002-10-31 | Byk Gulden Lomberg Chem Fab | Benzimidazois substituidos por fluoralcoxi e sua utilizacao como inibidores de fosfodiesterase nucleotidica ciclica |
| US5863560A (en) | 1996-09-11 | 1999-01-26 | Virotex Corporation | Compositions and methods for topical application of therapeutic agents |
| ES2354971T3 (es) | 2002-05-28 | 2011-03-21 | Nycomed Gmbh | Uso oftalmológico de roflumilast para el tratamiento de enfermedades de los ojos. |
| DE102004046235A1 (de) | 2004-09-22 | 2006-03-30 | Altana Pharma Ag | Arzneimittelzubereitung |
| US20200155524A1 (en) * | 2018-11-16 | 2020-05-21 | Arcutis, 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 |
| US11534493B2 (en) * | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
| CA3102689C (en) * | 2018-06-04 | 2023-08-29 | Arcutis, Inc. | Method and formulation for improving roflumilast skin penetration lag time |
-
2021
- 2021-01-29 AU AU2021214399A patent/AU2021214399A1/en active Pending
- 2021-01-29 IL IL295172A patent/IL295172A/en unknown
- 2021-01-29 BR BR112022015104A patent/BR112022015104A2/pt unknown
- 2021-01-29 KR KR1020227029999A patent/KR20220134617A/ko active Search and Examination
- 2021-01-29 MX MX2022009399A patent/MX2022009399A/es unknown
- 2021-01-29 WO PCT/US2021/015740 patent/WO2021155173A1/en unknown
- 2021-01-29 JP JP2022546613A patent/JP2023513092A/ja active Pending
- 2021-01-29 CA CA3166300A patent/CA3166300A1/en active Pending
- 2021-01-29 EP EP21708433.4A patent/EP4096630A1/en active Pending
- 2021-01-29 CN CN202180017566.3A patent/CN115551478A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| IL295172A (en) | 2022-09-01 |
| AU2021214399A1 (en) | 2022-08-25 |
| JP2023513092A (ja) | 2023-03-30 |
| CN115551478A (zh) | 2022-12-30 |
| MX2022009399A (es) | 2022-09-19 |
| EP4096630A1 (en) | 2022-12-07 |
| BR112022015104A2 (pt) | 2022-09-27 |
| KR20220134617A (ko) | 2022-10-05 |
| WO2021155173A1 (en) | 2021-08-05 |
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