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WO2023172148A1 - Médicament - Google Patents

Médicament Download PDF

Info

Publication number
WO2023172148A1
WO2023172148A1 PCT/NZ2023/050026 NZ2023050026W WO2023172148A1 WO 2023172148 A1 WO2023172148 A1 WO 2023172148A1 NZ 2023050026 W NZ2023050026 W NZ 2023050026W WO 2023172148 A1 WO2023172148 A1 WO 2023172148A1
Authority
WO
WIPO (PCT)
Prior art keywords
xylometazoline
ibuprofen
paracetamol
pharmaceutically acceptable
acceptable salt
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.)
Ceased
Application number
PCT/NZ2023/050026
Other languages
English (en)
Inventor
Hartley Atkinson
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.)
AFT Pharmaceuticals Ltd
Original Assignee
AFT Pharmaceuticals Ltd
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 AFT Pharmaceuticals Ltd filed Critical AFT Pharmaceuticals Ltd
Priority to AU2023230563A priority Critical patent/AU2023230563A1/en
Priority to EP23767227.4A priority patent/EP4489751A1/fr
Publication of WO2023172148A1 publication Critical patent/WO2023172148A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Definitions

  • This invention relates to medication for use in treating cold or flu.
  • references in this document to a “day” mean a 24 hour period.
  • a weight amounts are given forxylometazoline per se and it should be understood that these applies to the amount of xylometazoline base.
  • the weight will be higher depending on the molecular weight of the salt component.
  • 0.12 mg xylometazoline base weighs about the same as 0.14 mg of xylometazoline hydrochloride, i.e. on account of the extra weight attributable to the hydrochloride component.
  • the invention involves the use of paracetamol, ibuprofen and xylometazoline (or a pharmaceutically acceptable salt thereof) in the production of a medication for use in treating cold and/or flu in a human, by administering or taking (optionally during the same day): a) 1 ,000 mg ( ⁇ 5%) paracetamol, orally; b) 300 mg ( ⁇ 5%) ibuprofen orally; and c) 0.12 mg ( ⁇ 5%) xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril.
  • the medication is for use in treating cold and/or flu in a human, by administering or taking (optionally during the same day): a) about 1 ,000 mg paracetamol orally, about 300 mg ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed into each nostril; or b) about 975 mg paracetamol orally, about 293 mg (e.g. 292.5 mg) ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed into each nostril.
  • paracetamol, ibuprofen and xylometazoline are for administering or taking at the same dosage event, on at least some occasions during the same day.
  • the paracetamol and ibuprofen are for administering or taking at the same dosage event, and the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking at a different dosage event, on at least some occasions during the same day.
  • the medication is such that the paracetamol and ibuprofen are for administering or taking in the amounts stated four times each day, and the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking in the amount stated two to three times during the same day.
  • the medication is such that the paracetamol and ibuprofen are for administering or taking in one or more uniform combination tablets or capsules.
  • the medication is such that the amounts of paracetamol and ibuprofen are for administering or taking in two or three uniform combination tablets or capsules.
  • the medication is such that the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking in a liquid carrier.
  • the xylometazoline (or the pharmaceutically acceptable salt) is in the form of the pharmaceutically acceptable salt, for example xylometazoline hydrochloride.
  • the medication is such that the xylometazoline hydrochloride is for administering or taking in an amount of about 0.14 mg per nostril each time the xylometazoline hydrochloride is taken or administered.
  • the invention involves a method of treating cold and/or flu in a human, comprising administering or taking (optionally during the same day): a) 1 ,000 mg ( ⁇ 5%) paracetamol orally; b) 300 mg ( ⁇ 5%) ibuprofen orally; and c) 0.12 mg ( ⁇ 5%) xylometazoline (or an equivalent amount of a pharmaceutically acceptable salt thereof) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril.
  • the method comprises administering or taking (optionally during the same day): a) about 1 ,000 mg paracetamol orally, about 300 mg ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril; or b) about 975 mg paracetamol orally, about 293 mg (e.g. about 292.5 mg) ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril.
  • the paracetamol, ibuprofen and xylometazoline are administered or taken at the same dosage event on at least some occasions during the same day.
  • the paracetamol and ibuprofen are taken or administered at the same dosage event, and the xylometazoline (or the pharmaceutically acceptable salt) is administered or taken at a different dosage event, on at least some occasions during the same day.
  • paracetamol and ibuprofen are administered or taken in the amounts stated four times each day, and the xylometazoline (or the pharmaceutically acceptable salt) is administered or taken in the amount stated two to three times in the same day.
  • paracetamol and ibuprofen are administered or taken in one or more uniform combination tablets or capsules.
  • the amounts of paracetamol and ibuprofen are administered or taken in two or three uniform combination tablets or capsules.
  • the xylometazoline (or the pharmaceutically acceptable salt) is in a liquid carrier.
  • the method comprises administering or taking the pharmaceutically acceptable salt, for example xylometazoline hydrochloride.
  • the xylometazoline hydrochloride is administered or taken in an amount of about 0.14 mg per nostril each time the xylometazoline hydrochloride is taken or administered.
  • the invention involves a medication comprising paracetamol, ibuprofen and xylometazoline (or a pharmaceutically acceptable salt thereof), for use in treating cold and/or flu in a human by administering or taking (optionally during the same day): a) 1 ,000 mg ( ⁇ 5%) paracetamol orally; b) 300 mg ( ⁇ 5%) ibuprofen orally; and c) 0.12 mg ( ⁇ 5%) xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril.
  • a medication comprising paracetamol, ibuprofen and xylometazoline (or a pharmaceutically acceptable salt thereof), for use in treating cold and/or flu in a human by administering or taking (optionally during the same day): a) 1 ,000 mg ( ⁇ 5%) paracetamol orally; b) 300 mg ( ⁇ 5%)
  • the medication is for use in treating cold and/or flu in a human by administering or taking (optionally during the same day): a) about 1 ,000 mg paracetamol orally, about 300 mg ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril; or b) about 975 mg paracetamol orally, about 293 mg (e.g. about 292.5 mg) ibuprofen orally, and about 0.12 mg xylometazoline (or an equivalent amount of the pharmaceutically acceptable salt) sprayed, or applied [e.g. via a dropper] as one or more droplets, into each nostril.
  • paracetamol, ibuprofen and xylometazoline are for administering or taking at the same dosage event, on at least some occasions during the same day.
  • the paracetamol and ibuprofen are for administering or taking at the same dosage event, and the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking at a different dosage event, on at least some occasions during the same day.
  • paracetamol and ibuprofen are for administering or taking in the amounts stated four times each day, and the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking in the amount stated two to three times during the same day.
  • paracetamol and ibuprofen are for administering or taking in one or more uniform combination tablets or capsules.
  • the medication is such that the amounts of paracetamol and ibuprofen are for administering or taking in two or three uniform combination tablets or capsules.
  • the xylometazoline (or the pharmaceutically acceptable salt) is for administering or taking in a liquid carrier.
  • the pharmaceutically acceptable salt for example xylometazoline hydrochloride.
  • the xylometazoline hydrochloride is for administering or taking in an amount of about 0.14 mg per nostril each time the xylometazoline hydrochloride is taken or administered.
  • the invention involves a medication comprising the active agents paracetamol, ibuprofen and xylometazoline, and the use of the medication, for treating cold and/or flu in a human.
  • the paracetamol and ibuprofen are for oral administration and the xylometazoline is for administration as a nasal spray.
  • the medication may therefore be in the form of a pack or kit of more than one dosage form.
  • the paracetamol and ibuprofen are preferably in the form of tablets or capsules where each of these comprises a combination of both actives.
  • the xylometazoline is preferably in the form of a nasal spray, the active being dissolved or suspended in a suitable carrier liquid, preferably an aqueous carrier, in a spray bottle.
  • the paracetamol and ibuprofen may be in different tablets or capsules, and the xylometazoline may be in a liquid, preferably aqueous, carrier in a spray bottle.
  • the paracetamol is taken at each dosage event in the amount 1 ,000 mg or 975 mg orally, split evenly between two or three tablets or capsules.
  • the ibuprofen is taken at each dosage event in the amount 300 mg, split evenly between the same two or three tablets or capsules.
  • each tablet or capsule may comprise 500 mg paracetamol + 150 mg ibuprofen, or 325 mg paracetamol + about 98 (e.g. 97.5) mg ibuprofen.
  • the xylometazoline is taken as one spray of a 1 mg/ml xylometazoline hydrochloride aqueous solution per nostril. This equates with about 0.14 mg xylometazoline hydrochloride, or 0.12 mg xylometazoline base, per nostril.
  • the paracetamol and ibuprofen are taken in the amounts mentioned at each dosage event up to four times daily, and the xylometazoline is taken in the amount mentioned at dosage event up to two or three time daily.
  • the dosage events for taking paracetamol + ibuprofen may or may not coincide with the dosage events for taking the xylometazoline. On at least some occasions all three may be taken at the same time, and on at least some occasions just the paracetamol + ibuprofen may be taken, or just the xylometazoline.
  • the trial involved 30 healthy adult participants, aged 18-50, who were each given Treatment A, B or C below under fasting conditions (10 hours fasting prior, and 4 hours fasting after).
  • the blood samples were tested for C max , or in otherwise to see what the maximum concentration of active ingredient was in the blood, and also T max , or in other words the time it took to get to the maximum concentration in the blood.
  • the trial results are as follows.
  • the medication is taken daily for at least 1 day, 2 days, 3 days, 4 days, 5 days, 6 days, 7 days , 8 days, 9 days 10 days.
  • the medication is taken daily for 4-5 days, 4-6 days, 4-7 days, 4-8 days, 4-9 days or 4-10 days.

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)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne l'utilisation de paracétamol, d'ibuprofène et de xylométazoline (ou d'un sel pharmaceutiquement acceptable de ceux-ci) dans la production d'un médicament destiné à être utilisé dans le traitement d'un refroidissement et/ou de la grippe chez un être humain, par administration ou prise de : a) 1 000 mg (± 5 %) de paracétamol, par voie orale ; b) 300 mg (± 5 %) d'ibuprofène par voie orale ; et c) 0,12 mg (± 5 %) de xylométazoline (ou une quantité équivalente du sel pharmaceutiquement acceptable) pulvérisée, ou appliquée sous la forme d'une ou de plusieurs gouttelettes, dans chaque narine.
PCT/NZ2023/050026 2022-03-08 2023-02-23 Médicament Ceased WO2023172148A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2023230563A AU2023230563A1 (en) 2022-03-08 2023-02-23 Medication
EP23767227.4A EP4489751A1 (fr) 2022-03-08 2023-02-23 Médicament

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU2022201576A AU2022201576A1 (en) 2022-03-08 2022-03-08 Medication
AU2022201576 2022-03-08

Publications (1)

Publication Number Publication Date
WO2023172148A1 true WO2023172148A1 (fr) 2023-09-14

Family

ID=87935553

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/NZ2023/050026 Ceased WO2023172148A1 (fr) 2022-03-08 2023-02-23 Médicament

Country Status (3)

Country Link
EP (1) EP4489751A1 (fr)
AU (3) AU2022201576A1 (fr)
WO (1) WO2023172148A1 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070077297A1 (en) * 2004-09-30 2007-04-05 Scolr Pharma, Inc. Modified release ibuprofen dosage form
WO2009012590A1 (fr) * 2007-07-23 2009-01-29 Kingsway Pharmaceuticals Inc. Formulations thérapeutiques pour le traitement de symptômes apparentés au rhume et à la grippe
WO2022006946A1 (fr) * 2020-07-08 2022-01-13 江苏四环生物制药有限公司 Suspension de fibres iatriques d'ibuprofène et son procédé de préparation

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992017171A1 (fr) * 1991-04-01 1992-10-15 Merck & Co., Inc. Combinaisons d'ibuprofene et de decongestionnants
US6087295A (en) * 1992-12-14 2000-07-11 Asec Manufacturing Reduction of NOx in the exhaust gases from internal combustion engines containing excess oxygen
PT1804772E (pt) * 2004-08-12 2011-12-02 Reckitt Benckiser Healthcare Grânulos que compreendem um fármaco anti-inflamatório não esteróide e um álcool de açúcar feito por extrusão de fundido
US10022339B2 (en) * 2006-04-21 2018-07-17 The Procter & Gamble Company Compositions and methods useful for treatment of respiratory illness

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070077297A1 (en) * 2004-09-30 2007-04-05 Scolr Pharma, Inc. Modified release ibuprofen dosage form
WO2009012590A1 (fr) * 2007-07-23 2009-01-29 Kingsway Pharmaceuticals Inc. Formulations thérapeutiques pour le traitement de symptômes apparentés au rhume et à la grippe
WO2022006946A1 (fr) * 2020-07-08 2022-01-13 江苏四环生物制药有限公司 Suspension de fibres iatriques d'ibuprofène et son procédé de préparation

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ANONYMOUS: "About the eEML", WORLD HEALTH ORGANIZATION (WHO), 22 January 2021 (2021-01-22), XP093092280, Retrieved from the Internet <URL:https://list.essentialmeds.org/about> [retrieved on 20231017] *
ANONYMOUS: "Common colds: Relief for a stuffy nose, cough and sore throat", INFORMEDHEALTH.ORG, 17 August 2022 (2022-08-17), XP093092283, Retrieved from the Internet <URL:https://www.ncbi.nlm.nih.gov/books/NBK279542/> [retrieved on 20231017] *
ANONYMOUS: "World Health Organization Model List of Essential Medicines", WORLD HEALTH ORGANIZATION (WHO), 1 January 2019 (2019-01-01), XP093092276, Retrieved from the Internet <URL:https://www.who.int/publications/i/item/WHOMVPEMPIAU2019.06> [retrieved on 20231017] *

Also Published As

Publication number Publication date
EP4489751A1 (fr) 2025-01-15
AU2023222825A1 (en) 2023-09-28
AU2022201576A1 (en) 2023-09-28
AU2023230563A1 (en) 2024-09-05

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