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NZ766004B2 - Parenteral formulations and uses thereof - Google Patents

Parenteral formulations and uses thereof Download PDF

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Publication number
NZ766004B2
NZ766004B2 NZ766004A NZ76600419A NZ766004B2 NZ 766004 B2 NZ766004 B2 NZ 766004B2 NZ 766004 A NZ766004 A NZ 766004A NZ 76600419 A NZ76600419 A NZ 76600419A NZ 766004 B2 NZ766004 B2 NZ 766004B2
Authority
NZ
New Zealand
Prior art keywords
parenteral
pharmaceutical composition
solubiliser
composition according
oil
Prior art date
Application number
NZ766004A
Other versions
NZ766004A (en
Inventor
Andreea Sasarman
Pierre Vankan
Grasiela Bourscheit Willmbrink
Original Assignee
Eustralis Pharmaceuticals Limited (Trading As Pressura Neuro)
Filing date
Publication date
Application filed by Eustralis Pharmaceuticals Limited (Trading As Pressura Neuro) filed Critical Eustralis Pharmaceuticals Limited (Trading As Pressura Neuro)
Priority claimed from PCT/AU2019/050075 external-priority patent/WO2019148246A1/en
Publication of NZ766004A publication Critical patent/NZ766004A/en
Publication of NZ766004B2 publication Critical patent/NZ766004B2/en

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/08—Solutions
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

This invention relates generally to therapeutic parenteral formulations comprising particular substituted pyridine based compounds, their manufacture, and methods and uses of said formulations in treating elevated intracranial pressure for indications such as, but not limited to, traumatic brain injury and stroke.

Claims (10)

THE CLAIMS DEFINING THE INVENTION ARE AS FOLLOWS:
1. A parenteral, pharmaceutical composition comprising: (i) a 2HCl salt of a compound of Formula (I) or solvate thereof: Formula (I) wherein R is CH ; and (ii) at least one solubiliser selected from the group comprising of a glycerol, glycerin, dimethylacetamide, N-methylpyrrolidone, propylene glycol, polyethylene glycol 300, polyethylene glycol 400, ricinoleate based solubiliser, cyclodextrin, polyethoxylated castor oil based solubilisers, polysorbate 80 (Tween 80), castor oil, cottonseed oil, triglyceride, sesame oil, soybean oil, or safflower oil; and (iii) an infusion fluid wherein the infusion fluid is a 5% glucose solution.
2. The parenteral, pharmaceutical composition according to claim 1, wherein the composition has an osmolality of 200 mOsm/kg to 650 mOsm/kg.
3. The parenteral, pharmaceutical composition according to claim 1 or 2, wherein the wt/wt ratio of compound of Formula (I) or a pharmaceutically acceptable salt, or solvate thereof to solubiliser is 1:40 to 1:250.
4. The parenteral, pharmaceutical composition according to anyone of claims 1 to 3, wherein the wt/wt ratio of the at least one solubiliser to the infusion fluid is 1:10 to 1:2000.
5. The parenteral, pharmaceutical composition according to any of claims 1 to 4, wherein the composition is maintained at a pH of between 3 to 7.
6. Use of a parenteral, pharmaceutical composition comprising: (i) a 2HCl salt of a compound of Formula (I) or solvate thereof: Formula (I) wherein R1 is CH3; and (ii) at least one solubiliser selected from the group comprising of a glycerol, glycerin, dimethylacetamide, N-methylpyrrolidone, propylene glycol, polyethylene glycol 300, polyethylene glycol 400, ricinoleate based solubiliser, cyclodextrin, polyethoxylated castor oil based solubilisers, polysorbate 80 (Tween 80), castor oil, cottonseed oil, triglyceride, sesame oil, soybean oil, or safflower oil; and (iii) an infusion fluid wherein the infusion fluid is a 5% glucose solution, in the manufacture of a medicament for treating elevated intracranial pressure in a subject in need thereof.
7. Use of a parenteral, pharmaceutical composition according to claim 6, wherein the composition has an osmolality of 200 mOsm/kg to 650 mOsm/kg.
8. Use of a parenteral, pharmaceutical composition according to claim 6 or 7, wherein the wt/wt ratio of compound of Formula (I) or a pharmaceutically acceptable salt, or solvate thereof to solubiliser is 1:40 to 1:250.
9. Use of a parenteral, pharmaceutical composition according to anyone of claims 6 to 8, wherein the wt/wt ratio of the at least one solubiliser to the infusion fluid is 1:10 to 1:2000.
10. Use of a parenteral, pharmaceutical composition according to any of claims 6 to 9, wherein the composition is maintained at a pH of between 3 to 7.
NZ766004A 2019-02-01 Parenteral formulations and uses thereof NZ766004B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU2018900325A AU2018900325A0 (en) 2018-02-02 Parenteral Formulations and Uses Thereof
PCT/AU2019/050075 WO2019148246A1 (en) 2018-02-02 2019-02-01 Parenteral formulations and uses thereof

Publications (2)

Publication Number Publication Date
NZ766004A NZ766004A (en) 2024-11-29
NZ766004B2 true NZ766004B2 (en) 2025-03-04

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