WO2022162711A1 - Composition pour le traitement d'états douloureux et/ou inflammatoires - Google Patents

Composition pour le traitement d'états douloureux et/ou inflammatoires Download PDF

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Publication number
WO2022162711A1
WO2022162711A1 PCT/IT2022/050010 IT2022050010W WO2022162711A1 WO 2022162711 A1 WO2022162711 A1 WO 2022162711A1 IT 2022050010 W IT2022050010 W IT 2022050010W WO 2022162711 A1 WO2022162711 A1 WO 2022162711A1
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composition
cbd
substances
pain
inflammatory
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PCT/IT2022/050010
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English (en)
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Antonio SCIALPI
Claudio Sebastiano Gardana
Elena PAFUNDI
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Specchiasol S.R.L.
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Priority to EP22705910.2A priority Critical patent/EP4284351A1/fr
Publication of WO2022162711A1 publication Critical patent/WO2022162711A1/fr

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    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K31/12—Ketones
    • 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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/13—Coniferophyta (gymnosperms)
    • A61K36/15—Pinaceae (Pine family), e.g. pine or cedar
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
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    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/26—Aristolochiaceae (Birthwort family), e.g. heartleaf
    • A61K36/268—Asarum (wild ginger)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A61K36/324—Boswellia, e.g. frankincense
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A61K36/328—Commiphora, e.g. mecca myrrh or balm of Gilead
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/906—Zingiberaceae (Ginger family)
    • A61K36/9066—Curcuma, e.g. common turmeric, East Indian arrowroot or mango ginger
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/906—Zingiberaceae (Ginger family)
    • A61K36/9068—Zingiber, e.g. garden ginger
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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]

Definitions

  • Embodiments described here concern a composition based on cannabidiol (CBD), in particular for the therapeutic treatment of painful and/or inflammatory states. More specifically, the embodiments described here concern a composition comprising a synergistic combination of CBD or an extract containing CBD and one or more natural ingredients that help the pain relief and/or anti-inflammatory activity.
  • CBD cannabidiol
  • the composition described here can be formulated, for example, as a pharmaceutical composition or as a food supplement composition.
  • pharmacological agents generally used to treat the different types of painful states are many and include, for example, opiates, non-steroidal anti-inflammatory drugs (NSAIDs), anticonvulsants, antidepressants and ketamine.
  • NSAIDs non-steroidal anti-inflammatory drugs
  • anticonvulsants anticonvulsants
  • antidepressants antidepressants
  • ketamine the negative side effects of these drugs limit their therapeutic dosage, and in the final analysis reduce their therapeutic efficacy.
  • Document EP- A- 1.542.657 describes a liquid formulation of cannabinoid for administration via the mucosa, in particular by spraying.
  • one purpose of the present invention is to provide a composition in particular for the therapeutic treatment of painful and/or inflammatory states which prevents the side effects typical of synthetic painkillers.
  • the Applicant has devised, tested and embodied the present invention to overcome the shortcomings of the state of the art and to obtain these and other purposes and advantages.
  • the embodiments concern a composition comprising a synergistic combination of Cannabidiol (CBD), or an extract containing CBD, with one or more substances or molecules, and/or respective natural dry extracts, with pain-relieving and/or anti-inflammatory activity.
  • CBD Cannabidiol
  • CBD therapeutic action of CBD increases if associated with other molecules and/or natural extracts with pain- relieving and/or anti-inflammatory activity.
  • various associations provided here were found to be more effective against pain and inflammatory situations than the action of the individual functional principles.
  • the composition described here is a pharmaceutical composition.
  • the pharmaceutical composition also comprises one or more pharmaceutically acceptable excipients.
  • the composition described here is a food supplement.
  • the composition described here also comprises dry extracts, coenzymes or a combination thereof.
  • composition described here is free of terpenes.
  • the natural pain-relieving, antiinflammatory agents and the respective dry extracts present in the composition described here are selected from Palmitoylethanolamide (PEA) and/or L- acetylcamitine (LAC) and/or Boswellic acids from Boswellia serrata and/or Lipoic acid and/or furanodienes from Chommiphora myrrha and/or harpagoside from Harphagophytum Procumbens, and/or gingerols and shogaols from ginger and/or curcumin or a combination thereof.
  • PDA Palmitoylethanolamide
  • LAC L- acetylcamitine
  • Boswellic acids from Boswellia serrata and/or Lipoic acid and/or furanodienes from Chommiphora myrrha and/or harpagoside from Harphagophytum Procumbens
  • gingerols and shogaols from ginger and/or curcumin or
  • the composition as above comprises CBD and at least two natural pain-relieving and/or anti-inflammatory substances.
  • One of these two substances can for example be PEA and the other can be, for example, a plant-derived anti-inflammatory substance.
  • the composition as above comprises CBD and Palmitoylethanolamide (PEA), wherein the weight ratio of PEA:CBD in said composition is from 5:1 to 1:1, in particular from 3:1 to 1:1, more in particular from 2:1 to 1:1.
  • PDA Palmitoylethanolamide
  • An example of implementation can be 1 : 1.
  • composition as above comprises CBD, Palmitoylethanolamide (PEA) and one or more plant-derived anti-inflammatory substances.
  • PDA Palmitoylethanolamide
  • the plant-derived anti-inflammatory substances can be selected from gingerols and shogaols from ginger Zingiber officinale), curcumin from Curcuma longa, harpagoside from Harphagophytum Procumbens.
  • plant-derived anti-inflammatory substances can be standardized plant extracts.
  • the composition as above comprises CBD and PEA and is free of other plant-derived anti-inflammatory and/or pain- relieving substances and/or other active principles or substances, such composition possibly including suitable and pharmaceutically acceptable excipients.
  • the weight ratio of PEA:CBD in such composition is from 5:1 to 1 :1, in particular from 3:1 to 1:1, more in particular from 2:1 to 1 : 1.
  • An example of implementation can be 1:1.
  • composition that provides the association of the substances described above can be made in the form of powder, for example single- or multi-layer tablets, single- or multi-layer tablets with differentiated release, soluble sachets, hard gelatin capsules or softgels or any other form suitable for oral intake.
  • composition according to the embodiments described here can be made available, as well as in powder form, also in liquid form.
  • the liquid form can be made in the form of simple syrups, emulsified syrups, suspensions or preparations for extemporaneous use.
  • the present description also includes the intervals that derive from uniting or overlapping two or more intervals described, unless otherwise indicated.
  • the present description also includes the intervals that can derive from the combination of two or more values taken at different points, unless otherwise indicated.
  • CBD is a cannabinoid found in Cannabis sativa.
  • cannabinoid refers to compounds that activate G-protein coupled to cannabinoid receptors 1 and 2 (CB1 and CB2).
  • CB1 receptors located mainly on the neurons of the hippocampus and basal ganglia, mediate the psychoactive actions of cannabinoids.
  • CB2 receptors are found mainly on tissues and circulating cells of the immune system.
  • CBD Unlike the psychoactive constituent Tetrahydrocannabinol (THC), CBD does not exhibit psychoactive activity because it has no direct effect on CB1 and CB2 receptors, but it modulates the effect of the agonists, suggesting an allosteric function. Furthermore, CBD binds to PPARy, GPR3/6/12/18/55, TRPV1/2, TRPA1, to the 5-hydroxytryptamine receptor and to mitochondrial proteins. Furthermore, CBD is well tolerated even when administered in high concentrations and the therapeutic benefits it brings in the treatment of childhood epilepsy are well documented. On the contrary, until now its effects on inflammation have been mainly studied on animal models.
  • CBD fatty acid amide hydrolase
  • CBD also counteracts THC-induced psychoactivity, sedation and tachycardia.
  • CBD comes with a long list of medical properties.
  • the main one among these is the ability to relieve the symptoms of various ailments, such as chronic pain, inflammation, migraines, arthritis, spasms, epilepsy and schizophrenia.
  • CBD has some anti-cancer properties, and new uses and applications are constantly being discovered thanks to medical research.
  • the Applicant has found for the first time that the association of CBD with one or more natural ingredients or substances that act as agents with pain- relieving and/or anti-inflammatory properties, in particular molecules, and/or respective natural pain-relieving and/or anti-inflammatory dry extracts, more in particular one or more pain-relieving and anti-inflammatory substances present in nature, results in a synergistic combination between CBD and the above natural ingredients or substances that act as agents with pain-relieving and/or antiinflammatory properties.
  • This synergistic combination is particularly effective for therapeutic treatment, in particular of painful and/or inflammatory states.
  • the embodiments described here therefore provide a safe composition of CBD or a CBD-containing extract with one or more molecules and/or natural extracts with pain-relieving and/or anti-inflammatory properties, such composition exhibiting ameliorative and synergistic effects in therapeutic treatment, in particular of painful or inflammatory states, compared to CBD alone.
  • the composition described here comprises CBD from 5 to 90% w/w of the composition.
  • the composition described here comprises the one or more natural pain-relieving and/or anti-inflammatory substances as above from 0.5 to 90% w/w of the composition.
  • composition described here can be for human or veterinary use.
  • composition described here can be, in particular, a pharmaceutical composition.
  • composition as above can be provided or used in both powder and also liquid form.
  • the composition described here comprises CBD in liquid or solid form, wherein the quantity of CBD in the composition is from 5 to 1000 mg per unit dose.
  • the one or more natural pain-relieving and/or antiinflammatory substances as above are one or more selected from Palmitoylethanolamide (PEA) or L-acetylcamitine (LAC) and/or Boswellic acids from Boswellia serrata and/or Lipoic acid and/or a mixture of antioxidant substances extracted mainly from the bark of Maritime Pine (Pinus pinaster) and/or from the seeds of Vitis vinifera (for example Pycnogenol) and/or furanodienes from Chommiphora myrrha, or extract of Chommiphora myrrha as a source of furanodienes and/or harpagoside from Harphagophytum Procumbens, and/or gingerols and shogaols from ginger and/or curcumin from Curcuma longa, or a combination thereof.
  • the quantity of the natural pain-relieving and/or anti-inflammatory substances as above in the composition described here is from Palmitoylethanolamide
  • the composition described here comprises CBD and PEA.
  • composition described here is free of terpenes.
  • the composition as above comprises CBD and Palmitoylethanolamide (PEA), wherein the weight ratio of PEA:CBD in such composition is from 5:1 to 1:1, in particular from 3:1 to 1:1, more in particular from 2: 1 to 1 : 1.
  • PDA Palmitoylethanolamide
  • An example of implementation can be 1:1.
  • composition as above comprises CBD, Palmitoylethanolamide (PEA) and one or more plant-derived anti-inflammatory substances.
  • PDA Palmitoylethanolamide
  • such plant-derived anti-inflammatory substances are selected from gingerols and shogaols from ginger (Zingiber officinale , curcumin from Curcuma longa, harpagoside from Harphagophytum Procumbens.
  • plant-derived anti-inflammatory substances are standardized plant extracts.
  • composition described here comprises CBD, PEA and titrated dry extract of Commiphora myrrha.
  • composition described here comprises CBD, PEA and curcumin or an extract containing curcumin.
  • composition described here comprises CBD, titrated dry extract of Boswellia s errata and LAC.
  • composition described here comprises CBD and Lipoic acid.
  • the composition described here comprises CBD and a mixture of antioxidant substances extracted mainly from the bark of Maritime Pine (Pinus pinaster) and/or from the seeds of Vitis vinifera (for example Pycnogenol).
  • composition described here comprises CBD, PEA and ginger or an extract containing ginger.
  • composition described here comprises CBD, PEA and Harphagophytum Procumbens or an extract containing harpagoside from Harphagophytum Procumbens.
  • composition described here comprises CBD and LAC.
  • composition described here comprises CBD, PEA and LAC.
  • the composition described here can include one or more compounds with antioxidant activity, for example selected from a mixture of antioxidant substances extracted mainly from the bark of maritime pine Pinus pinaster) and/or from the seeds of Vitis vinifera (for example Pycnogenol), Lipoic acid, n-Acetyl cysteine, Polyphenols, Resveratrol, Polydatin, Quercetin, Rutin, Luteolin, or a combination thereof.
  • Such one or more compounds with antioxidant activity can for example be present between 5 and 60% w/w of the composition.
  • both the mixture of antioxidants extracted from Pinus pinaster and/or from Vitis vinifera (for example Pycnogenol) and also Lipoic acid are strong antioxidants that also have pain-relieving and/or anti-inflammatory properties and therefore can act as natural pain-relieving and/or antiinflammatory substances in the composition in accordance with the present description.
  • the composition described here can include CBD together with the mixture of antioxidants extracted from Pinus pinaster and/or from Vitis vinifera (for example Pycnogenol) and/or Lipoic acid.
  • composition described here can be made or supplied in the form of single- or multi-layer tablets, capsules, softgels, granules, powder, sachets, suspensions, solutions, formulations with modified release, double chamber sachets, topical formulations such as creams, ointments, emulsions and dispersions.
  • composition described here can comprise suitable and pharmaceutically acceptable excipients, such as diluents, disintegrants, binders, solubilizing agents, lubricants, sliding agents, solvents, desiccants, etc., or a combination thereof.
  • suitable and pharmaceutically acceptable excipients such as diluents, disintegrants, binders, solubilizing agents, lubricants, sliding agents, solvents, desiccants, etc., or a combination thereof.
  • the composition described here can comprise, in addition or as a replacement, further additives and/or excipients of pharmaceutical or food grade, that is, substances without therapeutic activity suitable for pharmaceutical or food use.
  • the ingredients acceptable for pharmaceutical or food use comprise all the auxiliary substances known to the person of skill in the art such as, as a nonlimiting example, diluents, solvents, solubilizers, thickeners, sweeteners, flavorings, dyes, lubricants, surfactants, antimicrobials, antioxidants, preservatives, buffers to stabilize the pH and mixtures thereof.
  • the excipients can be in powder form.
  • powdered excipients are selected from microcrystalline cellulose, lactose, starch, silica, ammonium alginate, calcium carbonate, calcium lactate, di- or tri-basic calcium phosphate, calcium silicate, calcium sulphate, com starch, pregelatinized starch, erythritol, ethyl cellulose, fructose, glyceryl palmitostearate, isomalt, kaolin, sugar alcohols, lactitol, magnesium carbonate, magnesium oxide, maltose, mannitol, medium chain triglycerides, sodium alginate, sodium chloride, sorbitol, P-cyclodextrins, talc, trehalose.
  • the quantity of excipient in the composition described here can, for example, be from 5 to 50% w/w of the composition.
  • the excipients can be liquid.
  • such liquid excipients act as a solvent of the substances present, that is, the CBD and the natural substances with pain-relieving and/or anti-inflammatory properties, for example PEA and the plant-derived anti-inflammatory substances described above.
  • Such liquid excipients can for example be selected from water, ethyl alcohol, isopropyl alcohol, propylene glycol, almond oil, benzyl alcohol, benzyl benzoate, butylene glycol, carbon dioxide, castor oil, com oil, cottonseed oil, dimethyl ether, albumin, dimethyl phthalate, dimethyl sulfoxide, dimethylacetamide, ethyl acetate, ethyl lactate, ethyl oleate, glycerin, glycofurol, isopropyl myristate, isopropyl palmitate, light mineral oil, medium chain triglycerides, methyl lactate, mineral oil, monoethanolamine, olive oil, peanut oil, polyethylene glycol, poly oxy 1 35 castor oil, propylene carbonate, pyrrolidone, safflower oil, sesame oil, soybean oil, sunflower oil, triacetin, tricaprilin, triethanolamine, triethyl
  • compositions in accordance with the embodiments described here are described below.
  • CBD Cannabidiol
  • PEA 0.5-90% (w/w)
  • CBD Cannabidiol
  • PEA 0.5-90% (w/w)
  • CBD Cannabidiol
  • PEA 0.5-90% (w/w)
  • Curcumin or extract containing curcumin 1-90% (w/w)
  • CBD Cannabidiol
  • CBD Cannabidiol
  • Lipoic Acid 0.5-90% (w/w)
  • CBD Cannabidiol
  • CBD Cannabidiol
  • PEA 0.5-90% (w/w)
  • Gingerols and shogaols from ginger (Zingiber officinale), dry extract: 1-90% (w/w)
  • CBD Cannabidiol
  • PEA 0.5-90% (w/w)
  • compositions of the examples described above could include suitable excipients, as described above.
  • the Applicant carried out a study to verify the synergistic action of a formulation containing CBD and PEA in reducing the levels of some pro- inflammatory cytokines in an in vitro model consisting of human leukocytes.
  • IFN-y Interferon y
  • TNF-a Tumor Necrosis Factor a
  • IL-6 interleukin-6
  • Table 1 Effect of the different treatments on the production of IL-6 caused by inflammation induced by TNF-a in human leukocyte cells.
  • Results are the mean of 3 wells in triplicate ⁇ S.D. The values with different letters within the same column in Table 1 are significantly different (P ⁇ 0.05).
  • CBD+PEA association in particular at low concentrations (in the example provided 5pM), has significantly suppressed the release of the pro-inflammatory cytokine, IL-6, induced by TNF-a, in significantly greater quantities than single treatments with CBD and PEA, demonstrating the presence of a synergistic effect.
  • This datum is particularly important for the formulation of CBD+PEA based products used as anti-inflammatories.
  • the Applicant carried out a study to verify the synergistic action of a formulation containing CBD, PEA and a Standardized Plant Extract (SPE) in reducing the levels of some pro-inflammatory cytokines in an in vitro model consisting of human leukocytes.
  • the plant extracts evaluated were: Curcuma longa - standardized in curcumin
  • IFN-y Interferon y
  • TNF-a Tumor Necrosis Factor a
  • Table 2 Effect of CBD on the production of IL-6 caused by inflammation induced by TNF-a in human leukocyte cells.
  • Results are the mean of 3 wells in triplicate ⁇ S.D. The values with different letters within the same column are significantly different (P ⁇ 0.05).
  • CBD+PEA at low concentrations, significantly suppressed the release of the pro-inflammatory cytokine, IL-6, induced by TNF-a, in significantly greater quantities than single treatments with CBD and PEA.
  • some dry plant extracts such as those mentioned above, in association with CBD and PEA, increase the anti-inflammatory effect of the preparation. This datum will be particularly important for the formulation of CBD+PEA+ SPV based products used as anti-inflammatories and/or pain relievers.

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  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne une composition comprenant du cannabidiol (CBD) et une ou plusieurs substances naturelles analgésiques et/ou anti-inflammatoires, lesdites substances comprenant du palmitoyléthanolamide (PEA), en particulier pour le traitement thérapeutique d'états douloureux et/ou inflammatoires.
PCT/IT2022/050010 2021-01-28 2022-01-28 Composition pour le traitement d'états douloureux et/ou inflammatoires WO2022162711A1 (fr)

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023046730A1 (fr) * 2021-09-22 2023-03-30 Bionorica Se Compositions cosmétiques comprenant du cannabidiol et un extrait de zingiber
WO2023233185A1 (fr) * 2022-06-01 2023-12-07 VOLPI, Simone Combinaison de cannabidiol et d'acide alpha-lipoïque destinée à être utilisée dans le traitement de ptsd
EP4353225A1 (fr) * 2022-10-12 2024-04-17 Erbozeta S.p.A. Composition nutraceutique ou pharmaceutique pour traiter la douleur pelvienne
WO2024124354A1 (fr) * 2022-12-16 2024-06-20 Aima Inc. Compositions et méthodes de traitement ou de prévention de la douleur ou d'autres troubles

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3417846A1 (fr) * 2017-06-19 2018-12-26 Gifar Srl Aliment et/ou composition nutraceutique
US10512615B1 (en) * 2018-08-27 2019-12-24 Axcess Global Sciences, Llc Compositions and methods for delivering cannabidiol and ketone bodies
US20210015774A1 (en) * 2018-04-03 2021-01-21 Pure Green, Llc Tablet or composition having n-acyl ethanolamine and cannabinoid
WO2021149064A1 (fr) * 2020-01-26 2021-07-29 Landver Guy Compositions et procédés pour le traitement d'états inflammatoires et de maladies de la peau

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3417846A1 (fr) * 2017-06-19 2018-12-26 Gifar Srl Aliment et/ou composition nutraceutique
US20210015774A1 (en) * 2018-04-03 2021-01-21 Pure Green, Llc Tablet or composition having n-acyl ethanolamine and cannabinoid
US10512615B1 (en) * 2018-08-27 2019-12-24 Axcess Global Sciences, Llc Compositions and methods for delivering cannabidiol and ketone bodies
WO2021149064A1 (fr) * 2020-01-26 2021-07-29 Landver Guy Compositions et procédés pour le traitement d'états inflammatoires et de maladies de la peau

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023046730A1 (fr) * 2021-09-22 2023-03-30 Bionorica Se Compositions cosmétiques comprenant du cannabidiol et un extrait de zingiber
WO2023233185A1 (fr) * 2022-06-01 2023-12-07 VOLPI, Simone Combinaison de cannabidiol et d'acide alpha-lipoïque destinée à être utilisée dans le traitement de ptsd
EP4353225A1 (fr) * 2022-10-12 2024-04-17 Erbozeta S.p.A. Composition nutraceutique ou pharmaceutique pour traiter la douleur pelvienne
WO2024124354A1 (fr) * 2022-12-16 2024-06-20 Aima Inc. Compositions et méthodes de traitement ou de prévention de la douleur ou d'autres troubles

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