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WO2025155937A1 - Formulations de cannabinoïdes et méthodes d'utilisation - Google Patents

Formulations de cannabinoïdes et méthodes d'utilisation

Info

Publication number
WO2025155937A1
WO2025155937A1 PCT/US2025/012233 US2025012233W WO2025155937A1 WO 2025155937 A1 WO2025155937 A1 WO 2025155937A1 US 2025012233 W US2025012233 W US 2025012233W WO 2025155937 A1 WO2025155937 A1 WO 2025155937A1
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
cannabis
thcv
oil
administration
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
Application number
PCT/US2025/012233
Other languages
English (en)
Inventor
Allen CAGLE
Troy ANDERLOHR
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.)
Taac Naturals Enterprises LLC
Original Assignee
Taac Naturals Enterprises LLC
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 Taac Naturals Enterprises LLC filed Critical Taac Naturals Enterprises LLC
Publication of WO2025155937A1 publication Critical patent/WO2025155937A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • 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
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/658—Medicinal preparations containing organic active ingredients o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol
    • 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
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Definitions

  • the invention described herein relates to cannabinoid formulation that enhance, sharpen, heighten, increase and/or improve cognitive function.
  • the invention also relates to cannabinoid formulations that alleviate, reduce, and/or shorten symptoms associated with the consumption of Cannabis or an extract thereof.
  • the invention relates to cannabinoid formulation that reset Cannabis tolerance, and/or reduce Cannabis tolerance, and/or result in an increase in a desired effect when consuming Cannabis or an extract thereof, and/or result in requiring less Cannabis or an extract thereof to achieve a desired effect, and/or reduce the time required for a tolerance break from Cannabis.
  • Cannabis has been consumed in part because of its non-lethality in large doses. However, in part because of its non-lethality in large doses, it is often the case that consumers intake more than an optimal amount of Cannabis, overshooting the desired effects and, instead, experiencing undesired effects, some of which may be potentially severe. Undesired effects of Cannabis can include anxiety, paranoia, tachycardia, ataxia/dizziness, sweating, nausea, vomiting, and/or a sensation of dying.
  • Cannabis tolerance refers to the phenomenon where a consumer of Cannabis products or extracts requires increasingly larger doses of cannabis to achieve the same effects once experienced with smaller amounts. This can develop due to the body’s adaptation to the active compounds in cannabis, particularly tetrahydrocannabinol (THC). Tolerance develops primarily due to downregulation of cannabinoid receptors in the brain, particularly CB1 receptors, which are the primary receptors affected by THC. Individuals may notice reduced effects from the same quantity of cannabis, leading to increased usage to achieve desired outcomes, such as euphoria, pain relief, or relaxation.
  • THC tetrahydrocannabinol
  • Embodiments of the invention relate to formulations for enhancing cognitive function including nano-emulsified THCV and an emulsifier.
  • the formulation further includes L-theanine.
  • the formulation further includes CBDV and/or CBC.
  • the formulation further includes beta caryophyllene and/or limonene.
  • the formulation further includes one or more compounds for enhancing cognitive function, increasing energy, replenishing electrolytes or enhancing focus.
  • the formulation is in the form of a powder.
  • the powder is a powder drink mix capable of being mixed with a liquid to form a beverage.
  • the powder is provided as a pre-measured, single-use packet.
  • the pre-measured, single-use packet is about 10 grams to about 20 grams.
  • the formulation is in the form of about a 2 oz beverage.
  • the formulation further includes a supplement, such as, for example, ashwagandha.
  • the formulation further includes an acid, such as, for example, citric acid, lemon juice, tartaric acid, white distilled vinegar, apple cider vinegar, ascorbic acid, and/or the like.
  • a method of enhancing cognitive function using the formulations disclosed herein including administering the formulation to a subject in an amount sufficient to enhance cognitive function.
  • the administration step includes administering at least 5 mg of THCV.
  • Embodiments of the invention relate to a formulation for the treatment of Cannabis toxicity comprising nano-emulsified THCV and an emulsifier.
  • the formulation can include L-theanine.
  • the formulation can be in the form of about a 2 oz beverage.
  • the formulation can further include a supplement.
  • the supplement is ashwagandha.
  • the formulation can further include an acid.
  • acid can be one or more of citric acid, lemon juice, tartaric acid, white distilled vinegar, apple cider vinegar, ascorbic acid, and/or the like.
  • the formulation includes one ore more of 73.536% - 99% water, 4.288% - 6.432% monk fruit/erythritol, 0.12% - 0.18% stevia, 0.104% - 0.156% citric acid, 0.56% - 0.84% lecithin, 0.056% - 0.084 xanthan gum, 0.40% - 0.6%, MCT/THCV, 0.072% - 0.108% caffeine, 0.144% - 0.216% L-theanine, 0. 144% - 0.216% choline, 0.008% - 0.012% black pepper extract, 0.56% - 0.84% natural and artificial flavors, 0.008% - 0.012% emulsifying system.
  • the formulation can be in the form of a transdermal patch.
  • the formulation can include one or more of THCV, a nanoemulsifying system, alpha-GPC, L-theanine, one or more terpenes, glycol, and/or the like.
  • the formulation can be in the form of liquid for IV administration.
  • the formulation can include one or more of THCV, a nanoemulsifying system, L-theanine, Cannabis-derived lipids, glycerin, water, and/or the like.
  • “dermal delivery” or “dermal administration” refers to a route of administration wherein the pharmaceutical dosage form is taken to, or through, the dermis (i.e., layer of skin between the epidermis (with which it makes up the cutis) and subcutaneous tissues).
  • pill typically refers to a small, round, solid pharmaceutical oral dosage form of medication that was in use before the advent of tablets and capsules. Pills were historically made by mixing the active ingredients with an excipient such as glucose syrup in a mortar and pestle to form a paste, then rolling the mass into a long cylindrical shape (called a “pipe”), and dividing it into equal portions, which were then rolled into balls, and often coated with sugar to make them more palatable.
  • pills include tablets, capsules, and variants thereof like caplets — essentially anything with medication that can be digested, minus the liquid forms, falls into the pill category.
  • osmotic delivery system or “osmotic controlled release oral delivery system” or “OROS” refers to a controlled release oral drug delivery system in the form of a tablet.
  • the tablet typically has a rigid water-permeable jacket with one or more small holes; typically, the small holes are laser-drilled. As the tablet passes through the body, the osmotic pressure of water entering the tablet pushes the active drug through the openings in the tablet.
  • adhesive topical patch or “transdermal patch” refers to a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream.
  • a transdermal patch or transdermal system is a medicated adhesive patch that is placed on the skin to deliver a specific dose of drug through the skin and into the bloodstream.
  • An advantage of a transdermal drug delivery route over other types of medication delivery such as oral, topical, intravenous, intramuscular, etc. is that the patch provides a controlled release of the medication into the patient, usually through either a porous membrane covering a reservoir of medication or through body heat melting thin layers of medication embedded in the adhesive.
  • the main disadvantage to transdermal delivery systems stems from the fact that the skin is a very effective barrier; as a result, only medications whose molecules are small enough to penetrate the skin can effectively be delivered by this method.
  • the transdermal patch serves as an alternative dosage form for patients who experience dysphagia (difficulty in swallowing). Additional reasons to use transdermal patches include the convenience of a dosage form that can be taken without water as well as the inability of the patient to eat or drink (e.g., nausea and/or vomiting).
  • “therapeutically effective amount” is intended to include an amount of a substance (or compound) described herein, or an amount of the combination of substances (or compounds) described herein, e.g., to treat or prevent the disease or disorder, or to treat the symptoms of the disease or disorder, in a host, for example by alleviating one or more symptoms of Cannabis toxicity.
  • the combination of substances (or compounds) is preferably a synergistic combination. Synergy, as described for example by Chou and Talalay, Adv. Enzyme ReguL, 22:27 (1984) (which is fully incorporated by reference herein), occurs when the effect of the compounds when administered in combination is greater than the additive effect of the compounds when administered alone as a single agent. In general, a synergistic effect is most clearly demonstrated at suboptimal concentrations of the compounds. Synergy can be in terms of lower cytotoxicity, increased activity, or some other beneficial effect of the combination compared with the individual components.
  • treating includes: (i) preventing a pathologic condition from occurring; (ii) inhibiting the pathologic condition or arresting its development; (iii) relieving the pathologic condition; and/or (iv) alleviating/diminishing symptoms associated with the pathologic condition.
  • alleviate can mean to lessen by any degree, for example by 1, 2, 3, 5, 10, 15, 20, 25, 30, 35, 40, 50% or more of a quantified symptom.
  • phrases “pharmaceutically acceptable” refers to those compounds, materials, compositions, and/or dosage forms that are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problems or complications commensurate with a reasonable benefit/risk ratio.
  • the formulation can include nano-emulsified THCV.
  • the formulation provides at least Img of THCV per dose.
  • the formulation can provide 1, 2, 3, 4, 5, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, 100, 200, 300, 400, 500, 600, 700, 800, 900, 1,000 or more mg per dose.
  • a “dose” refers to the amount used in a single administration of the formulation to a subject.
  • the formulation includes 0.0001% - 99% THCV or l%-50% THCV.
  • the formulation can include about 0.0001, 0.001, 0.002, 0.003, 0.1, 0.5, 1, 5, 10, 15, 20, 25, 50% or more THCV.
  • nano-emulsified can refer to using an emulsifying agent (also referred to as an emulsifier) to mix two immiscible liquids and form a single-phase liquid.
  • the resulting single-phase liquid can contain an emulsion structure(s) less than 100 nm in diameter.
  • the liquid can contain an emulsion structure of less than 100, 80, 60, 40, or 20 nm, or less.
  • the emulsion structure is 120, 150, or 200 nm, or more.
  • formulations disclosed herein include THCV, an emulsifier, and/or a base.
  • the formulations disclosed herein include one or more additional cannabinoids, including, for example, but not limited to, delta-9- tetrahydrocannabinol (delta 9-THC), delta-8-tetrahydrocannabinol (delta 8-THC), tetrahydrocannabinolic acid (THCA), cannabidiol (CBD), cannabidiolic acid (CBDA), cannabinol (CBN), cannabinolic acid (CBNA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabichromene (CBC), cannabichromenic acid (CBCA), cannabidivarin (CBDV), cannabidivarinic acid (CBDV A), tetrahydrocannabivarin (THCV), tetrahydrocannabivarinic acid (THCVA), cannabigerovarin (CBGV), cannabiger
  • Non-limiting examples of emulsifiers can include, but are not limited to, lecithin (e.g., sunflower lecithin), guar gum, egg yolk, mustard extract, and/or the like, and/or combinations thereof.
  • the formulation includes 0.001% - 60% emulsifier(s).
  • the formulation can include 0.001, 0.01, 0.1, 0.5, 1, 10, 25, 30, 35, 40, 45, 50, 55, 60% emulsifier(s).
  • Non-limiting examples of the base can be water, any MCT oil, and/or the like.
  • the MCT oil can be, but is not limited to hempseed oil, grapeseed oil, coconut oil, palm kernel oil, sunflower oil, olive oil, sesame oil, avocado oil, palm oil, soybean oil, corn oil, peanut oil, canola oil, corn oil, hazelnut oil, rice bran oil, linseed oil, safflower oil, sesame oil, passionfruit oil, fish oil, and/or the like.
  • the formulation includes 0.01% - 99.5% base.
  • the formulation can include 0.01, 0.1, 0.5, 1, 10, 25, 30, 35, 40, 45, 50, 55, 60, 65, 70, 75, 75, 80, 85, 90% base.
  • the formulation can include a nanoemulsion of an oil, such as MCT, and THCV.
  • Oils that can be used include, but are not limited to, vitamin E; vitamin B12; vitamin A; vitamin D; vitamin B; omega 3; astaxanthin; fish oil; long chain triglyceride (LCT) oil; coconut oil; palm oil; eicosapentaenoic acid (EP A); docosahexaenoic acid (DHA); essential oils such as but not limited to lemon oil, orange oil, peppermint oil, Ylang-Ylang oil, lemongrass oil, tea tree oil, rosemary oil, Australian sandalwood oil, grapefruit oil, frankincense oil, cedarwood oil, patchouli oil, cinnamon bark oil, bergamot oil, chamomile oil, lemon-eucalyptus oil, ginger oil, key lime oil, vanilla oil, clove oil; any other essential oil; and any combination thereof.
  • the formulation can include one or more terpenes.
  • the terpene can be myrcene, limonene, linalool, beta-caryophyllene, alpha-pinene and beta-pinene, alpha-bisabolol, eucalyptol, trans-nerolidol, humulene, delta-3 -carene, camphene, borneol, terpineol, valencene, geraniol, eugenol, sabinene, phellandrene, borneol, isobomeol, phytol, menthol, geraniol, citronellol, ocimene, halomon, thymol, carvacrol, thujene, camphene, camphor, verbenone, botrydial, ngaione, cuparane, labdane, ferruginol, cafe
  • the formulation can include one or more lipids or Cannabis- derived lipids or hemp derived lipids.
  • such lipids include waxes and other lipids naturally included in Cannabis.
  • the formulation includes 0.0001% - 80% lipids.
  • the formulation can include about 0.0001, 0.001, 0.002, 0.003, 0.01, 0.1, 1, 5, 10, 15, 20, 25, 30, 40, 50% or more lipids.
  • the formulation can include a base to bring the formulation to a desired volume.
  • the base can be water, any MCT oil, and/or the like.
  • the base can be olive oil, sunflower oil, coconut oil, canola oil, com oil, soybean oil, peanut oil, sesame oil, safflower oil, grapeseed oil, almond oil, walnut oil, hazelnut oil, pistachio oil, macadamia nut oil, avocado oil, flaxseed oil, pumpkin seed oil, hemp seed oil, rice bran oil, camelina oil, mustard oil, argan oil, black seed oil, pecan oil, cashew oil, marula oil, apricot kernel oil, squalane oil, emu oil, MCT (medium chain triglycerides) oil, fish oil (often consumed in supplement form), krill oil (also consumed in supplement form), evening primrose oil, borage oil, wheat germ oil, black currant seed oil, chia seed oil, rosehip oil, n
  • the formulation includes, for example, but not limited to, Conjugated Linoleic Acid (CLA), Gamma-Linolenic Acid (GLA), Eicosapentaenoic Acid (EP A), Docosapentaenoic Acid (DPA), Butyrate (Butyric Acid), Krill Oil, Seal Oil, and the like.
  • CLA Conjugated Linoleic Acid
  • GLA Gamma-Linolenic Acid
  • EP A Eicosapentaenoic Acid
  • DPA Docosapentaenoic Acid
  • Butyrate Butyric Acid
  • Krill Oil Seal Oil, and the like.
  • the formulation includes natural nootropic compounds, such as, for example, but not limited to, Alpha-GPC, CDP-Choline (Citicoline), Uridine Monophosphate, Sulbutiamine, Noopept, Vinpocetine, Galantamine, and the like.
  • the formulation includes racetams, for example, but not limited to, Piracetam, Oxiracetam, Aniracetam, Pramiracetam, Phenylpiracetam, Fasoracetam, Nefiracetam, and the like.
  • the formulation includes Centrophenoxine or Agmatine Sulfate.
  • the formulation includes hormone support and regulators, such as, for example, but not limited to, Pregnenolone, DHEA (Dehydroepiandrosterone), Melatonin, 5-HTP, L-DOPA (from Mucuna Pruriens), and the like.
  • the formulation includes algae and aquatic plants, for example, but not limited to, Astaxanthin (from Haematococcus Pluvialis), Fucoxanthin (from Brown Seaweed), Dunaliella Salina (Beta-Carotene Rich Algae), Phycocyanin (from Spirulina), Chondrus Crispus (Irish Moss), Kelp (Iodine Rich), and the like.
  • Astaxanthin from Haematococcus Pluvialis
  • Fucoxanthin from Brown Seaweed
  • Dunaliella Salina Beta-Carotene Rich Algae
  • Phycocyanin from Spirulina
  • Chondrus Crispus Irish Moss
  • Kelp Iodine Rich
  • the formulation includes plant extracts, such as, for example, but not limited to, Olive Oil Polyphenols, Pomegranate Extract (Punicalagins), Mangosteen (Xanthones), Acai Berry, Goji Berry, Noni Fruit, Camu Camu, Acerola Cherry (Vitamin C Rich), Seaweed Polyphenols, and the like.
  • plant extracts such as, for example, but not limited to, Olive Oil Polyphenols, Pomegranate Extract (Punicalagins), Mangosteen (Xanthones), Acai Berry, Goji Berry, Noni Fruit, Camu Camu, Acerola Cherry (Vitamin C Rich), Seaweed Polyphenols, and the like.
  • the formulation includes probiotics and gut-brain modulators, such as, for example, but not limited to, probiotic strains, such as, Lactobacillus Rhamnosus, Bifidobacterium Longum, Lactobacillus Plantarum, Akkermansia Muciniphila, and the like, and prebiotics, such as, Inulin, Fructooligosaccharides, Butyrate-Producing Probiotics, and the like.
  • the formulations include, for example, but not limited to, Guduchi (Tinospora Cordifolia), Calamus Root, Haritaki, Amalaki (Amla), Shankhpushpi, and the like.
  • the formulations include, for example, but not limited to, Colloidal Gold, Fullerene C60, Deprenyl (Selegiline Derivative), Methionine, 0x66 (solid molecular oxygen), and the like.
  • the formulation is in the form of a transdermal patch.
  • the topical adhesive patch can include a backing having a front side and a back side.
  • the patch includes a formulation that is in contact with the front side of the backing.
  • the formulation can include an adhesive and Cannabis concentrate.
  • the topical adhesive patch can be manufactured in a manner, employing suitable ingredients, such that any one or more of the desired pharmacokinetic metrics (e.g., dose, area under the curve, peak plasma concentration, dosing intervals, time to reach peak plasma concentration, clearance, bioavailability, etc.) are achieved.
  • the topical adhesive patch can be manufactured such that the topical adhesive patch provides for an immediate release (IR) or a time-release (e.g., controlled release (CR), modified release (MR), extended release (ER), or combination thereof) of active ingredient.
  • IR immediate release
  • MR modified release
  • ER extended release
  • the topical adhesive patch described herein therefore possesses the potential to allow the development of sensitive drug targets that may otherwise not be feasible in tablet or liquid formulations.
  • the suitable thickness allows for a flexible, bendable, pliable, vapor permeable, and/or a stretchable sheet of water insoluble porous material.
  • the thickness of the backing can be about 0.001 mm to about 5.0 mm, about 0.001 mm to about 3.0 mm, or about 0.025 mm to about 1.25 mm.
  • the backing can be manufactured from any suitable material.
  • the suitable material forms a flexible, bendable, pliable, and/or stretchable backing.
  • the backing includes a porous or non-porous sheet of water soluble or water insoluble material that provides support for the adhesive skin patch.
  • the backing can include water soluble or water insoluble polymeric fibers, a porous film, or any other kind of matrix with spaces within the matrix.
  • a specific backing is a lightweight, porous, pliable strip composed of a nonwoven fabric of polymeric or natural fibers such as polyester, cotton, or cellulose fibers bonded together with a sizing resin.
  • the backing can be woven or nonwoven. In one embodiment, the backing includes nonwoven fabric.
  • the backing can include polyester fibers, polyurethane fibers, polyolefin fibers, polyamide fibers, natural fibers, cotton fibers, copolyester, copolyester fibers, cellulose acetate fibers, polycellulose fibers, or any mixture thereof.
  • suitable backings are disclosed, e.g., in U.S. Pat. Nos. 4,675,009; 5,536,263; 4,696,854; 5,741,510; and references cited therein, are suitable as backings according to the present invention.
  • the infusion of the formulation into the backing can be accomplished, e.g., with the use of a continuous process mixer, as disclosed, e.g., in U.S. Pat. No. 5,536,263, and references cited therein; or as discussed herein. All of the foregoing references are fully incorporated by reference herein.
  • the backing can be manufactured from a substance or substances that are generally recognized as safe (GRAS) for topical use.
  • GRAS generally recognized as safe
  • the backing can be manufactured from a suitable non-woven fabric that is commercially available. [0098] Alternatively, the fibers of the backing can be interlocked mechanically by air or water.
  • the formulation can be located on the entire surface of the front side of the backing. In addition to being located on the surface of the front side of the backing, the formulation can be located in at least a portion of the underlying surface of the front side of the backing (e.g., the formulation can be partially embedded into the backing).
  • the formulation can penetrate a substantial portion of the front side of the backing, as disclosed, e.g., in U.S. Pat. No. 5,536,263, and references cited therein, which are all fully incorporated by reference herein.
  • the formulation can penetrate about one-tenth to about nine-tenths the thickness of the backing, or about one-fourth to about nine-tenths the thickness of the backing.
  • the formulation can be partially embedded into the backing.
  • the formulation can be located on the entire front side of the backing and partially in the front side of the backing (e.g., the formulation is partially embedded into the backing).
  • a portion of the front side of the backing can include the formulation and other portions of the front side of the backing can include any suitable and effective combination of the pressure sensitive adhesive and, optionally, the solvent.
  • a central circular portion of the front side of the backing can include the formulation while the remaining portions of the front side of the backing include only the pressure sensitive adhesive.
  • the formulation when partially embedded into the front side of the backing, can impart strength and structure into the adhesive patch. For example, when the formulation is partially embedded into the backing, the likelihood that the adhesive patch tears apart when separated from the release liner or when removed from the skin after use, is lowered.
  • the adhesive skin patch can be reversibly attached to a release liner.
  • the release liner helps to maintain the adhesiveness of the adhesive skin patch prior to use, such as during manufacturing, packaging, shipping, and/or storage. Any suitable release liner can be employed for use in the present invention.
  • Suitable release liners 10 are readily known to those of skill in the art. See, e.g., U.S. Pat. Nos. 4,675,009; 5,536,263; 4,696,854; 5,741,510; and references cited therein for further descriptions of release liners 10 useful in the present invention. All of the foregoing references are fully incorporated by reference herein.
  • the release liner can include a perforation that allows the tab section of the release liner to be removed. Removal of the tab section of the release liner can allow the adhesive skin patch to be removed from the release liner with relative ease.
  • the backing can be a porous or non-porous, self-supporting sheet of water insoluble or water soluble, polymeric or natural material that provides strength and integrity for the formulation.
  • the backing can be water insoluble polymeric fibers, open cell foam backing (e.g., polyurethane, polyvinyl chloride, or polyethylene), a porous film, or any other kind of matrix with spaces within the matrix.
  • the backing can include polyester, polyurethane, polyolefin, polyamide fibers, natural fibers, cotton fibers, polycellulose fibers, or any mixture thereof.
  • the back side of the backing of the patch can be relatively dry to the touch, such that upon contact, e.g., with a skin surface or article of clothing, no appreciable or significant amount of liquid, gel, ointment, fluid, lotion, and the like, present in the back side of the backing of the patch is transferred there from and deposited upon the skin surface or article of clothing.
  • the back side of the backing of the patch can have a relatively small degree of moisture, while still being considered a “dry” patch, and would still be relatively dry to the touch, such that upon contact, e.g., with a skin surface or article of clothing, no appreciable or significant amount of liquid, gel, ointment, fluid, lotion, and the like, present in the back side of the backing of the patch is transferred there from and deposited upon the skin surface or article of clothing.
  • the size of the patch can be about 1-10 square inches (6.5 to 65 square centimeters).
  • the patch can be 1, 1.5, 1.75, 2, 4, 6, 8, 10 square inches.
  • the formulation is formulated for use by IV administration.
  • the formulation is 100, 150, 200, 300, 400, 500, 600mL or more liquid suitable for IV administration in a bag.
  • Cannabis or an extract is consumed about 1-2 hours, or about 2-4 hours, or about 4-6 hours, or about 6-8 hours, or about 8-12 hours, or about 2 hours, or about 3 hours, or about 4 hours, or about 5 hours, or about 6 hours, or about 7 hours, or about 8 hours, or about 10 hours, or about 12 hours following administration of the formulation disclosed herein and a tolerance reset is observed, and/or an increase in a desired effect is observed, and/or a reduction in the amount of Cannabis or an extract to achieve a desired result is observed.
  • the reset in Cannabis tolerance is observed for about 8 hours, or about 7 hours, or about 6 hours, or about 5 hours, or about 4 hours, or about 3 hours, or about 2 hours following consumption of Cannabis or extract. In some embodiments, the reset in Cannabis tolerance is experienced for about 1 day, 2 days, 3 days, 4 days, 5 days, 6 days, 7 days, 2 weeks, 3 weeks, or a month following administration of the formulation.
  • spray-dried powders (a type of dry powder) is produced by atomizing a liquid into small droplets and then rapidly drying them with hot air.
  • the liquid which can be a solution, suspension, or emulsion, is sprayed into a drying chamber, where it is exposed to a stream of hot air.
  • the hot air evaporates the solvent, leaving behind tiny particles of dry powder.
  • the resulting powder is free-flowing, easy to handle, and can be packaged for long-term storage.
  • Example 1 provides a method of making the formulation of Example 1 :
  • a formulation in the form for subcutaneous injection in a small animal was used and found to alleviate one or more symptoms of Cannabis toxicity in dogs within 20-30 minutes of administration.
  • This example describes the components for one embodiment of a 2oz liquid beverage: a. Water - 73.536% - 99.99% b. MonkfruitZErythritol - 4.288% - 6.432% c. Stevia - 0.12% - 0.18% d. Citric Acid - 0.104% - 0.156% e. Lecithin - 0.56% - 0.84% f. Xanthan Gum - 0.056% - 0.084 g. MCT/THCV (ratio of 4: 1) - 0.40% - 0.6% h. Caffeine - 0.072% - 0.108% i. L-Theanine - 0.144% - 0.216% j. Choline - 0. 0.
  • the following is a table of specific concentrations of ranges of three different embodiments of the invention. These are only examples, and the invention includes variations on these concentrations.
  • the embodiments can be plus or minus 0.01, 0.05, 0.1, 0.25., 0.5, 0.75, 1, 2, 5, 10, 15, 20, 25%, 30%, 40%, 50%, 60% or more or less.
  • the embodiments can be plus 100%, 125%, 150%, 200% or more.
  • the ingredients listed in the table are optional and can be removed or replaced with a similar ingredient.
  • the ratios of the ingredients can vary.
  • [00162] Prepare the mixture. Begin by adding glycerin to a beaker. Heat the beaker and mix the glycol until it reaches a temperature of 150°C. This step ensures proper fluidity and facilitates the dissolution process.
  • THCV tetrahydrocannabivarin
  • Mix in terpenes Next, add the desired terpenes to the mixture. Mix the formulation to ensure even distribution of the terpenes throughout the solution.
  • Packaging At this point, the formulation is complete and ready injected into the reservoir of the transdermal patch.
  • Dissolve THCV Once the glycol has reached the desired temperature, add THCV to the beaker. Allow the mixture to continue mixing until the THCV is fully dissolved. Add in cannabis and or hemp lipids and let dissolve.
  • [00173] Incorporate nano complex Add the nano complex to the mixture in the beaker. Use a high shear mixer and continue mixing for 30 minutes. This ensures uniform distribution of the nano complex throughout the formulation, enhancing its effectiveness.
  • Packaging At this point, the formulation is complete and ready to be filled into the IV bag.
  • Dispose of the residue After the recommended duration, the medication or substance may have dissolved or lost its effectiveness. If any residue remains, it can be gently rinsed out with water or spit out, following appropriate disposal methods for the specific medication or substance.
  • Select an appropriate location Choose a location on the body where the skin is relatively thin, has good blood circulation, and is free from excessive hair, cuts, irritations, or rashes. Common areas include the upper arm, shoulder, back, abdomen, or thigh. follow any specific instructions provided with the medication regarding the application site.
  • the subject reported having consumed Cannabis for 5 years with a typical daily consumption of 5-20 milligrams of Cannabis edibles.
  • the subject refrained from consuming cannabis for 9.5 hours following administration of the formulation of Example 1.
  • the subject reported a stronger or heavier effect from subsequent Cannabis consumption for a typical dose of Cannabis edibles required to achieve the desired effect (10 mg edible), reporting that he “felt a lot more stoned than I normally would with that amount.”
  • the subject reported having consumed Cannabis for 18 years with a typical daily consumption of 4-7 grams of Cannabis (40-60 mg of an edible at night, 2-5 one-gram joints, 3-5 large bong rips). The subject refrained from consuming cannabis for 12 hours following administration of the formulation of Example 1. The subject reported a stronger or heavier effect from subsequent Cannabis consumption and a significant reduction in Cannabis required to achieve the desired effect (20 mg edible, 2 joints, 1 bong rip).
  • the subject reported her first hours following administration of the formulation without her regular coffee intake “were great” but later felt “sleepy” and needed her regular coffee.
  • the subject reported being “very focused” following her regular coffee intake.
  • the subject reported having consumed Cannabis for 10 years with a typical consumption of vapes, bowls, bongs, and joints throughout the day and consuming 30-50 mg of edibles.
  • the subject refrained from consuming cannabis for 11 hours following administration of the formulation of Example 1.
  • the subject reported a stronger or heavier effect from subsequent Cannabis consumption and a significant reduction in Cannabis flower required to achieve the desired effect (only a THC vape).
  • the subject reported being “surprised” at feeling “a heavier high than usual after smoking the same cartridge I’ve had for the whole week prior.”
  • the subject rated the typical desired effect of his Cannabis consumption as a 7 on a scale of 1 to 10 (1 being lowest) and the desired effect of his Cannabis consumption following administration of the formulation of Example 1 a 9 on a scale of 1 to 10 (1 being lowest).
  • the desired effect was increased and the amount of Cannabis required to achieve the desired effect was decreased following administration of the formulation of Example 1.
  • the subject reported having consumed Cannabis for 20 years with a typical consumption of “a couple hits a day.” The subject refrained from consuming cannabis for 12 hours following administration of the formulation of Example 1. The subject reported a stronger or heavier effect from subsequent Cannabis consumption and reported a Chillem to achieve the desired effect.
  • the subject rated the typical desired effect of his Cannabis consumption as a 7 on a scale of 1 to 10 (1 being lowest) and the desired effect of his Cannabis consumption following administration of the formulation of Example 1 a 10 on a scale of 1 to 10 (1 being lowest).
  • the desired effect was increased and the amount of Cannabis required to achieve the desired effect was decreased following administration of the formulation of Example 1.
  • Results show a 20-50% improvement in focus, reaction time, and working memory scores compared to baseline and placebo (cognitive enhancement); significant increases in self-reported energy levels and mood positivity 15-40% higher than placebo group (mood and energy); reduction in caloric intake by 200-300 kcal/day, reflecting appetite control (appetite suppression).

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  • Biomedical Technology (AREA)
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  • Molecular Biology (AREA)
  • Dispersion Chemistry (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une formulation de cannabinoïdes qui améliore, stimule, renforce, augmente et/ou optimise les fonctions cognitives. L'invention concerne également des formulations de cannabinoïdes qui soulagent, réduisent et/ou diminuent les symptômes associés à la consommation de cannabis ou d'un extrait de celui-ci. En outre, l'invention concerne une formulation de cannabinoïdes qui supprime la tolérance au cannabis, et/ou réduit la tolérance au cannabis, et/ou entraîne une augmentation d'un effet souhaité lors de la consommation de cannabis ou d'un extrait de celui-ci, et/ou entraîne une diminution de la quantité de cannabis ou d'un extrait de celui-ci nécessaire pour obtenir un effet souhaité, et/ou raccourcit le temps nécessaire pour rompre la tolérance au cannabis.
PCT/US2025/012233 2024-01-17 2025-01-17 Formulations de cannabinoïdes et méthodes d'utilisation Pending WO2025155937A1 (fr)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4675009A (en) 1977-11-07 1987-06-23 Lec Tec Corporation Drug dispensing device for transdermal delivery of medicaments
US4696854A (en) 1986-10-06 1987-09-29 Lectec Corporation Bilayer substrate
US5536263A (en) 1994-03-30 1996-07-16 Lectec Corporation Non-occulusive adhesive patch for applying medication to the skin
WO2021138456A1 (fr) * 2019-12-30 2021-07-08 Calibrated Therapeutics, Llc Compositions comprenant des terpènes, des huiles de cannabinoïdes, ou des flavonoïdes et leurs utilisations
US20230033276A1 (en) * 2021-07-22 2023-02-02 Nicoventures Trading Limited Active ingredient-containing nanoemulsions
WO2024015915A2 (fr) * 2022-07-14 2024-01-18 Taac Naturals Enterprises, Llc Formulations de cannabinoïdes

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4675009A (en) 1977-11-07 1987-06-23 Lec Tec Corporation Drug dispensing device for transdermal delivery of medicaments
US4696854A (en) 1986-10-06 1987-09-29 Lectec Corporation Bilayer substrate
US5536263A (en) 1994-03-30 1996-07-16 Lectec Corporation Non-occulusive adhesive patch for applying medication to the skin
US5741510A (en) 1994-03-30 1998-04-21 Lectec Corporation Adhesive patch for applying analgesic medication to the skin
WO2021138456A1 (fr) * 2019-12-30 2021-07-08 Calibrated Therapeutics, Llc Compositions comprenant des terpènes, des huiles de cannabinoïdes, ou des flavonoïdes et leurs utilisations
US20230033276A1 (en) * 2021-07-22 2023-02-02 Nicoventures Trading Limited Active ingredient-containing nanoemulsions
WO2024015915A2 (fr) * 2022-07-14 2024-01-18 Taac Naturals Enterprises, Llc Formulations de cannabinoïdes

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