EP3906025A1 - Formulations topiques comprenant un cannabinoïde - Google Patents

Formulations topiques comprenant un cannabinoïde

Info

Publication number
EP3906025A1
EP3906025A1 EP20736215.3A EP20736215A EP3906025A1 EP 3906025 A1 EP3906025 A1 EP 3906025A1 EP 20736215 A EP20736215 A EP 20736215A EP 3906025 A1 EP3906025 A1 EP 3906025A1
Authority
EP
European Patent Office
Prior art keywords
formulation
cannabinoid
cannabinoids
oil
phyto
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.)
Withdrawn
Application number
EP20736215.3A
Other languages
German (de)
English (en)
Other versions
EP3906025A4 (fr
Inventor
Aaron Michael DELY
Shaun BEN-ARI
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.)
Columbia Care LLC
Original Assignee
Columbia Care 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 Columbia Care LLC filed Critical Columbia Care LLC
Publication of EP3906025A1 publication Critical patent/EP3906025A1/fr
Publication of EP3906025A4 publication Critical patent/EP3906025A4/fr
Withdrawn legal-status Critical Current

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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A61K9/124—Aerosols; Foams characterised by the propellant
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • 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
    • 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)
    • A61K36/67—Piperaceae (Pepper family), e.g. Jamaican pepper or kava
    • 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)
    • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/4873—Cysteine endopeptidases (3.4.22), e.g. stem bromelain, papain, ficin, cathepsin H
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/22—Cysteine endopeptidases (3.4.22)
    • C12Y304/22002—Papain (3.4.22.2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2210/00—Anatomical parts of the body
    • A61M2210/04—Skin

Definitions

  • topical or transdermal formulations having a cannabinoid in combination with a phyto-compound excipient that facilitates absorption and bioavailability of the cannabinoid.
  • Cannabis is believed to provide benefits in the treatment of multiple disorders with safer and fewer serious side effects than most prescription drugs currently used as anti emetics, muscle relaxants, hypnotics, and analgesics.
  • a disadvantage in treating patients with cannabis is the psychoactive effect, especially in "naive" cannabis users.
  • Cannabis has also been used to treat the symptoms in patients suffering from serious medical conditions. For example, cannabis has been used to alleviate symptoms associated with cancer, anorexia, AIDS, chronic pain, muscle spasticity, glaucoma, arthritis, migraine, and many other illnesses. Cannabis is recognized as having antiemetic properties and has been successfully used to treat nausea and vomiting in cancer patients undergoing chemotherapy. Cannabis has also been used in treating the weight loss syndrome of AIDS and in treating glaucoma by reducing intraocular pressure. Cannabis is also known for its muscle relaxing and anti-convulsant effects.
  • Cannabis smoke carries more tar and other particulate matter than tobacco and may be a cause of lung diseases including lung cancer. Furthermore, many patients find the act of smoking unappealing, as well as generally unhealthy.
  • formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject.
  • the formulation is a topical or a transdermal formulation.
  • the formulation includes a first cannabinoid (e.g., THC or THCa) and a second cannabinoid (CBD or CBDa).
  • a first cannabinoid e.g., THC or THCa
  • CBDa cannabinoid
  • the formulation includes a first polymer (e.g., polyethylene glycol 1450) and a second polymer (e.g., polyethylene glycol 4000).
  • a first polymer e.g., polyethylene glycol 1450
  • a second polymer e.g., polyethylene glycol 4000
  • kits for treating a disease or disorder in a subject comprising administering to the subject, for example topically administering, a formulation disclosed herein.
  • the method comprises the steps of providing one or more cannabinoids; providing one or more phyto-compound excipients; and mixing said one or more cannabinoids with said one or more phyto-compound excipients.
  • metered dose devices having a formulation disclosed herein.
  • the device comprises a regulated pump. In certain embodiments, the device comprises a metered-dosing mechanism. In certain embodiments, the device comprises an air-tight container to store the formulation. In certain embodiments, the device comprises the formulation in a plurality of metered doses. In certain embodiments, the device is an aerosol spray device.
  • treatment or “therapy” (as well as different forms thereof) include preventative (e.g., prophylactic), curative, or palliative treatment.
  • treating includes alleviating or reducing at least one adverse or negative effect or symptom of a condition, disease, or disorder.
  • transdermal drug delivery is meant administration of a drug to the skin surface of an individual so that the drug passes through the skin tissue and into the individual's blood stream.
  • Topical administration is used in its conventional sense to mean delivery of an active agent to a body surface such as the skin or mucosa, as in, for example, topical drug administration in the prevention or treatment of various disorders, the application of cosmetics and cosmeceuticals (including moisturizers, masks, sunscreens, etc.), and the like.
  • Topical administration in contrast to transdermal administration, provides a local rather than a systemic effect.
  • transdermal is used herein, as in “transdermal drug administration” and “transdermal drug delivery systems,” it is to be understood that unless explicitly indicated to the contrary, “topical” administration and systems are intended as well.
  • subject refers to an animal, for example a human, to whom treatment, including prophylactic treatment with the pharmaceutical formulation, is provided.
  • the inventor of the instant application surprisingly and unexpectedly discovered a formulation which includes, in part, one or more cannabinoids in combination with one or more phyto-compound excipients.
  • the presence of a phyto-compound excipient in the formulation facilitates absorption of a cannabinoid through an epidermis and a dermis. Furthermore, the presence of a phyto-compound excipient improves bioavailability of a cannabinoid.
  • formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject.
  • the formulation is a topical formulation. In other embodiments, the formulation is a transdermal formulation.
  • compositions of one or more cannabinoids relate to compositions of one or more cannabinoids to provide, for example, a topical or a transdermal delivery of said one or more cannabinoids.
  • the cannabinoids are easily prepared and formulated to provide consistent, therapeutically effective dosage forms from lot to lot.
  • said formulation facilitates administration via a regulated pump or a metered-dosing device.
  • said formulation is a homogeneous formulation.
  • said cannabinoid is an extract from a cannabis plant.
  • the formulation has a combination of at least two cannabinoids. In certain embodiments, the formulation comprises a combination of at least two cannabinoids. In certain embodiments, the two cannabinoids are selected from
  • THCa Tetrahydrocannabinolic acid
  • CBDa Cannabidiolic acid
  • CBDa Cannabinolic acid
  • CBCa Cannabichromenic acid
  • THC Tetrahydrocannabinol
  • CBD Cannabidiol
  • CBDa Cannabigerol
  • CBGa Cannabigerolic Acid
  • CBDa Cannabichromene
  • CBC Cannabinol
  • CBN Cannabielsoin
  • iso-Tetrahydrocannabinol iso-THC
  • Cannabicyclol CBL
  • Cannabicitran CBT
  • Cannabivarin CBV
  • Tetrahydrocannabivarin THCV
  • Cannabidivarin CBDV
  • Cannabichromevarin CBCV
  • Cannabigerovarin CBGV
  • Cannabigerol Monomethyl Ether CBGM
  • derivatives include, but are not limited to, esters, amides, and ethers of the compounds disclosed herein.
  • the cannabinoid is a cannabinoid extract that contains a combination of at least two of the following: Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso- Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CBT),
  • Cannabivarin CBV
  • Tetrahydrocannabivarin THCV
  • Cannabidivarin CBDV
  • Cannabichromevarin CBCV
  • Cannabigerovarin CBGV
  • Cannabigerol Monomethyl Ether CBGM
  • the cannabinoid may be natural or synthetic.
  • the methods of making cannabinoids extract is well known in the art. The cannabis plants are grown, harvested, and the cannabinoids are extracted through, for example, a CO2 extraction process.
  • At least two cannabinoids are in a 1 : 1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 10: 1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 20: 1 proportion by weight. In certain embodiments, two cannabinoids are THC and CBD. In certain embodiments, two cannabinoids are THCa and CBDa.
  • the two cannabinoids are in a 1 : 1 proportion by weight. In certain embodiments, the two cannabinoids are in a 10: 1 proportion by weight. In certain embodiments, the two cannabinoids are in a 20: 1 proportion by weight. In certain embodiments, the two cannabinoids are THC and CBD. In certain embodiments, the two cannabinoids are THCa and CBDa.
  • the formulation includes a first cannabinoid and a second cannabinoid.
  • the first and second cannabinoids are in a ratio ranging from about 1 : 1 to about 20: 1 proportion by weight.
  • the first and second cannabinoids are in a 1 : 1 proportion by weight. In other embodiments, the first and second cannabinoids are in a 10: 1 proportion by weight. In yet other embodiments, the first and second cannabinoids are in a 20: 1 proportion by weight.
  • the first cannabinoid is THC or THCa and the second cannabinoid is CBD or CBDa.
  • the first cannabinoid is THC and the second cannabinoid is CBD.
  • the first cannabinoid is THCa and the second cannabinoid is CBDa.
  • the at least one cannabinoid is THC or THCa present in an amount ranging from about 0.01 mg to about 200 mg.
  • the at least one cannabinoid is CBD or CBDa present in an amount ranging from about 0.01 mg to about 200 mg.
  • the first cannabinoid can be present in an amount ranging from about 0.01 mg to about 200 mg.
  • the second cannabinoid also can be present in an amount ranging from about 0.01 mg to about 200 mg.
  • the cannabinoids are in equal proportion such as, for example, 2.5 mg THC to 2.5 mg CBD. Other embodiments include proportions of
  • THC/CBD of 0.25 mg THC to 5.0 mg CBD or 5.0 mg THC to 0.25 mg CBD.
  • the cannabinoid of the invention is any member of a group of substances that are structurally related to tetrahydrocannabinol and that bind to a cannabinoid receptor such as CB 1 or CB2 or both (‘THC’).
  • the cannabinoid can be a naturally occurring compound (e.g., present in Cannabis), a compound metabolized by a plant or animal, or a synthetic derivative.
  • the cannabinoid may be included in its free form or in the form of a salt; an acid addition salt of an ester; an amide; an enantiomer; an isomer; a tautomer; a prodrug; a derivative of an active agent; different isomeric forms (e.g., enantiomers and
  • the cannabinoids are further meant to encompass natural cannabinoids, natural cannabinoids that have been purified or modified, and synthetically derived cannabinoids.
  • Methods for purifying cannabinoids from plant material are well known in the art and fully described in, for example, United States Patent Application Publication 2005/0266108, which is incorporated by reference herein in its entirety.
  • the cannabinoids can be any of 9-tetrahydrocannabinol, 8-tetrahydrocannabinol, (+)- 1,1-dimethylheptyl analog of 7-hydroxy-delta-6-tetrahydrocannabinol, 3-(5 '-cyano-1 ',G- dimethylpentyl)- 1 -(4-N-morpholinobutyryloxy)-delta-8-tetrahydrocannabinol hydrochloride, dexanabinol, nabilone, levonantradol, and N-(2-hydroxyethyl)hexadecanoamide.
  • the cannabinoids can be any of the non-psychotropic cannabinoid 3- dimethylnepty 11 carboxylic acid homologine 8 and delta-8-tetrahydrocannabinol.
  • the cannabinoid extract comprises cannabinoids tincture.
  • tincture refers to an alcoholic extract of plant material.
  • the method of tincture preparation comprises the steps of combining medium chain triglycerides and polysorbate in a mixing vessel to form a first combination; mixing the first combination; adding the cannabinoid extract to the first combination to form a second combination; mixing the second combination; adding 200 proof ethanol to the second combination to form a third combination; and mixing the third combination for an extended period of time in order to obtain the cannabinoids tincture.
  • the duration of the final mixing step may vary depending on many factors and can be easily optimized by a skilled artisan.
  • the final mixing step ranges from about 5 to about 60 minutes. In other embodiments, the final mixing step ranges from about 10 to about 50 minutes. In other embodiments, the final mixing step ranges from about 15 to about 45 minutes. In other embodiments, the final mixing step ranges from about 20 to about 40 minutes.
  • formulations further comprising one or more phyto compound excipients.
  • the at least one phyto-compound excipient facilitates absorption of said at least one cannabinoid or said derivative through an epidermis or a dermis of the subject.
  • the at least one phyto compound excipient improves bioavailability of said at least one cannabinoid or said derivative in said subject.
  • Examples of a phyto-compound excipient include, for example, but are not limited to, a terpene, an essential oil, papain, pipeline, capsaicin, or an extract of Myristica fragrans.
  • the at least one phyto-compound excipient is a terpene, an essential oil, papain, pipeline, capsaicin, or an extract of Myristica fragrans.
  • Examples of a terpene include, for example, but are not limited to, beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, famesol, menthol, eucalyptol, eugenol, and borneol.
  • the terpene is selected from beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol.
  • an essential oil examples include, for example, but are not limited to, eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
  • the essential oil is selected from eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
  • the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In other embodiments, the minor and major phyto compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation. [0051] In some embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In other embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation.
  • the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the topical formulation.
  • the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the formulation.
  • the formulation of the invention may also include additional ingredients such as solvents, carriers, or excipients.
  • the formulation further comprises a solvent.
  • the solvent comprises ethanol, methanol, isopropanol, chloroform, propylene glycol, polyethylene glycol, glycerine, limonene, myrcene, linalool, alpha bisabolol, delta 3 carene, borneol, alpha-pinene, beta-pinene, eucalyptol, terpineol, caryophyllene, camphene, or combinations thereof.
  • the solvent is ethanol.
  • the formulation further comprises a pharmaceutically acceptable carrier.
  • the carrier comprises cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, starch, pregelatinized starch, dicalcium phosphate, tricalcium phosphate, or mixtures thereof.
  • the carrier may be comprised of a water-soluble sugar or sugar alcohol.
  • Examples include, but not limited to, lactose, sucrose, dextrose, polydextrose, fructose, maltose, maltodextrin, dextrate, dextrin, lactitol, mannitol, erythritol, maltitol, sorbitol, or xylitol, and mixtures thereof.
  • the formulation may further contain an ingredient commonly used in the pharmaceutical field.
  • the ingredient include, but are not limited to, a diluent, a disintegrant, a binder, a lubricant, a colorant, a pH adjusting agent, a surfactant, a stabilizing agent, a sour agent, a flavor, a glidant, and the like. These ingredients are used in an amount commonly used in the pharmaceutical field unless otherwise specifically stated.
  • diluent examples include, but are not limited to, a sugar or a sugar alcohol such as lactose (e.g., lactose monohydrate), fructose, glucose, mannitol or sorbitol; a starch such as com starch, potato starch, wheat starch, rice starch, partially pregelatinized starch, pregelatinized starch or porous starch; microcrystalline cellulose; anhydrous calcium phosphate, precipitated calcium carbonate, calcium silicate, and the like.
  • lactose e.g., lactose monohydrate
  • fructose glucose
  • starch such as com starch, potato starch, wheat starch, rice starch, partially pregelatinized starch, pregelatinized starch or porous starch
  • microcrystalline cellulose anhydrous calcium phosphate, precipitated calcium carbonate, calcium silicate, and the like.
  • the diluent is used in an amount to give a content of from 5% to 95% by weight based on 100 parts by weight of the formulation.
  • Examples of a disintegrant include, but are not limited to, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl starch sodium,
  • the amount of the disintegrant can be an amount to give a content of from 0.5 to 25 parts by weight based on 100 parts by weight of the formulation or the topical formulation.
  • Examples of a binder include, but are not limited to, hydroxypropyl cellulose (e.g., grade: L, SL, SSL (trade name); Nippon Soda Co., Ltd.), hydroxypropylmethyl cellulose (e.g., hypromello se 2910 (e.g., TC-5 (grade: MW, E, EW, R, RW) (trade name); Shin-Etsu Chemical Co., Ltd.)), polyvinylpyrrolidone (povidone), and gum arabic.
  • hydroxypropyl cellulose e.g., grade: L, SL, SSL (trade name); Nippon Soda Co., Ltd.
  • hydroxypropylmethyl cellulose e.g., hypromello se 2910 (e.g., TC-5 (grade: MW, E, EW, R, RW) (trade name); Shin-Etsu Chemical Co., Ltd.)
  • polyvinylpyrrolidone povidone
  • the binder is used in an amount to give a content of from 1% to 20% by weight based on 100 parts by weight of the formulation or the topical formulation.
  • Examples of the lubricant include, but are not limited to, magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, sodium stearyl fumarate and the like.
  • the used amount of the lubricant is an amount to give a content of from about 0.5% to 2% by weight based on 100 parts by weight.
  • Examples of the colorant include, but are not limited to, a food dye (e.g., food yellow No. 5, food red No. 2, food blue No. 2), a food lake color, iron oxide red, and iron oxide yellow.
  • pH adjusting agent examples include, but are not limited to, citrate, phosphate, carbonate, tartrate, fumarate, acetate, and amino acid salt.
  • surfactant examples include, but are not limited to, sodium lauryl sulfate, polysorbate 80, and polyoxyethylene (160) polyoxypropylene (30) glycol.
  • the formulation may include a stabilizing agent that prevents separation or decomposition upon being transferred to a container or during transit or storage of said container.
  • Examples of the stabilizing agent include, but are not limited to, tocopherol, tetrasodium edetate, nicotinamide, and a cyclodextrin.
  • Examples of the sour agent include, but are not limited to, ascorbic acid, citric acid, tartaric acid, and malic acid.
  • Examples of the flavor include, but are not limited to, menthol, Mentha oil, lemon oil, and vanillin.
  • Examples of the glidant include, but are not limited to, colloidal silicon dioxide, aqueous silicon dioxide, and talc.
  • the above ingredients may be used by combining two or more members at an appropriate ratio.
  • the formulations disclosed herein include a composition for daily administration.
  • the therapeutic effect is maintained with one unit, twice daily.
  • the therapeutic effect is maintained with one unit, three times daily.
  • the duration of each dose's effect is between four (4) to six (6) hours.
  • the formulation can be of any suitable form, for example, a cream, a lotion, or a gel. In certain embodiments, the formulation is a cream or lotion.
  • provided herein are methods of treating a disease in a subject, the method comprising administering a formulation described herein. In other aspects, provided herein are methods of treating a disease in a subject, the method comprising administering to the subject a formulation described herein.
  • the formulation is administered topically. In other embodiments, the formulation is administered transdermally.
  • a disease or a disorder that can be treated by the invention include, but are not limited to, a skin disease or disorder, pain associated with cancer, neuropathic pain and HIV-associated sensory neuropathy, side effects of chemotherapy including nausea and pain, symptoms of neurological and neurodegenerative diseases such as Huntington's disease, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, multiple sclerosis, epilepsy, post-traumatic stress disorder (PTSD), alcohol abuse, bipolar disorder, depression, anorexia nervosa; cancer such as gliomas, leukemia, skin tumors, colorectal cancer; diseases including hepatitis C, methicillin-resistant Staphylococcus aureus (MRSA), pruritus, psoriasis, asthma, sickle-cell disease, sleep apnea, digestive diseases, collagen- induced arthritis, atherosclerosis
  • MRSA methicillin-resistant Staphy
  • Examples of a skin disease or disorder include, but are not limited to, itch, pain, and inflammation.
  • kits for manufacturing a formulation described herein may include the steps of: providing one or more
  • cannabinoids providing one or more phyto-compound excipients; and blending or mixing said one or more cannabinoids with said one or more phyto-compound excipients.
  • the device is an aerosol spray device which can spray the formulation on a skin of a subject.
  • the device includes a regulated pump.
  • the device includes a metered-dosing mechanism.
  • the device may include an air-tight container to store said formulation.
  • the formulation is stored in a plurality of metered doses.
  • the device comprises the formulation in a plurality of metered doses.
  • the device is an aerosol spray device.
  • the formulation is a therapeutic cream for topical or transdermal administration.
  • the formulation includes a mixture of a therapeutic agent (e.g., cannabinoid extract) and a phyto-compound excipient.
  • a therapeutic agent e.g., cannabinoid extract
  • a phyto-compound excipient e.g., phyto-compound excipient
  • the formulation is suitable for topical or transdermal administration using a metered-dose aerosol spray device.

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Abstract

L'invention concerne des formulations de cannabinoïde et des procédés d'utilisation associés. L'invention concerne plus particulièrement des formulations topiques ou transdermiques comprenant un cannabinoïde en combinaison avec un excipient phytocomposé qui facilite l'absorption et la biodisponibilité du cannabinoïde.
EP20736215.3A 2019-01-04 2020-01-03 Formulations topiques comprenant un cannabinoïde Withdrawn EP3906025A4 (fr)

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US201962788494P 2019-01-04 2019-01-04
PCT/US2020/012187 WO2020142692A1 (fr) 2019-01-04 2020-01-03 Formulations topiques comprenant un cannabinoïde

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US12016829B2 (en) 2019-10-11 2024-06-25 Pike Therapeutics Inc. Pharmaceutical composition and method for treating seizure disorders
CA3155181A1 (fr) 2019-10-14 2021-04-22 Pike Therapeutics, Inc., 1219014 B.C. Ltd. Administration transdermique de cannabidiol
MX2023000316A (es) * 2020-08-17 2023-02-22 Pike Therapeutics Inc Composiciones farmaceuticas y metodos para el tratamiento de la enfermedad de parkinson.
WO2022217147A1 (fr) * 2021-04-09 2022-10-13 Rosenfeld Mark J Procédés d'amélioration de la perméation cutanée de cannabinoïdes et d'amides d'acides gras
CN113244410A (zh) * 2021-05-28 2021-08-13 哈尔滨工业大学 基于多孔淀粉的增加大麻二酚水溶性的包合物制备方法
PL443690A1 (pl) * 2023-02-05 2024-08-12 Rodakowska Ewelina Kompozycja składników pochodzenia roślinnego, sposób jej otrzymywania oraz zastosowanie w celach leczniczych

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US10610512B2 (en) * 2014-06-26 2020-04-07 Island Breeze Systems Ca, Llc MDI related products and methods of use
US9375417B2 (en) * 2014-12-04 2016-06-28 Mary's Medicinals LLC Transdermal cannabinoid formulations
US20160309774A1 (en) * 2015-04-27 2016-10-27 Michael D. Wand Terpene carrier
EP3452036A4 (fr) * 2016-05-04 2019-11-06 Inmed Pharmaceuticals Inc. Utilisation de formulations topiques de cannabinoïdes pour le traitement de l'épidermolyse bulleuse et de troubles du tissu conjonctif connexes
BR112018075073A2 (pt) * 2016-06-02 2019-04-30 Acerus Pharmaceutical Corporation composições nasais de canabidiol
EP3493799A4 (fr) * 2016-08-03 2020-04-01 Zelda Therapeutics Operations Pty Ltd Composition pharmaceutique decannabis
WO2018236957A1 (fr) * 2017-06-20 2018-12-27 Nexien Biopharma, Inc. Procédé et compositions permettant de traiter le syndrome des jambes sans repos

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