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US-12616704-B2 - Cannabichromene formulation for pain management

US12616704B2US 12616704 B2US12616704 B2US 12616704B2US-12616704-B2

Abstract

A formulation for pain management is provided comprising cannabichromene as the primary cannabinoid together with an excipient and, optionally, one or more secondary cannabinoids in an amount of up to 5% by weight of the primary cannabinoid. The formulation is essentially free of tetrahydrocannabinol. The types of pain to be managed with the formulation include but are not limited to the treatment of neuropathic pain, pain due to cancer, injury, accident, surgery, or tissue damage. Methods of use of the formulation, doses and dosage forms are described.

Inventors

  • Mahsa ABRISHAMI

Assignees

  • ZYUS LIFE SCIENCES INC.

Dates

Publication Date
20260505
Application Date
20210331

Claims (14)

  1. 1 . A formulation for use in pain management by administration to a subject in need thereof, said formulation comprising a primary cannabinoid and an excipient, diluent or carrier; wherein said primary cannabinoid consists of cannabichromene (CBC), wherein said formulation is essentially free of tetrahydrocannabinol (THC), and wherein the pain management comprises an analgesic effect without a sedative effect.
  2. 2 . The formulation for use in pain management by administration to a subject in need thereof according to claim 1 , wherein the pain management comprises treatment of pain due to neuropathic pain, cancer, chemotherapy, inflammation, diabetes, diabetic neuropathy, post-shingles neuralgia, peripheral neuropathy, multiple sclerosis, injury, accident, surgery, or tissue damage.
  3. 3 . The formulation for use in pain management by administration to a subject in need thereof according to claim 1 , additionally comprising one or more secondary cannabinoids present in an amount of up to 15% by weight of the primary cannabinoid, wherein the one or more secondary cannabinoids comprises cannabidiol (CBD).
  4. 4 . The formulation for use in pain management by administration to a subject in need thereof according to claim 1 , wherein the formulation is prepared in a dosage form of a pill, tablet, gel capsule, syrup, oil-based spray, or liquid oil form.
  5. 5 . The formulation for use in pain management by administration to a subject in need thereof according to claim 1 , wherein the formulation provides a total amount of from 1 mg to 25 mg of primary cannabinoid per dose.
  6. 6 . A method for pain management in a subject in need thereof, comprising administering to said subject an effective amount of a formulation comprising a primary cannabinoid and an excipient, diluent, or carrier; wherein said primary cannabinoid consists of cannabichromene (CBC), wherein said formulation is essentially free of tetrahydrocannabinol (THC); and wherein the pain management comprises an analgesic effect without a sedative effect.
  7. 7 . The method according to claim 6 , wherein the pain management comprises alleviating pain due to neuropathic pain, cancer, chemotherapy, inflammation, diabetes, diabetic neuropathy, post-shingles neuralgia, peripheral neuropathy, multiple sclerosis, injury, accident, surgery, or tissue damage.
  8. 8 . The method according to claim 6 , wherein the formulation additionally comprises one or more secondary cannabinoids present in the formulation in an amount of up to 15% by weight of the primary cannabinoid, and wherein the one or more secondary cannabinoids comprises cannabidiol (CBD).
  9. 9 . The method according to claim 6 , wherein the formulation is administered in a dosage form of a pill, tablet, gel capsule, syrup, oil-based spray, or liquid oil form.
  10. 10 . The method according to claim 6 , wherein the formulation provides to the subject a total amount of from 1 mg to 25 mg of primary cannabinoid per dose.
  11. 11 . The method according to claim 10 , wherein the formulation provides to the subject a total amount of from 5 mg to 20 mg of primary cannabinoid per dose.
  12. 12 . The formulation for use in pain management by administration to a subject in need thereof according to claim 5 , wherein the formulation provides a total amount of from 5 mg to 20 mg of primary cannabinoid per dose.
  13. 13 . The formulation for use in pain management by administration to a subject in need thereof according to claim 1 , wherein said formulation comprises cannabichromene (CBC) and an excipient, diluent or carrier; wherein said formulation comprises 1% or less by weight of THC as compared to CBC.
  14. 14 . The method for pain management according to claim 6 , wherein said formulation comprises cannabichromene (CBC) and an excipient, diluent or carrier; wherein said formulation comprises 1% or less by weight of THC as compared to CBC.

Description

CROSS REFERENCE TO RELATED APPLICATIONS This application claims the benefit of and priority to U.S. Provisional Patent Application No. 63/015,039 filed on Apr. 24, 2020; U.S. Utility patent application Ser. No. 17/038,048 filed on Sep. 30, 2020; and U.S. Provisional Patent Application No. 63/145,040 filed on Feb. 3, 2021, the entire content of each being hereby incorporated by reference. FIELD The present disclosure relates generally to a formulation for medicinal use. More particularly, the present disclosure relates to a cannabinoid formulations for use in pain management. BACKGROUND Individuals managing pain often turn to medicinal options that offer pain alleviation, but are accompanied by unintended side-effects such as stomach upset, constipation, and risk of addiction. Alternatives to opiate drugs are urgently needed. Cannabinoids are a group of structurally similar compounds isolated from cannabis plants, which activate cannabinoid receptors in cells. Cannabinoids may be synthesized or may be isolated from cannabis plants or plant extracts (herein: a cannabinoid-containing plant extract). Cannabinoids can be isolated from plants or extracts to the extent that they are obtained in nearly pure, or essentially pure form, free of significant amounts of other naturally occurring compounds, such as other cannabinoids or plant-derived molecules such as terpenes. Known cannabinoids include but are not limited to tetrahydrocannabinol (THC); cannabidiol (CBD), cannabichromene (CBC); tetrahydrocannabidivarin (THCV); tetrahydrocannabinolic acid (THCA); cannabigerol (CBG); cannabidivarin (CBDV), cannabinol (CBN), and cannabidiolic acid (CBDA). Cannabis plants may be bred to have different amounts of a certain cannabinoid, as may be desirable for different purposes. THC and CBD have, to date, been considered as the predominant cannabinoids of interest. CBD has been widely studied medicinal effects. CBD is regarded as having an effect on 5HT1A receptor-mediated neurotransmission, as well as on anandamide metabolism and activation of TRPV1 receptor channels that facilitate CB1- and CB2-mediated responses (Crippa J S 2018). Δ9-THC exerts partial agonistic activity on CB1 and CB2 receptors with high binding affinity with CB1 receptor leading to its psychoactive activity. Cannabichromene (CBC) is a major non-psychotropic cannabinoid naturally found in the Cannabis sativa plant. The proportion of each of these cannabinoids in the cannabis plant is, however, dependent on environmental growth conditions, geographical location, genetics, and chemotype (Lewis M A 2017). CBC has moderate affinity (Ki˜100 nanomolar) only for CB2 receptors and binds to CB1 receptors only at concentrations higher than 1 micromolar (Shinjyo N 2013). The major CBC activity in brain has been suggested to be partly dependent on indirect activation of CB1 receptor by inhibition of cellular uptake of anandamide (De Petrocellis L 2011) and activation of TRPA1 (Transient Receptor potential A1) channels (Izzo and Capasso R 2012). In fact, CBC is found to be the most potent agonist of all the phytocannabinoids at TRPA1 channels (Maione S 2011). CBC has also shown anti-inflammatory effects (Izzo and Capasso R 2012). It has been demonstrated that CBD can act synergistically with Δ9-THC and contribute to the analgesic effect of medicinal-based cannabis extract (Russo 2011). The agonistic activity of CBC with CB1 and CB2 receptors can offer a promising approach to potentiate the effect of other cannabinoids that exert their activities via binding and activation of CB1 an CB2 receptors. Medicinal uses of cannabinoids are known, and formulations specifically to treat pain have been described. WO2007/083098 A1 (GW Pharma Ltd) describes cannabinoid-containing plant extracts for treatment of neural degeneration. U.S. Patent Publication No. US2016/0106705 (United Cannabis Corp.) describes cannabis extracts having at least four cannabinoids and a terpene or flavonoid for use in relieving anxiety, pain, and related disorders. WO2016/044370 A1 (India Globalization Capital Inc.) teaches a topical pain-relieving formulation containing a combination of THC, CBD and cobalamin. WO2013/165251 A1 (ECHO Pharmaceuticals BV) describes a thin film evaporation method for obtaining THC-containing isolates, which may have trace only amounts of CBN or CBD. In WO2012/144892 A1 (Fytagoras BV), the use of acidic cannabinoids such as THC, CBD, and other cannabinoids for enhancing an animal's natural cellular resistance to disease is described. Further, in WO2012/160358 A1 (GW Pharma Ltd.), the use of at least one of CBG, CBC, CBDV and THCV as a treatment of neuropathic pain is described. The potential of certain individual cannabinoids to have primary medicinal effects, apart from the THC, not been fully explored. It is desirable to provide a cannabinoid formulation with beneficial properties for use in the management of pain. SUMMARY It is an object of the present disclosure to obvia