Cannabinoid composition and method of sublingual, buccal and oral mucosa delivery

Abstract

A formulation includes a cannabinoid extract that is pharmaceutically effective by systemic delivery via a recipient's oral mucosal lining. The method of delivery avoids the digestive tract processing and liver metabolizing of the active ingredients of the formulation, whereby lower doses cause a desired therapeutic effect or other intended effect. Variations of the formulation include a cannabinoid extract and one or more of pregelatinized tapioca starch polymethylsilsesquioxane, bromelain, volume Fenugreek gum, vitamin B12, luo han guo fruit extract, mannitol, microcrystalline cellulose, sodium alginate, gellan gum, menthol Natural peppermint flavor or oil, Grapefruit flavored powder or oil, magnesium stearate and/or citric acid. The cannabinoid extract may include Tetrahydrocannabinol, tetrahydrocannabinolic acid, Cannabidiol, Cannabidiol acid, and/or other cannabinoid sourced from a cannabis sativa plant. The formulation includes at least one cannabinoid in a volume and measure that is pharmaceutically effective and/or effectual in achieving an intended systemic state or response of the recipient.

1 .- 21 . (canceled) 
     
     
         22 . A unit dose sublingual composition, comprising:
 (a) an extract of a cannabinoid containing Cannabis plant material, said extract comprising (i) one or more cannabinoid active agent(s) or (ii) a combination of said extract and one or more additional cannabinoid active agent(s), said additional cannabinoid active agent(s) selected from the group consisting of partially or completely purified cannabinoid compounds, synthetic cannabinoid compounds, and mixtures thereof;   (b) an amount per unit dose of pregelatinized tapioca starch, wherein the amount of pregelatinized tapioca starch is 0.25 mg-2.0 mg per unit dose; and   (c) an amount per unit dose of bromelain, wherein the amount of bromelain per unit dose is 0.05 mg-3.0 mg.   
     
     
         23 . The unit dose sublingual composition of  claim 22 , wherein:
 i) the amount of pregelatinized tapioca starch is 0.75 mg per unit dose; and   ii) the amount of bromelain is 0.05 mg per unit dose.   
     
     
         24 . The unit dose sublingual composition of  claim 22 , further comprising one or more ingredient(s) selected from the group consisting of sodium alginate, magnesium stearate, sunflower lecithin, silica dioxide, dicalcium phosphate, microcrystalline cellulose, acacia gum, fenugreek gum, gellan gum, and citric acid. 
     
     
         25 . The unit dose sublingual composition of  claim 24 , wherein the one or more ingredient(s) is present in an amount of:
 (a) up to 8.0 mg per unit dose, preferably 5.0 mg, of sodium alginate;   (b) 0.25 mg-1.0 mg per unit dose, preferably 0.25 mg, of magnesium stearate;   (c) up to 5.0 mg per unit dose, preferably 5.0 mg, of sunflower lecithin;   (d) up to 5.0 mg per unit dose, preferably 5.0 mg, silica dioxide;   (e) up to 5.0 mg per unit dose, preferably 5.0 mg, dicalcium phosphate;   (f) 3.0 mg-15 mg per unit dose, preferably 8.0 mg, microcrystalline cellulose;   (g) up to 5.0 mg, preferably 5.0 mg, acacia gum;   (h) up to 5.0 mg per unit dose preferably 2.0 mg, fenugreek gum;   (i) up to 5.0 mg per unit dose, preferably 2.0 mg, of gellan gum; and   (j) up to 2.0 mg per unit dose, preferably 1.95 mg, of citric acid;   wherein each range of amounts is inclusive.   
     
     
         26 . The unit dose sublingual composition of  claim 22 , further comprising one or more flavoring(s) selected from the group consisting of peanut butter, lemon, licorice, peppermint, grapefruit, passion flower, and lavender. 
     
     
         27 . The unit dose sublingual composition of  claim 26 , wherein the one or more flavoring(s) is present in an amount per unit dose of:
 (a) 0.5 mg-100 mg per unit dose, preferably 100 mg, of peanut butter flavoring;   (b) up to 2.0 mg per unit dose of lemon flavoring;   (c) 20 mg-100 mg per unit dose, preferably 100 mg, of licorice flavoring;   (d) up to 2.0 mg per unit dose, preferably 1.0 mg, of peppermint flavoring   (e) up to 1.0 mg per unit dose of grapefruit flavoring;   (f) 20 mg-100 mg per unit dose, preferably 100 mg, of passion flower flavoring; and   (g) 0.015 mg-1.0 mg per unit dose, preferably 1.0 mg, of lavender flavoring;   wherein each range of amounts is inclusive.   
     
     
         28 . The unit dose sublingual composition of  claim 22 , further comprising one or more sweetener(s) selected from mannitol and luo han guo extract. 
     
     
         29 . The unit dose sublingual composition of  claim 28 , further comprising up to 50 mg per unit dose, preferably 10 mg, of mannitol, and/or 0.25 mg-2.0 mg per unit dose, preferably 1.0 mg, of luo han guo extract; wherein each range of amounts is inclusive. 
     
     
         30 . The unit dose sublingual formulation of  claim 22 , further comprising one or more of a vitamin, an amino acid, and magnesium enzyme wherein:
 (a) the one or more vitamin(s) is selected from the group consisting of vitamin B12, vitamin A, vitamin D, and vitamin C; and   (b) the amino acid is gamma aminobutyric acid (GABA) or 5-hydroxytryptophan.   
     
     
         31 . The unit dose sublingual formulation of  claim 30 , wherein the one or more (a) vitamin(s), (b) amino acid(s), and (c) magnesium enzyme is/are present in an amount per unit dose of:
 (a) up to 3.0 mg per unit dose, preferably 1.0 mg, of vitamin B12, 1.0 mg-7.0 mg per unit dose, preferably 7.0 mg, of vitamin A, 5.0 μg -100 μg per unit dose, preferably 100 μg, of vitamin D, and 5.0 mg-75 mg per unit dose, preferably 75 mg, of vitamin C;   (b) 20 mg-75 mg per unit dose, preferably 75 mg, of GABA, and 20 mg-100 mg per unit dose, preferably 100 mg, of 5-hydroxytryptophan; and   (c) 10 μg-75 μg per unit dose, preferably 75 μg, of magnesium enzyme;   wherein each range of amounts is inclusive.   
     
     
         32 . A method of manufacturing a unit dose sublingual composition, comprising:
 (a) adding an extract of a cannabinoid containing Cannabis plant material, an amount of pregelatinized tapioca starch, and an amount of bromelain into a blender or tumbler;   (b) blending the ingredients together, thereby producing blended ingredients; and   (c) compressing the blended ingredients using a tablet press;   wherein the sublingual composition is a tablet for sublingual administration to a subject.   
     
     
         33 . The method of  claim 32 , wherein step (a) further comprises adding magnesium stearate and blending for at least 45 minutes and/or until the magnesium stearate has bound the other ingredients. 
     
     
         34 . The method of  claim 32 , wherein prior to step (c):
 i) the blended ingredients are sifted, thereby eliminating clumping; and/or   ii) the sifted ingredients flow onto a rotary tablet press.   
     
     
         35 . The method of  claim 32 , wherein step (c) comprises using a tablet press to compress the blended ingredients into tablets. 
     
     
         36 . The method of  claim 32 , wherein:
 i) the amount of pregelatinized tapioca starch is 0.25 mg-2.0 mg per unit dose; and   ii) the amount of bromelain is 0.05 mg-3.0 mg per unit dose.   
     
     
         37 . The method of  claim 36 , wherein:
 i) the amount of pregelatinized tapioca starch is 0.75 mg per unit dose; and   ii) the amount of bromelain is 0.05 mg per unit dose.   
     
     
         38 . The method of  claim 32 , wherein step (a) further comprises adding an amount of GABA to the blender or the tumbler, wherein the amount of GABA is 20 mg-75 mg per unit dose. 
     
     
         39 . The method of  claim 32 , wherein step (a) further comprises adding an amount of B12 to the blender or the tumbler, wherein the amount of B12 is up to 3.0 mg per unit dose. 
     
     
         40 . A sublingual composition comprising an extract of a cannabinoid containing Cannabis plant material, pregelatinized tapioca starch, and bromelain prepared by the method of  claim 32 . 
     
     
         41 . A method of administering the unit dose sublingual composition of  claim 22 , comprising placing the unit dose sublingual composition underneath the tongue of a subject in need thereof. 
     
     
         42 . A method for reducing anxiety in a subject in need thereof, comprising administering to the subject a sublingual composition comprising:
 (a) an extract of a cannabinoid containing Cannabis plant material comprising (i) one or more cannabinoid active agent(s) or (ii) a combination of said extract and one or more additional cannabinoid active agent(s), said additional cannabinoid active agent(s) selected from the group consisting of partially or completely purified cannabinoid compounds, synthetic cannabinoid compounds, and mixtures thereof,   (b) pregelatinized tapioca starch; and   (c) bromelain;   wherein the sublingual composition is placed underneath the tongue of the subject.