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.

Claims

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.

Description

BRIEF DESCRIPTIONS OF THE DRAWINGS

[0021] The invention will now be further and more particularly described, by way of example only, and with reference to the accompanying drawings in which:

[0022] FIG. 1 is a process chart of fabricating various alternate preferred embodiments of the invented formulations in accordance with the invented method; c

[0023] FIG. 2 is a formulary chart presenting various essential and optional ingredients and compositional ranges thereof of various alternate preferred embodiments of the invented formulation that may be generated in accordance with the method of FIG. 1; and

[0024] FIG. 3 an additional formulary chart presenting various additional optional ingredients and compositional ranges thereof of various alternate preferred embodiments of the invented formulation of the invented formulation that may be generated in accordance with the method of FIG. 1.

DETAILED DESCRIPTION

[0025] Referring now generally to the Figures and particularly to FIG. 1, FIG. 1 is a process chart of fabricating various alternate preferred embodiments of the invented formulations in accordance with the invented method.

[0026] In a first step 1.00 of the method of FIG. 1, a process of formulating a present mixture is initiated. In step 1.02, the compounder selectively adds one or more of the ingredients disclosed herein into a V-shaped blending or tumbler machine, to include adding two or more substances listed in FIG. 2 or FIG. 3 or otherwise disclosed in the present Application.

[0027] In step 1.04 the compounder utilizes the V-shaped blending or tumbler machine of step 1.02 to tumble the ingredients for a duration of 45 minutes or until the ingredient magnesium stearate has bound the ingredients. In step 1.06 the compounder empties the blended mixture of ingredients (hereinafter the “powder”) out of the blender and into a bin. In step 1.08 the compounder scoops the powder into a hopper with sieves to eliminate clumping in the powder. In step 1.10, the holes in the sieves of the hopper allow the powder to fall through, and empty into a rotary tablet press. In step 1.12, the powder flows into dies in the rotary tablet press and is thus measured into metered amounts. In step 1.14 the compounder compresses the powder in the dies into hard tablets by means of upper punches and lower punches of the rotary tablet press. In step 1.16 the compounder raises the lower punches and ejects the compressed powder tablets (hereinafter, the “mints”) from the dies of the rotary tablet press. In step 1.18 the compounder allows the mints and any loose excess powder to fall down a chute and into a perforated cylinder. In step 1.20 the compounder rotates the perforated cylinder to allow the loose excess powder to fall away through the perforations. Finally, in step 1.22 the finished mints are collected into a container and the process of FIG. 1 ends at step 1.24.

[0028] Referring now generally to the Figures and particularly to FIG. 2, FIG. 2 is an ingestible formulary table 200 of unit dose formulation listings and presenting both an exemplary unit dose formulation of alternate preferred embodiments of the invented formulation. Various possible, alternative and optional ingredients of alternate preferred embodiments of the invented formulation are listed in a first column 202. Exemplary ingredient measures are listed in a second column 204 and are associated by inclusion in a same row with individual alternative and optional ingredients. Ranges of ingredient magnitudes of said alternative and optional ingredients thereof presented in a third column 206 and are associated by inclusion in a same row with individual alternative and optional ingredients. Brief descriptions of a function and potential benefits derived from including the listed ingredients may be displayed in a fourth column 208.

[0029] A header row 210A labels the first column 202, the second column 204, the third column 206, and the fourth column 208 for easy legibility of the table 200. A row 210B indicates that, for the ingredient Cannabinoids, CBD and other variations, an exemplary unit dose is 5.0 milligrams, the unit dose range is 5.0 milligrams-20 milligrams, and its function is as the key ingredient.

[0030] A row 210C indicates that, for the ingredient Mannitol, an exemplary unit dose is 10 milligrams, the unit dose range is zero to 50 milligrams, and its function is to provide sweetness.

[0031] A row 210D indicates that, for the ingredient Microcrystalline cellulose, an exemplary unit dose is 8 milligrams, and the unit dose range is 3.0 milligrams-15.0 milligrams.

[0032] A row 210E indicates that, for the ingredient Sodium Alginate, an exemplary unit dose is 5 milligrams, and the unit dose range is zero to 8.0 milligrams.

[0033] A row 210F indicates that, for the ingredient Gellan Gum, an exemplary unit dose is 2 milligrams, and the unit dose range is 0 milligrams-5 milligrams.

[0034] A row 210G indicates that, for the ingredient Fenugreek gum, an exemplary unit dose is 2 milligrams, the unit dose range is from zero to 5.0 milligrams, and its function is as an alternative to guar gum that may optionally be accepted as a vegan identified substance.

[0035] A row 210H indicates that, for the ingredient B12, an exemplary unit dose is 1 milligram, the unit dose range is zero to 3.0 milligrams, and its function is as a liposomal delivery system and inflammation reducer.

[0036] A row 210I indicates that, for the ingredient Menthol/Mentha piperita (Peppermint) oil, an exemplary unit dose is 1 milligram, the unit dose range is 0 milligrams-2.0 milligrams, and its function is as natural menthol or smaller peppermint.

[0037] A row 210J indicates that, for the ingredient Citrus grandis (Grapefruit) peel oil, an exemplary unit dose is 0 milligrams, and the unit dose range is 0 milligrams-1.0 milligram.

[0038] A row 210K indicates that, for the ingredient Bromelain, an exemplary unit dose is 0.05 milligrams, the unit dose range is 0.05 milligram-3.0 milligrams, and its function is reducing inflammation and improving absorption.

[0039] A row 210L indicates that, for the ingredient Luo Han Guo fruit (Monk Fruit) extract, an exemplary unit dose is 1 milligram, the unit dose range is 0.25 milligram-2.0 milligrams, and its function is as a strong sweetener that's also safe for diabetics.

[0040] A row 210M indicates that, for the ingredient Magnesium Stearate, an exemplary unit dose is 0.25 milligram, and the unit dose range is 0.25 milligram-1.0 milligram.

[0041] A row 210N indicates that, for the ingredient Pregelatinized Tapioca starch polymethylsilsesquioxane, an exemplary unit dose is 0.75 milligram, the unit dose range is 0.25 milligram-2.0 milligrams, and its function is as v. talc.

[0042] A row 210O indicates that, for the ingredient Citric acid, an exemplary unit dose is 1.95 milligram, and the unit dose range is from zero to 2.0 milligrams.

[0043] A row 210P lists that the total volume of the listed ingredients in an exemplary ingestible unit dose combined may be 50 milliliters, and the total volume of the combined ingredients will range from 50 milligrams to 75 milligrams.

[0044] Referring now generally to the Figures and particularly to FIG. 3, FIG. 3 is an ingestible formulary table 300 of alternate and optional ingredients of various alternate preferred embodiments of the invented formulation. Various possible, alternative and optional ingredients of alternate preferred embodiments of the invented formulation are listed in a first column 302. Exemplary low end ingredient measures of a unit dose of the invented formulation of the named ingredients are presented in a second column 304 and are associated by inclusion in a same row with individual alternative and optional ingredients. Exemplary magnitudes of measures of a unit dose of the invented formulation of the named ingredients are presented in a third column 306 and are associated by inclusion in a same row with individual alternative and optional ingredients.

[0045] A header row 308A labels the first column 302, the second column 304, and the third column 306for easy legibility of the additional ingredient table 300.

[0046] A row 308B indicates that the optional ingredient Vitamin A may be combined in the step 1.02 in the range that includes a low measure of 1,000 microGram (hereinafter. “mcg”) and a preferred measure of 7,000 mcg.

[0047] A row 308C indicates that the optional ingredient Vitamin D may be combined in the step 1.02 in the range that includes a low measure of 5.0 mcg and a preferred measure of 100 mcg.

[0048] A row 308D indicates that the optional ingredient Vitamin C may be combined in the step 1.02 in the range that includes a low measure of 5.0 mcg and a preferred measure of 75 mcg.

[0049] A row 308E indicates that the optional ingredient Magnesium enzyme may be combined in the step 1.02 in the range that includes a low measure of 10.0 mcg and a preferred measure of 75 mcg.

[0050] A row 308F indicates that the optional ingredient Gaba amino acid may be combined in the step 1.02 in the range that includes a low measure of 20.0 milliGrams (hereinafter, “mg”) and a preferred measure of 75 mg.

[0051] A row 308G indicates that the optional ingredient 5-hydroxytryptophan amino acid may be combined in the step 1.02 in the range that includes a low measure of 20.0 mg and a preferred measure of 100 mg.

[0052] A row 308H indicates that the optional ingredient Passionflower/Passiflora oil may be combined in the step 1.02 in the range that includes a low measure of 20.0 mg and a preferred measure of 100 mg.

[0053] A row 308I indicates that the optional ingredient Lavender oil may be combined in the step 1.02 in the range that includes a low measure of 1.015 mg and a preferred measure of 1.0 mg.

[0054] A row 308J indicates that the optional ingredient licorice extract may be combined in the step 1.02 in the range that includes a low measure of 20 mg and a preferred measure of 100 mg.

[0055] A row 308K indicates that the optional ingredient of a volume of liposomes may be combined in the step 1.02 in the range that includes a low measure of none to 0.25 mg and a preferred measure of 5.0 mg.

[0056] A row 308L indicates that the optional ingredient of a volume of peanut butter powder or oil may be combined in the step 1.02 in the range that includes a low measure of 0.5 mg and a preferred measure of 100 mg.

[0057] A row 308M indicates that the optional ingredient of a volume of liver powder or liver element may be combined in the step 1.02 in the range that includes a low measure of 5.0 mg and a preferred measure of 100 mg.

[0058] A row 308N indicates that the optional ingredient of a volume of acacia gum may be combined in the step 1.02 in the range that includes a low measure of zero to 0.25 mg and a preferred measure of 5 mg. It is understood that the volume of acacia gum may optionally be included in certain various alternate preferred embodiments of the invented formulation to provide fiber and act as a binder of various alternate preferred embodiments of the invented formulation the process of FIG. 1.

[0059] A row 308O indicates that the optional ingredient of a volume of Sunflower lecithin powder may be combined in the step 1.02 in the range that includes a low measure of zero to 0.5 mg and a preferred measure of 5 mg.

[0060] A row 308P indicates that the optional ingredient of a volume of Silica. Dioxide may be combined in the step 1.02 in the range that includes a low measure of zero to 0.25 mg and a preferred measure of 5 mg. It is understood that Silica Dioxide may optionally be included in certain various alternate preferred embodiments of the invented formulation to absorb liquid and thereby turn other liquid ingredients of the invented formulation into free-flowing powders that can be better combined in the process of FIG. 1.

[0061] A row 308Q indicates that the optional ingredient of a volume of Dicalcium Phosphate may be combined in the step 1.02 in the range that includes a low measure of zero to 0.25 mg and a preferred measure of 5 mg. It is understood that Dicalcium Phosphate may optionally be included in certain various alternate preferred embodiments of the invented formulation to better ensure that tablets fabricated by the method of FIG. 1 might be shaped and solidified with ease.

[0062] A row 308R indicates that the optional ingredient of a volume of lemon balm may be combined in the step 1.02 preferably within the range of from zero to 2.0 milligrams.

[0063] The terms “formulation”, “mixture”, “combination”, and “blend” are each defined herein to have a range of meaning that includes a substance made of two or more different materials, such as solutions, emulsifications, stirred materials, mixed materials, combinations, chemically-reacted or -reacting materials, compounded materials, adhering materials, and/or other suitable substances comprising chemical substances located within a gel, ointment, cataplasm, poultice, paste, cream, lotion, plaster, or jelly. The terms “mixing” “combining” and “blending ” are each defined herein to have a range of meaning that includes a process of one or more steps that joins or co-locates two or more differing materials to form one or more suitable substances type known in the art, such as solutions, emulsifications, blends, stirred materials, mixed materials, combinations, chemically-reacted or -reacting materials, compounded materials, adhering materials, and/or other suitable substances comprising chemical substances located or positioned within a gel, ointment, cataplasm, poultice, paste, cream, lotion, plaster, or jelly.

[0064] In understanding the scope of the present invention, the term “comprising” and its derivatives, as used herein, are intended to be open ended terms that specify the presence of the stated features, elements, components, groups, integers, and/or steps, but do not exclude the presence of other unstated features, elements, components, groups, integers and/or steps. The foregoing also applies to words having similar meanings such as the terms, “including”, “having” and their derivatives. Also, the terms “part”, “section”, “portion”, “member”, or “element” when used in the singular can have the dual meaning of a single part or a plurality of parts. Finally, terms of degree such as “substantially”, “about”, and “approximately” as used herein mean a reasonable amount of deviation of the modified term such that the end result is not significantly changed.

[0065] While selected embodiments have been chosen to illustrate the invented system, it will be apparent to those skilled in the art from this disclosure that various changes and modifications can be made herein without departing from the scope of the invention as defined in the appended claims. For example, the size, shape, location, or orientation of the various components can be changed as needed and/or desired. Components that are shown directly connected or contacting each other can have intermediate structures disposed between them. The functions of one element can be performed by two, and vice versa. The structures and functions of one embodiment can be adopted in another embodiment, it is not necessary for all advantages to be present in a particular embodiment at the same time. Every feature which is unique from the prior art, alone or in combination with other features, also should be considered a separate description of further inventions by the applicant, including the structural and/or functional concepts embodied by such feature(s). Thus, the foregoing descriptions of the embodiments according to the present invention are provided for illustration only, and not for the purpose of limiting the invention as defined by the appended claims and their equivalents.