STABLE NON-AQUEOUS COMPOSITIONS OF FUNCTIONAL INGREDIENTS AND METHODS OF MAKING THE SAME
Provided is a non-aqueous suspension, comprising: a first plurality of active ingredients, wherein: the first plurality of active ingredients are soluble in the non-aqueous suspension; and one or more nanoparticles, wherein: the one or more nanoparticles encapsulate a second plurality of active ingredients; the second plurality of active ingredients are insoluble in the non-aqueous suspension; the one or more nanoparticles solubilize the second plurality of active ingredients in the non-aqueous suspension; the one or more nanoparticles have a Z-average diameter between 50 to 950 nanometers; the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 40° C. for four weeks; and the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 90° C. for 30 minutes.
1 . A composition for oral consumption, comprising:
a non-aqueous suspension, comprising:
a first plurality of active ingredients, wherein:
the first plurality of active ingredients are soluble in the non-aqueous suspension; and
one or more nanoparticles, wherein:
the one or more nanoparticles encapsulate a second plurality of active ingredients;
the second plurality of active ingredients are insoluble in the non-aqueous suspension;
the one or more nanoparticles solubilize the second plurality of active ingredients in the non-aqueous suspension;
the one or more nanoparticles have a Z-average diameter between 50 to 950 nanometers;
the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 40° C. for four weeks; and
the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 90° C. for 30 minutes.
2 . The composition of claim 1 , wherein:
the first plurality of active ingredients is selected from the group consisting of Echinacea purpurea, Echinacea angustifolia, Echinacea pallida, Acmella oleracea, Helichrysum umbraculigerum, Radula marginata, Kava, Kanna, black truffle, Syzygium aromaticum, Rosmarinus officinalis, Sceletium tortuosum, Holy basil, Oregano, Lavender, Cinnamon, Malabathrum, Cananga odorata, Ginkgo biloba, Bacopa, and Rhodiola rosea, Ashwagandha, Astragalus, Chaga, Cordyceps, Corydalis, Curcumin, Damiana, Eleuthero, Ginger root, Ginseng, Gotu Kola, Lion's Mane, Maca, Passionflower, Saffron, Schisandra, St. John's Wort, Turmeric, Turkey Tail, Valerian root, and Yohimbe.
3 . The composition of claim 1 , wherein:
the first plurality of active ingredients is selected from the group consisting of cannabidiol, cannabichromene, cannabigerol, cannabicyclol, cannabinol, cannabigerolic acid, cannabigerolic acid monomethylether, cannabigerol monomethyl ether, cannabichromanon, cannabichromenic acid, cannabichromevarin, cannabichromevarinic acid, tetrahydrocannabinol, iso-tetrahydrocannabinol, cannabinol methylether, cannabinol-C4, cannabinol-C2, cannabiorcol, cannabinodiol, cannabielsoin, cannabielsoic acid A, cannabielsoic acid B, cannabicyclol, cannabicyclolic acid, cannabicyclovarin, cannabicitran, cannabitriol, cannabitriolvarin, ethoxy-cannabitiolvarin, cannabivarin, cannabinodivarin, tetrahydrocannabivarin, cannabidivarin, cannabigerovarin, cannabigerovarinic acid, cannabifuran, dehydrocannabifuran, and cannabiripsol cannabinoids.
4 . The composition of claim 1 , wherein the composition is a tincture.
5 . The composition of claim 1 , wherein the one or more nanoparticles further comprising:
a plurality of emulsifying agents selected from the group consisting of a plurality of emulsifying agents selected from the group consisting of an extract of polyglycerol polyricinoleate, Span 85, Span 65, Span 83, Span 80, Span 60, Span 40, lecithin, chemically modified lecithin, purified components of lecithin, phosphatidylcholine, phosphatidylglycerol, phosphatidic acid, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, sphingomyelin, and cardiolipin, hydrogenated soybean phosphatidylcholine, hydrogenated soybean phosphatidylcholine, fatty acid mono and di-glycerides, sodium stearoyl lactylate, triglycerol monooleate, hexaglycerol octasterate, polyglycerol esters of oleic acid, decaglycerol mono- and di-oleate, glyceryl caprylate, glyceryl caprate, glyceryl caprate/caprylate, glyceryl monooleate, glyceryl monostearate, or combinations thereof.
6 . The composition of claim 1 , wherein the one or more nanoparticles further comprising:
a first polymer selected from the group consisting of alginic acid, gum Arabic, locust bean gum, sodium alginate, potassium alginate, calcium alginate, agar, guar gum, and xanthan gum.
7 . The composition of claim 6 , wherein the first polymer retards the release of the second plurality of active ingredients after consumption.
8 . The composition of claim 1 , wherein:
the second plurality of active ingredients is selected from the group consisting of methylphenidate, dextroamphetamine, amphetamine, dextroamphetamine, Caffeine, nicotine, Methamphetamine, 3,4-Methylenedioxymethamphetamine, Methylenedioxypyrovalerone, Mephedrone, Phenylpropanolamine, Propylhexedrine, Pseudoephedrine, Catha edulis, Modafinil, xanthine derivatives, theophylline, and theobromine.
9 . The composition of claim 1 , wherein the non-aqueous suspension further comprising:
a first polymer selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, shellac, ethyl methyl cellulose, carboxymethyl cellulose, ethyl cellulose, microcrystalline cellulose, cellulose, 12-hydroxystearic acid, and a combination thereof.
10 . The composition of claim 1 , wherein the one or more nanoparticles are 0.01 wt % to 70 wt % of the composition.
11 . The composition of claim 1 , wherein:
the non-aqueous suspension is selected from the group consisting of short-chain triglycerides, medium-chain triglycerides, long-chain triglycerides, medium-chain partial glycerides, polyoxyethylated fatty alcohols, polyethylene glycol, and vegetable oil, shellac, methyl cellulose, hydroxy propyl cellulose, hydroxypropyl-methyl cellulose, ethyl methyl cellulose, carboxy methyl cellulose, ethyl cellulose, microcrystalline cellulose, cellulose, hypro mellose, hydroxyl propyl methyl cellulose, or combinations thereof.
12 . The composition of claim 1 , wherein:
the composition is spray dried to obtain a population of beads, wherein:
the population of beads has a Z-average diameter between 100 and 900 microns.
13 . The composition of claim 1 , wherein the composition further comprises:
a wax is selected from the group consisting of bees wax, carnauba wax, rice bran wax, camauba wax, candelilla wax, or combinations thereof.
14 . The composition of claim 1 , wherein the mean diameter of the one or more nanoparticles changes by less than or equal to 100% upon 6 months of storage of the composition at 25° C.
15 . The composition of claim 1 , wherein:
at least 60% by weight of the second active ingredient is not released within 30 minutes after oral consumption of the composition; and
at least 20% by weight of the second active ingredient is not released within 2 hours after oral consumption of the composition.
16 . The composition of claim 1 , wherein the composition further comprises a bioenhancer ingredient selected from the group consisting of naringin, naringenin, piperine, capsaicin, curcumin, demethoxycurcumin, bis-demethoxycurcumin, quercetin, allicin, lysergol, genistein, sinomenine, gallic acid, glycodeoxycholic acid, docosahexaenoic acid, eicosapentaenoic acid, epicatechin, cyclosporine, diosmin, emodin, fulvic acid genistein, lycopene, trans-resveratrol, cis-resveratrol, capric acid, cholic acid, deoxycholic acid, tamarixetin, glycocholic acid, taurocholic acid, limonene carvone, tangeretin, nobiletin, bergamottin, 6′,7′-dihydroxybergamottin, L-palmitoylcarnitine, and quinidine.
17 . The composition of claim 1 , wherein the composition further comprises a third plurality of active ingredients selected from the group consisting of Withaferin, Astragalosides, Bacoside, Betulinic Acid, Betulinic Acid, L-Tetrahydropalmatine, Dehydrocorybulbine, Apigenin, Eleutherosides, Gingerenone, Shogaol, Gingerol, Diterpenes, Ginkgetin, Bilobetin, Sciadopitysin, Ginsenoside, Eugenol, Mesembrine, Kavain, Hericenone, Erinacine, Macamides, Chrysin, Coumerin, Umbelliferone, Triterpenoids, Rhodiolin, Crocetin, Schisandrin A, Schisandrin B, Schisandrin C, Hypericin, Hyperforin, Valerenic Acid, Yohimbine, Melatonin, Vitamin A, Vitamin D3, Vitamin E, and Vitamin K.
18 . The composition of claim 1 , wherein the one or more nanoparticles further comprises an emulsifying agent that has a hydrophilic-lipophilic balance less than 5.
19 . The composition of claim 1 , wherein the one or more nanoparticles has a polydispersity of less than or equal to 0.25.
20 . A composition for oral consumption, comprising:
a non-aqueous suspension, comprising:
a first polymer selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, shellac, ethyl methyl cellulose, carboxymethyl cellulose, ethyl cellulose, microcrystalline cellulose, cellulose, 12-hydroxystearic acid, and a combination thereof;
a first plurality of active ingredients, wherein:
the first plurality of active ingredients are soluble in the non-aqueous suspension;
the first plurality of active ingredients is selected from the group consisting of cannabidiol, cannabichromene, cannabigerol, cannabicyclol, cannabinol, cannabigerolic acid, cannabigerolic acid monomethylether, cannabigerol monomethyl ether, cannabichromanon, cannabichromenic acid, cannabichromevarin, cannabichromevarinic acid, tetrahydrocannabinol, iso-tetrahydrocannabinol, cannabinol methylether, cannabinol-C4, cannabinol-C2, cannabiorcol, cannabinodiol, cannabielsoin, cannabielsoic acid A, cannabielsoic acid B, cannabicyclol, cannabicyclolic acid, cannabicyclovarin, cannabicitran, cannabitriol, cannabitriolvarin, ethoxy-cannabitiolvarin, cannabivarin, cannabinodivarin, tetrahydrocannabivarin, cannabidivarin, cannabigerovarin, cannabigerovarinic acid, cannabifuran, dehydrocannabifuran, and cannabiripsol cannabinoids;
a bioenhancer ingredient selected from the group consisting of naringin, naringenin, piperine, capsaicin, curcumin, demethoxycurcumin, bis-demethoxycurcumin, quercetin, allicin, lysergol, genistein, sinomenine, gallic acid, glycodeoxycholic acid, docosahexaenoic acid, eicosapentaenoic acid, epicatechin, cyclosporine, diosmin, emodin, fulvic acid genistein, lycopene, trans-resveratro,l cis-resveratrol, capric acid, cholic acid, deoxycholic acid, tamarixetin, glycocholic acid, taurocholic acid, limonene carvone, tangeretin, nobiletin, bergamottin, 6′,7′-dihydroxybergamottin, L-palmitoylcarnitine, and quinidine; and
one or more nanoparticles, wherein:
the one or more nanoparticles encapsulate a second plurality of active ingredients, the second plurality of active ingredients is selected from the group consisting of methylphenidate, dextroamphetamine, amphetamine, dextroamphetamine, Caffeine, nicotine, Methamphetamine, 3,4-Methylenedioxymethamphetamine, Methylenedioxypyrovalerone, Mephedrone, Phenylpropanolamine, Propylhexedrine, Pseudoephedrine, Catha edulis, Modafinil, xanthine derivatives, theophylline, and theobromine;
the second plurality of active ingredients are insoluble in the non-aqueous suspension;
the one or more nanoparticles solubilize the second plurality of active ingredients in the non-aqueous suspension;
the one or more nanoparticles have a Z-average diameter between 50 to 950 nanometers;
the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 40° C. for four weeks;
the Z-average diameter of the one or more nanoparticles changes less than 20% when the non-aqueous suspension is incubated at 90° C. for 30 minutes;
wherein the one or more nanoparticles has a polydispersity of less than or equal to 0.25; and
the non-aqueous suspension is selected from the group consisting of short-chain triglycerides, medium-chain triglycerides, long-chain triglycerides, medium-chain partial glycerides, polyoxyethylated fatty alcohols, polyethylene glycol, and vegetable oil.