IP Library Granted Patent US 11,129,897
Granted Patent B2
US 11,129,897 · App. 16/805,356 · Granted Sep 28, 2021

Fast-acting plant-based medicinal compounds and nutritional supplements

Inventors: Andrea Leone-Bay (Ridgefield, CT); Gregory Wesner (Bainbridge Island, WA)
Assignee: Receptor Holdings, Inc.
A61K47/18A23L33/105A61K9/0053A61K9/0056A61K9/0095A61K9/2013A61K9/4808A61K9/4858A61K9/4891A61K31/047A61K31/20A61K31/352A61K31/353A61K36/185A61K45/06A61K9/20
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Quick Facts
Patent No.
US 11,129,897
App. No.
16/805,356
Granted
Sep 28, 2021
Kind
B2
Abstract

Plant-based medicinal compounds or nutritional supplements in various carrier combinations are described. The carriers can include N-acylated fatty amino acids, penetration enhancers, and/or various other beneficial carriers. The plant-based composition/carrier combinations can create administration benefits.

Claims (45)

1. A method of providing increased bioavailability of a cannabinoid with an aqueous solubility of less than 0.1 mg/ml in an oral formulation when administered to a subject wherein the method comprises

adding an N-acylated fatty amino acid or a salt thereof comprising the formula:

to the oral formulation

wherein X and Z are independently hydrogen, a monovalent cation, a divalent metal cation, or an organic cation

thereby providing increased bioavailability of the cannabinoid when administered to the subject as compared to the same oral formulation without the added N-acylated fatty amino acid or salt thereof

and wherein the oral formulation further comprises an excipient.

2. The method of claim 1 , wherein the N-acylated fatty amino acid or a salt thereof comprises N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC).

3. The method of claim 1 , wherein X is hydrogen, the monovalent cation is sodium or potassium, the divalent metal cation is calcium or magnesium, or the organic cation is ammonium or tetramethylammonium.

4. The method of claim 1 , wherein Z is hydrogen, the monovalent cation is sodium or potassium, or the divalent cation is calcium or magnesium.

5. The method of claim 1 , wherein X is hydrogen and Z is hydrogen.

6. The method of claim 1 , wherein X is hydrogen and Z is sodium.

7. The method of claim 1 , wherein X is sodium and Z is sodium.

8. The method of claim 1 , wherein the adding comprises adding 100-200 mg of the N-acylated fatty amino acid to the oral formulation.

9. The method of claim 1 , wherein the cannabinoid comprises Tetrahydrocannabinol (THC), cannabidiol (CBD), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), cannabinodiol (CBDL), cannabicyclol (CBL), cannabivarin (CBV), tetrahydrocannabivarin (THCV), cannabidivarin (CBDV), cannabichromevarin (CBCV), cannabigerovarin (CBGV), cannabigerol monomethyl ether (CBGM), cannabinerolic acid, cannabidiolic acid (CBDA), Cannabinol propyl variant (CBNV), cannabitriol (CBO), tetrahydrocannabinolic acid (THCA), tetrahydrocannabivarinic acid (THCVA) and/or mixtures thereof.

10. The method of claim 1 , wherein the cannabinoid comprises THC and/or CBD.

11. The method of claim 10 , wherein the THC and/or CBD is extracted from a Cannabis sativa plant, a Cannabis ruderalis plant, or a Cannabis indica plant.

12. The method of claim 1 , wherein the oral formulation comprises up to 1 gram of the cannabinoid.

13. The method of claim 1 , wherein the excipient comprises a surfactant.

14. The method of claim 1 , wherein the excipient comprises a flavorant.

15. The method of claim 14 , wherein the flavorant comprises vanilla, vanillin, cocoa, chocolate, menthol, peppermint oil, clove oil, bay oil, eucalyptus , thyme oil, cedar leave oil, cassia oil, a citrus oil, citric acid or malic acid.

16. The method of claim 1 , wherein the excipient comprises a sweetener.

17. The method of claim 16 , wherein the sweetener comprises aspartame, dextrose, fructose, high fructose corn syrup, maltodextrin, monoammonium glycyrrhizinate, neohesperidin dihydrochalcone, potassium acesulfame, saccharin sodium, stevia , sucralose, or sucrose.

18. The method of claim 1 , wherein the oral formulation further comprises flavonoid compounds, terpenes, or terpenoids.

19. The method of claim 1 , wherein the oral formulation comprises a solution formulation or a suspension formulation.

20. The method of claim 19 , wherein the solution formulation or the suspension formulation is within a gelcap.

21. An oral formulation comprising:

a cannabinoid with an aqueous solubility of less than 0.1 mg/ml, an N-acylated fatty amino acid or a salt thereof comprising the formula:

wherein X and Z are independently hydroqen, a monovalent cation, a divalent metal cation, or an organic cation, and an excipient.

22. The oral formulation of claim 21 , wherein the N-acylated fatty amino acid or a salt thereof comprises N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC).

23. The oral formulation of claim 21 , wherein X is hydrogen, the monovalent cation is sodium or potassium, the divalent metal cation is calcium or magnesium, or the organic cation is ammonium or tetramethylammonium.

24. The oral formulation of claim 21 , wherein Z is hydrogen, the monovalent cation is sodium or potassium, or the divalent cation is calcium or magnesium.

25. The oral formulation of claim 21 , wherein X is hydrogen and Z is hydrogen.

26. The oral formulation of claim 21 , wherein X is hydrogen and Z is sodium.

27. The oral formulation of claim 21 , wherein X is sodium and Z is sodium.

28. The oral formulation of claim 21 , comprising 100-200 mg of the N-acylated fatty amino acid.

29. The oral formulation of claim 21 , wherein the cannabinoid comprises Tetrahydrocannabinol (THC), cannabidiol (CBD), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), cannabinodiol (CBDL), cannabicyclol (CBL), cannabivarin (CBV), tetrahydrocannabivarin (THCV), cannabidivarin (CBDV), cannabichromevarin (CBCV), cannabigerovarin (CBGV), cannabigerol monomethyl ether (CBGM), cannabinerolic acid, cannabidiolic acid (CBDA), Cannabinol propyl variant (CBNV), cannabitriol (CBO), tetrahydrocannabinolic acid (THCA), tetrahydrocannabivarinic acid (THCVA) and/or mixtures thereof.

30. The oral formulation of claim 21 , wherein the cannabinoid comprises THC and/or CBD.

31. The oral formulation of claim 30 , wherein the THC and/or CBD is extracted from a Cannabis sativa plant, a Cannabis ruderalis plant, or a Cannabis indica plant.

32. The oral formulation of claim 21 , wherein the oral formulation comprises up to 1 gram of the cannabinoid.

33. The oral formulation of claim 21 , wherein the excipient comprises a surfactant.

34. The oral formulation of claim 21 , wherein the excipient comprises a flavorant.

35. The oral formulation of claim 34 , wherein the flavorant comprises vanilla, vanillin, cocoa, chocolate, menthol, peppermint oil, clove oil, bay oil, eucalyptus , thyme oil, cedar leave oil, cassia oil, a citrus oil, citric acid or malic acid.

36. The oral formulation of claim 21 , wherein the excipient comprises a sweetener.

37. The oral formulation of claim 36 , wherein the sweetener comprises aspartame, dextrose, fructose, high fructose corn syrup, maltodextrin, monoammonium glycyrrhizinate, neohesperidin dihydrochalcone, potassium acesulfame, saccharin sodium, stevia , sucralose, or sucrose.

38. The oral formulation of claim 21 , wherein the oral formulation further comprises flavonoid compounds, terpenes, or terpenoids.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 1, 2023
From: RECEPTOR HOLDINGS INC.
To: SPOKE SCIENCES, INC
Reel/Frame 065427/0133 →
CHANGE OF NAME Recorded Apr 10, 2020
From: RECEPTOR LIFE SCIENCES, INC.
To: RECEPTOR HOLDINGS INC.
Reel/Frame 052372/0832 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2020
From: LEONE-BAY, ANDREA
To: RECEPTOR LIFE SCIENCES, INC.
Reel/Frame 052265/0203 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2020
From: WESNER, GREGORY
To: RECEPTOR LIFE SCIENCES, INC.
Reel/Frame 052265/0211 →