FOOD SUPPLEMENT FOR ALZHEIMER

Abstract

The present invention is in the field of a Food supplement for Alzheimer. Alzheimer's disease (AD), and likewise associated or similar discomforts, is a chronic neurodegenerative disease that usually starts slowly and gradually worsens over time. The present invention provides a food supplement for preventing Alzheimer's disease, for delaying Alzheimer's disease, for decline of ageing, or combinations thereof.

Claims

1. A food supplement for use in the treatment of Alzheimer, the supplement comprising 0.1-90 wt. % of at least one active cannabinoid, wherein the origin of the cannabinoid is selected from phyto, endo, and synthetic origin, wherein the cannabinoid is extracted from biological plant species, 0.1-90 wt. % of at least one active phytosterol, wherein the phytosterol is extracted from biological species, wherein the food supplement is selected from a food supplement as such, from a pharmaceutically acceptable salt, and from a solvate thereof, wherein all wt. % are based on a total weight of the food supplement.

2. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the food supplement is for at least one of preventing Alzheimer's disease, delaying Alzheimer's disease, and maintaining activity of the brain endocannabinoid system (ECS).

3. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the cannabinoid is selected from Tetrahydrocannabinolic acid (THCA), Cannabidiolic acid (CBDA), Cannabigerolic Acid (CBGA), cannabichromenic acid (CBCA), cannabinol acid (CBNA), tetrahydrocannabivarin acid (THCVA), cannabielsoin acid (CBEA), cannabicycol acid (CBLA), cannabicitran acid (CBTA), there iso-forms, their cyclic forms, and their active neutral forms.

4. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the phytosterol is selected from saringosterols.

5. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the at least one cannabinoid and phytosterols are each individually >90% pure, and wherein a total amount of active cannabinoid and active phytosterol is between 0.1-60 wt. %.

6. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the at least one cannabinoid and phytosterols are each individually extracted by super-critical CO.sub.2.

7. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein the food supplement comprises <5 ppm solvent.

8. The food supplement for use in the treatment of Alzheimer according to claim 1, comprising 5-50 wt. % of edible oil, and edible fat.

9. The food supplement for use in the treatment of Alzheimer according to claim 1, in a capsule, where the capsule material is selected from polysaccharides, waxes, fats, proteins, and mixture thereof.

10. The food supplement for use in the treatment of Alzheimer according to claim 1, wherein a ratio between weights of cannabinoid and phytosterol is from 1:1000 to 1000:1.

11. The food supplement for use in the treatment of Alzheimer according to claim 1, further comprising at least one carrier selected from oils, powders, and mixtures thereof.

12. The food supplement for use in the treatment of Alzheimer according to claim 1, further comprising one or more of a pharmaceutically acceptable excipient.

13. A food supplement comprising 0.1-90 wt. % of at least one active cannabinoid, wherein the origin of the cannabinoid is selected from phyto, endo, and synthetic origin, wherein the cannabinoid is extracted from biological plant species, 0.1-90 wt. % of at least one active phytosterol, wherein the phytosterol is extracted from biological species, wherein the food supplement is selected from a food supplement as such, from a pharmaceutically acceptable salt, and from a solvate thereof, wherein all wt. % are based on a total weight of the food supplement.

14. A method of providing a food supplement, the food supplement comprising 0.1-90 wt. % of at least one active cannabinoid, wherein the origin of the cannabinoid is selected from phyto, endo, and synthetic origin, wherein the cannabinoid is extracted from biological plant species, 0.1-90 wt. % of at least one active phytosterol, wherein the phytosterol is extracted from biological species, wherein the food supplement is selected from a food supplement as such, from a pharmaceutically acceptable salt, and from a solvate thereof, wherein all wt. % are based on a total weight of the food supplement, the method comprising super critical CO.sub.2 extraction under increased pressure of >10 kPa, a temperature of >20° C., during a period of >1 h.

15. The method according to claim 14, wherein the phytosterol is extracted from algae, wherein the algae is selected from macro algae of the order Fucales, of the family Phaeophyceae, of the family Ascophyllum, and of the family Sargassaceae, and of the order Laminariales.

16. A dosage comprising a food supplement, the food supplement comprising 0.1-90 wt. % of at least one active cannabinoid, wherein the origin of the cannabinoid is selected from phyto, endo, and synthetic origin, wherein the cannabinoid is extracted from biological plant species, 0.1-90 wt. % of at least one active phytosterol, wherein the phytosterol is extracted from biological species, wherein the food supplement is selected from a food supplement as such, from a pharmaceutically acceptable salt, and from a solvate thereof, wherein all wt. % are based on a total weight of the food supplement, the dosage comprising 0.1-60 wt. % food supplement, and 1-1000 mg of as active ingredient, wherein the active ingredient comprises the at least one active cannabinoid.

17. The food supplement according to claim 1 in a method selected from at least one of the treatment of Alzheimer from preventing Alzheimer's disease, from delaying Alzheimer's disease, from maintaining activity of the brain endocannabinoid system (ECS), from restoring CB1 receptor expression and coupling to G proteins, from treatment of a person with a genetically increased chance for Alzheimer's disease, from treating a degenerative disease, from lowering a blood cholesterol level, from anti-cancer treatment, from depletion of cancer tumour, from reducing blood platelet aggregation, from providing anti-oxidative effect, from providing anti-diabetic effect, and from providing anti-obesity.

Description

FIGURES

[0039] The invention although described in detailed explanatory context may be best understood in conjunction with the accompanying figures.

[0040] FIG. 1a-b show a Saringosterol and a fucosterol.

[0041] FIG. 2 shows Focus veziculosus.

[0042] FIG. 3 shows an experimental set-up.

[0043] FIG. 4 shows milled seaweed.

[0044] FIG. 5a,b Seaweed extract collected from separator.

[0045] FIGS. 6a-c show Extract and CBD, Coating phase, and Emulsion.

[0046] FIG. 7 shows dry powder.

[0047] FIG. 8a,b show SEM micrographs (different magnifications of the coated particles.

[0048] FIG. 9: drying process.

[0049] FIGS. 10a,b obtained products.

DETAILED DESCRIPTION OF THE FIGURES

[0050] FIG. 1a-b show a Saringosterol (PubChem CID 14161394) and a fucosterol (CAS 17605-67-3).

[0051] Seaweed Extraction Tests

[0052] Example 1

[0053] Tested Material: Bladder wrack known also as rockweed or bladder fucus (Focus veziculosus) harvested form North Sea (see FIG. 2).

[0054] It is currently used as a dietary supplement as an accelerator for basal metabolism or as a mean to muscle recovery from intensive physical training. It also helps weight loss and its control.

[0055] Due to its rich extracts like fucoidans, alginic acids, and laminarin has wide recommendations for its positive results in reducing blood glucose levels, or reducing the plasma cholesterol levels. It has a high content of iodine which give a certain restriction for usage specially for people with thyroid disorders, hypertension, bleeding problems or pregnant women. However, the iodine content recommends this seaweed also for hypothyroidism.

[0056] Milled Seaweed: 400 g

[0057] Super critical (Sc) CO.sub.2 extraction setup was used for extracting the active ingredients from this seaweed (see FIG. 3). 400 g of milled dry algae is placed into a 1L extractor and CO2 under supercritical conditions is brought in contact with the algae. The active ingredients from the algae are solubilized into the scCO.sub.2 at operating conditions (30000 kPa (300 bar), 40° C., for 4 h). And the CO.sub.2 flow rich in extract is passed into the separator where because of solubility differences (due to pressure differences) the extracts are separated from the scCO.sub.2 and further collected in the extract vessel (FIG. 5a,b).

[0058] The extract contains Fucosterol and Saringosterol (rations S/F=0.23). The extract contains also some water which is co-extracted together with the sterol fraction.

[0059] The water fraction is removed and the sterol fraction is mixed with CBD supplied via separate extraction form hemp flowers (following the present procedure) a coating material containing modified starch and maltodextrin (Capsule:MD5:MD20). The ration used in this example was: approx. 87% coating comprise of approximately 35% MD20, 8.7% MDS, and 43.5% Capsule. The loading used was approximately 13%, comprising of 10.4% seaweed extract (with a ration Saringosterol/Fucosterol of 0.23) and 2.5% CBD (99% purity) extracted also by scCO.sub.2 from dry hemp flowers.

[0060] The two phases are mixed to form emulsion. FIGS. 6a-c show Extract and CBD, Coating phase, and Emulsion. The mixture coating/extract forms a stable emulsion which is further used to dry it by scCO.sub.2 spraying process.

[0061] Dry powder (FIG. 7) consists of encapsulated extracts and CBD in a coated matrix of Modified starch (Capsule) and maltodextrin (MD20 and MD5).

[0062] During the drying process, based on the material crystallization properties, the coating matrix will form around the extract mixture a solid thin protective layer which entrap the sterols and CBD inside the capsule material.

[0063] SEM micrographs (FIGS. 8a,b) show different magnifications of the coated particles.

[0064] The encapsulation efficiency can also be computed based on PL/PT determinations (Journal of AOAC International, 2005, Vol 88, pg 1271-1274). PL/PT stands for active ingredient found on the exterior of the particles and total active ingredients fund in a specific amount of encapsulated powder.

[0065] The spray drying process is done in a closed system with CO.sub.2 continuous recirculation (FIG. 9), and Schematic presentation of the encapsulation process.

[0066] Example 2

[0067] Same extraction process as in example 1.

[0068] For loading we used only seaweed extract without CBD.

[0069] The product is lighter in colour compared to the one produced with CBD. FIGS. 10a,b show obtained products.

[0070] Example 3

[0071] Sargasum recovery from Fucus Vesiculosis using scCO2 and Hemp oil.

[0072] The use of ethanol as modifier in sccO2 extraction almost double the Saringosterol extraction from Fucus Vesiculosis (from 0.242 μg/mg to 0.427 μg/mg). Other oils like MCT (from coconut) or hemp oil (cold pressed) proved to have a positive role in scCO2 extraction of Saringosterol from Fucus Vesiculosis seaweed as well. In the case of hemp oil our experiments proved that the high concentration of Fucosterol in the extract is a result of Fucosterol presence in the hemp oil itself.

TABLE-US-00002 Co-solvent used in Seaweed type scCO2 Fucosterol Iso-Fucosterol Saringosterol (Name) extraction μg/mg μg/mg μg/mg Asc Nodosum — 58.77 0.597 0.084 Hijiki 126.37 0.928 5.571 Hijiki C2H5OH 114.09 0.815 7.272 Brown algae 30.31 0.377 0.124 Fucus Fucos 55.67 0.662 0.239 Vesiculosis Fucos C2H5OH 48.57 0.697 0.383 Vesiculosis Co-solvent Fucosterol Iso-Fucosterol Saringosterol used μg/μl μg/μl μg/μl Fucos MCT 95.62 1.479 Vesiculosis (coconut oil) Fucos Hemp oil 354.43 1.480 Vesiculosis Fucos Hemp oil 321.68 29.12 1.107 Vesiculosis — Hemp oil 242.89 30.76 —

[0073] This result in the following conclusions: the combination between hemp oil and algae extract is beneficial. The results showed that in the hemp oil is sufficient Fucosterol. Literature mention Fucosterol in clinical phase 2 studies. So far, clinical studies demonstrated that dietary intake of plant sterols might help to lower blood cholesterol levels. Fucosterol also shows a cholesterol lowering effect by competing with cholesterol absorption, which is the same effect as plant sterols. In addition, fucosterol shows anti-cancer, antioxidative, and anti-diabetic effects. Fucosterol is present in brown algae in relatively large quantities: 0.9 mg/g to 13.4 mg/g dry weight. Now we have proved that other algae can yield important fucosetrol amounts next to Saringosterol. More over other plants like Hemp can be also an important source of Fucosterol. (Anti-obesity and anti-diabetic activities of algae. Fucosterol is also partially co-extracted from seaweed as proved in the current patent. Thus in combination with algae extract, Fucosterol may bring additional benefits in curing Alzheimer disease as well as depletion of some cancer tumours.

[0074] It is found that the sterols present in hemp oil are steroid aliphatic alcohols which proved to act positively in lowering the cholesterol as well as reducing the platelet aggregation. Phytol and tocopherol both have not only remarkable antioxidant activities but also beneficial results against degenerative diseases such as atherosclerosis and Alzheimer's. Next to that hemp oil has additional nutritional benefits due to high level of vitamin (A,C,E), beta-carotene, minerals (like phosphorus, K, Ca, Mg) and its excellent balance of polyunsaturated fatty acids. None of prior art specifically relates to Fucosterol presence in the hemp oil. In this example inventors have shown its presence in the seaweed extract which aims to be used to reduce the effects of Alzheimer's disease.

[0075] The extract is used further as such or encapsulated (see previous example).