Oral composition

Abstract

To provide an oral composition that exhibits excellent absorption-promoting properties for cannabidiol. [Solution] An oral composition for promoting the absorption of cannabidiol, characterized by containing at least one functional ingredient selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, and krill.

Description

Technical Field

[0001] The present invention relates to an oral composition containing cannabidiol, and particularly to an oral composition in which the absorption of cannabidiol is enhanced.

Background Art

[0002] As a component expected to have a new pharmacological action, cannabidiol (CBD) has attracted attention. Cannabidiol is a kind of cannabinoid contained in hemp, and for example, therapeutic agents for epilepsy seizures and therapeutic compositions for tuberous sclerosis have been developed (Patent Document 1, Patent Document 2).

[0003] With the expectation of such pharmacological effects of cannabidiol, various studies have been conducted. However, since cannabidiol is oil-soluble, it is difficult to be absorbed in the body, and it has been difficult to obtain sufficient pharmacological effects.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0005] Therefore, the present inventors have made various studies with the problem of enhancing the absorption promoting action of cannabidiol in the body.

Means for Solving the Problems

[0006] As a result, the present inventors have succeeded in developing an oral composition in which the absorption of cannabidiol is promoted by blending a functional component of a specific component together with cannabidiol, and have completed the present invention.

[0007] In other words, the present invention is as follows: <1> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least one functional ingredient selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, and krill. <2> An oral composition containing cannabidiol and at least one selected from polyamine, astaxanthin, and krill. <3> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least one functional ingredient selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, and krill, and cannabidiol. <4> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least two functional ingredients selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, krill, safflower oil, olive oil, medium-chain triglyceride oil, and linseed oil. <5> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least two functional ingredients selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, krill, safflower oil, olive oil, medium-chain triglyceride oil, and linseed oil, along with cannabidiol. <6> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least two functional ingredients selected from safflower oil, olive oil, medium-chain triglyceride oil, and linseed oil. <7> An oral composition for promoting the absorption of cannabidiol, characterized by containing at least two functional ingredients selected from safflower oil, olive oil, medium-chain triglyceride oil, and linseed oil, and cannabidiol. [Effects of the Invention]

[0008] According to the present invention, by including specific functional components together with cannabidiol, the absorption of cannabidiol is enhanced, and the various physiological effects of cannabidiol can be efficiently enjoyed. [Modes for carrying out the invention]

[0009] The solid compositions of the present invention will be described in detail below. However, the present invention is not limited to the embodiments shown below, and can be modified, added, altered, or deleted to the extent that a person skilled in the art can conceive of it. Any embodiment that achieves the effects and functions of the present invention is included within the scope of the present invention.

[0010] <Cannabidiol> Cannabidiol is a type of cannabinoid and is known to be found in hemp. Cannabidiol is known to have different pharmacological effects from tetrahydrocannabinol, another type of cannabinoid. In this invention, cannabidiol can be extracted and purified from plants such as hemp or citrus peels, or synthesized, but it is preferable to use a synthesized form in order to enhance safety and stability and enable continuous oral intake over a long period of time.

[0011] The cannabidiol content in the oral composition of the present invention is not particularly limited. For example, it is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, and is particularly preferred at 0.01% by mass or more, as it offers excellent stability and allows for easy and long-term oral intake. It is also preferably 99.9% by mass or less, and more preferably 99.5% by mass or less. In this specification, solids refer to the amount of water removed from the composition.

[0012] In the present invention, the cannabidiol content in the oral composition can be quantified, for example, by high-performance liquid chromatography (HPLC). For HPLC, for example, an Intact Co., Ltd. Unison UK-C18HT column (particle size 3 μm) φ4.6 × 150 mm is used, a water / acetonitrile mixture is used as the mobile phase, the gradient conditions are as shown in Table 1 below, the column temperature is 55°C and the flow rate is 1.0 ml / min.

[0013] [Table 1]

[0014] <Functional ingredients> The oral composition of the present invention is characterized by containing at least one functional component selected from Astragalus membranaceus, Panax ginseng, bitter orange, rice, liver oil, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, Haematococcus algae, and krill. By containing these functional components, it is possible to promote the absorption of cannabidiol into the body. In the present invention, from the viewpoint of enhancing the absorption of cannabidiol, it is preferable that the functional components be blended together with cannabidiol in the same composition. Furthermore, in the present invention, one or more of these functional components can be used. In particular, when safflower oil, olive oil, medium-chain fatty acid oil, or linseed oil are blended as functional components, it is preferable to use two or more functional components from the viewpoint of improving absorption promotion.

[0015] (Yellow Astragalus) Astragalus membranaceus, also known as Huanghua Huangqi, is a perennial plant belonging to the genus Astragalus in the legume family. It is known to contain flavonoids and saponins. As the part of Astragalus membranaceus to be used, the whole plant can be used, or specific parts such as leaves, flowers, stems, seeds, buds, roots, and underground stems (rhizomes, corms, tubers, bulbs) can also be used, without particular limitation. However, from the points of being easily available, containing a large amount of saponins, and having an excellent effect of promoting the absorption of cannabidiol, the above-ground parts such as leaves, flowers, and stems are preferred.

[0016] In the present invention, the treatment method of Astragalus membranaceus is not particularly limited. However, from the points of being easily available, containing a large amount of saponins, and having an excellent effect of promoting the absorption of cannabidiol, pulverized products, juice extracts, and extracts are preferred, and extracts are particularly preferred. In the case of extracts, the extraction solvent is not particularly limited as long as it is usually used in oral compositions. For example, water, ethanol, or a mixture thereof is preferred. The treated product of Astragalus membranaceus can be obtained, for example, by the method described below.

[0017] (Sanchi Ginseng) Panax notoginseng, also known as Sanchi Ginseng, is a plant belonging to the genus Panax in the Araliaceae family, and is also called Denshi Ginseng (Tianqi Ginseng) as an alias. It is known to contain saponins. As the part of Panax notoginseng to be used, the whole plant can be used, or specific parts such as leaves, flowers, stems, seeds, buds, roots, and underground stems (rhizomes, corms, tubers, bulbs) can also be used, without particular limitation. However, from the points of being easily available, containing a large amount of saponins, and having an excellent effect of promoting the absorption of cannabidiol, roots, underground stems, leaves, flowers, and stems are preferred, and the above-ground parts such as leaves, flowers, and stems are particularly preferred.

[0018] In the present invention, the method for treating sanshichininjin is not particularly limited. However, from the viewpoints of easy availability, high content of saponin, and excellent effect of promoting the absorption of cannabidiol, a pulverized product, a juice extract, or an extract is preferable, and an extract is particularly preferable. In the case of an extract, the extraction solvent is not particularly limited as long as it is usually used in an oral composition. For example, water, ethanol, or a mixture thereof is preferable. The treated product of sanshichininjin can be obtained, for example, by the method described below.

[0019] (Daidai) Daidai (orange; scientific name Citrus Aurantium) is a plant of the genus Citrus in the family Rutaceae, a green-leaved tree. It is known that synephrine is contained in the fruit of daidai. As the part of daidai to be used, the whole may be used, or specific parts such as the leaves, flowers, stems, seeds, buds, roots, and underground stems (rhizomes, bulbs, tubers, corms) of the plant may be used, and there is no particular limitation. However, from the viewpoints of easy availability, high content of synephrine, and excellent effect of promoting the absorption of cannabidiol, the fruit is preferable.

[0020] In the present invention, the method for treating daidai is not particularly limited. However, from the viewpoints of easy availability, high content of synephrine, and excellent effect of promoting the absorption of cannabidiol, a pulverized product, a juice extract, or an extract is preferable, and an extract is more preferable. In the case of an extract, the extraction solvent is not particularly limited as long as it is usually used in an oral composition. For example, water, ethanol, or a mixture thereof is preferable. The treated product of daidai can be obtained, for example, by the method described below.

[0021] (Polyamine) Polyamines are a general term for linear aliphatic hydrocarbons in which three or more primary amino groups are bonded together. Examples include spermine, spermidine, and putrescine. Polyamines are known to be found in fish milt, shellfish, legumes, and plants such as rice. In the present invention, the origin of the polyamine is not particularly limited, but rice is preferred, and rice germ is particularly preferred, due to its ease of use, high polyamine content, and excellent cannabidiol absorption-promoting effect. Rice (scientific name Oryza sativa) is a plant of the genus Oryza in the family Poaceae. Rice germ is known to contain polyamines.

[0022] In the present invention, there are no particular restrictions on the method of processing rice, but due to their ease of use, high polyamine content, and excellent cannabidiol absorption-promoting effect, pulverized products, juices, and extracts are preferred, extracts are more preferred, and extracts of citric acid aqueous solution are particularly preferred. The processed rice product can be obtained, for example, by the method described later.

[0023] (Squalene) Squalene is an oily substance belonging to the triterpene family. Squalene is known to be found in liver oil and olive oil. In this invention, the origin of squalene is not particularly limited, but liver oil is preferred because it is easy to use, contains a large amount of squalene, and has excellent cannabidiol absorption-promoting properties. Liver oil is the liquid contained in the liver of cod, sharks, or rays, or the fat extracted from that liquid. In this invention, when liver oil is used as squalene, shark liver oil is particularly preferred. Liver oil can be used as is or as an extract, but it is preferable to use purified liver oil or its extract because it contains a large amount of squalene.

[0024] (spore-forming lactic acid bacteria) Spore-forming lactic acid bacteria are lactic acid bacteria that form spores and are characterized by their resistance to dryness, heat, and acid. Examples of spore-forming lactic acid bacteria include bacteria belonging to the genera Bacillus and Sporolactobacillus. In this invention, Bacillus bacteria are preferred, and Bacillus coagulans is particularly preferred, due to their ease of use and excellent ability to promote cannabidiol absorption. In this invention, commercially available products that are normally available as food ingredients can be used.

[0025] (Tartaric acid) Tartaric acid is a hydroxy acid represented by (CH(OH)COOH)2. In this invention, commercially available products that are commonly available as food ingredients can be used.

[0026] (Docosahexaenoic acid) Docosahexaenoic acid (DHA) is a type of omega-3 fatty acid, an unsaturated fatty acid, and is a general term for carboxylic acids with a 22-carbon chain containing six double bonds. It is also known as DHA. It is an essential fatty acid.

[0027] (Eicosapentaenoic acid) Eicosapentaenoic acid (EPA) is a type of omega-3 fatty acid, an unsaturated fatty acid, and is a 20-carbon carboxylic acid with five cis double bonds. It is also known as EPA or eicosapentaenoic acid. It is an essential fatty acid.

[0028] (Astaxanthin) Astaxanthin is a red pigment. It is a type of carotenoid and is classified as a xanthophyll. Astaxanthin is known to be found in Haematococcus algae, crustaceans such as shrimp and crabs, and salmon. The astaxanthin that can be used in this invention is not particularly limited, but astaxanthin derived from Haematococcus algae is preferred because it is easy to use and has excellent cannabidiol absorption-promoting properties. Haematococcus pluvialis is a type of microalgae.

[0029] (Krill) Krill are crustaceans belonging to the order Ophiopogon, superorder Eucarida, suborder Eumalacostraca, class Malacostraca. Examples of krill include Antarctic krill (Euphausia superba), hornless krill (Euphausia pacifica), ice krill (Euphausia crystallorophias), round krill (Thysanopoda obtusifrons), and broad krill (Stylocheiron carinatum). In the present invention, krill extracts are preferred, and krill oil is more preferred, particularly krill oil, due to its ease of use and excellent ability to promote cannabidiol absorption.

[0030] (Safflower oil) Safflower oil is a vegetable oil extracted from the seeds of the safflower plant, which belongs to the genus Carthamus in the Asteraceae family. It is also known as red flower oil or safflower oil.

[0031] (olive oil) Olive oil is a vegetable oil obtained from the fruit of the olive tree, which belongs to the Oleaceae family.

[0032] (Medium-chain triglyceride oil) Medium-chain fatty acid oil is a glyceride composed of saturated fatty acids having 8 to 12 carbon atoms. Fatty acids with 8 to 10 carbon atoms are more preferable as constituents of medium-chain fatty acid oil. Furthermore, the medium-chain fatty acid oil used in this invention is preferably one or more selected from medium-chain fatty acid triglycerides, diglycerides, and monoglycerides, and is particularly preferable if it contains medium-chain fatty acid triglycerides (MCTs) as essential components.

[0033] (Flaxseed oil) Linseed oil is a vegetable oil extracted from the seeds of the Linum plant (Franciscana), and is also known as flaxseed oil or linseed oil.

[0034] (Methods for disposing of plants) Examples of processed plant materials include, but are not limited to, dried powder obtained by drying and grinding plant bodies (hereinafter also referred to as "dried and ground powder"), fragmented plant bodies and their dried products, plant juice and its dried powder, plant extracts and their dried powder. However, from the viewpoint of ease of processing, storage, and transportation, and versatility of use, it is preferable that the final product be in the form of a powder. In this specification, when simply referred to as "powder," it usually includes any of dried and ground powder, dried powder of fragmented material, dried powder of juice, and dried powder of extract. Furthermore, processed plant materials may also be fermented plant products or their dried powder. Fermented plant products are obtained by fermenting plant bodies or their ground products, juice, extracts, or fragments.

[0035] Plant-based materials can be processed by conventionally known methods. For example, as a method for drying and pulverizing plant materials, a method combining drying and pulverization can be used. Drying and pulverization may be performed in either order, but drying is preferable. This drying and pulverization method may be combined with one or more additional treatments, such as sterilization, as needed. Furthermore, the pulverization process may be performed one or more times, but it is preferable to perform coarse pulverization followed by fine pulverization.

[0036] The drying process is not particularly limited, but examples include drying the plant body so that its moisture content is 10% or less, preferably 8% or less. The drying process can be carried out by any method known to those skilled in the art, such as hot air drying, high-pressure steam drying, electromagnetic wave drying, or freeze-drying. Drying by heating can be carried out, for example, at a temperature and time such that the plant body does not discolor due to heating, at a temperature of 40°C to 140°C, preferably 80°C to 130°C.

[0037] The crushing process is not particularly limited, but examples include crushing the plant material using crushing equipment and tools such as crushers, mills, blenders, and millstones, in any method commonly used by those skilled in the art. The crushed plant material is sieved as needed, and it is preferable to use the plant material powder that passes through, for example, 30 to 250 mesh. By using a particle size that passes through 250 mesh or less, the plant material powder becomes easier to handle during further processing, and by using a particle size that passes through 30 mesh or more, uniform mixing of the plant material powder with other materials becomes easier.

[0038] The method for fragmenting plant material is not particularly limited, but methods commonly used by those skilled in the art for fragmenting plant material, such as slicing, crushing, and shredding, can be used. As an example of fragmentation, slurrying may be performed. Slurrying is done by putting the plant material through a mixer, juicer, blender, or muscoloider to create a thick, porridge-like consistency (a suspension of liquid and solid). When heating the fragmented seeds, water may be added to this liquid and boiled down, and then the crude solids may be removed by means of sieving or filtration before using the liquid portion.

[0039] The method of extracting juice from plants is not particularly limited, but examples include methods of pressing the plant or its fragments, or methods of centrifuging or filtering the fragments of plant material. A specific example of a juice extraction method is to extract juice using mechanical crushing means such as a mixer or juicer, and then, if necessary, remove the coarse solids by means of sieving or filtration to obtain the juice.

[0040] The method for obtaining a plant extract is not particularly limited, but examples include adding an extraction solvent commonly used by those skilled in the art, such as ethanol, water, acid, aqueous ethanol, or an acidic aqueous solution, to a plant or its pulverized or dried form, and then stirring and / or heating as necessary to extract the extract. The crude solids may then be removed by means of sieving, filtration, etc., to obtain the extract. For example, the extract obtained by adding water to pulverized (ground) soybeans, boiling it down, and then filtering out the solids is known as soy milk. The extract may be concentrated as necessary.

[0041] The method for fermenting plant material involves adding lactic acid bacteria, yeast, koji mold, natto bacteria, acetic acid bacteria, etc., to the plant material or its pulverized, juiced, extracted, or fragmented form. These may be one type or a combination of two or more types. The lactic acid bacteria referred to here may be bifidobacteria, or general lactic acid bacteria other than bifidobacteria.

[0042] The juice obtained from the above-described fragmentation process, the liquid extract obtained from the extraction process, and the liquid or slurry obtained after fermentation can all be dried and powdered by any method known to those skilled in the art, such as hot air drying, high-pressure steam drying, electromagnetic wave drying, or freeze-drying. Excipients such as dextrin may be added at this time.

[0043] In the oral composition of this embodiment, the plant treatment may be in solid form, or it may be in liquid, syrup, paste, gel, jelly, cream, emulsion, spray, mousse, lotion, or other fluid form. Examples of solid forms include powder, granules, tablets, chewables, capsules, and soft capsules.

[0044] The content of the functional component in the oral composition of the present invention is not particularly limited. For example, it is preferably 0.0001% by mass or more, more preferably 0.0005% by mass or more, and particularly preferably 0.001% by mass or more, in terms of its excellent absorption-promoting effect of cannabidiol. It is also preferably 99.9% by mass or less, more preferably 98% by mass or less, and particularly preferably 95% by mass or less. If multiple types of functional components are included, this refers to their total amount.

[0045] The ratio of cannabidiol to functional ingredients in the oral composition of the present invention is not particularly limited. For example, in terms of solid content, the ratio of functional ingredients to cannabidiol is preferably 1:0.00001 or higher, more preferably 1:0.0001 or higher, and preferably 1:0.001 or higher from the viewpoint of excellent absorption-promoting effect of cannabidiol. Furthermore, 1:1000 or lower is preferred, 1:200 or lower is more preferred, and 1:10 or lower is particularly preferred. Note that if multiple types of functional ingredients are contained, the ratio refers to their total amount.

[0046] <Other ingredients> In addition to the components mentioned above, the oral composition of the present invention may contain other components as needed. These other components may include, for example, excipients, lubricants, dietary fiber such as water-soluble and insoluble dietary fiber, proteins, various vitamins and minerals, algae, yeast and other microorganisms. Furthermore, as needed, sweeteners, acidulants, nutritional supplements, stabilizers, binders, glazing agents, thickeners, colorants, diluents, emulsifiers, food additives, and seasonings commonly used in the food industry may be added. The content of these other components can be appropriately selected depending on the form of the composition of the present invention.

[0047] <Absorption-enhancing composition> The oral composition of the present invention can be used in various forms for the purpose of obtaining an absorption-enhancing effect of cannabidiol.

[0048] The absorption-enhancing composition of the present invention is characterized by containing at least one functional component selected from Astragalus membranaceus, Panax ginseng, bitter orange, polyamine, squalene, spore-forming lactic acid bacteria, tartaric acid, docosahexaenoic acid, eicosapentaenoic acid, astaxanthin, and krill. These functional components may be used in a composition separate from cannabidiol, but from the viewpoint of promoting the absorption of cannabidiol, it is preferable to use them in a composition containing cannabidiol.

[0049] Furthermore, the absorption-enhancing composition of the present invention is characterized by containing at least two functional components selected from safflower oil, olive oil, medium-chain triglyceride oil, and linseed oil. These functional components may be used in a composition separate from cannabidiol, but from the viewpoint of promoting the absorption of cannabidiol, it is preferable to use them in a composition containing cannabidiol.

[0050] In the present invention, when the functional component is a composition separate from cannabidiol, there are no particular limitations on the method of ingesting the composition containing the functional component. For example, it is preferable to ingest it 3 hours to 3 hours before to ingest cannabidiol, more preferably 2 hours to 2 hours before to ingest it, particularly preferably 1 hour before to 1 hour before to ingest it, and especially preferable to ingest it simultaneously with cannabidiol.

[0051] The oral composition of the present invention is not particularly limited as long as it is in a form suitable for oral use, but from the viewpoint of ease of administration, it may be in a liquid form such as liquid, syrup, paste, gel, jelly, cream, emulsion, spray, mousse, or lotion. Examples of solid forms include powder, granules, tablets, chewables, capsules, and soft capsules.

[0052] The daily dosage of the oral composition of the present invention is not particularly limited and can be appropriately set depending on the mode of use and the user's usage. For example, the daily dosage of the oral composition of the present invention is preferably 0.01 to 1000 mg / kg, more preferably 0.1 to 500 mg / kg, and even more preferably 1 to 100 mg / kg, based on the user's body weight and in terms of solid content.

[0053] Similarly, there are no particular limitations on the amount of the oral composition of the present invention used in a single dose. For example, the amount of the oral composition of the present invention used in a single dose is preferably 0.001 to 2000 mg / kg, more preferably 0.01 to 1000 mg / kg, based on the user's body weight and calculated in terms of solid content, and even more preferably 0.1 to 100 mg / kg, from the viewpoint of exerting the effects of the oral composition of the present invention.

[0054] Furthermore, the daily amount of the oral composition of the present invention is not particularly limited. For example, in terms of solid content, it is preferably 0.001 to 20 g, more preferably 0.005 to 10 g, and particularly preferably 0.01 to 5 g, from the viewpoint of exhibiting the effects of the oral composition of the present invention.

[0055] The amount of the oral composition of the present invention used in a single dose is not particularly limited. For example, in terms of solid content, it is preferably 0.00001 to 20 g, more preferably 0.00005 to 10 g, and particularly preferably 0.0001 to 5 g, from the viewpoint of exhibiting the effects of the oral composition of the present invention.

[0056] Furthermore, the amount of cannabidiol in the daily dose of the oral composition of the present invention is not particularly limited. For example, it is preferably 0.00001 to 1 g, more preferably 0.00005 to 0.5 g, and particularly preferably 0.0001 to 0.1 g, from the viewpoint of exhibiting the effects of the oral composition of the present invention.

[0057] The cannabidiol content in the daily dose of the oral composition of the present invention is not particularly limited. For example, it can be 0.000001 to 1 g, more preferably 0.000005 to 0.5 g, on a solid content basis, and particularly preferably 0.00001 to 0.1 g, from the viewpoint of exhibiting the effects of the oral composition of the present invention.

[0058] The packaging form of the oral composition of the present invention is not particularly limited and can be appropriately selected depending on the dosage form, etc., but examples include blister packs such as PTP; strip packaging; heat seal; aluminum pouch; film packaging using plastic or synthetic resin; glass containers such as vials; plastic containers such as ampoules. [Examples]

[0059] The present invention will be described below based on examples. However, the scope of the present invention is not limited to these examples.

[0060] Cannabidiol absorption-promoting effect (1) <Test substance> The following substances were used as test materials. • Cannabidiol: Commercially available synthetic product used • Astragalus membranaceus: A water-containing ethanol extract (containing saponins) of the above-ground parts of Astragalus membranaceus was used. • Panax sanshoensis: A water-containing ethanol extract (containing saponins) of the above-ground parts of Panax sanshoensis was used. • Bitter orange: A water-containing ethanol extract of bitter orange peel (containing 6% or more cyphnelin) is used. • Polyamine: Using a citric acid aqueous extract of rice germ (containing 0.2% polyamine). • Squalene: Refined from shark liver oil • Spore-forming lactic acid bacteria: Using commercially available Bacillus coagulans • DHA: Using refined fish oil (DHA 8.5% or higher) • EPA: Made using refined fish oil (EPA 1.2% or higher) • Astaxanthin: Using astaxanthin derived from Haematococcus algae. • Krill: Using krill oil • Safflower oil: Made using oil derived from safflower seeds. • Olive oil: Made from oil derived from olive fruit. • Medium-chain triglyceride oil: Using MCT powder • Linseed oil: Made from oil derived from flax seeds. • Oleic acid: Using a commercially available standard reagent. • Deoxycholic acid: Using commercially available standard reagents In Example 1, a mixture of Astragalus membranaceus extract and Ginseng sansinensis extract (1:1), and refined fish oil containing Example DHA and EPA were used.

[0061] <Cannabidiol absorption-enhancing effect> 1. Preparation of HBSS(+) HEPES Buffer (hereinafter also referred to as "buffer") 2.38 g of HEPES, 100 mL of 10×HBSS(-), 350 mg of NaHCO3, 140 mg of CaCl2, 100 mg of MgCl2·6H2O, and 100 mg of MgSO4·7H2O were dissolved in 850 mL of ultrapure water, and the pH was adjusted to 7.4 with 1 M NaOH. The total volume was then increased to 1 L to prepare the buffer.

[0062] 2. Cell culture and addition of test substance (1) 75cm in a 37℃, 5% CO2 incubator 2 Human colorectal cancer-derived cells (Caco-2) were cultured in flasks. The culture medium used was 1% NEAA (MEM Non-Essential Amino Acids Solution) - 10% FBS - DMEM. (2) Add 600 μL of culture medium to a 24-well plate and transfer the insert wells. (3) Cells suspended by trypsin treatment are transferred from a 75 cm² flask to insert wells in a 4.0 × 10⁶ container. 4 100 μL of seeds were seeded to achieve a cell density of cells / well. (4) The cultures were incubated at 37°C in a 5% CO2 incubator, and the culture medium was changed every 2-3 days. The medium change was performed by changing 1600 μL of 1% NEAA-10% FBS-DMEM in the outer well (basement membrane side well) and 350 μL in the inner well (luminal side well) of the insert well. The electrical resistance was measured using Millicell ERS-2, and the cultures were continued until the resistance reached 1500 Ω or higher before being used for testing. (5) The insert wells were washed twice with buffer and transferred to a 24-well plate. 350 μL of buffer was added to the luminal wells and 1600 μL of buffer was added to the basement membrane wells. (6) The cells were cultured in a CO2 incubator for 30 minutes to acclimate them to the buffer. (7) After removing 175 μL of buffer from the inside of the insert well, 175 μL of the test substance solution was added in batches and shaken in an incubator for 2 hours. Cannabidiol was dissolved in a surfactant (PEG40 hydrogenated castor oil), and the functional component was dissolved in DMSO or a 0.5% DMSO-containing buffer. After adding to cells, the solution was adjusted to contain 500 μg / mL of cannabidiol (0.5% surfactant (PEG40 hydrogenated castor oil)) and 2.5 μg / mL of the functional component (0.125% DMSO), and then added to the cells. (8) After shaking for 2 hours, the entire volume of the sample from the luminal well was collected into a 1.5 mL tube.

[0063] 3. Measurement of cannabidiol concentration using dinitrophenol (1) Transfer the luminal well sample collected in 2(8) above, the solution containing 500 μg / mL of cannabidiol before addition to cells, and 50 μL of the calibration curve sample to a 1.5 mL tube, and add 250 μL of 4 M sodium hydroxide solution. Then add 200 μL of 0.1 (W / V)% dinitrophenol solution and mix. The calibration curve was prepared using serially diluted cannabidiol dissolved in ethanol. (2) The mixture was heated at 100°C for 50 minutes, mixed by vortexing, and then centrifuged (room temperature, 10 minutes, 20,000g). (3) The supernatant after centrifugation was transferred to a 96-well assay plate and the absorbance was measured (500 nm, 650 nm (turbidity)). (4) The cannabidiol concentration in each sample was evaluated from the calibration curve using the value obtained by subtracting the absorbance (turbidity) at 650 nm from the absorbance at 500 nm. (Reference for measurement method: T Aman et al. Spectrophotometric Determination of Cannabidiol. ANALYTICAL LETTERS (1993) 26(10)) The decrease in cannabidiol (μg) was calculated from the concentration of cannabidiol in the solution containing 500 μg / mL before addition to cells and from the concentration of cannabidiol in the luminal well samples. The relative value was calculated with the decrease in Comparative Example 1 (which contained only cannabidiol, no functional components) set to 1. The results are shown in Tables 2 and 3.

[0064] [Table 2]

[0065] [Table 3]

[0066] Caco-2 cells are commonly used as a model cell for the intestinal tract to evaluate the intestinal absorption of test substances. When Caco-2 cells are differentiated into a monolayer in an insert well and the test substance is added to the culture supernatant on the luminal side, the test substance is taken up into the cells passively or actively, and after some of it is metabolized and degraded, it is secreted into the permeate on the basement membrane side. By measuring the amount of test substance contained in the permeate, the intestinal absorption of the test substance can be evaluated. In this evaluation system, the decrease in the test substance in the culture supernatant correlates with the increase in the test substance in the permeate (Reference: Food Functionality Evaluation Manual Collection, Vol. III, "Experimental Method for Substance Permeation Using Caco-2 Cell Layers," Makoto Shimizu et al.). From this, it is thought that the amount of decrease in the test substance in the culture supernatant reflects the amount of uptake into the cells. When micellar cannabidiol was added to Caco-2 cells differentiated into monolayer cells, the amount of cannabidiol in the culture supernatant decreased. Although cannabidiol was not detected in the permeate, it was confirmed that cannabidiol did not adhere to the cell surface and that it was not degraded in the culture medium. Therefore, it is thought that the cannabidiol that decreased in the culture supernatant was taken up into the cells. Thus, the decrease in cannabidiol in the culture supernatant can be evaluated as the amount of cannabidiol taken up into the cells (amount of cannabidiol absorbed). Examples 1-13, in which functional ingredients were added along with cannabidiol, showed that more than 1.2 times more cannabidiol was absorbed compared to Comparative Example 1, in which no functional ingredients were added. Furthermore, it was found that cannabidiol absorption was enhanced even when compared to oleic acid and deoxycholic acid, which are known to enhance the absorption-promoting effect of cannabidiol. Therefore, it was suggested that the oral composition of the present invention promotes the absorption of cannabidiol in intestinal cells by containing specific functional components.

[0067] Cannabidiol absorption-promoting effect (2) <Test substance> The following substances were used as test materials. • Cannabidiol: Commercially available synthetic product used • Squalene: Refined from shark liver oil • Piperine: Uses piperine derived from black pepper.

[0068] Male SD rats were acclimatized for at least 5 days and then divided into three groups. After group division, the test substance was administered orally. Two hours after administration, blood was collected from the jugular vein using a syringe containing an anticoagulant (heparin sodium), and the plasma was collected by centrifugation. After deproteinization as a pretreatment, the cannabidiol concentration in the plasma was analyzed by high-performance liquid chromatography (HPLC).

[0069] (Analysis conditions) Column: Unison UK-C18HT (particle size 3μm), manufactured by Intact Co., Ltd., φ4.6 × 150 mm Mobile phase: Water / acetonitrile mixture Gradient conditions: Table 4 Column temperature: 55℃ Flow rate: 1.0ml / min

[0070] [Table 4]

[0071] Table 5 shows the dosage of the test substance and the amount of cannabidiol in the plasma 2 hours after administration of the test substance.

[0072] [Table 5]

[0073] As is clear from Table 5, Example 14, which used cannabidiol and squalene, showed a significant increase in the amount of cannabidiol in plasma compared to Comparative Example 4, which used cannabidiol alone, indicating that squalene enhances the absorption of cannabidiol into the body. This result is supported by the fact that Example 4 showed a higher absorption-enhancing effect compared to Comparative Example 1 in "Cannabidiol Absorption-Enhancing Effect (1)," suggesting that the composition of the present invention enhances the absorption of cannabidiol into the body by using specific functional components together with cannabidiol. Furthermore, it was found that the composition of the present invention enhances the absorption of cannabidiol even when compared to the case where piperine, which is known to enhance cannabidiol absorption, was used in combination with cannabidiol (Comparative Example 5).

[0074] <Manufacturing Example 1> Tablets (250 mg per tablet) were manufactured according to the composition shown in Table 6 below. The amounts listed in the table represent mass percentages. The oral composition obtained in the manufacturing example below has a high absorption-promoting effect on cannabidiol, so taking two tablets once a day allows you to enjoy the excellent effects of cannabidiol.

[0075] [Table 6]

[0076] <Manufacturing Example 2> Tablets (200 mg per tablet) were manufactured according to the composition shown in Table 7 below. The amounts listed in the table represent mass percentages. The oral composition obtained in the manufacturing example below has a high absorption-promoting effect on cannabidiol, so taking three tablets once a day allows you to enjoy the excellent effects of cannabidiol.

[0077] [Table 7]

[0078] <Manufacturing Example 3> The soft capsule contents were prepared according to the composition shown in Table 8 below. The amounts listed in the table are expressed in mass percent. The obtained contents were encapsulated in a gelatin film to produce soft capsules (300 mg per capsule). The oral composition obtained in the following manufacturing example has a high absorption-promoting effect on cannabidiol, so taking one capsule once a day allows you to enjoy the excellent effects of cannabidiol.

[0079] [Table 8]

[0080] <Manufacturing Example 4> Oral oil was prepared according to the composition shown in Table 9 below. The amounts listed in the table are expressed in mass percent. The oral composition obtained in the following manufacturing example has a high absorption-enhancing effect on cannabidiol, so the excellent effects of cannabidiol can be enjoyed by taking 0.1 mL once a day.

[0081] [Table 9] [Industrial applicability]

[0082] The oral composition of the present invention, by containing specific functional ingredients, can provide an oral composition with excellent absorption-promoting properties for cannabidiol, and therefore has high potential for industrial application.

Claims

[Claim 1] An oral composition characterized by containing cannabidiol, and at least one component selected from astaxanthin, eicosapentaenoic acid, docosahexaenoic acid, squalene, and krill.

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