Oily components

Abstract

The present invention provides an oily composition having excellent carotenoid absorption properties in the body, and a capsule preparation containing the oily composition. [Solution] An oily composition containing (A) a carotenoid and (B) a rooibos extract, and a capsule formulation containing this oily composition.

Description

[Technical Field]

[0001] The present invention relates to an oily composition that can be used in foods, medicines, quasi-drugs, etc., and a capsule preparation containing this oily composition. [Background technology]

[0002] Carotenoids such as astaxanthin, lutein, and β-carotene have been reported to have various health-promoting effects, including antioxidant and anticancer effects. Because carotenoids are oil-soluble and poorly soluble in water, they are generally formulated as capsule preparations in which an oily composition containing a high concentration of carotenoids is encapsulated in a capsule. Carotenoids are oil-soluble but poorly soluble in water, and therefore have low absorbability in the body when orally ingested. As means for increasing the absorbability of oil-soluble, water-soluble components such as carotenoids in the body, for example, Patent Documents 1 to 3 propose a method of adding an emulsifier, Patent Documents 4 and 5 propose a method of adding lecithin to promote absorption, and Patent Document 6 proposes a method of encapsulating the carotenoids in β-cyclodextrin. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Patent Publication No. 2021-93979 [Patent Document 2] International Publication No. 2019 / 172454 [Patent Document 3] Japanese Patent Publication No. 2020-15669 [Patent Document 4] International Publication No. 2016 / 031954 [Patent Document 5] Japanese Patent Application Laid-Open No. 2016-29031 [Patent Document 6] International Publication No. 96 / 39870 Summary of the Invention [Problem to be solved by the invention]

[0004] There is a need to increase the bioavailability of carotenoids, but the dissolution rate from capsule formulations after ingestion affects their bioavailability. An object of the present invention is to provide an oily composition that allows carotenoids to be absorbed into the body with excellent absorption, and a capsule preparation containing this oily composition. [Means for solving the problem]

[0005] The means for solving the problems of the present invention are as follows. 1. An oily composition comprising (A) a carotenoid and (B) a rooibos extract. 2. The oily composition according to 1, wherein the carotenoid (A) is either astaxanthin or lutein, or both. 3. A capsule preparation characterized by encapsulating the oily composition described in 1. or 2. [Effects of the Invention]

[0006] The oily composition of the present invention has excellent absorbability of orally ingested carotenoids. Since the oily composition of the present invention reduces the proportion of orally ingested carotenoids that are not absorbed and are excreted, the amount of carotenoid ingested orally can be reduced. Therefore, the capsule formulation of the present invention containing this oily composition can be made smaller in size, making it easier to swallow. DETAILED DESCRIPTION OF THE INVENTION

[0007] In this specification, the expression "A to B" (A and B are numerical values ​​or ratios) means a numerical range that includes both ends. "Oil-based composition" The oily composition of the present invention contains (A) a carotenoid and (B) a rooibos extract. (A) Carotenoids Carotenoids have a basic skeleton (chemical formula C) that is composed of eight isoprene units. 40 H 56) and is a natural pigment component that absorbs visible light in the range of 400 to 500 nm due to the conjugated double bonds in this basic skeleton, resulting in yellow, orange, red, etc. Carotenoids are known to have various physiological effects and health-promoting effects.

[0008] In the present invention, carotenoids such as astaxanthin and lutein may be derivatives thereof such as esters, etc. The carotenoids used in the present invention may be derived from natural products such as plants, algae, crustaceans, bacteria, or synthetic or semi-synthetic products, but because the oily composition of the present invention is intended for oral intake, those derived from natural products are preferred from the standpoint of safety. The carotenoid contained in the oily composition of the present invention is not particularly limited and includes astaxanthin, lutein, α-carotene, β-carotene, γ-carotene, lycopene, zeaxanthin, fucoxanthin, etc., and one or more of these may be contained. Among these, one or more selected from astaxanthin, lutein, and β-carotene are preferred, and either or both of astaxanthin and lutein are more preferred.

[0009] <Astaxanthin> Examples of astaxanthin derived from natural products include astaxanthin derived from the red yeast Phaffia, Haematococcus algae, marine bacteria (e.g., Paracoccus), krill, Adonis (Adonis flower), etc. As astaxanthin derived from natural products, it is possible to use astaxanthin that has been separated and extracted from these natural products and, if necessary, purified.

[0010] As astaxanthin, astaxanthin extracted from Haematococcus algae (also called Haematococcus algae extract) and astaxanthin derived from krill pigment (also called krill extract) are preferred from the standpoints of quality and productivity. Commercially available astaxanthin products can also be used. Examples of commercially available Haematococcus algae extracts include AstaReal L10 (oil containing 10% astaxanthin: Fuji Chemical Industry Co., Ltd.), AstaReal Oil 50F (oil paste containing 5% astaxanthin: Fuji Chemical Industry Co., Ltd.), AstaReal Oil 5F (oil containing 0.5% astaxanthin: Fuji Chemical Industry Co., Ltd.), ASTOTS-S (oil containing 10-22% astaxanthin: Fujifilm Corporation), and ASTOTS-SS (oil paste containing 33-37% astaxanthin: Fujifilm Corporation). An example of a commercially available krill extract is Astax-ST (Marine Daio Co., Ltd.). It is preferable to use these edible oil suspensions.

[0011] <Lutein> Lutein, in the form of lutein fatty acid ester, is found in fruits such as oranges, peaches, papayas, prunes, and mangoes, and is also found in many flowers and vegetables, and is known to be particularly abundant in the petals of marigolds (Tagetes erecta WILLD.), a plant of the Asteraceae family. These plant extracts can be used to obtain lutein. For example, dried and crushed marigold flowers can be extracted with hydrocarbons such as hexane or petroleum ether, or chlorinated hydrocarbon solvents such as dichloromethane, and then the solvent is removed from the extract to obtain marigold oleoresin, which contains a high concentration of lutein. Most marigold oleoresins are solid or highly viscous pastes at room temperature, and the content of purified lutein fatty acid esters in the oleoresins is usually 14-20% as esters.

[0012] As lutein, commercially available products can be used, such as AKY-2182 (35% lutein content, Inabata Fragrance Co., Ltd.), marigold oleoresin (20% lutein content, Bioactives Co., Ltd.), marigold oleoresin beads (15% lutein content, Riken Vitamin Co., Ltd.), and Xanmax 2004 (20% lutein suspension, Catra Phytochem Co., Ltd.).

[0013] Other carotenoids include, for example, β-carotene, such as Carotene 30 SUN Oil (containing 30% beta-carotene, sunflower oil suspension: BASF Japan Ltd.).

[0014] The content of the (A) carotenoid in the oily composition of the present invention is not particularly limited as long as the effects of the present invention are achieved. For example, the content of one type of carotenoid relative to the entire oily composition is preferably 0.1% by mass or more and 5% by mass or less, more preferably 0.5% by mass or more, and more preferably 3% by mass or less. Specifically, the content of astaxanthin is preferably 0.1% to 5% by mass, more preferably 0.5% to 3% by mass, based on the total oil-based composition, while the content of lutein is preferably 0.1% to 5% by mass, more preferably 0.5% to 3% by mass, based on the total oil-based composition. When the oily composition of the present invention contains two or more types of carotenoids, it is preferable that the content of each of them is within the above-mentioned range.

[0015] (B) Rooibos extract Rooibos (Aspalathus linearis) is a legume native to South Africa, and its leaf extract is consumed as rooibos tea. The rooibos extract used in the present invention is not particularly limited as long as it is an extract of rooibos, but an extract of leaves is preferred, and an extract of fermented leaves is more preferred.

[0016] Examples of extraction solvents that can be used to obtain rooibos extract include alkaline solutions such as sodium hydroxide, alcohols such as methanol, ethanol, and propanol, ketones such as acetone and methyl ethyl ketone, nitriles such as acetonitrile, ethers such as tetrahydrofuran and diethyl ether, halogenated hydrocarbons such as dichloromethane and chloroform, esters such as ethyl acetate and ethyl formate, hexane, and water. Mixed solvents of two or more compatible solvents can also be used. Among these, water, ethanol, and mixed solvents of water and ethanol are preferred from the standpoint of safety, with water being more preferred. The extraction method is not particularly limited, but methods using two-phase solvent partitioning or high-performance partition chromatography are preferred. The extraction temperature is usually within the range of 0 to 100° C. When extraction is performed with water, the extraction temperature is preferably 50° C. or higher, more preferably 70° C. or higher, and even more preferably 90° C. or higher. The amount of extraction solvent is 1 to 100 times, preferably 5 to 10 times, the amount of the extract to be extracted.

[0017] The extract can be purified by known methods, for example, after removing insoluble matter by filtration, centrifugation, decantation, etc., the extract can be fractionated, purified, and concentrated using an adsorbent such as activated carbon, activated clay, silica gel, or activated alumina synthetic resin, or by solvent fractionation, reverse osmosis membrane, ion exchanger, etc., for the purpose of decolorization and deodorization, as needed. The obtained extract may be used as it is, as a concentrated liquid, or as a powder obtained by vacuum concentration, spray drying, freeze drying or the like. Commercially available rooibos extracts can also be used, such as Pure Rooibos Extract L (Maruzen Pharmaceuticals Co., Ltd.), Green Rooibos Extract (Tama Biochemical Co., Ltd.), and Rooibos Tea Dried Extract F (Maruzen Pharmaceuticals Co., Ltd.).

[0018] The content of (B) rooibos extract in the oily composition of the present invention is not particularly limited as long as the effects of the present invention are achieved, but for example, it is preferably 1% by mass or more and 40% by mass or less, more preferably 3% by mass or more, even more preferably 5% by mass or more, even more preferably 10% by mass or more, more preferably 35% by mass or less, even more preferably 30% by mass or less, even more preferably 25% by mass or less, and even more preferably 20% by mass or less, relative to the entire oily composition. Furthermore, the mass ratio (A:B) of (A) carotenoid to (B) rooibos extract is not particularly limited as long as it achieves the effects of the present invention, but for example, this mass ratio may be 1:99 to 50:50, preferably 3:97 to 45:65, more preferably 5:95 to 40:60, even more preferably 7:93 to 30:70, and even more preferably 10:90 to 25:75.

[0019] Oily ingredients The composition of the present invention is an oily composition and contains an oily component. The oil component used in the present invention may be any edible oil capable of dissolving and dispersing (A) carotenoid, such as food-grade fatty acid triglycerides and animal and vegetable oils and fats, and two or more of these may be used. Examples of fatty acid triglycerides include medium-chain fatty acid triglycerides in which the fatty acids constituting the triglyceride have 8 to 10 carbon atoms, and long-chain fatty acid triglycerides in which the fatty acids have 12 or more carbon atoms. Examples of animal and vegetable oils include vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, sunflower oil, safflower oil, coconut oil, wheat germ oil, corn germ oil, olive oil, and rice bran oil, and animal oils such as liver oil, fish oil, and whale oil. The content of the oily component in the oily composition of the present invention is not particularly limited as long as the effects of the present invention are achieved, but for example, it is preferably 30 to 95% by mass, and more preferably 40 to 90% by mass, of the entire oily composition.

[0020] ·emulsifier The oily composition of the present invention contains an emulsifier. As the emulsifier, any known emulsifier can be used, such as glycerin fatty acid esters and polyglycerin fatty acid esters.

[0021] Other ingredients In addition to the above-mentioned components, the oily composition of the present invention may contain other components as needed, for example, physiologically active components such as nutritional components, active ingredients, pharmacological components, antioxidants, sugars, etc. Such components can be used without any particular limitation as long as they are usable in foods, beverages, and pharmaceuticals.

[0022] The oily composition of the present invention preferably contains an antioxidant. The antioxidant is not particularly limited, and examples thereof include at least one compound selected from the group consisting of ascorbic acid, ascorbic acid derivatives, and salts thereof, vitamin E such as tocopherol and derivatives thereof, vitamin A, retinoic acid, retinol, retinol acetate, retinol palmitate, retinyl acetate, retinyl palmitate, and tocopheryl retinoate.

[0023] "Method of manufacturing oily composition" The oily composition of the present invention is prepared by weighing out (A) carotenoid, emulsifier, oily component, etc., and then stirring and mixing. If a thickener is included, the mixture is heated to 50 to 70°C, preferably 60°C, while mixing. The weighted (B) rooibos extract is then added and stirred to adjust the consistency. A thickener may also be added to increase the viscosity, if necessary. Examples of thickeners include emulsifiers and beeswax that are solid at room temperature. If the solution after mixing contains air bubbles, it is preferable to remove the air bubbles by a method such as vacuum degassing.

[0024] <Capsule formulation> The capsule formulation of the present invention contains the above-mentioned oily composition. The capsule formulation may be either a soft capsule formulation or a hard capsule formulation. The capsule shell components of the soft capsule preparation and hard capsule preparation can be any conventionally known components without any particular limitations.

[0025] The shape and size of the capsule are not particularly limited and can be set depending on the intake amount of the oily composition of the present invention, but for example, the major axis (diameter in the case of a spherical shape) of the capsule formulation is preferably 2 to 20 mm, more preferably 15 mm or less, more preferably 4 mm or more, and even more preferably 6 mm or more. [Example]

[0026] The present invention will be specifically described below with reference to examples and comparative examples. ·Raw materials (A) Astaxanthin (AstaReal L10, Fuji Chemical Industry Co., Ltd., oil containing 10% astaxanthin) (A) Lutein (AKY-2182, Inabata Perfume Co., Ltd., oil containing 35% lutein) (B) Rooibos extract (Pure Rooibos Extract L, Maruzen Pharmaceutical Co., Ltd.) (b) Bilberry extract (Bilberry dried extract ET / M, Indena SpA) (b) Rosehip extract (Rosehip Polyphenol MJ, Morishita Jintan Co., Ltd.) (b) α-cyclodextrin (Kabamax W6, CycloChem Co., Ltd.) (b) β-cyclodextrin (Celdex B-100, Nihon Shokuhin Kako Co., Ltd.)

[0027] Oily ingredients PS-Base LT (NOF Corporation) Dinner Oil 200 (NOF Corporation) Dinner Oil (NOF Corporation) Palm oil (The Nisshin Oillio Group, Ltd.) EPA-70 (Tama Biochemical Co., Ltd.) Grapeseed oil (Nisshin Oillio Group, Ltd.) Rice oil (Nisshin Oillio Group Co., Ltd.)

[0028] emulsifier Polyglyceryl-2 oleate (Sunsoft Q-17D; Taiyo Kagaku Co., Ltd.) Pentaglycerin monooleate (Sunsoft A171E; Taiyo Kagaku Co., Ltd.) TAISET ADR (Taiyo Kagaku Co., Ltd.) Other ingredients Beeswax FY-100 (Toa Kasei Co., Ltd.) Vitamin raw materials (pyridoxine hydrochloride, DSM Vitamins (Shanghai) Ltd.; riboflavin FP, BASF Company Ltd., Gunsan Site) Antioxidant (Sankator No. 1, Taiyo Kagaku Co., Ltd.)

[0029] "Experiment 1" Capsule formulation manufacturing Of the ingredients, all ingredients except (B) rooibos extract were mixed to the composition shown in Tables 1 and 2. If solid ingredients with high melting points were included, they were heated to 70°C and mixed. Then, (B) rooibos extract was added in the amount shown in Tables 1 and 2, and the mixture was stirred in an emulsifier at 10,000 rpm for 5 minutes to prepare the content liquid. 300 mg of the prepared content liquid was filled into one No. 2 hard capsule to obtain a hard capsule formulation. A separation confirmation test was conducted at 40°C for one day to confirm that the filled content liquid did not separate.

[0030] Evaluation method One hard capsule formulation was placed in a beaker containing 100 ml of water at 37°C and stirred at 50 rpm for 3 hours. After 3 hours of stirring, 1 ml of the liquid was sampled with a syringe and filtered through a 0.45 μm filter. The lutein and astaxanthin contents in the filtrate were quantified by HPLC under the following conditions.

[0031] HPLC conditions (common) Analyzer: SHIMADZU prominence Column: InerSustain C18 HP 3μm 3.0×100mm Mobile phase A: water Mobile phase B: acetonitrile:methanol = 1:1 (lutein) Gradient conditions: 0 min (A / B = 25 / 75) →1min-5min(A / B=5 / 95) →6min-10min(A / B=25 / 75) Column temperature: 40℃ Flow rate: 0.7mL / min Detection: UV 445nm (astaxanthin) Gradient conditions: 0-20 min (A / B=5 / 95) Column temperature: 40℃ Flow rate: 1mL / min Detection: UV 475nm

[0032] Using the concentrations of lutein and astaxanthin in the Reference Example as the standard, the evaluation was made as "Good" if the dissolution properties of both lutein and astaxanthin were improved, and "Poor" if neither of them was improved. The results are shown in Tables 1 and 2.

[0033] [Table 1]

[0034] [Table 2]

[0035] "Experiment 2" The effect of adding rooibos extract on improving the dissolution of astaxanthin and lutein was evaluated in the same manner as in Experiment 1. The results are shown in Tables 3 and 4. [Table 3] [Table 4]

[0036] The oily compositions obtained in Examples 1 to 12 containing (A) carotenoid and (B) rooibos extract of the present invention had improved dissolution rates for both lutein and astaxanthin compared to Reference Example 1. Furthermore, in comparison with the lutein and astaxanthin-only groups, Examples 13 and 14 containing (B) rooibos extract had improved dissolution rates compared to Reference Examples 2 and 3, respectively. In contrast, the oily composition obtained in Comparative Example 1, which did not contain (B) rooibos extract, the oily compositions obtained in Comparative Examples 2 to 6, which used other plant extracts instead of (B) rooibos extract, and the oily compositions obtained in Comparative Examples 7-8, 9, and 10, which used an encapsulating agent instead of (B) rooibos extract, all showed reduced dissolution of at least one of lutein and astaxanthin compared to the Reference Examples.

Claims

[Claim 1] (A) Carotenoids, (B) Rooibos extract, oily components, (A) the carotenoid is either astaxanthin or lutein, or both; (B) The rooibos extract is an extract of any one of water, ethanol, and a mixed solvent of water and ethanol; the mass ratio of (A) to (B) (A:B) is 1:99 to 50:50; A capsule preparation containing an oily composition containing 30 to 95% by mass of an oily component based on the total mass.

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