apple extract-containing composition

Abstract

To provide an apple extract-containing composition that is less prone to sticking during a formulation process.SOLUTION: An apple extract-containing composition contains (A) an apple extract of 3 wt.% or more and 35 wt.% or less and (B) ang-khak, with a weight ratio of (A) to (B) (A / B) of 0.1 or more and 3.5 or less.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a composition containing an apple extract.

Background Art

[0002] Apples are fruits with high nutritional value, and the saying "An apple a day keeps the doctor away" is also used in the English-speaking world. Apples contain a lot of polyphenols. For example, Patent Document 1 proposes a cholesterol metabolism regulator containing an apple extract as an active ingredient, and Patent Document 2 proposes a proteasome activator containing an apple extract as an active ingredient.

[0003] Hongqu is a kind of koji produced by growing Monascus bacteria on rice or the like. It has a long history of being used as food in East Asian regions. In China and Taiwan, it is used in red wine, aged wine, and red fermented bean curd, and in Okinawa, it is used like tofu. It has been reported that monacolin K, a Hongqu polyketide, inhibits cholesterol biosynthesis in the liver by antagonistically inhibiting HMG-CoA reductase (Non-Patent Document 1). Monacolin K reduces cholesterol biosynthesis by inhibiting HMG-CoA reductase in the liver, and promotes the uptake of LDL cholesterol into the liver by increasing the expression of LDL receptors in the liver, resulting in a decrease in blood cholesterol.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Non-Patent Documents

[0005]

Non-Patent Document 1

[0006] It has been found that when apple extract is used as a raw material for supplements, tableting problems (sticking) are likely to occur when forming compression-molded formulations such as tablets and hard capsules. Sticking of compositions containing apple extract could not be resolved with lubricants such as stearic acid and sucrose esters, which are commonly used in formulation. The object of this invention is to provide an apple extract-containing composition that is less prone to sticking during formulation. [Means for solving the problem]

[0007] The inventors diligently researched additives that could prevent sticking during formulation and discovered that sticking could be prevented by incorporating a specific amount of red yeast rice, which is known to have a blood cholesterol-lowering effect. This led to the completion of the present invention. In other words, the means for solving the problems of the present invention are as follows. 1. (A) Apple extract: 3% to 35% by weight (B) Red yeast rice An apple extract-containing composition comprising (A) and (B), wherein the weight ratio (A / B) of (A) is 0.1 or more and 3.5 or less. 2. (A) The apple extract-containing composition according to 1, wherein the apple extract contains procyanidin. 3. (B) The apple extract-containing composition according to 1. or 2., wherein the red yeast rice contains red yeast rice polyketide. 4. (B) An apple extract-containing composition according to any of 1. to 3., comprising 3% to 45% by weight of red yeast rice. 5. A compression-molded formulation containing apple extract as described in any of 1 to 4. [Effects of the Invention]

[0008] The composition of the present invention contains apple extract and red yeast rice, and is therefore expected to have high health-promoting effects. The composition of the present invention is less prone to sticking during formulation and has excellent productivity. [Modes for carrying out the invention]

[0009] The present invention (A) Apple extract 3% to 35% by weight (B) Red yeast rice This invention relates to an apple extract-containing composition comprising (A) and (B), wherein the weight ratio (A / B) of (A) is 0.1 or more and 3.5 or less.

[0010] (A) Apple extract The apple (Malus pumila) varieties used in this invention are not particularly limited and include, for example, Fuji, Kokko, Ohrin, Kogyoku, Jonagold, Delicious, Sansa, and Senshu. The part of the apple used for extraction is not particularly limited; for example, it could be the fruit, leaves, trunk, or flowers, but the fruit is preferred. The fruit can be unripe (young fruit) or fully ripened, but young fruit with a high polyphenol content is preferred. The part of the fruit used for extraction is not particularly limited; for example, it could be the whole fruit, pulp, peel, or seeds. Apple extract can be obtained by extracting these parts individually or in combination of two or more.

[0011] Apples, especially young apples, are rich in polyphenols. The apple extract used in this invention is It is preferable that the material contains procyanidin, a type of polyphenol. Procyanidins are compounds formed by condensation or polymerization using flavan-3-ol derivatives as structural units. Examples of flavan-3-ol derivatives include catechin, epicatechin, gallocatechin, epigallocatechin, afzeletin, and epiafzeletin.

[0012] The extraction solvent for obtaining apple extract is not particularly limited, but in order to obtain an extract rich in procyanidins, it is preferable to use 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; water, etc. The extraction method is not particularly limited, but methods using two-phase solvent partitioning or high-speed partition chromatography are preferred. The extraction temperature is usually in the range of 0 to 100°C, and preferably 5 to 50°C. The amount of extraction solvent is 1 to 100 (w / w) times the amount of the extract, preferably 5 to 10 (w / w). In addition, proteolytic enzymes may be added during extraction to perform hydrolysis.

[0013] The extract can be purified by known methods. For example, after removing insoluble matter by filtration, centrifugation, decantation, etc., it can be fractionated, purified, and concentrated as needed using adsorbents such as activated carbon, activated clay, silica gel, or activated alumina synthetic resin for decolorization and deodorization purposes, or by solvent fractionation, reverse osmosis membrane, ion exchange, etc. However, since apple extract contains various useful components other than procyanidins, such as polyphenols, organic acids, and amino acids, it is preferable not to perform purification. The obtained extract can be used as is, or after being powdered by methods such as vacuum concentration, spray drying, or freeze-drying.

[0014] The apple extract-containing composition of the present invention contains (A) apple extract in an amount of 3% to 35% by weight on a dry weight basis of the total composition. The apple extract content (dry weight) is preferably 5% or more, and preferably 30% or less on a dry weight basis.

[0015] (B) Red yeast rice Red yeast rice can be used in the form of a powder obtained by drying and grinding the cells of Monascus purpureus, a red yeast rice extract, or a dried red yeast rice extract. The red yeast rice used in the present invention preferably contains red yeast rice polyketides. Red yeast rice polyketides are metabolites of Monascus purpureus and have a chemical structure similar to HMG-CoA. Red yeast rice polyketides inhibit cholesterol synthesis by competing with HMG-CoA. Red yeast rice polyketides preferably contain monacolin K.

[0016] In the composition containing apple extract of the present invention, the weight ratio (A / B, dry weight) of (A) apple extract to (B) red yeast rice is 0.1 or more and 3.5 or less. This weight ratio (A / B, dry weight) is preferably 0.125 or more and preferably 3.0 or less. In addition, the composition containing apple extract of the present invention preferably contains (B) red yeast rice at 3% to 45% by dry weight based on the whole composition. The content of this red yeast rice is preferably 5% or more and preferably 40% or less. In the composition containing apple extract of the present invention, the amount of apple-derived procyanidins per single intake is preferably 10 mg or more and 50 mg or less, more preferably 15 mg or more and 45 mg or less, and even more preferably 20 mg or more and 40 mg or less. In the composition containing apple extract of the present invention, the amount of red yeast rice polyketides per single intake is preferably 0.1 mg or more and 10 mg or less, more preferably 0.5 mg or more and 5 mg or less, and even more preferably 1 mg or more and 3 mg or less.

[0017] The composition of the present invention can be taken as it is or dissolved in water for drinking, but it is preferably formulated by adding various excipients. Examples of the preparation include granules, tablets, and capsules, and tablets which are compression molded preparations and hard capsules are preferred. When formulating the composition, additives may be incorporated to the extent that they do not hinder the purpose of the composition of the present invention. Specifically, these may include dietary fibers and thickeners derived from sources other than vegetables, such as hemicellulose, lignin, guar gum, konjac mannan, isagol, alginic acid, agar, carrageenan, chitin, carboxymethylcellulose, and polydextrose; minerals such as calcium, iron, sodium, zinc, copper, potassium, phosphorus, magnesium, iodine, manganese, and selenium; fat-soluble or water-soluble vitamins such as vitamin A, vitamin C, vitamin D, vitamin E, vitamin K, niacin, folic acid, and pantothenic acid; glycerin fatty acid esters, etc. Examples of lubricants include sugar fatty acid esters, sorbitan fatty acid esters, propylene glycol fatty acid esters, phospholipids, gum arabic, xanthan gum, tragacanth gum, locust bean gum, emulsifiers and dispersants, fillers, excipients, preservatives and antioxidants, flavor modifiers and fragrances, tasters such as sodium chloride, monosodium glutamate, glycine, succinic acid, and sodium lactate, acidulants such as citric acid, sodium citrate, acetic acid, adipic acid, fumaric acid, and malic acid, low-calorie sweeteners such as maltitol and aspartame, and colorants. However, since the composition of the present invention can prevent sticking without using a large amount of lubricant, it is preferable that the content of lubricants such as calcium stearate and sucrose esters is low. Specifically, it is preferable that the content of lubricants relative to the total composition be 5% by weight or less, and more preferably 2% by weight or less. [Examples]

[0018] ·raw materials Apple Extract: ApplePhenon Apple Procyanidin (Arista Health & Nutrition Science, contains 18.4% apple-derived procyanidin) Red yeast rice: Red yeast rice BY-1000 (Yaegaki Fermentation Technology Co., Ltd., contains 9.5-10.5 mg / g of natural statins and 1.0% of polyketides) Starch: PCF FC-30 (Asahi Kasei) Cellulose: Ceolus UF-F702 (Asahi Kasei) Calcium stearate: Food additive calcium stearate (Sakai Chemical Industry) Sucrose ester: Ryoto Sugar Ester B-370F (Mitsubishi Chemical Foods) Silicon dioxide: Silopage 702 (Fuji Silicia)

[0019] "tablet" Of the formulations shown in Table 1, all ingredients except the lubricant (calcium stearate and sucrose ester) were sieved (30 mesh), mixed, and then the lubricant was added and mixed as needed. The resulting mixture was compressed into tablets using a single-shot tablet press. The tablets were φ9mm, R12, and weighed 300mg / tablet, compressed at a pressure of 1000kgf.

[0020] When removing the resulting tablets from the pestle, their adhesion to the pestle was evaluated according to the following criteria. The results are shown in Table 1. ○: No adhesion to the pestle was observed. ×: Adhesion to the pestle was observed. Furthermore, if the material adheres to the pestle, it can cause sticking during production, leading to serious problems.

[0021] [Table 1]

[0022] The compositions of Examples 1 to 6 of the present invention did not adhere to the pestle, preventing sticking. Furthermore, as shown in the reference example, when the content of (A) apple extract was low, it did not adhere to the pestle. In contrast, Comparative Examples 1-5, which did not contain (B) red yeast rice, Comparative Examples 6 and 8, in which the weight ratio of (A) apple extract / (B) red yeast rice was outside the range of the present invention, and Comparative Example 7, which contained a large amount of (A) apple extract, showed adhesion to the pestle.

[0023] "Hard capsules" Hard capsules (size 2) were manufactured using a standard method with a daikon press-type hard capsule filling machine, according to the formulations shown in Table 2. [Table 2]

[0024] The formulation of Example 7 allowed for the successful manufacture of hard capsules without any problems.

Claims

1. (A) Apple extract 3% to 35% by weight (B) Red yeast rice 3% to 45% by weight A compression-molded formulation comprising an apple extract-containing composition having (A) and (B) weight ratio (A / B) of 0.1 or more and 3.5 or less.

2. (A) The compression-molded formulation according to claim 1, wherein the apple extract contains procyanidin.

3. (B) The compression molded formulation according to claim 1 or 2, wherein the red yeast rice contains red yeast rice polyketide.

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