KR101991746B1 - Agent for improvement of cathechin bioavailability - Google Patents

Abstract

The present invention discloses a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol. The present invention also relates to a pharmaceutical composition comprising: And a catechin bioavailability enhancer. The composition for antioxidation and the composition for inhibiting aging are disclosed.

Description

Catechin bioavailability enhancer {Agent for improvement of cathechin bioavailability}

The present invention relates to a catechin bioavailability enhancer.

Tea (tea) has been consumed since B.C 2000 in China and India. It is supposed to be the first beverage that mankind has begun to drink. One of the main potent components of such tea is catechins, which are polyphenolic compounds. In general, catechins are catechin, catechin, epicatechin (EC), gallocatechin (GC), (-) - epigallocatechin, EGC ), Epicatechin gallate (ECG), gallocatechin gallate (GCG), (-) - epicatechin gallate (CG), catechin gallate Epigallocatechin gallate (EGCG), a total of 8 species are known.

Catechins are known to have antioxidative, antiviral and anticancer effects, and are known to have excellent body fat and weight loss effects. However, catechin has a low bioavailability and is not very useful.

Korean Patent Publication No. 10-2007-0027710 (Published on Mar. 9, 2007) Specification

The present invention provides a catechin bioavailability enhancer. The present invention also relates to a catechin; And a catechin bioavailability enhancer, a composition for antioxidation and a composition for inhibiting aging.

One aspect of the present invention provides a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol.

Another aspect of the present invention is a catechin; And a composition for reducing body fat, an antioxidant composition and a composition for inhibiting aging, which contain the catechin bioavailability enhancer.

The catechin bioavailability enhancer according to the present invention can effectively enhance the bioavailability of catechin by containing at least one of an acid and a sugar alcohol. Also, the composition comprising the catechin and the catechin bioavailability enhancer is effective as a diet and anti-obesity composition because it does not contain a high-calorie component and is excellent in weight loss and reduction of body fat by enhancing bioavailability of catechin. In addition, the composition has an excellent antioxidative effect and effectively inhibits active oxygen in vivo, thereby improving skin wrinkles and skin elasticity and aging symptoms.

BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 is a graph showing the antioxidative effect of a composition comprising catechin and a catechin bioavailability enhancer according to the present invention.

The lower bioavailability of catechins is believed to be due to the sensitivity of catechin to intestinal digestive juices, the low absorption rate for small intestinal cells, and the rapid metabolism and secretion in the small intestine. On the basis of this, the catechin is mainly decomposed in the upper part of the small intestine where the pH is high during the digestion process and the active oxygen is present, and the phenomenon that catechin is unable to permeate the small intestine cell by the reverse transport protein such as P- have.

On the other hand, when sugar is added to tea extract, it is known that the stability of catechin in digestive organs is increased and the accumulation rate of catechin in small intestine cells is increased, which may increase the absorption rate of catechin in the body due to addition of sugar . However, sugar has a problem of low nutrition and high calorie content, which may adversely affect the health of some users. Therefore, another method is needed to increase the bioavailability of catechin.

One aspect of the present invention provides a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol. The acid or sugar alcohol contained in the enhancer acts as a buffer against the pH change during the digestion process and changes the water activity (Aw) of the catechin in the digestive organs to increase the catechin residual ratio in the small intestine, It is believed to be possible.

Another aspect of the present invention is a catechin; And a composition for reducing body fat, an antioxidant composition and a composition for inhibiting aging, which contain the catechin bioavailability enhancer. Since the composition contains a catechin bioavailability enhancer containing at least one of an acid and a sugar alcohol, the bioavailability of the catechin is improved, thereby exhibiting excellent weight loss and body fat reduction. In addition, the above composition has an excellent antioxidative ability by increasing the antioxidative effect of catechin, which means that it has excellent effect of inhibiting active oxygen, so that the composition can have an excellent antioxidative effect.

As used herein, "catechins" is tea plant, Camellia i.e. sinen sheath (Camellia means an efficacious ingredient contained in at least one of the roots, stems, leaves, fruits, flowers and other parts of the sinensis . The term "extract" of Camellia sinensis herein means a solution obtained by extracting at least one of roots, stems, leaves, fruits, flowers and other parts of Camellia sinensis before or after processing, , A solution obtained by concentrating at least one of the above-mentioned portions, and a solid preparation obtained by processing at least one of the above-mentioned portions.

In one aspect of the invention, the catechin may be included in the composition in the form of an extract of Camellia sinensis , specifically tea extract. In another aspect of the invention, the tea extract may comprise at least 30 wt.%, In particular at least 50 wt.% Catechins, based on the total weight of the extract.

In the present specification, an acid means a substance which ionizes when dissolved in water to produce a hydrogen ion, and includes those allowed as food additives. Acid as a food additive means a food additive that has an acidic taste and is used to increase the acidity. In one aspect of the invention, the acid comprises a weak acid, specifically an edible acid, and an acid derived from a natural food such as fruit. More specifically, the acid includes at least one member selected from the group consisting of citric acid, malic acid, tartaric acid, acetic acid, oxalic acid, tannic acid, butyric acid, lactic acid, glacial acetic acid and ascorbic acid.

In the present specification, the sugar alcohol means an alcohol having two or more hydroxy groups formed by reducing the carbonyl group of a monosaccharide or a compound belonging to such a family, and includes those allowed as food additives. In one aspect of the invention, the sugar alcohol comprises at least one sugar alcohol selected from the group consisting of xylitol, isomalt, maltitol, sorbitol, erythritol, mannitol, lactitol and mannitol. Since the acid and sugar alcohol are low calorie foods, they do not adversely affect weight loss and body fat reduction effects of the composition according to the present invention.

When the enhancer according to one aspect of the present invention includes an acid and a sugar alcohol together, the bioavailability of the catechin can be further increased, and further, the effect of reducing catechin weight, reducing body fat, antioxidative ability and antioxidation effect can be further enhanced . In this case, the weight ratio of the acid and the sugar alcohol may be 1,000: 1 to 1: 1,000, specifically 100: 1 to 1: 100, more specifically 1:10 to 10: 1, To 1: 5 to 5: 1. When it is included in the above weight ratio, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy both the stability and safety of the composition and may be suitably included in the weight ratio in terms of cost effectiveness.

A catechin according to one aspect of the present invention; And a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol, wherein at least one of the acid and the sugar alcohol is used in an amount of 10 parts by weight to 10,000 parts by weight, particularly 20 to 100 parts by weight, 100 to 1,000 parts by weight. When it is included in the above range, it is not only suitable for exhibiting the intended effect of the present invention but also can satisfy both the stability and safety of the composition and may be suitably included in the above range in terms of cost effectiveness. Specifically, in order to exhibit the catechin bioavailability improvement effect, it is preferable to treat at least one of the acid and the sugar alcohol with a sufficient amount. Therefore, the catechin content should be 10 parts by weight or more based on 100 parts by weight of the catechin, More than 10,000 parts by weight will be difficult.

An aspect of the present invention relates to a catechin; And a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol. The food composition may be a health food, a functional food, and a food additive composition. The composition can be applied to various formulations such as tablets, pills, capsules, granules, drinks, caramels, diet bars, and tea bags through a conventional method including adding various kinds of excipients or additives. Depending on the formulation or purpose of use, the compositions may be formulated without difficulty by those of ordinary skill in the art, in addition to the active ingredients, which are conventionally used in the art, and synergistic effects may occur when combined with other ingredients.

The dosage of the active ingredient is within the level of those skilled in the art, and its daily dose can be divided into, for example, 100 to 1,000 mg, preferably 300 to 500 mg catechin in one to three divided doses, And may vary depending on various factors such as the age, health condition, complications, etc. of the subject to be administered.

An aspect of the present invention relates to a catechin; And a catechin bioavailability enhancer comprising at least one of an acid and a sugar alcohol. The pharmaceutical composition may have effects of weight loss, reduction of body fat, and further prevention and improvement of obesity. The pharmaceutical composition also has excellent antioxidant ability and can inhibit aging.

The pharmaceutical composition according to the present invention may be administered orally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, etc. in the form of a solid, semi-solid or liquid with the addition of a compatible inorganic or organic carrier .

Examples of the agent for oral administration include tablets, pills, soft and hard capsules, powders, granules, granules, solutions, emulsions, syrups, . Examples of the parenteral administration agent include injections, drops, ointments, lotions, sprays, suspensions, emulsions, suppositories, and the like.

The pharmaceutical composition according to the present invention can be easily formulated according to the conventional method. Surfactants, excipients, coloring agents, spices, preservatives, stabilizers, buffers, suspending agents or other adjuvants can be suitably used.

In addition, the dosage of the active ingredient will vary depending on the age, sex, body weight and the disease or condition to be treated, the route of administration, or the judgment of the prescriber. Dosage determinations based on these factors are within the level of those skilled in the art and may be administered in divided doses of, for example, 100 to 1,000 mg, preferably 300 to 500 mg, of catechin one to three times a day, Method is not limited to the scope of the present invention.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to Examples, Comparative Examples and Experimental Examples. However, these examples, comparative examples, and experimental examples are provided for illustrative purposes only in order to facilitate understanding of the present invention, and the scope and scope of the present invention are not limited thereto.

[Examples and Comparative Examples] Preparation of catechin composition

The tea leaves were extracted with water and alcohol, and purified by using a column to prepare a tea extract having a catechin content of 50% or more.

Ascorbic acid was prepared by reacting glucose or sorbitol with alcohol and esterifying it, and then treating it with a base to obtain a general synthetic ascorbic acid used as a food additive.

Xylitol was purchased from the general xylitol used as a food additive, which was prepared through hydrogenation using xylose as a base material in corn or birch.

Citric acid, sugar, and glucose were also purchased and used as a food additive.

Each of the examples and comparative examples was prepared with the components and contents as shown in the following table using the above components.

ingredient Example 1 Catechin 100mg + ascorbic acid 30mg Example 2 Catechin 100mg + ascorbic acid 30mg + xylitol 100mg Example 3 Catechin 100 mg + ascorbic acid 30 mg + xylitol 500 mg Example 4 Catechin 100 mg + ascorbic acid 30 mg + xylitol 1000 mg Example 5 Catechin 100mg + citric acid 30mg Example 6 Catechin 100mg + citric acid 30mg + xylitol 200mg Example 7 Catechin 100mg + citric acid 30mg + xylitol 500mg Example 8 Catechin 100mg + citric acid 30mg + xylitol 1000mg Comparative Example 1 Catechin 100 mg Comparative Example 2 Catechin 100mg + ascorbic acid 30mg + sugar 200mg Comparative Example 3 Catechin 100mg + ascorbic acid 30mg + sugar 500mg Comparative Example 4 Catechin 100mg + ascorbic acid 30mg + sugar 1000mg Comparative Example 5 Catechin 100mg + ascorbic acid 30mg + glucose 280mg Comparative Example 6 Catechin 100mg + ascorbic acid 30mg + glucose 700mg Comparative Example 7 Catechin 100mg + ascorbic acid 30mg + glucose 1400mg Comparative Example 8 Catechin 100mg + citric acid 30mg + sugar 1000mg Comparative Example 9 Catechin 100mg + citric acid 30mg + glucose 200mg Comparative Example 10 Catechin 100mg + citric acid 30mg + glucose 280mg Comparative Example 11 Catechin 100mg + citric acid 30mg + glucose 500mg Comparative Example 12 Catechin 100mg + citric acid 30mg + glucose 700mg Comparative Example 13 Catechin 100mg + citric acid 30mg + glucose 1400mg

[Experimental Example 1] Evaluation of effect of acid or sugar alcohol on bioavailability of catechin

When acid or sugar alcohols were included with catechin, the bioavailability was assessed by assessing how much catechin was absorbed.

Each example and comparative example was continuously cultured in artificial digestive juice, which is an in vitro biomimetic system mimicking the physiological and biochemical conditions of the human digestive organs such as the mouth, stomach and small intestine. The concrete method is as follows. First, catechin-containing tea extract, acid and sugar alcohol were dissolved in a phosphate buffer, and amylase was added thereto. The pepsin solution was added, the pH was adjusted to 2 with hydrochloric acid, and then cultured again for 1 hour. Subsequently, sodium hydrogencarbonate (NaHCO ₃ ) was added and the pH was adjusted to 5.3. The mixture of small intestine enzymes was added and the pH was adjusted to 7 using NaOH solution. After culturing for 2 hours, the cells were centrifuged and a certain amount of catechins (카테 catechin / ㎎ protein) was analyzed by HPLC. The results are shown in the table below.

Catechin absorption Catechin absorption Example 1 1763.52 Comparative Example 4 1070.42 Example 2 2189.87 Comparative Example 5 1352.53 Example 3 2066.07 Comparative Example 6 1152.83 Example 4 1704.06 Comparative Example 7 1645.56 Example 5 88.72 Comparative Example 8 253.87 Example 6 1005.70 Comparative Example 9 145.88 Example 7 601.75 Comparative Example 10 214.82 Example 8 787.43 Comparative Example 11 165.66 Comparative Example 1 87.56 Comparative Example 12 192.05 Comparative Example 2 1762.24 Comparative Example 13 173.78 Comparative Example 3 1242.60

As can be seen from the above results, the catechin uptake of the compositions of the Examples containing ascorbic acid or citric acid or xylitol was higher than that of Comparative Example 1 containing only catechin. In particular, the catechin uptake of Examples 2 to 4 including ascorbic acid and xylitol was very high. That is, when the catechin-containing composition comprises an acid or a sugar alcohol, the bioavailability of the catechin contained therein is improved.

[Experimental Example 2] Evaluation of body weight reduction effect of catechin composition containing acid and sugar alcohol (animal experiment)

Sixty-four male ICR mice with an average body weight of 24.23 g were divided into four groups of 16 animals each and classified into a control group and experimental groups 1, 2 and 3. The animals were preliminarily fed for one week with a general compound feed, Prior to fasting, the mice were orally administered to each group by the method shown in Table 3.

Contents Control group Each experimental animal was orally administered 100 mg of tea extract having a catechin content of 50% at 10 ml / kg. Experiment 1 100 mg of green tea extract having a catechin content of 50% and 100 mg of ascorbic acid were mixed with purified water to give a ratio of catechin: ascorbic acid of 2: 1 to each of the experimental animals at a dose of 10 ml / kg. Experiment 2 100 mg of green tea extract having a catechin content of 50% and 100 mg of xylitol were mixed with purified water in each experimental animal and orally administered at a dose of 10 ml / kg at a catechin: xylitol ratio of 2: 1. Experiment group 3 Each experimental animal was orally administered with 10 ml / kg of a composition prepared by mixing 100 mg of green tea extract having a catechin content of 50%, 100 mg of ascorbic acid and 100 mg of xylitol in purified water so that the ratio of catechin: ascorbic acid: xylitol was 2: 1: Respectively.

At 8 weeks after oral administration, the body weights of the experimental animals in each group were measured. The results are shown in the table below.

　
　 Control group Experimental group Experiment 1 Experiment 2 Experiment group 3 Weight loss (Δg) 0.3 ± 0.72 1.3 ± 0.35 1.9 ± 0.41 3.1 ± 0.46

As can be seen from the above results, when administering a catechin composition comprising ascorbic acid or xylitol, the body weight reducing effect is superior to the composition comprising only catechin, and the effect is achieved by administering a composition comprising ascorbic acid and xylitol together It is even better if you do. That is, the catechin composition containing an acid and a sugar alcohol has an excellent weight loss effect.

[Experimental Example 3] Evaluation of weight loss effect of catechin composition containing acid and sugar alcohol (Clinical Experiment)

The effect of body weight and body fat reduction on catechin composition containing acid and sugar alcohol was evaluated through clinical experiments. Subjects were overweight or abdominal obese adults aged from 19 to 60 years with a body mass index (BMI) of 25 or more and a PIBW (ideal body weight percentage) of 110% or more or a waist circumference of 90cm, The characteristics of each group are shown in the table below.

In the experimental group (n = 10) Control group (n = 10) Age (years) 34.2 ± 3.2 34.7 ± 4.3 Height (m) 163.1 ± 4.8 165.2 ± 7.1

Twenty (20) of the total volunteers were divided into two groups (5 males and 5 females), and one group (experimental group) was compared with the composition of Example 2, and the other group (control group) Were consecutively consumed daily for 12 weeks after meals three times a day. The mean body index of each group after 12 weeks is shown in the table below in comparison with before the experiment.

In the experimental group (n = 10) Control group (n = 10) 0 weeks 12 weeks 0 weeks 12 weeks BMI (Kg / m ² ) 28.4 ± 0.72 26.2 ± 0.68 28.8 ± 0.84 28.2 ± 0.24 % Body fat 39.6 ± 1.41 36.7 ± 1.27 38.8 ± 1.65 38.0 + - 1.41 Weight loss (Δkg) - 3.9 ± 0.61 - 1.2 ± 0.86

As shown in the above results, body weight, BMI, and body fat percentage were all decreased, and statistical significance (p <0.05) was shown in the experimental group. On the other hand, the control group showed little change in all values. In particular, the weight loss of the experimental group is remarkably higher than that of the previously studied results. When the catechin-containing composition contains acid and sugar alcohol, weight loss and body fat reduction effect of catechin are maximized.

[Experimental Example 4] Evaluation of antioxidative effect of catechin composition containing acid and sugar alcohol (Clinical Experiment)

The antioxidative effects of catechin compositions containing acids and sugar alcohols were evaluated through clinical trials. We selected healthy adult women in the 20-30 age group. The characteristics of each group are shown in the table below.

The experimental group (n = 8) Control group (n = 3) Age (years) 31.5 ± 5.5 28.5 ± 5.5 Height (m) 165.0 + - 7.0 163.5 ± 3.5 Weight (kg) 50.5 ± 8.5 51.5 ± 10.5

The test group was prepared from the composition of Example 2, and the control group was made from the composition of Comparative Example 1, so that three eggs per day were taken with 100 ml of water. Blood was taken for a certain period of time (0.5, 1.5, 3, 5 hours before and after ingestion) to assess plasma antioxidant capacity. The results are shown in Fig.

As shown in FIG. 1, the test group showed significantly higher antioxidant ability than the control group at all time points after ingestion, and also showed statistical significance (p <0.05). Thus, it can be seen that the antioxidant ability is maximized when the catechin-containing composition contains an acid and a sugar alcohol. Furthermore, the present composition having enhanced antioxidant ability of catechin will have an excellent effect in inhibiting active oxygen which is a source of aging and improving the aging symptoms such as skin wrinkles and elasticity due to the increase of antioxidant ability.

Formulation examples of compositions according to one aspect of the present invention are described below, but may be applied to various other formulations, which are not intended to be limiting but merely illustrative of the invention.

[Formulation Example 1] Preparation of health drinks

EXAMPLES &lt; RTI ID = 0.0 &gt;

Enzymatic treatment Stevia ...................... 100 mg

Grapefruit concentrate ............................... 2 g

Taurine .................................... 1 g

Purified water was added to the whole to give 900 ml

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was heated at 80-90 DEG C for about 1 hour, and the resulting solution was filtered to obtain a sterilized container. The resulting solution was sealed and sterilized, Used for manufacturing.

Although ingredients suitable for health beverages have been appropriately mixed and prepared in the above, composition ratios may be modified according to the regional and national preferences such as the demand class, the demanding country, and the use purpose.

[Formulation Example 2]

20% by weight of tea extract with a catechin content of 50%, 10% by weight of citric acid, 10% by weight of xylitol, 10% by weight of corn starch, 20% by weight of glycerin and 20% by weight of sorbitol are mixed and a ring is prepared using a ventilator.

[Formulation Example 3] Tablets

40.5% by weight of tea extract with a catechin content of 50%, 10% by weight of ascorbic acid, 7% by weight of xylitol, 20% by weight of dextrin and 20% by weight of crystalline cellulose were granulated and granulated using a fluidized bed drier, ester) was added thereto and the tablet was tableted.

[Formulation Example 4]

20% by weight of catechin content tea extract, 10% by weight of ascorbic acid, 10% by weight of xylitol, 5% by weight of enzyme treated stevia and 65% by weight of isomalt were mixed and molded into granules using a fluidized bed granulator, .

Claims (9)

An acid and a sugar alcohol,
The acid is a weak acid,
The weak acid includes at least one selected from the group consisting of citric acid, malic acid, tartaric acid, acetic acid, oxalic acid, tannic acid, butyric acid, lactic acid, glacial acetic acid, and ascorbic acid,
Wherein the sugar alcohol comprises at least one selected from the group consisting of xylitol, isomalt, maltitol, sorbitol, erythritol, mannitol, lactitol and mannitol.
delete delete delete delete The method according to claim 1,
Wherein the acid and sugar alcohol are contained in a weight ratio of 1,000: 1 to 1: 1,000.
Catechin; And
An antioxidative food composition comprising the food additive composition according to any one of claims 1 to 6 as an active ingredient.
delete Catechin; And
A food composition for inhibiting aging comprising the food additive composition according to any one of claims 1 to 6 as an active ingredient.

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