JP5683768B2 - Composition containing coenzyme Q10 - Google Patents

Description

TECHNICAL FIELD OF THE INVENTION

  The present invention relates to a composition containing coenzyme Q10, and more particularly to a superabsorbent composition of coenzyme Q10 containing sesamin and a food and drink containing the same.

Conventional technology

Coenzyme Q10, also known as coenzyme Q10, vitamin Q, ubiquinone and ubidecalenone (molecular formula: C ₅₉ H ₉₀ O ₄ , molecular weight: 863.36), has a melting point of about 48 ° C. and is hardly soluble in water. Although it is a substance, it is known as a substance that exhibits high solubility in ether and decomposes by light to produce hydroquinone, ubichromenol, and the like.

  This coenzyme Q10 is an essential substance as a coenzyme when the mitochondria of animal cells produce energy, and is known as a vitamin-like substance having an action of improving oxygen utilization efficiency.

  The main pharmacological actions of coenzyme Q10 include antioxidant action, energy production promoting action, cardiopulmonary function enhancing action, immunostimulating action, aging preventing action, etc., as an additive to food or as a component in a dietary supplement It is also used as.

  In addition, in foods, meat and eggs are contained in the order of several μg / g, and are also synthesized in vivo. However, the amount of synthesis in vivo decreases with age and tends to be deficient. However, since there are very few natural food materials with a high coenzyme Q10 content, it is difficult to ingest an amount of coenzyme Q10 that compensates for the deficiency with only a normal meal. In addition, it is desirable to supplement coenzyme Q10 from nutritional supplements or fortified foods in order to prevent heart disease such as ischemic heart disease that is common in elderly people or to reduce symptoms.

Furthermore, since this coenzyme Q10 is a lipophilic solid having a low melting point, is hardly soluble in water, and has extremely low solubility in a base such as fats and oils, it is known to have low absorbability in oral administration. It is required to improve the absorbability of coenzyme Q10 and prevent crystallization, aggregation precipitation and the like. Moreover, since it is taken orally, various examinations are made in order to improve absorbability, considering that it is also important that the safety of the coenzyme Q10-containing composition is high. For example, heat-dissolving coenzyme Q10 in oil (Patent Document 1), using a technique for water-solubilization (Patent Document 2), and using a technique of inclusion with cyclodextrin (Patent Document 3) Has been proposed.
Japanese Patent No. 3549019 JP 2003-169630 A Japanese translation of PCT publication No. 2003-520827

  As described above, although various coenzyme Q10-containing materials are known, there are no materials that can be satisfied from the viewpoint of in vivo absorbability and productivity. For example, the coenzyme Q10-containing material obtained by heating and dissolving Coenzyme Q10 described in Patent Document 1 in oil has a problem that absorption in the body by oral administration is not sufficient. In the technology for water-solubilizing coenzyme Q10 described in Patent Document 2, it is necessary to pass through a step of freeze-drying after mixing and stirring casein Na, dextrin and coenzyme Q10. In addition, in the technique for inclusion of coenzyme Q10 with cyclodextrin described in Patent Document 3, a complicated process for inclusion is required. As described above, the water-solubilization technology described in Patent Document 2 and the cyclodextrin inclusion technology described in Patent Document 3 have complicated manufacturing processes, and the production cost of the coenzyme Q10-containing material obtained by these technologies is high. There was a problem.

  Therefore, an object of the present invention is to provide a coenzyme Q10-containing composition having improved in-vivo absorbability by a production method that is industrially easy to produce and low in production cost.

  As a result of diligent research to solve the above problems, the present inventor found that the in vivo absorbability of coenzyme Q10 was significantly improved by incorporating coenzyme Q10 with sesamin, and thus completed the present invention. is there.

That is, the present invention has the following configuration.
1. A composition comprising sesamin and coenzyme Q10.
2. 2. The composition according to 1 above, wherein the blending weight ratio of sesamin to coenzyme Q10 is 1/10 or more.
3. 3. The composition according to 2 above, wherein the blending weight ratio is 1/3 to 1/1.
4). 4. The composition according to any one of 1 to 3 above, wherein the sesamin is a sesamin concentrate containing 1% or more of the sesamin.
5. 5. The composition according to 4 above, wherein the sesamin concentrate contains 20% or more of sesamin.
6). 6. The composition according to any one of 1 to 5 above, wherein the sesamin is sesamin and / or episesamin.
7). Food / drink containing the composition in any one of said 1-6.
8). A method for increasing the in vivo absorbability of coenzyme Q10, comprising combining sesamin with coenzyme Q10.

BEST MODE FOR CARRYING OUT THE INVENTION

(Sesamin)
This invention improves the in-vivo absorbability of coenzyme Q10 by mix | blending sesamin with coenzyme Q10. Examples of sesamin that can be used in the present invention include sesamin and its analogs. Examples of sesamin analogs include episesamin and dioxabicyclo [3] described in JP-A-4-9331. .3.0] octane derivatives. Specific examples of sesamin can include sesamin, sesaminol, episesaminol, sesamorin and the like. Among these, sesamin and episesamin can be exemplified as a more preferred embodiment because they are thought to be able to exert various physiological actions of these in addition to or synergistically with the action of coenzyme Q10. Here, as physiological functions of sesamin and episesamin, Δ5 desaturase inhibitory action (and anti-inflammatory action, antithrombotic action, blood pressure lowering action, etc. resulting from the action: S. Shimizu et al., J. Am Oil Chem. Soc., 66, 237-241 (1989); S. Shimizu et al., Lipid, 26, 512 (1991); Japanese Patent Laid-Open No. 3-27319), Antioxidant action on lipids (Japanese Patent Laid-Open No. 5-051388) And JP-A-2001-139579), antihypertensive action (JP-A-8-268887), liver function improving action (JP-A-4-099331), active oxygen scavenging action (JP-A-6-227777), blood cholesterol lowering action and / or Or cholesterol lowering action (Japanese Patent No. 3001589 and Japanese Patent Laid-Open No. 4-159221), in vivo stabilization action of polyunsaturated fatty acid (Japanese Patent Laid-Open No. 11-269456), anti-intoxication action (Japanese Patent No. 3124062) And the like.

In addition, as long as the metabolite of sesamin shows the effect of this invention, it is a sesamin analog contained in the sesamin of this invention, and can be used for this invention.
The sesamin used for this invention is not restrict | limited at all by the form, manufacturing method, etc. For example, when sesamin is selected as the sesamin, usually sesamin extracted from sesame oil by a known method (for example, the method described in JP-A-4-9331) (referred to as sesamin extract or purified product) Although it can also be used, commercially available sesame oil (liquid form) can also be used as it is. However, when sesame oil is used, the flavor unique to sesame oil may be evaluated to be sensory unfavorable, so a sesamin extract extracted from tasteless odorless sesame oil (or a sesamin purified product) is used. It is preferable. In addition, when sesame oil is used, since the sesamin content is low, if an attempt is made to add a preferable amount of sesamin, the volume of the selected coenzyme Q10-containing composition becomes too large, which may cause inconvenience in consumption. In particular, when it is formulated for oral administration, the formulation (tablets, capsules, etc.) becomes large and obstructs intake. Therefore, it is preferable to use a sesamin extract (or a sesamin purified product) from sesame oil from the viewpoint that the intake may be small.
(Coenzyme Q10-containing composition)
Regarding the blending amount of sesamin in the composition according to the present invention, the blending weight ratio of sesamin to coenzyme Q10 is preferably 1/10 or more. When blended in the above ratio, the in vivo absorbability of coenzyme Q10 can be improved (Example 3). However, when the blended weight ratio of sesamin to coenzyme Q10 is 1/15 or less, the in vivo absorbability of coenzyme Q10. Can be improved only slightly (Example 4).

  As described above, the composition containing the sesamin of the present invention and coenzyme Q10 not only improves the in vivo absorbability of coenzyme Q10, but also adds various physiological actions of sesamin to the action of coenzyme Q10. If it is considered that the physiological action of sesamin is exerted, there is no upper limit of the blending ratio. However, if sesamin is added for the purpose of improving the in vivo absorbability of coenzyme Q10, the ratio of sesamin to coenzyme Q10 is 1/3 to 1/1, and the in vivo absorbability of coenzyme Q10 is almost constant. (Examples 1-4, FIG. 5), the blending ratio of sesamin to coenzyme Q10 is preferably 1/10 or more, and more preferably 1/3 to 1/1. preferable. In humans who ingested a composition containing 1/3 of sesamin to coenzyme Q10 at a compounding ratio, the in vivo absorbability of coenzyme Q10 was examined. Coenzyme Q10 was better than that of humans who were not ingesting sesamin simultaneously. It has been confirmed that the blood concentration of is increased, that is, the absorbability in the body is improved (Example 7).

  In the present invention, any desired component can be blended in addition to the sesamin and coenzyme Q10 as long as the effect is not impaired. For example, vitamins such as vitamin E and vitamin C, and emulsifiers, tonicity agents (isotonic agents), buffers, solubilizers, preservatives, stabilizers, antioxidants, etc. that are usually added when preparing soft capsule Etc. can be suitably blended.

  The daily dose of coenzyme Q10 used in the present invention varies depending on the health condition of the intake person, but is usually in the range of 1 to 300 mg, preferably 10 to 100 mg. The daily dose of sesamin is usually 1 to 60 mg, preferably 5 to 60 mg.

  In the composition containing coenzyme Q10 and sesamin of the present invention, coenzyme Q10 is usually used at the above-mentioned daily dose, and sesamin can be blended at a weight ratio of 1/10 to 1/1. .

  Since the composition containing coenzyme Q10 and sesamin of the present invention is excellent in in vivo absorbability of coenzyme Q10, the physiological action of coenzyme Q10 (for example, antioxidant action, energy production promoting action, action for enhancing cardiopulmonary function) , Immunostimulatory action, aging preventive action) can be efficiently exhibited, and can be used as a health food having these physiological actions. The health food here is, for example, a preparation or food containing the composition itself containing the coenzyme Q10 of the present invention and sesamin as an active ingredient, such as capsules and tablets, and the composition of the present invention in general foods. Name functional foods (including special health foods and conditional special health foods) that are made by adding food as a component and adding various functions such as antioxidants to living organisms. Can do. Furthermore, foods and the like characterized by having a biological antioxidant effect, which are used to prevent or suppress an oxidation reaction in the living body or a disorder caused thereby, are also included.

The form of the health food containing coenzyme Q10 and sesamin is not particularly limited. For example, it is a solid such as powder, granule or tablet; a solution such as liquid or emulsion; or a paste It can be prepared in any form such as a semi-solid form. For example, in the case of a food containing a composition containing coenzyme Q10 and sesamin and / or episesamin as an active ingredient, since all of these ingredients are fat-soluble, microcapsules By encapsulating in soft capsules or hard capsules, it can be formulated as a nutritional supplement or supplementary nutritional supplement for the purpose of supplementing nutritional components, and coenzyme Q10 can be efficiently ingested.
(Method for preparing coenzyme Q10-containing composition)
The composition containing sesamin and coenzyme Q10 of the present invention is preferably taken after being dissolved in oil. The oil that can be used is not particularly limited as long as it can dissolve sesamin and coenzyme Q10. Specifically, soybean oil, rapeseed oil, safflower oil, olive oil, cottonseed oil, which is a liquid oil at room temperature, Natural animal and vegetable oils such as corn oil, palm oil, rice bran oil, wheat germ oil, sunflower oil, safflower oil, peanut oil, whale oil, sardine oil, squid oil, medium chain length fatty acid triglyceride, monohydric fatty acid having 4 to 22 carbon atoms , Di- and triglycerides or a mixture thereof. Further, a mixture of lard, beef tallow, hydrogenated fish oil, margarine, shortening, etc., which is semi-solid or solid, and liquid oil at normal temperature as described above can also be used.

  Below, the manufacturing method of the composition of this invention containing sesamin and coenzyme Q10 is demonstrated. However, the composition of the present invention is not limited to those produced by these production methods, and may be produced by any production method easily conceived by those skilled in the art.

  First, sesamins are dissolved in fats and oils. At this time, it is preferable to heat the oil and fat, and the temperature is usually 70 to 150 ° C, preferably 100 to 120 ° C. After dissolving the sesamins, coenzyme Q10 is added to this solution. Since coenzyme Q10 is unstable at high temperatures, when the oil is heated to 70 ° C or higher, it is preferable to add coenzyme Q10 after cooling to 40 to 60 ° C, preferably about 50 ° C. In addition, you may add the process of adding beeswax, glycerin fatty acid ester, vitamin E, etc. which are emulsifiers in an arbitrary stage, and making it a suspension form as needed.

  In addition, since coenzyme Q10 is susceptible to photodegradation, for example, a composition containing coenzyme Q10 is encapsulated in a capsule prepared using a capsule material mixed with caramel dye as a coloring dye, and the content liquid is exposed to light. It is preferable to prevent alteration of coenzyme Q10.

EXAMPLES Hereinafter, although this invention is demonstrated based on an Example, these Examples are not for limiting this invention. The coenzyme Q10 used in the examples was coenzyme Q10 manufactured by Nisshin Pharma Co., Ltd.
[Example 1] Evaluation of absorbability of coenzyme Q10 in rats (1)
As the sesamin, sesamin (manufactured by Takemoto Oil and Fats, sesamin: episesamin = 56: 44) was used. SD male rats (8 weeks old) were divided into a control (olive oil) group, a coenzyme Q10 group, and a coenzyme Q10 + sesamin group (4 mice in each group). As shown in Table 1 below, a composition was prepared by dissolving each component in olive oil, and blood was collected at 0, 2, 4, 6 and 7 hours after a single administration to obtain a plasma coenzyme. The change with time of the Q10 concentration was measured.

[Example 2] Evaluation of coenzyme Q10 absorbency in rats (2)
A time course change of plasma coenzyme Q10 concentration was measured in the same manner as in Example 1 except that a composition containing coenzyme Q10 and sesamin was prepared to have the formulation shown in Table 2 below. The blood collection times were 0, 2, 4, 6, 8, 10, 24 hours. As a comparative example, a similar experiment was conducted for a composition containing vitamin E, which is known as an antioxidant, instead of sesamin.

[Example 3] Evaluation of absorbability of coenzyme Q10 in rats (3)
Coenzyme Q10-containing composition and coenzyme Q10 and sesamin-containing composition were prepared in the same manner as in Example 2 except that the composition shown in Table 3 was prepared. did.

[Example 4] Evaluation of absorbability of coenzyme Q10 in rats (4)
From the results of Examples 1 to 3, Tmax (time for showing the maximum blood concentration) when coenzyme Q10 was orally administered once was 6 hours, and in particular, sesamin increased the blood concentration at 6 hours. The effect of sesamin on the blood concentration of coenzyme Q10 was evaluated using the blood concentration at 6 hours as an index. A composition containing coenzyme Q10 and sesamin was prepared to have the composition shown in Table 4 below, and the blood coenzyme Q10 concentration at 6 hours after single oral administration was measured.

  The results of Examples 1 to 4 are shown in FIGS. As is apparent from the figure, under the conditions of Examples 1 to 3, a significant amount of coenzyme Q10 was observed in the coenzyme Q10 + sesamin (dissolved in olive oil) group combined with sesamin compared to the group in which coenzyme Q10 was dissolved in olive oil. An increase was observed. Further, from FIG. 2, vitamin E, which is known as an antioxidant, cannot improve the in vivo absorption of coenzyme Q10, suggesting that sesamin specifically improves the in vivo absorption of coenzyme Q10. Therefore, it has been clarified that when the coenzyme Q10-containing material (composition) of the present invention is used, extremely high coenzyme Q10 absorbability can be realized without going through a complicated process.

Also, from the results of FIGS. 1 to 4, the increase ratio of the plasma concentration (absorption amount) of coenzyme Q10 (absorption amount of the composition of the present invention / absorption amount of coenzyme Q10 alone) by the sesamin combination was determined, Plotted against the blending ratio of coenzyme Q10 and sesamin in the composition (FIG. 5). From FIG. 5, it was suggested that sesamin can increase the amount of coenzyme Q10 absorbed in the body by adding 1/10 or more of the coenzyme Q10.
[Example 5]
A composition containing coenzyme Q10 and sesamin was prepared with the formulation shown in Table 5 below. These compositions were subjected to sensory evaluation by the following 10 ranks (A, B, C) for the odor of sesame oil, aftertaste and difficulty in drinking. Moreover, sensory evaluation was implemented about which coenzyme Q10 containing composition is relatively preferable. The amount of coenzyme Q10 was adjusted to 30 mg, and the sesamin content was adjusted to 10 mg (sesamin content in sesame oil was about 0.5%).

  The results of the test (sensory evaluation) are shown in Table 6 and Table 7.

* 1st place: 5 points, 2nd place: 3 points, 3rd place: 1 point converted results As is clear from the results in Tables 6 and 7 above, the flavor unique to sesame oil was evaluated to be sensuously unfavorable. In the practice of the present invention, it is preferable to use an extract (purified) from sesame oil that is tasteless and odorless. Moreover, when mix | blending the composition of this invention with other food-drinks, it is more convenient that it is tasteless and odorless so that the original taste and fragrance of the food-drinks may not be impaired.

In addition, as shown in Table 7, when sesame oil is used, the sesamin content is as low as about 0.5%, so if you want to ingest a certain sesamin, you must ingest 8 capsules of 250 mg / capsule. On the other hand, in the case of sesame oil extract (purified product), it is preferable to use the sesame oil extract (purified product) from the viewpoint that it becomes two grains and only a small amount may be consumed.
[Example 6]
With the formulation shown in Table 8 below, the liquid contents of Formulation Examples 1, 2, and 3 were produced by the following method. All the raw materials were mixed and homogenized to obtain a coenzyme Q10-containing material. Next, gelatin, glycerin, and caramel were added, swollen, and soft capsules were produced by a punching method using the dissolved gelatin sheet.

[Example 7]
Using the soft capsule prepared according to Example 6, the blood concentration in humans was measured. The subjects were 11 healthy men and women (6 men, 5 women), divided into two groups, A and B. Group A (n = 5) was ingested with CoQ10 + sesamin E, Group B (n = 6) Was taken as a group taking only CoQ10. The drinking period of the test sample was 1 week, blood was collected before and after that, and the amount of CoQ10 in the blood was measured. As a result, as shown in Table 9, it was clarified that the amount of blood change in group A was higher than that in group B.

  As described above, according to the present invention, the in vivo absorbability of coenzyme Q10 is increased by mixing sesamin and coenzyme Q10 without going through a complicated process. Improvement of biological functions such as a preventive action can be achieved efficiently, and in addition, the effect of sesamin can be achieved.

It is a graph which shows the amount of coenzyme Q10 in the plasma by the compounding ratio CoQ10: sesamin = 1: 1. It is a graph which shows the amount of coenzyme Q10 in the plasma by the compounding ratio CoQ10: sesamin = 3: 1. It is a graph which shows the amount of coenzyme Q10 in the plasma by the compounding ratio CoQ10: sesamin = 10: 1. It is a graph which shows the amount of coenzyme Q10 in the plasma 6 hours after administration by mixing ratio CoQ10: sesamin = 15: 1. It is a graph which shows the influence of the compounding ratio of CoQ10 and sesamin on the increase rate of the amount of coenzyme Q10 in plasma.

Claims (4)

A composition comprising a sesamin concentrate and coenzyme Q10, wherein the sesamin concentrate is a sesamin concentrate containing 1% or more of sesamin and / or episesamin, and contains sesamin and / or episesamin for coenzyme Q10 The composition having a weight ratio of 1/3 to 1/1. The composition according to claim 1, wherein the sesamin concentrate contains 20% or more of sesamin and / or episesamin . A food or drink containing the composition according to claim 1 or 2. A method for increasing the in vivo absorbability of coenzyme Q10, comprising combining coenzyme Q10 with sesamin and / or episesamin in a weight ratio of 1/3 to 1/1 with respect to coenzyme Q10 .

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