JP2018168122A - Coenzyme q10-containing preparation - Google Patents

Abstract

To provide a coenzyme Q10-containing composition in which stability of coenzyme Q10 is improved even in the coexistence with vitamin E.SOLUTION: A coenzyme Q10-containing composition contains coenzyme Q10, vitamin E and a surfactant with an HLB of 4 or less.SELECTED DRAWING: None

Description

  The present invention relates to a coenzyme Q10-containing composition having improved stability of coenzyme Q10 in the presence of vitamin E.

  Coenzyme Q10 (coenzyme Q10) is a vitamin-like fat-soluble substance that exists in mitochondria throughout the body. Since coenzyme Q10 functions as a coenzyme in electron transfer in oxidative phosphorylation, it is involved in systemic energy production and has an antioxidant function, thus protecting cells from oxidative stress. Coenzyme Q10 is widely used not only as a therapeutic agent for cardiovascular diseases such as congestive heart failure but also as a supplement or food. However, coenzyme Q10 is a fat-soluble substance having a low melting point, and has a problem that it is unstable and decomposes by heat or the like to generate ubichromenol.

  Vitamin E is a kind of fat-soluble vitamin, which exists widely in nature and functions as an antioxidant throughout the body. Vitamin E is contained in general foods, but is also widely used as a supplement or food.

  It has been reported so far that various antioxidant components function in vivo, but in recent years, these antioxidant components are not functioning individually but functioning while being involved with each other. It has become clear. That is, when a certain antioxidant component exhibits an antioxidant function, the antioxidant component itself is oxidized, which may adversely affect the living body. In such a case, another type of antioxidant component can regenerate its original antioxidant component to regenerate the antioxidant function. From such a viewpoint, a combination of a plurality of antioxidant components has also been provided as a supplement or food.

   Patent Document 1 describes an antioxidant supplement containing a plurality of antioxidant components such as vitamin E, vitamin C, coenzyme Q10, and α-lipoic acid. Patent Document 2 describes a pharmaceutical containing a plurality of antioxidant components such as coenzyme Q10, cysteine, and vitamins. However, as a result of studies by the present inventor, it has been clarified that coenzyme Q10 is rapidly decomposed even in a solid state and coenzyme Q10 content is reduced when coenzyme Q10 and vitamin E coexist. It was. On the other hand, it has been conventionally known that coenzyme Q10 is easily decomposed by heat and light. Patent Document 3 discloses that HLB containing coenzyme Q10, monoglycerin fatty acid organic acid ester and polyglycerin condensed ricinoleate is 8 or more. And a hydrophilic polyhydric alcohol fatty acid ester. Patent Document 4 describes a composition in which various surfactants of HLB4.5 to 11 are combined with coenzyme Q10 using a supercritical fluid. However, when coenzyme Q10 and vitamin E coexist, there has not yet been a means for solving the problem that coenzyme Q10 is easily decomposed.

JP 2015-218140 A JP 2011-236191 A Japanese Patent No. 4444586 Japanese Patent No. 4997449

  An object of the present invention is to provide a coenzyme Q10-containing composition in which the stability of coenzyme Q10 is improved even in the presence of vitamin E.

The above problems can be solved by the following composition.
1. A coenzyme Q10-containing composition comprising coenzyme Q10, vitamin E, and HLB 4 or less surfactant.
2. The coenzyme Q10-containing composition according to 1 above, wherein the surfactant having an HLB of 4 or less is at least one selected from lecithin, glycerin fatty acid ester, polyglycerin fatty acid ester or sucrose fatty acid ester.
3. 3. The coenzyme Q10-containing composition according to 1 or 2 above, which is in the form of a solid agent.
4). Coenzyme Q10 containing composition of said 1-3 which is a powder form.
5. Coenzyme Q10 containing composition of said 1-4 whose content of surfactant is 5-40 mass% in 100 mass% of compositions.

  Since the coenzyme Q10-containing composition of the present invention has coenzyme Q10 and vitamin E coexisting in two coexisting components, the stability of coenzyme Q10 is enhanced. As described above, it can be stored for a long period of time, and by taking it as necessary, it is possible to easily and continuously take a plurality of antioxidant components, coenzyme Q10 and vitamin E.

  The coenzyme Q10-containing preparation of the present invention contains coenzyme Q10, vitamin E, and a surfactant. These are preferably used in the form of solid preparations such as tablets, capsules, granules, and powders, but are preferably used in the form of powders (fine particles) in consideration of absorbability and handleability. The shape of the fine particles may be, for example, a spherical shape, a deformed spherical shape such as football, a rod shape such as a cylinder, a rectangular column shape such as a square column, a spherical shape having a convex portion such as confetti, and the average particle size is 0. The thickness is about 1 μm to 1 mm, preferably about 1 μm to 0.1 mm. In the present specification, the average particle diameter means a volume average diameter (MV) of a particle size distribution calculated by a laser diffraction / scattering method.

  Coenzyme Q10 and vitamin E used in the present invention are preferably in the form of a water-soluble solid because they are excellent in absorbability to the living body after ingestion. Such water-soluble solubilized coenzyme Q10 (hereinafter sometimes referred to as water-soluble coenzyme Q10) and vitamin E (hereinafter sometimes referred to as water-solubilized vitamin E) may float or form a lump in an aqueous medium. In contrast, coenzyme Q10 and vitamin E that can be emulsified, dispersed, or suspended in an aqueous medium are included, and the form is not particularly limited. Examples of the aqueous medium include, but are not limited to, water and a mixture of water and a lower alcohol such as ethanol.

  The production method of water-soluble coenzyme Q10 is not particularly limited, and a known method can be performed. Specifically, examples of the following patent documents can be preferably exemplified. Water-soluble vitamin E can also be produced by a method according to water-soluble coenzyme Q10 by using vitamin E instead of coenzyme Q10 in the above method.

Composition described in Japanese Patent No. 3549197 One selected from the group consisting of gum arabic, agar, water-soluble corn fiber, starch, gelatin, xanthan gum, casein, dextrin, carmellose sodium, polyvinylpyrrolidone in the presence of an organic acid Coenzyme Q10 dispersed and emulsified in the above water-soluble substance.

Coenzyme Q10 described in Japanese Patent No. 4842824 is dispersed and emulsified in an aqueous liquid containing a water-soluble substance composed of octenyl succinic acid starch and dextrin and glycerin, so that Coenzyme Q10 is 1 to 50% by mass, glycerin is 0.01 to A coenzyme Q10-containing liquid composition containing 10% by mass, 4-30% by mass of a water-soluble substance and 40-94% by mass of water, and dried.

  The compounding quantity of coenzyme Q10 in the coenzyme Q10-containing preparation of the present invention is 2 to 40% by mass, preferably 4 to 30% by mass, in 100% by mass of the preparation. If it is less than 2% by mass, it is difficult to obtain a health function, and if it exceeds 40% by mass, decomposition tends to occur. Moreover, the compounding quantity of the vitamin E in the coenzyme Q10 containing formulation of this invention is 1-40 mass% in a formulation 100 mass%, Preferably it is 2-30 mass%. If it is less than 1% by mass, it is difficult to obtain a health function.

  The compounding ratio of coenzyme Q10 and vitamin E in the coenzyme Q10-containing preparation of the present invention is 10: 1 to 1: 5, preferably 8: 1 to 1: 2, as a mass ratio of coenzyme Q10 and vitamin E.

  In the coenzyme Q10-containing preparation of the present invention, a surfactant having an HLB of 4 or less is blended in order to enhance the stability of coenzyme Q10 in the presence of vitamin E. Here, HLB is an index indicating the hydrophobicity and hydrophilicity of the surfactant, and the smaller the value, the more hydrophobic it is. When HLB exceeds 4, Coenzyme Q10 is easily decomposed.

  The blending amount of the surfactant in the coenzyme Q10-containing preparation of the present invention is 5 to 40% by mass, preferably 8 to 30% by mass, in 100% by mass of the preparation. If it is less than 5% by mass, the degradation of coenzyme Q10 tends to occur, and if it exceeds 40% by mass, the blending amount of coenzyme Q10 and vitamin E is relatively reduced, and it becomes difficult to obtain a health function.

  The surfactant having a HLB of 4 or less used in the coenzyme Q10-containing preparation of the present invention is a highly hydrophobic surfactant, and one or more selected from lecithin, glycerin fatty acid ester, polyglycerin fatty acid ester or sucrose fatty acid ester Is preferably used. In the case of these fatty acid esters, the properties such as HLB generally change depending on the type of fatty acid to be bonded, the position to be bonded, and the number of fatty acids to be bonded. However, various surfactants with known HLB are commercially available. It can be selected and used from now on. Moreover, since the said surfactant is surfactant with high safety | security which can be used as a food additive, it is advantageous for the formulation of this invention.

  A surfactant having an HLB of 4 or less used in the coenzyme Q10-containing preparation of the present invention is preferably used in a solid form because the stability of coenzyme Q10 is increased. In addition, even if it is surfactant of a liquid form, it can also be made into a solid form by drying with a suitable excipient | filler, When using surfactant of the solid form obtained in that way, The advantageous effects described above can be obtained.

  The method for preparing the coenzyme Q10-containing composition of the present invention is not particularly limited. For example, the coenzyme Q10, vitamin E, and surfactant can be mixed to prepare a powdery composition. When the mixing step is performed at a temperature not exceeding the melting point of Coenzyme Q10, preferably at a product temperature of 50 ° C. or lower, more preferably 40 ° C. or lower, the stability of Coenzyme Q10 can be further improved.

  When preparing a powdery composition, auxiliary agents such as excipients and fluidizing agents can be mixed in order to improve fluidity and uniformity. For example, starches, saccharides, dextrin, cellulose, silicon dioxide, sugar alcohol and the like can be mentioned. These auxiliaries may be used alone or in combination of two or more. When the coenzyme Q10-containing composition of the present invention is made into a tablet form, it can be produced by tableting the powdery composition obtained as described above according to a conventional method. In this case, a known lubricant, antistatic agent, or the like can be blended as the auxiliary agent.

  When the coenzyme Q10-containing composition of the present invention is in the form of a capsule, the powdery composition obtained as described above can be filled into a capsule according to a conventional method. The base material of the capsule is not limited to a specific one, and it is preferable to use commonly used alkali-treated gelatin or acid-treated gelatin, but using a plant raw material film such as pullulan or carrageenan. There is no problem.

  The coenzyme Q10-containing composition of the present invention may be in the form of foods, cosmetics and feeds containing it. The food of the present invention includes health foods and functional foods. Specifically, there is no limitation as long as the solid form of coenzyme Q10, vitamin E and a surfactant can be blended, and the food of the present invention includes bread, confectionery, noodles such as udon, cookies, chocolate, candy, Examples include sweets such as rice crackers, spreads such as sprinkles and butter. The cosmetics of the present invention include soaps, facial cleansers, toothpastes, jelly-like cosmetics, cream-like cosmetics and the like. Examples of the feed of the present invention include powders, granules, and pellets.

  The daily intake of coenzyme Q10 in the coenzyme Q10-containing composition of the present invention varies depending on age, body weight and health condition, but is usually about 5 to 300 mg, preferably about 10 to 100 mg for adults. The daily intake of vitamin E varies depending on the age, weight and health, but is usually 0.5 to 10 mg, preferably about 1 to 7 mg for adults.

  As long as the effects of the present invention are not lost, the coenzyme Q10-containing composition of the present invention further contains fat-soluble vitamins, water-soluble vitamins, minerals, dietary fiber, other nutrients, other functional ingredients, pigments, and fragrances , Seasonings and other food ingredients may be added and blended.

  EXAMPLES Next, although an Example is shown and this invention is demonstrated further in detail, this invention is not limited to a following example.

(Examples 1-7 and Comparative Examples 1-9)
Coenzyme Q10 powder, vitamin E powder (containing 50% vitamin E), additives listed in Table 2, crystalline cellulose, reduced maltose and lubricant ("calcium stearate") in the amounts shown in Table 1 as the amount per grain And mixed for 5 minutes. This mixture was put into a rotary tableting machine and tableted with a tableting pressure of 2000 N to produce tablets with a diameter of 10 mm and 450 mg per tablet. Separately, a tablet of Reference Example 1 was produced in which the surfactant was not added and replaced with reduced maltose.

(Test Example 1)
The tablets of each example were packaged in aluminum pouch bags after production and stored at 60 ° C. for 1 week. Thereafter, the tablets were taken out, pulverized, and the amount of coenzyme Q10 contained was measured by high performance liquid chromatography. Table 2 shows the remaining amount of coenzyme Q10. Moreover, the improvement rate of stability with respect to Reference Example 1 was calculated by the following formula. The results are shown in Table 2.
Stability improvement rate = ((residual rate of example / residual rate of reference example) -1) × 100

(Example 8 and Comparative Example 10)
Water-soluble coenzyme Q10 powder (containing 40% coenzyme Q10), vitamin E powder (containing 50% vitamin E), additives listed in Table 4, crystalline cellulose, reduced maltose and lubricant ("calcium stearate") per grain Was added to the mixer in the amount shown in Table 3 and mixed for 5 minutes. This mixture was put into a rotary tableting machine and tableted with a tableting pressure of 2000 N to produce tablets with a diameter of 10 mm and 450 mg per tablet. Separately, a tablet of Reference Example 2 in which the reduced malt sugar was replaced without adding a surfactant was produced. These tablets were evaluated in the same manner as in Test Example 1. The results are shown in Table 4.

  From the above results, even when coenzyme Q10 and vitamin E coexist, when coenzyme Q10 and vitamin E that do not contain any additives are coexisting when a surfactant of HLB4 or lower is contained. In comparison, it was found that the stability improved by 20% or more. In order to achieve stability improvement of 20% when coenzyme Q10 and vitamin E coexist, it was necessary to package in a vacuum so far, so that a surfactant of HLB4 or less should be included. As a result, it was surprising that the stability of the normal packaging can be improved to be equal to or higher than that of the vacuum packaging without using the vacuum packaging.

Claims (5)

  A coenzyme Q10-containing composition comprising coenzyme Q10, vitamin E, and HLB 4 or less surfactant.   The coenzyme Q10-containing composition according to claim 1, wherein the surfactant having an HLB of 4 or less is at least one selected from lecithin, glycerin fatty acid ester, polyglycerin fatty acid ester or sucrose fatty acid ester.   The coenzyme Q10-containing composition according to claim 1 or 2, which is in the form of a solid agent.   The coenzyme Q10-containing composition according to any one of claims 1 to 3, which is in the form of a powder.   Coenzyme Q10 containing composition of any one of Claims 1-4 whose content of surfactant is 5-40 mass% in 100 mass% of compositions.