JP2009114106A - Anti-osteoporosis agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an anti-osteoporosis agent containing sesamin, having high safety and an excellent anti-osteoporosis effect, since as an important issue in an aging society of recent years, the outgrowth of osteoporosis by which bone density is decreased and the bone becomes weak, is cited, and the osteoporosis accompanies symptoms such as the warpage of the bone, pain, bone fracture, etc., an effective method for treating the same is called for. <P>SOLUTION: This anti-osteoporosis agent is characterized by containing sesamins, vitamin E and/or coenzyme Q10. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to an anti-osteoporosis agent.

An important problem of the aging society in recent years is the occurrence of osteoporosis in which bone density decreases and bones become brittle. Osteoporosis is accompanied by symptoms such as bone curvature, pain, and fracture, and an effective treatment method is required.
As therapeutic agents for osteoporosis, active vitamin D ₃ , female hormone (estrogen), calcitonin, ipriflavone, bisphosphonate, vitamin K and the like can be mentioned, but a great effect cannot be expected. It is important to prevent osteoporosis by paying attention to proper exercise and foods taken daily. Concerning the above foods, intake of dairy products and fish containing a large amount of calcium is recommended. Furthermore, the use of health foods including calcium, magnesium, vitamin D, casein phosphopeptide (which is said to have an action of promoting calcium absorption from the intestinal tract) and the like is also recommended.
Patent Document 1 listed below proposes an anti-osteoporosis agent containing vitamin K and soy soflavone as active ingredients, having a vitamin K concentration in a dry weight of 100 ppm or more and a soy isoflavone concentration of 5000 ppm or more. .

On the other hand, sesamin is one of the main lignan compounds contained in sesame and is contained in sesame in an amount of about 0.5 to 1%. Sesamin is known to have many physiological activities, for example, an antioxidant action, an antihypertensive action, an anti-inflammatory action and the like are known.
Sesamin is also known to affect bone formation (Patent Document 2).
Japanese Patent No. 3250071 JP 2003-522787 A

  An object of the present invention is to provide an anti-osteoporosis agent that contains sesamin, has high safety, and has an excellent anti-osteoporosis action.

  The present inventors have found that a composition obtained by adding vitamin E and / or coenzyme Q10 to sesamin provides a significantly superior anti-osteoporosis effect as compared with the case of using only sesamin. It came to be completed.

The invention according to claim 1 is an anti-osteoporosis agent characterized by containing sesamin and vitamin E.
The invention according to claim 2 is an anti-osteoporosis agent characterized by containing sesamin and coenzyme Q10.
Invention of Claim 3 contains sesamin, vitamin E, and coenzyme Q10, It is an anti-osteoporosis agent characterized by the above-mentioned.

  According to the present invention, since vitamin E and / or coenzyme Q10 are blended with sesamin, the anti-osteoporosis action that sesamin originally has can be dramatically increased.

(Sesamin)
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. Of these, sesamin and episesamin are preferable.

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) Can be used.

(Coenzyme Q10)
Coenzyme Q10 is a commercially available compound known as coenzyme Q10, vitamin Q, ubiquinone and ubidecalenone. In addition, coenzyme Q10 is preferable because a reduced type is excellent in anti-osteoporosis action. The method for obtaining reduced coenzyme Q10 is not particularly limited. For example, after obtaining coenzyme Q10 by a conventionally known method such as synthesis, fermentation, extraction from natural products, etc., reduced coenzyme in the effluent is obtained by chromatography. A method of concentrating the Q10 section can be adopted. In this case, a general reducing agent such as sodium borohydride or sodium dithionite (hydrosulfite sodium) is added to the coenzyme Q10 as necessary, and the coenzyme Q10 is added to the coenzyme Q10 by a conventional method. The oxidized coenzyme Q10 contained may be reduced to form reduced coenzyme Q10, followed by concentration by chromatography. It can also be obtained by a method in which the above reducing agent is allowed to act on existing high-purity coenzyme Q10.

(Vitamin E)
Vitamin E as used in the present invention includes derivatives, and examples thereof include α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, α-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol, tocopherol acetate, tocopherol nicotinate and the like can be mentioned.

  In the anti-osteoporosis agent of the present invention, when sesamin is set to 1 (mass basis), vitamin E is preferably blended at a ratio of 0.1 to 10 and coenzyme Q10 at a ratio of 0.1 to 10.

  The daily intake of sesamin is usually 1-60 mg, preferably 5-60 mg, and the daily intake of coenzyme Q10 is usually in the range of 1-300 mg, preferably 10-100 mg, vitamin E. Since the daily intake of is usually 10 mg to 800 mg, it is desirable that the human intake of the anti-osteoporosis agent of the present invention falls within this range.

  Any desired component can be blended with the anti-osteoporosis agent of the present invention as long as the effect is not impaired. For example, emulsifiers, tonicity agents (isotonizing agents), buffers, solubilizers, preservatives, stabilizers, antioxidants, etc. that are usually added when preparing vitamins such as vitamin C and soft capsules Can be blended.

  The form of the anti-osteoporosis agent of the present invention is not particularly limited, but it is preferably encapsulated in a microcapsule, soft capsule or hard capsule by a known method.

  EXAMPLES Hereinafter, although an Example demonstrates this invention further, this invention is not limited to the following example. Coenzyme Q10 used in Examples 1 to 3 is Coenzyme Q10 manufactured by Nisshin Pharma Co., Ltd., and vitamin E is α-tocopherol.

Example 1
As the sesamin, sesamin (manufactured by Takemoto Oil and Fats, sesamin: episesamin = 56: 44) was used.
Sesamin and vitamin E were dissolved in olive oil and used as a test sample of this example.

In order to examine the anti-osteoporosis effect on the test sample, the following animal experiments were conducted.
Osteoporosis Improvement Effect Test SD rat (22 weeks old) female ovaries were surgically removed to create osteoporosis model rats. The ovariectomized rats were divided into 6 groups of 7 animals, and every other day (total 17 times) during the 35-day test period, the test samples were fed with 1 mg / kg of sesamin and 5 mg / kg of vitamin E. Orally administered to give kg. The feed was the solid feed CRF-1 for mice, rats and hamsters from Oriental Yeast Co., Ltd. There was no difference in food intake between groups during the study period. On the 35th day after the start of the test, the weight of the rat was measured, and then the femur was removed. The femur was used for analysis with the adhesive tissue and muscle removed. After measuring the volume of the femur, it was washed three times with ethanol, then washed three times with acetone, dried overnight, and then weighed to determine the dry weight of the femur. From the volume and dry weight, the bone density (dry weight g / volume mm ³ ) was measured. As a control experiment, Table 1 shows the results together with an example (comparative example) in which the above experiment was repeated except that olive oil not containing the test sample was administered to rats.

  When Example 1 was compared with the comparative example, a significant difference was found in Example 1 with a risk factor of p <0.05.

Example 2
In Example 1, Example 1 was repeated except that the intake amount of sesamin was 0.5 mg / kg. As a result, the bone density of Example 2 was 1.076 ± 0.004 mg / mm ³ .

Comparative Example 1
In Example 1, Example 1 was repeated except that vitamin E was not used. As a result, the bone density was 1.011 ± 0.007 mg / mm ³ .

Example 3
In Example 1, Example 1 was repeated except that Coenzyme Q10 was used instead of Vitamin E. The dose of coenzyme Q10 is also the same as in Example 1 (5 mg / kg). As a result, the bone density was 1.085 ± 0.004 mg / mm ³ .

Example 4
In Example 1, Example 1 was repeated except that Coenzyme Q10 was used in addition to sesamin and vitamin E. The dose of coenzyme Q10 is also the same as in Example 1 (5 mg / kg). As a result, the bone density was 1.091 ± 0.007 mg / mm ³ .

Example 5
Sesamin 0.25g
Tocopherol acetate 0.25g
Coenzyme Q10 0.1g
Silica anhydride 20.5g
Corn starch 79g
Were mixed uniformly. To this compound, 100 ml of a 10% hydroxypropylcellulose / ethanol solution was added, kneaded as usual, extruded, and dried to obtain granules.

Example 6
Sesamin 3.5g
Tocopherol acetate 0.5g
Coenzyme Q10 0.5g
Silica anhydride 20g
10g microcrystalline cellulose
Magnesium stearate 3g
Lactose 60g
Were mixed, and tableted with a single tableting machine to produce tablets with a diameter of 7 mm and a weight of 100 mg.

Example 7
Gelatin 70.0%
Glycerin 22.9%
Methyl paraoxybenzoate 0.15%
Propyl paraoxybenzoate 0.51%
Water meter 100%
The composition shown below was filled in the soft capsule skin made of the above components by a conventional method to obtain 200 mg of soft capsules.
Sesamin / episesamin (1: 1) mixture 10.8%
α-tocopherol 20%
Coenzyme Q10 5%
Wheat bead wax 30%
Palm oil 10%
Wheat germ oil 100% as appropriate

  The anti-osteoporosis agent of the present invention is useful as a pharmaceutical, food, feed or pet food.

Claims (3)

  An anti-osteoporosis agent characterized by containing sesamin and vitamin E.   An anti-osteoporosis agent comprising sesamin and coenzyme Q10.   An anti-osteoporosis agent comprising sesamin, vitamin E, and coenzyme Q10.