SE512781C2 - Oil preparations with high activity antioxidants, and process for their preparation - Google Patents

Abstract

An oily preparation and its production method where the activity of antioxidant substances as effective components are high and the penetrating ability into the inside of the cell in 8 disease portion is high, and its production method. The oily preparation is prepared by heating a cereal raw material comprising rice germ and/or wheat germ and soybean at a temperature not exceeding 100(C; making it fine powder after koji is added to the heated material to brew it; and adding thus brewed powder to an oil mixture comprising an oil obtained from sesame heated in the same manner and an oil obtained from raw sesame, wherein a ratio of oil mixture to a total amount of the fine powder and the oil mixture is 60 to 95 % by weight. This oily preparation can be used to prevent and treat various inflammations and inveterate diseases resulting from or worsened by destruction of cellular organization by reactive oxygen and lipid peroxide produced in a human body.

Description

15 20 25 30 35 512781 2 The botanical nutrient of heading 1 366 268 is obtained by mixing fresh tea powder, heat-treated powder, unpolished rice and soybean powder; adding a small amount of koji mushrooms to the mixture; then immersing this powder mixture in a mixture of sesame oil and soybean oil for about 4 days to extract effective components; removal of precipitates by centrifugation: and encapsulation of residual oils in a capsule made of gelatin or the like.

The antioxidant composition of heading 63-79834 is obtained by gentle heating of plant seeds or seeds thereof so as not to burn upon it; then fermenting these heated plant materials by adding a microorganism; and adding a vegetable oil obtained from a plant which is also mildly heated. Vitamin C, vitamin C derivatives or a plant body containing these may be added to the composition.

As plant seeds, a seed containing antioxidants is used, such as the above-mentioned flavonoids, polyphenols, tannic acids, tocopherols, B vitamins and the like, including hatomugi (pearl barley) and peas. As vegetable oil, sesame oil, evening primrose rice, wheat, barley, soybeans, adzuki beans, corn, soybean oil, cottonseed oil, corn oil, safflower oil, light oil, rice oil, rapeseed oil, olive oil and the like are used. in No. 1 366 268, however, has low antioxidant activity due to the treatment The botanical nutrient process for the raw plant material. No. 63-79834 eliminated such a problem by remarkably increasing the Antioxidant composition of Niwa, the activity of the antioxidants by gently heating the crude plant material with infrared radiation in the long wave. Thus, deactivation of the antioxidants due to high temperature range was prevented from burning. at that. lucky. In this way, the raw material was released and converted into efficient components with low molecular weight. The heat-treated material thus fermented to promote further release and conversion to the low molecular weight effective substances. However, according to the study conducted by the present inventors since then, it has been clarified that although the above-mentioned antioxidants markedly suppress the production of the reactive oxygen and lipid peroxide in test tubes, the antioxidant activities do not prove to be sufficient. in the human body.

It is considered necessary for the antioxidants to pass through the cell membranes, which cover the surface of the cells, to allow the antioxidants to enter the inside of cells suffering from a disease, such as an inflammatory reaction or the like, on due to reactive oxygen and lipid peroxide. However, the human cell membrane is rich in oil and fat components and thus has such a property that only oil substances are allowed to pass through. Thus, the above-mentioned low oil content antioxidant composition has little opportunity to pass through the cell membrane to penetrate the inside of the cell.

Thus, the present inventors have repeated the studies to improve the ability of the antioxidant composition to pass through the cell membrane, while making further improvements in the choice of plant species, as a raw material, and its production process. As a consequence, an oil preparation has been obtained in which the activity of the antioxidants, as effective components, is high and the permeability to the inside of the cell, which suffers from a disease, is high, this constituting the present invention.

DESCRIPTION OF THE PRESENT INVENTION An object of the present invention is to provide an oil preparation and its manufacturing process, in which preparation the activity of antioxidants, as effective components, is high and the permeability to the inside of the cell at a disease site is high.

The manufacturing process of the oil composition of the present invention comprises: heating rice sprouts and / or wheat sprouts and soybeans at a temperature not exceeding 100 ° C; supply of koji to the heated material; fermentation of the mixture; then pulverizing the mixture; and feeding the resulting powdered mixture to an oil mixture comprising one obtained from sesame, oil heated at a temperature not exceeding 100 ° C, and an oil obtained from crude sesame, wherein a ratio between the oil mixture and a total amount of the powder mixture and the oil mixture is 60-95% by weight.

As a starting material, which contains abundant antioxidants, in addition to rice sprouts, wheat sprouts and soybeans, one can list plant species described in Japanese Laid-Open, Unexamined Patent Application No. 63-79834, i.e. barley, adzuki bean, corn, hatomugi (pearl barley), peas and the like. According to the study of the present inventors, rice sprouts, wheat sprouts and soybeans are the most preferred starting materials.

Next to rice sprouts, wheat sprouts and soybeans, you can list rice bran, hatomugi (pearl barley) and wheat. Therefore, as a starting material, at least one of rice bran, hatomugi (pearl barley) and wheat may be included together with rice sprouts. In any case, the relationship between the sprouts (rice sprouts and / or wheat sprouts) and / or wheat sprouts. in the seed starting material, preferably at least more than or equal to 1% by weight.

The antioxidants in the seed starting material, as described above, form a complex macromolecular polymer together with other substances and therefore have no activity as such. Thus, it is necessary to cut off the macromolecular bonds by gentle heating or the like to release the low molecular weight antioxidants. However, if the heating temperature is too high, the low molecular weight antioxidants are deactivated, so it is necessary to choose a heating condition with this fact in mind.

In order to satisfy such conditions, it is necessary to heat the semen starting material at a temperature not exceeding 100 ° C, slowly and for a sufficiently long time. a vessel made of ceramic. In detail, the seed starting material is inserted as clay or the like, which is preferably with wavelengths of 4-14 μm, and heating is performed emitting infrared rays in the long-wave region, with slow stirring and maintaining the temperature at about 90- 96 ° C.

The heating time varies depending on the cereals, so it can not be arbitrarily defined. However, it is preferably about 30 minutes to 3 hours. Otherwise, the heating process is not limited to the above-mentioned method, provided that the antioxidants in the semen starting material are released sufficiently as low molecular weight substances, while deactivation thereof is prevented.

After the heat treatment, as described above, koji (Aspergillus orizae) is added to the starting material to ferment it. The fermentation condition is preferably 20-36 ° C for 2-6 days. When fermentation is performed using a fermenter, about 2-3 hours is sufficient. This fermentation is carried out to further promote the release and conversion of the antioxidants in the seed starting material into low molecular weight substances, and through this fermentation step the activity of the antioxidants is remarkably increased compared to a starting material which has only been subjected to heat treatment.

The fermented material is then ground to a fine powder. Painting can be performed using a commercially available grinder. However, some types of grinders generate high temperatures during use, which deactivate the antioxidants. Therefore, it is preferred to use those mills which do not generate high temperatures during use. A stone mill can be used, for example.

Thereafter, the oil is prepared by mixing an oil obtained from heated sesame (hereinafter referred to as sesame paste oil) with an oil obtained from crude sesame, in a suitable ratio, and the above-mentioned fine powder is added to the oil mixture. The sesame paste oil is an oil obtained by grinding and pressing raw sesame, which is slowly heated at a temperature not exceeding 100 ° C, for a sufficiently long time, the fine, solid content, remains as it is, so that the appearance constitutes a paste- formed by painting sesame, however, stand. This sesame paste oil contains abundant amounts of the low molecular weight antioxidants, and by using the sesame paste oil it is possible to obtain the oil preparation with a high activity of the antioxidant.

However, this sesame paste oil has a high viscosity, and the size of a drop is also large, thus the preparation in which only the sesame paste oil was added to the fine powder described above has a poor penetration possibility into the inside of cells in a diseased part. However, when the sesame oil obtained from raw sesame is added to the sesame paste oil, the droplet size is small and the possibility of penetration into the inside of the cells in a diseased part is improved.

The oil, which is collected from crude sesame, is an oil obtained by grinding raw sesame as it is and pressing, after which the solid content is removed and the oil is commercially available as a regular sesame oil. Since the mixing ratio between the sesame paste oil and the ordinary sesame oil also differs depending on the amount to be added, the ratio cannot be defined arbitrarily. Preferably it is 1-3 of the fine powder, parts by weight of the ordinary sesame oil per 1 part by weight of the sesame paste oil.

The ratio of the oil mixture to the fine powder added thereto is such that the mixed oil constitutes 60-95% by weight of the total amount of both.

If the oil mixture is less than 60% by weight, the ability of the oil preparation to pass through the cell membrane is poor.

On the other hand, if the oil mixture exceeds 95% by weight, the concentration of the antioxidants, low, reactive oxygen and lipid peroxide, also decreases. as effective components, the effect of dampening the preparation of the oil preparation of the present invention, which is taken orally, can be prepared by adding the fine powder to the oil mixture by enclosing it in a gelatin capsule or the like. as soon as the oil mixture is prepared. However, the material mixture may mature preferably at 20-35 ° C for about 3-30 days, even more preferably at 28-30 ° C for about 1 week before encapsulation.

By applying the maturation treatment, the release and conversion of the antioxidants to low molecular weight substances proceeds by means of koji, which remain in the fine powder, and the antioxidants mix well with the oil mixture, whereby the activity of the reactive components and the osmotic ability in, the inside of the cells is further improved.

The oil composition of the present invention may also comprise a seed starting material comprising rice sprouts or wheat sprouts and soybeans, and optionally at least one of rice bran, hatomugi (pearl barley) or wheat, which is converted into a fine powder as it is without heating and fermentation, and added to the oil mixture together with the heated and fermented fine powder, as described above.

In the fine powder of the seed starting material, which is not heated and fermented, the antioxidants are not released and converted as effective components into low molecular weight substances¿ When added to the oil mixture together with the heated and fermented fine powder, however, the release of the antioxidants gradually proceeds. and conversion to low molecular weight substances even after encapsulation fine due to koji remaining in the fermented powder, thus there is the advantage that the effect of suppressing the production of reactive oxygen and lipid peroxide is maintained for a long period .

In contrast, the antioxidants, as an effective component, are broken down in the oil preparation, in which only hot and fermented fine powder is used, due to enzyme reactions and the like, which continue continuously even after encapsulation. Thus, the effective period is short compared to a preparation in which the untreated fine powder has been added.

However, in cases where the amount of additive of the untreated fine powder is too large, the activity of the effective component decreases. Thus, it is preferred that the untreated, about 0.5-l weight part based on a part by weight of the heated and fine powder be present in an amount of fermented, fine powder. Incidentally, even in this case, where two types of fine powders are included, the oil mixture is 60-95% by weight of the total amount.

In the oil preparation thus obtained according to the present invention, both the activity of the antioxidants and the osmotic force inside the cell are high. As has also been clarified from the results of clinical trials, which are described below, the preparation has a remarkable effect against various inflammations and ingrained diseases for which the therapeutic effects have been insufficient by conventional, anti-inflammatory agents.

The oil composition of the present invention may be encapsulated with gelatin or the like and taken orally as a medicament. freckles and the like or wrinkles and the like. In case of abnormal pigmentation, such as dermatitis, chloasma, the oil preparation can be applied directly to the affected part. In addition to dermatitis and the like, the oil composition of the present invention can also be applied to adult diseases and ingrained diseases, such as chronic articular rheumatoid thrombophlebitis, progressive systemic sclerosis, difficult-to-treat skin ulcers. also has effects in the treatment and prevention of other pollutant-causing diseases, burns, external wounds, fatigue, hangovers. In addition, the oil preparation according to the present has constipation and the like. no side effects, since only grain, koji and sesame are used as starting materials, thus the preparation can be taken orally as a health food for the maintenance and enhancement of health. Needless to say, one can add auxiliary drugs or components which are useful for health, such as various vitamins, minerals and the like, and flavors, taste adjusting agents, coloring agents and the like in the preparation of the preparation.

Embodiment Each portion of rice sprouts, soybeans, rice bran, hatomugi (pearl barley) and wheat was loaded into a vessel made of clay, which radiated infrared radiation in the long-range range of 4-14 microns, and heated at 90-96 ° C for 3 hours. while stirring slowly so as not to burn. Then the koji was added in an amount of 3% of the total amount for fermentation at 36-40 ° C for 72 hours. Then the fermented material was converted into a fine powder using a stone mill. In addition, the above-mentioned five varieties of seed starting material, which were not heated and fermented, were ground with a stone mill to obtain fine powder in the same amount. On the other hand, sesame was heated in the same manner as the materials identified above, and after grinding with a stone grinder, it was pressed to obtain a sesame paste oil.

Then, 28.1 parts by weight of sesame paste oil was mixed with 48.9 parts by weight of a commercially available sesame oil; to which mixture was added 11.5 parts by weight of the heated and fermented, untreated, one was stirred until homogeneous. The resulting fine powder and 11.5 parts by weight of the fine powder; and the resulting mixture was allowed to mature at 28 ° C for one week and then encapsulated in gelatin to obtain an oil preparation.

Effect of the present invention [I] "In vitro" test (1) For an "in vitro" test with respect to the ability to reach and penetrate oily sites, the oil preparation according to the embodiment was added to a TBA (thiobarbituric acid) reaction system. , in which an oily, unsaturated fatty acid (decosahexanoic acid) was reacted with reactive oxygen, which was generated by means of ultraviolet rays and which gave lipid peroxide, and the degree of suppression of the production of lipid peroxide was measured.

To 0.1 cm 3 of decosahexanoic acid, which is diluted 100 times, was added 1.8 mg / ml of the test sample of the oil preparation of the present invention, and the prepared lipid peroxide in the TBA reaction was mixed 0.2 2 ml of 0.1 N HCl and 0.3 ml of phos- 1.8 mg / ml of the test sample was added to mixed by the TBA reaction. ml 7% sodium dodecyl sulphate, tungstic acid; ningen; 1 ml of a reagent in which 0.67% TBA was mixed with acetic acid at 1: 1 was added; with excitation at 515 nm and emission at 553 nm with the measurement and measurement, reversal of a fluorescence spectrophotometer was performed.

As a comparative example, the botanical nutrient of Japanese Patent Specification No. 1,366,268 (Comparative Example 1) and the antioxidant composition described in Japanese Laid-Open, Unexamined Patent Application No. 63-79834 (Comparative Example 2) were used, the measurements being performed - des in the same way. The results are shown in Table 1.

TABLE 1 Mean Test sample (6 min value) Control 461 in 62 (UV +) Oil preparations according to the present 121 1 13 *** invention (1.8 mg / ml) Comparative Example l 271 1 34 ** (1.8 Ing / ml) Comparative Example 2 358 + 45 * (1.8 mg / ml) UV +: ultraviolet radiation ***: 0.01 <P <0.05 (comparison with control) **: P <0.01 (comparison with control) *: P <0.000l (comparison with control) 10 15 20 25 30 35 512781 ll Test results Although any of the test samples markedly suppressed the generation of lipid peroxide (TBA-reactive substances) from the unsaturated fatty acid (docosahexaenoic acid) by radiation of ultraviolet rays (102), in particular, suppressed the oil preparation of the present invention. remarkable this generation (P <0.000l). The result supports the fact that the oil preparation according to the present invention has a higher activity of the antioxidant and a higher penetration possibility inside the cell in which a disease occurs, compared to conventional preparations (Comparative Examples 1 and 2). (2) A (3,4-3H2] -antioxane was prepared, the low molecular weight antioxidant present in the oil composition of the present invention being labeled with an isotope (3H); test tube; and the number (cpm) [3H2], bound to the cell preparation was added to a human tissue in a membrane was measured using a scintillation counter, examining the possibility of reaching the cell membrane (labeled, titrated thymidine was 2 Ci / mM).

The same experiments were also performed for Comparative Examples 1 and 2. The results are shown in Table 2. As shown in Table 2, the oil preparation of the present invention had the highest affinity on the cell membrane compared to Comparative Examples 1 and 2.

TABLE 2 Test sample cpm contained Control 15643 cpm / 103 cells Oil preparation according to 56372 cpm / 103 cells present invention (1.8 mg / ml) Comparative Example 1 33451 cpm / 103 cells (1.8 mg / ml) Comparative Example 2 30567 cpm / 103 cells (1.8 mg / ml) (3) The oil preparation of the present invention was subjected to ultrasonic treatment and added to a system which generated reactive oxygen (neutrophil and xanthine xanthine oxidase) so that the conversion concentration in the living body became 1.6 mg / ml; and three types of reactive oxygen (O 2, H 2 O 2 and OH 2) were measured to compare with the case of no addition (control). The conversion percentage to exist in a living body is the amount that is assumed in the blood when an ordinary amount taken per day (9 g in the case of the oil preparation of the present invention) is absorbed in a living body.

The measurement procedure for the three types of reactive oxygen is as follows. With respect to O 2 -, the method was used in which reduct was measured at a wavelength of 550 nm with a spectrophotometer of the type amount of ferric cytochrome C using O 2 Beckman, and this was converted to the amount O 2 -.

With respect to HZOZ, the degree of reduction of scopoletin fluorescence using scopoletin and peroxidase was measured due to the fact that H by Hitachi Ltd with excitation at 370 nm and emission at 460 nm.

With respect to OH ', the method was used in which a principle was used that α-keto-methiol-butyl acid (KMB) was reacted with OH- to generate ethylene gas, the ethylene gas being quantified with a gas chromatograph made by Hitachi Ltd. and wherein this quantification was converted to OH-. The same experiments were also performed for Comparative Examples 1 and 2. The results are shown in Table 3. TABLE 3 Reactive Oxygen Test Sample O 2 H 2 O 2 OH.

Control 1.532 nmol 485 pmol 854 pmol Oil preparation according to the pre-0.589 nmol 161 pmol 283 pmol of the present invention (1.3 mg / ml) Comparative Example 1 1.285 nmol 403 pmol 707 pmol (1.8 Ing / ml) Comparative Example 2 0.231 nmol 538 pmol 108 pmol (1.8 mg / ml) Test results The antioxidant effect of the oil preparation of the present invention was slightly worse than that of Comparative Example 2, but showed an antioxidant effect greater than that of Comparative Example 1. As clarified from the above tables 1 and 2, however, Comparative Example 2 has a lower content of oil substances, whereby it has a poorer possibility of reaching the cell in which a disease occurs.

Thus, when an overall assessment is made, the oil composition of the present invention, in which the antioxidant effect is high and the penetration ability, inside the cell in a diseased part, is highest, very excellent as an antioxidant.

[II] Clinical trial The therapeutic effect was studied in 96 patients with autoimmune disease, collagenosis, such as chronic joint rheumatism, hemastenosis, nephritis, hepatocirrosis, chloasma, freckles and the like, which have hitherto resisted or worsened with any of the nonsteriodic , the antiphlogistic drugs, steroids and antioxidant composition of Comparative Example 2. The results are shown in Table 4.

TABLE 4 Oil preparations according to the present test Test Comparative Example 1 Comparative Example 2 Finding Disease (1.8 mg / ml) (1.8 mg / ml) (1.8 mg / ml) Chronic 13/18 (72 %) 0/7 (O%) 4/14 (28%) joint rheumatism Indicated 3/5 (60%) 0/3 (O%) 1/4 (25%) Forward- 9/12 (75%) 2/10 (20%) 6/12 (50%) dande systemic sclera Dermato- 6/8 (75%) 2/12 (16%) 6/13 (46%) myosytis Thrombo- 2/3 (66 %) 0/4 (O%) 1/5 (20%) phlebitis Burgers 6/8 (75%) U / 3 (O%) 3/6 (50%) Raynaud's disease 10/12 (83%) 3 / 8 (37%) 7/12 (58%) Disease Crus 8/11 (72%) 4/9 (44%) 11/15 (73%) Varicose Violence Treatment- 3/5 (60%) 1/5 (20 %) 2/6 (33%) added skin ulcer Kloasma, 11/14 (78%) 4/12 (33%) 17/25 (68%) freckles the values in the table show the proportion of patients with positive results in each of the cases .

Claims (7)

10 15 20 25 30 512781 15 PATENT REQUIREMENTS An oil preparation obtained by: heating a seed starting material comprising rice sprouts and / or wheat sprouts and soybeans at a temperature not exceeding 10 ° C; adding koji to the heated material and fermenting the heated material; W transfer of the fermented material to fine powder; and feeding the powdered material to an oil mixture comprising a paste oil obtained from sesame, heated at a temperature not exceeding 10 ° C, a ratio of the oil mixture to the total and an oil obtained from crude sesame, wherein the amount of the fine powder and the oil mixture is 60-95% by weight. An oil preparation according to claim 1, further comprising a seed starting material comprising rice sprouts and / or wheat sprouts and soybeans, which have been transferred to fine powder without heating and fermentation. An oil preparation according to claim 1 or 2, wherein the heated or unheated seat starting material comprises, soybeans, at least one of rice bran, hatomugi in addition to rice sprouts and / or wheat sprouts and (pearl barley) or wheat. which in- or one An oil preparation according to claim 1 or 2, is encapsulated to be taken orally as a medicinal health food. A process for producing an oil precursor 1, 2 or 3 is heated with infrared radiation in the long-wave pair, the seed starting material according to the range having a wavelength of 4 to 14 μm. A process for the preparation of an oil preparation, wherein the seed starting material according to claim 1, 2 or 2 is fermented at 20-36 ° C for 2-6 days after heat treatment. A process for the preparation of an oil composition, wherein the fine powder according to claim 1, 2 or 3 is added to the oil mixture to mature at 20-35 ° C for 3-30 days.