JP5323127B2 - Antiallergic composition - Google Patents

Description

The present invention relates to a composition having high antiallergic properties.

  Jabara is a citrus fruit that is only grown in Kitayama Village, Wakayama Prefecture, Japan. It is a citrus fruit that belongs to yuzu, daidai, kabosu, and has a mellow flavor.

  Jabara fruit juice contains a lot of vitamins and minerals, and also contains Nariltin, which has antiallergic action, and it has already been confirmed that by continuing to drink it, it has antiallergic action, specifically anti-hay fever action. (See Non-Patent Document 1).

  However, since the rose juice is a liquid, it must be stored in a container, and if it is not refrigerated in a refrigerator, it will rot within a few days after squeezing. There was a problem that it was inconvenient to carry around. In addition, since the amount of each dose is smaller than the capacity of the container for storing the rose juice, the container has to be opened and closed frequently, which has a problem in terms of hygiene. In addition, after squeezing the fruit juice, a large amount of peel remains, and there is a problem that a large amount of fuel is required to incinerate the peel.

Monthly “Clinical Immunology and Allergy”, 50 (3): 360-364, 2008

Accordingly, an object of the present invention is to provide an antiallergic composition that has high antiallergic properties, is easy to store, and is environmentally friendly.

As a result of intensive studies, the inventors have found that the peel after squeezing the fruit juice contains a lot of naryltin, and this is dried by the freeze-drying method and then dried by the heat-drying method. The present invention was completed by finding that it has the characteristics. That is, the anti-allergic composition of the present invention is characterized in that it contains a dried jade peel that is dried by a freeze drying method and then dried by a heat drying method . In addition, the antiallergic composition of this invention may use the dried fruit peel processed into the granular form, and may contain components other than the dried fruit peel, such as reduced maltose.

The anti-allergic composition of the present invention has higher anti-allergic properties than Jabara fruit juice, and is excellent in preservability because it is a solid unlike juniper fruit juice. In addition, it is environmentally friendly because it can use the peels that had been discarded by incineration.

The antiallergic composition of the present invention is characterized in that it contains rose peel. Therefore, the jade peel and its processing method will be described below.

(1) Jara pericarp The Jara perilla used in the present invention can be used without any particular limitation. Among them, since the content of narirutin per unit weight is large, the fruit or pericarp that has been plucked is yellowed. The immature stage fruit is preferred. Here, specifically, the immature stage fruit is preferably a fruit that has been harvested three to four months after fruit set. In addition, since potatoes generally fruit around June, fruits harvested around September to October are preferable.

  Jabara peels can be peeled off from the fruit by hand, peeled off by a known automatic peeler, or residues left after squeezing the fruit juice from the juice press. The residue is preferred.

(2) Manufacturing Method bellows dried peel, after it is or minced pericarp, then this was dried in a freeze-dry method, is produced by heat drying method of drying by a dryer. The drying by the heat drying method is preferably performed at 80 ° C.

After drying with freeze-dry method, followed by drying with heat drying method, while maintaining high Nariruchin concentration, evaporation of the limonene contained in dry pericarp, can suppress the bitter taste.

  Although this dried peel can be used as it is, it is more preferable to use it after it is processed into a powder form by a general method, that is, a ball mill or the like in consideration of ease of eating.

  Dried pericarp processed into powder can be used alone, but it improves the taste by mixing with flakes, tea sauce, etc., or by mixing with sugars such as reduced maltose and granulating it. Can be made. The dried pericarp processed into granules may be contained in capsules such as enteric capsules to form capsules, mixed with known additives such as magnesium stearate, shaping, etc., and by known formulation techniques It may be a tablet.

  Hereinafter, the present invention will be described more specifically based on examples. However, these examples do not limit the invention described in the claims in any way.

1. Measurement of Nariltin Content in Jara Fruits with Different Harvest Times (1) Preparation of Standard and Preparation of Calibration Curve Dehydrated dry kala peel powder (35 g) is defatted with hexane and extracted with methanol to obtain a methanol extract It was. Use silica gel column chromatography (mobile layer: methylene chloride / methanol system), gel filtration chromatography (Selfadex LH-20, mobile layer: methanol), preparative HPLC (mobile layer: 20% acetonitrile) from methanol extract. Then, nariltin was isolated and purified to obtain 130 mg of a sample.

A calibration curve was prepared by a conventional method using the obtained nariltin and the HPLC method (Y = 1461387X-497, r = 0.9999, 0.0051-5.1 μg). The measurement conditions in the HPLC method are as follows: column: COSMOSIL 5C ₁₈ -AR-II (diameter 4.6 mm × 250 mm), column temperature: 40 ° C., moving bed: 20% acetonitrile (0.8% acetic acid), moving bed flow rate: 1.0 mL / min, detection: UV detector (280 nm).

(2) Measurement of Nariltin content in Jara fruit Five Jara fruits are collected and frozen every month for about one month from September to December from the same tree in Matsue-kita, Wakayama City, Wakayama Prefecture. did. The frozen fruit was thawed overnight in a refrigerator, and then peeled off by hand. The fruit peeled off was squeezed with a juicer to obtain fruit juice. The weight of the obtained peel and fruit juice was measured.

  Nine times the amount of distilled water was added to 5 g of the peel and homogenized. 0.5 g of homogenized fruit and fruit juice was weighed accurately, 50% methanol was added to make exactly 10 mL, and then filtered through a 0.45 μm filter to obtain an analytical sample. The nariltin concentration of this analytical sample was measured by the calibration curve prepared in (1). The results are shown in Table 1.

  From Table 1, it can be seen that pericarp has a higher concentration of nariltin and the amount of nariltin per fruit than fruit juice. In addition, it can be seen that the fruit collected in September for both the peel and fruit juice has a higher narilutin concentration, and the narilutin concentration decreases as the maturity increases with the passage of time from fruit. On the other hand, it can be seen that the amount of nariltin per fruit increases with the passage of time. This is considered to be because the fruit is small if the period from fruit set to fruit picking is short.

  From these results, in order to obtain a high concentration of nariltin, it is appropriate to use the japonica fruit that was harvested from March to April, that is, from September to October. In order to do this, it can be seen that it is appropriate to use the jade fruit that has been harvested from May to June, ie, from November to December.

2. Preparation of anti-allergic composition (thermal drying method) and its anti-allergic effect (1) Preparation of anti-allergic composition Splashes of jello fruits (collected in November) were cut with a knife and halved with the fruits lying beside. The bisected fruit was squeezed with a fruit press and separated into peel and juice. The obtained peels were coarsely crushed, arranged in a drying tray, and dried with hot air at 80 ° C. for 15 hours until the water content was less than 5 wt%. The dried pericarp was pulverized with a ball mill until the average particle size became 100 μm or less. 50% by weight of the crushed pericarp and 50% by weight of powdered reduced maltose (MR-50, Mitsubishi Corporation Foodtech) were mixed. The mixture was granulated and 2 g of the granules were stick-packaged.

(2) Measurement of Nariltin Concentration Extracted from 2 g of the antiallergic composition prepared in (1) with a dimethyl sulfoxide / methanol solution. The volume of the extracted solution was measured, filtered, and used as an analysis sample. The concentration of nariltin in the extract was measured by the HPLC method with reference to the standard substance according to the literature (Kawai et al., J. Agric. Food. Chem., 2001, 49, 3982-3986.). As a result, the concentration of nariltin in the antiallergic composition was 40.4 mg / g.

  The measurement conditions in the HPLC method are as follows: Column: YMC Pack Pro C18 RS (diameter 4.6 mm x 150 mm), column temperature: 40 ° C, moving bed: A (10 mM phosphate buffer), B (methanol) Use a layer to feed A80% and B20% at a rate of 2 minutes, then use a gradient with a linear concentration gradient so that A55% and B45% 43 minutes after the start of delivery, flow rate of moving bed: 1.0 mL / min, detection: UV detector (280 nm).

(3) The antiallergic composition prepared with anti-allergic effect of antiallergic composition (2), 30 adults a sufferer hay fever (18 men, women 12 people), the depending on the conditions I was allowed to drink. As a result, 15 people (10 men, 5 women) with relatively mild symptoms of hay fever were allowed to take the antiallergic composition once a day (dose of nariltin: about 40 mg in total). 1 to 3 hours after drinking, the symptoms were alleviated 100%. In addition, 10 people (5 men, 5 women) who have moderate symptoms of hay fever are taken by taking the antiallergic composition twice a day (drinking amount of narirutin: about 80 mg in total). 1 to 3 days later, the symptoms were 100% alleviated. Furthermore, five people (three men and two women) who have relatively severe symptoms of hay fever are allowed to take the antiallergic composition three times a day (nariltine dose: about 120 mg in total). The symptoms were 100% alleviated 1 to 7 days after the ingestion.

3. Preparation of anti-allergic composition (freeze-dry method) and its anti-allergic effect (1) Preparation of anti-allergic composition Spatter of jallah fruit (collected in November) was cut with a knife and divided into two halves. The bisected fruit was squeezed with a roller-type fruit press and separated into fruit peel and fruit juice. The resulting peel was crushed and placed in a drying tray and rapidly frozen to -80 ° C. As a result of freezing, the skin was dried and the vacuum was reduced with the drying tray, and dried by evaporating water at room temperature of -5 ° C. As a result, a dried skin having a water content of less than 5% by weight was obtained.

The dried skin was pulverized with a ball mill until the average particle size became 100 μm or less. 50% by weight of crushed pericarp and 50% by weight of powdered reduced maltose were mixed. The mixture was granulated and 2 g of the granules were stick-packaged. The concentration of nariltin in the obtained antiallergic composition was measured in the same manner as in Example 2. As a result, the concentration of nariltin in the antiallergic composition was 55.6 mg / g.

(2) anti-allergy composition prepared by antiallergic effect of antiallergic composition (1), 30 adults a sufferer hay fever (13 male persons, women 17 people), the depending on the conditions I was allowed to drink. As a result, 10 people (5 men, 5 women) who have relatively mild symptoms of hay fever are allowed to take the antiallergic composition once a day (dose of nariltin: about 55 mg in total). 1 to 3 hours after drinking, the symptoms were alleviated 100%. In addition, 10 people (3 men and 7 women) who have moderate symptoms of hay fever are taken by taking the antiallergic composition twice a day (dose of narirutin: about 110 mg in total). 1 to 2 days after the symptom was alleviated 100%. Furthermore, 10 people (5 men, 5 women) who have relatively severe symptoms of hay fever are allowed to take the antiallergic composition three times a day (dose of nariltine: about 165 mg in total). One to three days after drinking, the symptoms were alleviated 100% .

4 . Preparation of anti-allergy composition (troche) (heat drying method) and its anti-allergic effect (1) Preparation of anti-allergic composition Cut off the spruce of jallah fruit (collected in November) with a knife and lay the fruit sideways Divided. The bisected fruit was squeezed with a fruit press and separated into peel and juice. The obtained peels were coarsely crushed, arranged in a drying tray, and dried with hot air at 80 ° C. for 15 hours until the water content was less than 5 wt%. The dried skin was pulverized with a power mill, and the dried skin powder that passed through a 30-mesh sieve was recovered. The concentration of nariltin in the dried fruit skin powder was measured in the same manner as in Example 2. As a result, it was 60.0 mg / g.

Dry skin powder 12.5 wt%, glucose (Glufinal, Sanei saccharification) 63.5 wt%, crystalline cellulose (microcrystalline cellulose S102, ISP Japan) 10.0 wt%, sucrose fatty acid ester (Ryoto Sugar ester S-370F, Mitsubishi Chemical Foods) 5.0% by weight, anhydrous citric acid (anhydrous citric acid pulverized product, Kyokuto Kasei Kogyo) 4.0% by weight, citrus flavor (dry coat grapefruit # 3261 0.5% by weight, dry coat orange # 1400 1% by weight, Dry coat lime # 2961 1% by weight, Takada fragrance 2.0% by weight, Neotame (Mirassy 200, Dainippon Sumitomo Pharma) 1.0% by weight, fine silicon dioxide (Carburex FPS-500, DSL Japan) 2.0% by weight Mixed. This mixed powder was tableted with a rotary tableting machine so as to have a flat diameter of 20 mm. As a result, a troche-type antiallergic composition (nariltin concentration: 15 mg / tablet) having an average weight of 2020 mg, a tablet thickness of 5.23 mm, a water content of 6.59 wt% and a hardness of 16.3 kg was obtained.

(2) the anti-allergy composition prepared by the anti-allergic effect of the anti-allergic composition (1), adult 20 people are sufferers of hay fever (10 men, women 10 people) four times a day to ( Nariltin drinking dose: about 60 mg in total) administered sublingually. As a result, 5 men and 4 women showed improvement in symptoms, and 5 men and 6 women showed significant improvement in symptoms. In addition, 6 men and 7 women confirmed the effect 5 minutes after administration, and 4 men and 3 women confirmed the effect 10 minutes after administration.

By the way, Non-Patent Document 1 shows that the score of pollinosis symptoms such as watery, sneezing, nasal congestion, etc. is obtained by drinking 5 ml of Jara juice twice a day in the morning and 10 ml / day for 2 weeks to 4 weeks. There has been described that it has improved by about 50%.

From the above results, it was proved that the composition of the present invention using the rose peel had higher antiallergic activity than the conventional one using the rose juice.

Claims (5)

An antiallergic composition containing dried rose peels dried by freeze drying and then dried by heat drying . The antiallergic composition according to claim 1, which is heat-dried at 80 ° C. Bellows pericarp, antiallergic composition according to claim 1 or claim 2, which is a granular. The antiallergic composition according to any one of claims 1 to 3 , wherein the roses collected from March to April after fruit set are used. The antiallergic composition according to any one of claims 1 to 4 , comprising reduced maltose.