JP6165586B2 - Oral composition - Google Patents

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JP6165586B2
JP6165586B2 JP2013219342A JP2013219342A JP6165586B2 JP 6165586 B2 JP6165586 B2 JP 6165586B2 JP 2013219342 A JP2013219342 A JP 2013219342A JP 2013219342 A JP2013219342 A JP 2013219342A JP 6165586 B2 JP6165586 B2 JP 6165586B2
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oral composition
oryzanol
tableting
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discoloration
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JP2015081238A (en
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服部 祐子
祐子 服部
三谷 信
信 三谷
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Pola Chemical Industries Inc
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Description

本発明は、血管拡張効果を有する天然成分とγオリザノールを組み合わせた経口用組成物に関する。   The present invention relates to an oral composition in which a natural component having a vasodilatory effect and γ oryzanol are combined.

近年、偏った食事のため、必要な栄養素が不足してしまい、また、健康志向により、食事だけでは摂取が難しい栄養素を栄養補助食品により摂取することが一般的になってきている。加えて、平均寿命は男女とも約80歳以上となり、高齢化にともない、食事量を増やせない高齢者では特に気軽に摂取可能な栄養補助食品は人気が高い。   In recent years, due to an uneven diet, the necessary nutrients have been insufficient, and due to health consciousness, it has become common to take in nutrients that are difficult to ingest with diet alone. In addition, the average life expectancy is about 80 years old for both men and women, and dietary supplements that can be easily consumed are particularly popular among elderly people who cannot increase the amount of meals as the population ages.

栄養補助食品も目的別に多種多様な商品が発売されており、特に女性では美容、美肌目的に発売された商品が人気で、コラーゲン、コンドロイチン硫酸塩、セラミドを配合されたものが報告されている(例えば、特許文献1、2参照)。また、人参、枸杞子、大棗、桂皮、鬱金、酸棗仁、陳皮、冬虫夏草等の古来より、生薬として使用されてきたものを配合したもの(例えば、特許文献3参照)、疲労回復、老化抑制、抗酸化、代謝促進、血行促進目的にショウガを配合した商品等も依然人気が高い(例えば、特許文献4参照)。   Nutritional supplements are also available in a wide variety of products for different purposes, especially for women, products released for beauty and skin care are popular, and those containing collagen, chondroitin sulfate, and ceramide have been reported ( For example, see Patent Documents 1 and 2). In addition, it has been used as a herbal medicine since ancient times, such as carrots, coconut, daikon, cinnamon, cinnamon, acid jinjin, chenseed, cordyceps, etc. Also, products containing ginger for the purpose of antioxidant, metabolism promotion and blood circulation promotion are still popular (see, for example, Patent Document 4).

一方、食事の西洋化に伴い、高脂血症の患者は増加しており、このような患者では脂質が血管に付着し、血管のつまりを生じ、場合によっては死に至る場合もある。このような血管状態の悪化を防ぐ目的で、血管拡張効果を有する天然成分を配合する栄養補助食品は用いられ、例えば、丹参葉は血管拡張、脳血流量増加、抗凝血、血圧降下作用を持ち、鶏血藤は血行改善、造血促進作用を持ち、山査子は血管拡張、血圧降下、血脂の減少の作用を持ち、これらを配合した栄養補助食品が知られている(例えば、特許文献5参照)。   On the other hand, with the westernization of the diet, patients with hyperlipidemia are increasing, and in such patients, lipids adhere to blood vessels, causing clogging of blood vessels, and in some cases, death. For the purpose of preventing the deterioration of the vascular condition, dietary supplements containing natural ingredients having a vasodilatory effect are used. For example, Tansan leaves have vasodilation, increased cerebral blood flow, anticoagulation and blood pressure lowering action. Chicken blood wisteria has blood circulation improvement and hematopoiesis promoting action, and Yamako has action of vasodilation, blood pressure lowering, blood fat reduction, and dietary supplements containing these are known (see, for example, Patent Document 5) ).

これらの血管拡張作用が期待される栄養補助食品は、摂取の簡便さから錠剤で提供されることが多い。錠剤の課題として、製造時にラミネーション、キャッピング等の打錠障害を生じることがあり(例えば、特許文献6,7)、そのため、打錠時の圧力等を随時調整したり、賦形剤の種類を調整する等の打錠障害を生じない条件を検討しなければならず、煩雑な作業が必要であった。   Nutritional supplements that are expected to have a vasodilatory effect are often provided in tablets for ease of consumption. As a problem of tablets, tableting troubles such as lamination and capping may occur at the time of production (for example, Patent Documents 6 and 7). Conditions that do not cause tableting troubles such as adjustment had to be studied, and complicated work was required.

栄養補助食品では、経時的な退色や褐変等の変色が課題になっており、ビタミン等の添加剤で変色を改善することが報告されているが、組成により使用できなかったり、風味等に影響を与える場合があり、より汎用性の高い変色改善技術が求められていた(例えば、特許文献7,8)。   In dietary supplements, discoloration such as discoloration and browning over time has become an issue, and it has been reported that additives such as vitamins can improve discoloration, but it cannot be used depending on the composition, or it affects the flavor, etc. There has been a demand for a more versatile discoloration improvement technique (for example, Patent Documents 7 and 8).

特開2009−073735号公報JP 2009-073735 A 特開2013−138632号公報JP 2013-138632 A 特開2002−275075号公報JP 2002-275075 A 特開2007−222116号公報JP 2007-222116 A 特開2002−233331号公報JP 2002-233331 A 特開2007−181441号公報JP 2007-181441 A 特開2013−179905号公報JP 2013-179905 A 特開平4−166061号公報Japanese Patent Laid-Open No. 4-166061

本発明は、このような状況下なされたものであり、血管拡張効果を有する天然成分を含有する経口用組成物において、錠剤のラミネーション、キャッピング等の打錠障害を改善し、製造後の経時的な変色を抑制するために、血管拡張効果を有する天然成分にγオリザノールを組み合わせた経口用組成物を提供することを課題とする。   The present invention has been made under such circumstances, and in an oral composition containing a natural ingredient having a vasodilatory effect, the tableting troubles such as tablet lamination and capping are improved, and after the production, It is an object of the present invention to provide an oral composition in which γ-oryzanol is combined with a natural ingredient having a vasodilatory effect in order to suppress discoloration.

本発明者らは、ラミネーション、キャッピング等の打錠障害を改善可能な経口用組成物を提供すべく研究を進め、意外にも、血管拡張作用を有する天然成分を含む経口用組成物に、特定の脂質を加えることにより顕著な打錠障害改善効果、更には経時的な変色を防ぐことを見出した。特にフェルラ酸とステロールとが縮合したエステルであるγオリザノールを加えることにより、顕著に打錠障害の改善、変色の改善を見出し、本発明を完成させた。本発明の経口用組成物により、従来の複雑な打錠障害改善の検討なしに、割れやヒビ等の錠剤製造時の課題を解決することができるのみならず、製造後の変色も改善できる。
<1> 血管拡張効果を有する天然成分及びγオリザノールを含有する経口用組成物。
<2> 前記血管拡張効果を有する天然成分が、鶏血藤、丹参、山査子からなる群から選択される少なくとも1種を含む、<1>に記載の経口用組成物。
<3>錠剤の形態であることを特徴とする、<1>または<2>に記載の経口用組成物。
The present inventors have advanced research to provide an oral composition that can improve tableting troubles such as lamination and capping, and surprisingly have been identified as an oral composition containing a natural ingredient having a vasodilatory effect. It was found that by adding the lipids, a significant tableting trouble-improving effect and further, discoloration with time was prevented. In particular, by adding γ-orizanol, which is an ester obtained by condensing ferulic acid and sterol, the inventors have found that tableting problems are improved significantly and discoloration is improved, thereby completing the present invention. The oral composition of the present invention can not only solve problems in tablet production such as cracks and cracks, but also improve discoloration after production, without studying the conventional complicated tableting problems.
<1> An oral composition containing a natural ingredient having a vasodilatory effect and γ oryzanol.
<2> The oral composition according to <1>, wherein the natural component having a vasodilatory effect includes at least one selected from the group consisting of chicken blood wisteria, tansan, and yamako.
<3> The oral composition according to <1> or <2>, which is in the form of a tablet.

以下、本発明の経口用組成物について説明するが、本発明の技術的範囲は、以下の具体的な実施形態にのみ限定されるものではない。   Hereinafter, although the composition for oral use of this invention is demonstrated, the technical scope of this invention is not limited only to the following specific embodiments.

本発明の実施態様は、血管拡張効果を有する天然成分とγオリザノールを含有する経口用組成物である。
本実施態様に係る経口用組成物は、本発明者らが得た知見である、血管拡張効果を有する天然成分と特定の脂質を組み合わせることにより、錠剤製造時のラミネーション、キャッピング等の打錠障害を改善でき、更に製造後の変色を抑制することができる。
An embodiment of the present invention is an oral composition containing a natural ingredient having a vasodilatory effect and γ oryzanol.
The composition for oral administration according to this embodiment is a finding obtained by the present inventors, which is a tableting disorder such as lamination and capping during tablet production by combining a natural component having a vasodilatory effect and a specific lipid. Can be improved, and further discoloration after production can be suppressed.

(1)血管拡張効果を有する天然成分
本発明の血管拡張効果とは、血管を拡張して血液量を増やす効果、血流を高める効果等を意味し、FMD(血流依存性血管拡張反応)測定や超音波測定、血流測定装置等により測定することができる。
本発明の血管拡張効果を有する天然成分は、市販の天然成分で血管拡張効果を有するものであれば、特段限定されないが、例えば、鶏血藤、丹参、山査子、ニンニク、ショウガ、陳皮、オタネニンジンが例示できる。このうち、鶏血藤、丹参、山査子が好ましく、特に鶏血藤が好ましい。
これらの天然成分は血管拡張効果を有する植物の根、茎、枝、葉、種、全草をそのまま粉砕、又は乾燥したもの、エタノール、水等の極性溶媒で抽出した抽出液、その抽出液を乾燥し粉末にしたもの、これらの粉砕物、抽出物、乾燥物等をカラムや溶液間の分配により精製し、有効成分を高めたもの等が好ましく例示できる。
鶏血藤としては、マメ科植物のSpatholobus
suberectusの抽出物、乾燥物を用いることができ、特に、茎を乾燥したもの、水等の極性溶媒で抽出したもの、抽出物を乾燥させたものを用いることが好ましい。
丹参としては、シソ科植物のSalvia
miltiorrhizaの抽出物、乾燥物を用いることができ、特に、葉を乾燥したもの、水等の極性溶媒で抽出したもの、抽出物を乾燥させたものを用いることが好ましい。
山査子としては、バラ科植物のCrataegus
cuneataの抽出物、乾燥物を用いることができ、特に、果実を乾燥したもの、水等の極性溶媒で抽出したもの、抽出物を乾燥させたものを用いることが好ましい。
また、血管拡張効果を有する可能性のある天然成分を経口用組成物として調製し、一定量を摂取し、摂取前後の血管拡張の度合いをFMD(血流依存性血管拡張反応)測定や超音波測定等により測定し、血管拡張度合いの高い天然成分を選択し、使用してもよい。
(1) Natural component having vasodilator effect The vasodilator effect of the present invention means an effect of expanding blood vessels to increase blood volume, an effect of increasing blood flow, etc., and FMD (blood flow dependent vasodilator reaction). It can be measured by measurement, ultrasonic measurement, blood flow measurement device or the like.
The natural component having a vasodilator effect of the present invention is not particularly limited as long as it is a commercially available natural component and has a vasodilator effect. For example, chicken blood wisteria, tansan, yamako, garlic, ginger, crust, ginseng It can be illustrated. Of these, chicken blood wisteria, tansan, and yamako are preferable, and chicken blood wisteria is particularly preferable.
These natural components include roots, stems, branches, leaves, seeds, whole plants of plants that have a vasodilatory effect, or an extract extracted with a polar solvent such as ethanol or water. Preferable examples include those obtained by drying and powdering, those obtained by purifying these pulverized products, extracts, dried products, etc. by partitioning between columns and solutions to increase the active ingredients.
For chicken blood rattle, Spatholobus of legumes
An extract or dried product of suberectus can be used, and it is particularly preferable to use a product obtained by drying a stem, a product extracted with a polar solvent such as water, or a product obtained by drying the extract.
As for Dansan, the Labiatae plant Salvia
An extract or dried product of miltiorrhiza can be used, and it is particularly preferable to use a product obtained by drying leaves, a product extracted with a polar solvent such as water, or a product obtained by drying the extract.
As a mountain checker, the Rosaceae Crataegus
An extract or dried product of cuneata can be used, and it is particularly preferable to use a product obtained by drying a fruit, a product extracted with a polar solvent such as water, or a product obtained by drying the extract.
In addition, natural ingredients that may have a vasodilatory effect are prepared as an oral composition, a certain amount is ingested, and the degree of vasodilation before and after ingestion is measured by FMD (blood flow-dependent vasodilator response) or ultrasound A natural component having a high degree of vasodilation may be selected and used by measurement.

本発明の前記天然成分は、通常使用される範囲で経口用組成物に含有させることができるが、0.1〜90質量%が好ましく、より好ましくは0.5〜70質量%であり、更に好ましくは1〜60質量%である。上限を超えると打錠適性上の課題を生じる場合もあり、下限未満では血管拡張作用を求めるため、多量に摂取する必要があるため、前記の範囲で用いることが好ましい。   The natural component of the present invention can be contained in the composition for oral use within the range usually used, but is preferably 0.1 to 90% by mass, more preferably 0.5 to 70% by mass, Preferably it is 1-60 mass%. If it exceeds the upper limit, there may be a problem in tableting suitability, and if it is less than the lower limit, a vasodilator action is required.

(2)γオリザノール
本発明のγオリザノールは、市販のγオリザノールを使用することができる。例えば、γ-オリザノール(オリザ油化株式会社製)やオリザノール(株式会社岡安商店製)が例示できる。
また、γオリザノールを含有する植物の根、茎、枝、葉、種、全草をそのまま粉砕、又は乾燥したもの、エタノール、水等の極性溶媒で抽出した抽出液、その抽出液を乾燥し粉末にしたものを使用することもできる。
玄米表皮・玄米胚芽由来の植物油、米糠にはγオリザノールを含有することが知られており、γオリザノールとして、これらのγオリザノールを含有する植物の一部、抽出油等を使用することもできる。
(2) γ oryzanol As the γ oryzanol of the present invention, commercially available γ oryzanol can be used. Examples thereof include γ-oryzanol (manufactured by Oriza Oil Co., Ltd.) and oryzanol (manufactured by Okayasu Shoten Co., Ltd.)
In addition, roots, stems, branches, leaves, seeds, whole plants of γ-oryzanol-containing plants are crushed or dried as they are, extracts extracted with polar solvents such as ethanol and water, and the extracts are dried and powdered It is also possible to use what has been made.
It is known that brown rice epidermis / brown rice germ-derived vegetable oil and rice bran contain γ oryzanol, and as γ oryzanol, a part of the plant containing γ oryzanol, extracted oil, and the like can also be used.

本発明の前記γオリザノールは、通常使用される範囲で経口用組成物に含有させることができるが、0.001〜50質量%を含有させることが好ましく、より好ましくは0.01〜20質量%であり、更に好ましくは0.1〜10質量%である。γオリザノールを含有する植物抽出物を用いる場合は、γオリザノールが前記の含有量となるように抽出物を含有させることが好ましい。例えば、市販の米胚芽油ガンマ(築野食品工業株式会社製)であれば、0.001〜10質量%含有させることが好ましく例示できる。
上限を超えると打錠適性上の課題を生じる場合もあり、下限未満では打錠障害の改善効果が発揮できない場合があるため、前記の範囲で含有させることが好ましい。
The γ-oryzanol of the present invention can be contained in an oral composition within a range that is usually used, but preferably contains 0.001 to 50% by mass, more preferably 0.01 to 20% by mass. More preferably, it is 0.1-10 mass%. When using the plant extract containing (gamma) oryzanol, it is preferable to contain an extract so that (gamma) oryzanol may become said content. For example, in the case of commercially available rice germ oil gamma (manufactured by Tsukino Food Industry Co., Ltd.), it is preferably exemplified that 0.001 to 10% by mass is contained.
If it exceeds the upper limit, there may be a problem in tableting suitability, and if it is less than the lower limit, the effect of improving the tableting failure may not be exhibited. Therefore, it is preferably contained in the above range.

(3)本発明の経口用組成物
本発明の経口用組成物は、血管拡張効果を有する天然成分とγオリザノールを含有することを特徴とする。かかる構成により、錠剤製造時のラミネーション、キャッピング等の打錠障害を改善でき、更に製造後の変色を抑制することができる。
本発明の経口用組成物に於いては、前記の成分以外に、通常の食品、栄養補助食品、医療用食品等で使用される任意の成分を含有することが出来る。かかる任意成分としては、例えば、ショ糖脂肪酸エステルや、グリセリンモノ脂肪酸エステル、ソルビタン脂肪酸エステルなどの界面活性剤、α化されていても良いデンプン、結晶セルロース、乳糖などの賦形剤、ヒドロキシプロピルセルロース、アラビアガム、糖アルコール、還元麦糖水等の結合剤、ステアリン酸マグネシウムやステアリン酸亜鉛、ステアリン酸カルシウムなどの滑沢剤、クエン酸トリエチル、カプリン酸モノグリセリドなどの可塑剤などが例示出来る。また、錠剤として用いることが好ましく、錠剤として使用する場合、のみやすくするため、糖衣等のコーティングを施すことが好ましい。

以下に実施例を挙げて本発明について詳細に説明を加えるが、本発明はかかる実施例にのみ限定されないことは言うまでもない。
(3) Oral composition of the present invention The oral composition of the present invention is characterized by containing a natural component having a vasodilatory effect and γ oryzanol. With such a configuration, it is possible to improve tableting troubles such as lamination and capping during tablet production, and to suppress discoloration after production.
In the oral composition of the present invention, in addition to the above-mentioned components, any component used in normal foods, nutritional supplements, medical foods, and the like can be contained. Examples of such optional components include surfactants such as sucrose fatty acid esters, glycerin monofatty acid esters and sorbitan fatty acid esters, starches that may be pregelatinized, crystalline cellulose, excipients such as lactose, hydroxypropylcellulose, and the like. Examples thereof include binders such as gum arabic, sugar alcohol and reduced maltose water, lubricants such as magnesium stearate, zinc stearate and calcium stearate, and plasticizers such as triethyl citrate and monoglyceride caprate. In addition, it is preferably used as a tablet, and when used as a tablet, it is preferable to apply a coating such as sugar coating to make it easy.

Hereinafter, the present invention will be described in detail with reference to examples, but it goes without saying that the present invention is not limited to such examples.

以下の表1に従い本発明の経口用組成物を作製した。表1の血管拡張効果を有する天然成分、γオリザノールに還元麦芽糖、結晶セルロース、ショ糖脂肪酸エステルを造粒後、打錠して錠剤状の経口用組成物を作製した。 An oral composition of the present invention was prepared according to Table 1 below. Tablets were prepared by granulating reduced maltose, crystalline cellulose, and sucrose fatty acid ester into γ oryzanol, a natural component having a vasodilatory effect shown in Table 1, and then tableting to prepare a tablet-like oral composition.

Figure 0006165586
Figure 0006165586

<比較例>
表1と同様に以下の表2に従い、比較例の経口用組成物を作製した。
<Comparative example>
In the same manner as in Table 1, an oral composition of a comparative example was prepared according to Table 2 below.

Figure 0006165586
Figure 0006165586

<試験例1>
実施例1〜4及び比較例1〜4の打錠時の打錠障害の有無について、作製した錠剤100錠のうち、ラミネーション、キャッピングがあった錠剤の数を数え表3に示した。
<Test Example 1>
Table 3 shows the number of tablets with lamination and capping among the 100 tablets produced in Examples 1 to 4 and Comparative Examples 1 to 4.

Figure 0006165586
Figure 0006165586

表3の結果から明らかに実施例の血管拡張を有する天然成分にγオリザノールを含有した錠剤では、顕著にラミネーション、キャッピング等の打錠障害が改善されることがわかる。また、γオリザノールの代わりにγオリザノール以外の油成分である紅花油を加えても、打錠障害は改善できないことが明らかである。   The results in Table 3 clearly show that tableting troubles such as lamination and capping are remarkably improved in the tablet containing γ-oryzanol as a natural ingredient having vasodilation in the examples. Further, it is clear that the tableting failure cannot be improved by adding safflower oil, which is an oil component other than γ oryzanol, instead of γ oryzanol.

<実験例2>実施例1〜4及び比較例1〜3の錠剤について、打錠障害のなかった100個を選択し、30℃にて1か月保存した場合、50℃にて1週間保存した場合の変色の有無について目視により確認し、結果を表4に示した。判定は以下の基準を用いた。
(判定基準)
変化なし→○、ようやく認識できるレベルの変色→△、明らかな変色→×
<Experimental example 2> For the tablets of Examples 1 to 4 and Comparative Examples 1 to 3, when 100 tablets without any tableting trouble were selected and stored at 30 ° C for 1 month, stored at 50 ° C for 1 week The presence or absence of discoloration was confirmed visually, and the results are shown in Table 4. The following criteria were used for judgment.
(Criteria)
No change → ○, finally recognized color change → △, obvious color change → ×

Figure 0006165586
Figure 0006165586

表4の結果から明らかに比較例に比べ実施例では、経時的な変色が顕著に改善されることがわかる。また、γオリザノールの代わりにγオリザノール以外の油成分である紅花油を加えても、変色は抑制されないことが明らかである。   From the results of Table 4, it can be seen that the discoloration with time is remarkably improved in the example as compared with the comparative example. Further, it is apparent that discoloration is not suppressed even when safflower oil, which is an oil component other than γ oryzanol, is added instead of γ oryzanol.

本発明によれば、錠剤製造時のラミネーション、キャッピング等の打錠障害を改善でき、更に製造後の変色を抑制することができる。   According to the present invention, tableting troubles such as lamination and capping during tablet production can be improved, and further discoloration after production can be suppressed.

Claims (2)

血管拡張効果を有する天然成分及びγオリザノールを含有する経口用組成物であって、前記血管拡張効果を有する天然成分として、鶏血藤、丹参、山査子からなる群から選択される少なくとも1種を含むことを特徴とする、経口用組成物。 An oral composition containing a natural component having a vasodilatory effect and γ oryzanol, the natural component having a vasodilatory effect comprising at least one selected from the group consisting of chicken blood wisteria, tansan, and Yamako Oral composition characterized by the above-mentioned. 錠剤の形態であることを特徴とする、請求項1に記載の経口用組成物。 The oral composition according to claim 1, characterized in that it is in the form of a tablet.
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