TWI603732B - Contains sesamin-class and γ-furfuryl alcohol and room germ oil composition - Google Patents

Contains sesamin-class and γ-furfuryl alcohol and room germ oil composition Download PDF

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TWI603732B
TWI603732B TW102120899A TW102120899A TWI603732B TW I603732 B TWI603732 B TW I603732B TW 102120899 A TW102120899 A TW 102120899A TW 102120899 A TW102120899 A TW 102120899A TW I603732 B TWI603732 B TW I603732B
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mysterol
germ oil
sesamin
rice germ
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Yu Ipponmatsu
Yoshiko Ono
Namino Tomimori
Daisuke Takemoto
Toshiaki Sueyasu
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Description

含有芝麻素類及γ-米糠醇及米胚芽油之組成物 Composition containing sesamin and gamma-mysterol and rice germ oil

本發明係有關芝麻素類之體內吸收促進劑,以及利用該等飲食品或醫藥組成物等之組成物。另外,本發明亦有關將該組成物使用為抗氧化劑。 The present invention relates to an in vivo absorption enhancer for sesamin, and a composition using the food or drink, a pharmaceutical composition or the like. In addition, the invention also relates to the use of the composition as an antioxidant.

芝麻素類係芝麻中含有的木酚素化合物之一。其中,關於芝麻素與其立體異構物之表芝麻素,已知具有降低血中膽固醇作用以及降低血中中性脂質作用、改善肝功能作用、去除活性氧作用、阻礙△5不飽和化酵素作用、抑制過氧化脂質生成作用、抗高血壓作用、防止爛醉作用、抑制乳癌作用等各種生理活性(專利文獻1)。 Sesamin is one of the lignan compounds contained in sesame. Among them, sesamin with respect to sesamin and its stereoisomers is known to have a role in lowering blood cholesterol, lowering blood neutral lipids, improving liver function, removing reactive oxygen species, and inhibiting Δ5 desaturase. It inhibits various physiological activities such as a lipid peroxidation, an antihypertensive action, a detoxification prevention, and a breast cancer action (Patent Document 1).

然而,包含芝麻素類之木酚素類化合物,除了幾乎不溶於水之外,對可用於醫藥用或食用之有機溶媒,亦僅能溶解至某種程度。由於具有這般的難溶性,而存在木酚素類化合物在生體內難以被吸收之問題。 However, the lignan compound containing sesamin is only soluble in water, and it can only be dissolved to some extent in an organic solvent which can be used for medical use or consumption. Due to such poor solubility, there is a problem that lignan compounds are difficult to be absorbed in the living body.

提高包含芝麻素類之木酚素類化合物之體內吸收性之方法,已提案有例如利用乳化之方法(專利文獻1及2)。然而,更簡便之方法,例如僅藉由與其他化合物組合而提 高芝麻素類的體內吸收性例子之報告,並不多見。 A method of improving the in vivo absorbability of a lignan compound containing a sesamin-based compound has been proposed, for example, by a method of emulsification (Patent Documents 1 and 2). However, a simpler method, such as by simply combining with other compounds Reports of in vivo absorption of high sesamin are rare.

另一方面,已知含有芝麻素類及γ-米糠醇之組成物(專利文獻3)。另外,亦已知含有芝麻素類及米胚芽油之組成物(專利文獻4)。然而尚未明瞭該等組成物是否可提高芝麻素類之體內吸收性。 On the other hand, a composition containing sesamin and γ -mysterol is known (Patent Document 3). Further, a composition containing sesamin and rice germ oil is also known (Patent Document 4). However, it has not been known whether these compositions can increase the in vivo absorption of sesamin.

專利文獻1:WO2006/106926 Patent Document 1: WO2006/106926

專利文獻2:WO2008/044550 Patent Document 2: WO2008/044550

專利文獻3:特開2009-73749號公報 Patent Document 3: JP-A-2009-73749

專利文獻4:WO2007/037385 Patent Document 4: WO2007/037385

為使其形成目的為提高吸收性之乳化狀,必須使脂溶性物質均勻地乳化,且由於必須進行複雜的步驟,存在與成本增高相關的問題。本發明之課題係提供可解決該等問題點,且目的為促進芝麻素類之體內吸收之新穎的方法。 In order to form an emulsified form for the purpose of improving absorption, it is necessary to uniformly emulsify a fat-soluble substance, and since it is necessary to carry out complicated steps, there is a problem associated with an increase in cost. An object of the present invention is to provide a novel method which can solve such problems and which aims to promote absorption of sesamin in the body.

本發明團隊為解決上述課題專心檢討後,發現當組合使用芝麻素類、γ-米糠醇以及米胚芽油時,可促進芝麻素類之體內吸收。其效果於以特定比例使用γ-米糠醇以及米胚芽油時特別顯著。 In order to solve the above problems, the team of the present invention found that when sesamin, gamma -mysterol, and rice germ oil are used in combination, the in vivo absorption of sesamin can be promoted. The effect is particularly remarkable when γ -methanol and rice germ oil are used in a specific ratio.

因此,本發明係包含下述內容,但並未僅限定於此。 Therefore, the present invention includes the following contents, but is not limited thereto.

1. 一種組成物,其係含有至少一種芝麻素類、至少一種 γ-米糠醇、及米胚芽油之組成物,其特徵為:該γ-米糠醇之總重量:(該γ-米糠醇之總重量與該米胚芽油之重量的合計量)=1:4~1:66。 1. A composition, which system contains at least one sesamin-class compound, at least one of γ - m furfuryl alcohol, and the composition of the rice germ oil, wherein: the γ - m on the total weight of the furfuryl alcohol :( γ - m furfuryl alcohol The total weight is the sum of the weight of the rice germ oil) = 1:4~1:66.

2. 如1之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:20~1:60。 2. The composition of 1, wherein the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the alcohol with the total amount of rice germ by weight of the oil) = 1:20 to 1: 60

2a. 如2之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:25~1:55。 .. 2A The composition of 2, wherein the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the alcohol and the total amount of the rice germ oil by weight) = 1: 25 to 1:55.

2b. 如2a之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:32~1:54。 . The compositions 2b 2a of which the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the alcohol with the total amount of rice germ by weight of the oil) = 1: 32 to 1:54.

3. 如1~2b項中任一項之組成物,其中使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上。 3. The composition according to any one of items 1 to 2, wherein, when the total weight of the sesamin-class is 1, the total weight of the gamma -mysterol is 0.3 or more.

4. 如1~3項中任一項之組成物,其中前述芝麻素類係芝麻素及/或表芝麻素。 4. The composition according to any one of items 1 to 3, wherein the sesamin-class is sesamin and/or episesamin.

5. 如1~4項中任一項之組成物,其係經口用。 5. A composition according to any one of items 1 to 4 which is used orally.

6. 如1~5項中任一項之組成物,其係飲食物。 6. The composition according to any one of items 1 to 5, which is a food or drink.

7. 如1~6項中任一項之組成物,其係抗氧化劑。 7. The composition of any one of items 1 to 6, which is an antioxidant.

8. 一種促進體內吸收劑,其係促進至少一種芝麻素類之體內吸收,其係含有至少一種γ-米糠醇及米胚芽油作為有效成分。 8. An in vivo absorption promoting agent which promotes in vivo absorption of at least one sesamin, which comprises at least one gamma -mysterol and rice germ oil as an active ingredient.

9. 一種使用,其特徵為含有至少一種γ-米糠醇及米胚芽油作為有效成分之組成物用於製造至少一種芝麻素類之促 進體內吸收劑之使用。 9. Use of a composition comprising at least one gamma -mysterol and rice germ oil as an active ingredient for the manufacture of at least one sesamin-promoting in vivo absorbent.

10. 如8之促進體內吸收劑或9之使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:4~1:66。 10. The promotion of 8 or 9 of the absorbent body, wherein the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the furfuryl alcohol and the weight of rice germ oil total amount) = 1: 4 to 1 :66.

11. 如10之促進體內吸收劑或使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:20~1:60。 11. The absorbent body of promoting or 10, wherein the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the alcohol with the total amount of rice germ by weight of the oil) = 1: 20 ~ one sixty .

11a. 如11之促進體內吸收劑或使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:25~1:55。 11a of absorber 11 such as the promotion or in vivo, wherein the γ - :( total weight of the furfuryl alcohol meters γ - the total weight of the rice and the rice germ furfuryl alcohol by weight of the total amount of oil) = 1: 25 to 1:55 .

11b. 如11a之促進體內吸收劑或使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:32~1:54。 11a 11b The use of absorbers or promote in vivo, wherein the γ - :( total weight of the furfuryl alcohol meters γ - m on the total weight of the total amount of alcohol and the weight of the oil of the rice germ) = 1: 32 to 1:54 .

12. 如8~11b項中任一項之促進體內吸收劑或使用,其中使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上。 12. The in-vivo absorbent or use according to any one of items 8 to 11b, wherein the total weight of the sesame-containing sterol is 1 or more, and the total weight of the gamma -mysterol is 0.3 or more.

13. 如8~12項中任一項之促進體內吸收劑或使用,其中前述芝麻素類係芝麻素及/或表芝麻素。 13. The in vivo absorption or use according to any one of items 8 to 12, wherein the sesamin-class is sesamin and/or episesamin.

14. 如8~13項中任一項之促進體內吸收劑或使用,其中前述促進體內吸收劑係經口用。 14. The in vivo absorption or use of an absorbent according to any one of clauses 8 to 13, wherein the aforementioned in vivo absorption of the absorbent is oral.

15. 如1~7項中任一項之組成物,其中芝麻素類之總量係相對於組成物全量為1w/w%以上。 15. The composition according to any one of items 1 to 7, wherein the total amount of sesamin is 1 w/w% or more based on the total amount of the composition.

16. 一種方法,其係為了促進至少一種芝麻素類之體內吸收,其特徵為:該方法係包含投予該芝麻素類、至少一種 γ-米糠醇以及米胚芽油。 16. A method for promoting in vivo absorption of at least one sesamin, characterized in that the method comprises administering the sesamin, at least one gamma -mysterol, and rice germ oil.

根據本發明,將芝麻素類、γ-米糠醇以及米胚芽油組合使用時,可提高芝麻素類之體內吸收性。其效果於使後2成分之量以特定比例使用時特別顯著。因此,可不增加芝麻素類之投予量,而使其可更有效率地發揮生理活性。另外,本發明亦可顯著提高含芝麻素類、γ-米糠醇以及米胚芽油之組成物之抗氧化作用。因此,本發明亦提供可發揮優異的抗氧化作用之抗氧化劑。 According to the present invention, when sesamin, γ -mysterol, and rice germ oil are used in combination, the in vivo absorption of sesamin can be improved. This effect is particularly remarkable when the amount of the latter two components is used in a specific ratio. Therefore, the dosage of sesamin can be increased without increasing the physiological activity. Further, the present invention can also remarkably enhance the antioxidant action of a composition comprising sesamin, γ -mysterol and rice germ oil. Therefore, the present invention also provides an antioxidant which can exert an excellent antioxidant action.

另外,已知γ-米糠醇具有降低血中中性脂質作用、調節內分泌/自律神經作用、保護胃黏膜作用等各種生理作用。進而,由於芝麻素類及γ-米糠醇係來自植物而具有極高的安全性。因此本發明不僅可提高芝麻素類的吸收性,亦可期待γ-米糠醇所具有的有效的生理作用,並可提供可安全且可持續攝取的飲食品、醫藥用組成物。 In addition, γ -mysterol is known to have various physiological effects such as lowering the effect of neutral lipids in the blood, regulating endocrine/autonomic nerve action, and protecting the gastric mucosa. Further, since sesamin and γ -methanol are derived from plants, they are extremely safe. Therefore, the present invention can not only improve the absorbability of sesamin, but also an effective physiological action of γ -methanol, and can provide a food or drink and a pharmaceutical composition which can be safely and continuously ingested.

[圖1]圖1係表示腸道內被吸收之芝麻素以及表芝麻素量之圖。 Fig. 1 is a view showing the amount of sesamin and episesamin absorbed in the intestinal tract.

[圖2]圖2係表示△ORAC值之AUC之圖。 Fig. 2 is a view showing an AUC of a ΔORAC value.

[圖3]圖3係表示△ORAC值之AUC之圖。 Fig. 3 is a view showing an AUC of a ΔORAC value.

(芝麻素類) (sesame)

本發明之芝麻素類係包含芝麻素及其同功異質體全部的化合物之總稱。前述之芝麻素類同功異質體除表芝麻素外,可例舉如特開平4-9331號公報所記載之雙氧雜二環[3.3.0]辛烷衍生物。芝麻素類之具體例為芝麻素、芝麻醇、表芝麻醇、芝麻素酚等,可單獨使用其立體異構物或光學異構物體,或將其混合使用,於本發明中,以使用芝麻素及/或表芝麻素為佳。另外,芝麻素類之代謝體(例如記載於特開2001-139579號公報者),亦可於表現本發明效果之範圍內,做為包含於本發明芝麻素類之芝麻素類同功異質體,而使用於本發明。 The sesamin-class of the present invention is a generic term for all compounds including sesamin and its isoforms. In addition to the episesamin, the above-mentioned sesamin-based isoforms may, for example, be a dioxabicyclo[3.3.0]octane derivative described in JP-A-4-9331. Specific examples of the sesamin are sesamin, sesame alcohol, epiformyl alcohol, sesaminol, and the like, and stereoisomers or optical isomers thereof may be used singly or in combination, and in the present invention, sesame is used. It is better to use vegetarian and/or episesamin. In addition, the sesamin-like metabolites (for example, those disclosed in JP-A-2001-139579) may be used as the sesamin-like isoforms of the sesamin-containing compounds of the present invention within the range in which the effects of the present invention are exhibited. And used in the present invention.

本發明所使用的芝麻素類,未因其形態或製造方法等而有任何限制。例如選擇芝麻素作為芝麻素類時,一般可使用自芝麻油中以周知之方法(例如特開平4-9331號公報所記載之方法)所萃取出之芝麻素(稱為芝麻素萃取物或濃縮物),或直接使用市售之芝麻油(液狀)。但使用芝麻油時,因芝麻素的含量極低(一般未達1%),為獲得芝麻素之生理作用而欲摻混所需芝麻素時,因經配方組成物之單位投予量之體積過大,會造成不易攝取的情況。特別是進行經口投予用製劑化後,因製劑(錠劑、膠囊等)過大而發生攝取上的障礙。因此,自攝取量較少為佳之觀點而言,以使用自芝麻油之芝麻素萃取物(或芝麻素濃縮物)為佳。另外,因芝麻油特有風味而可能得到不佳的官能評價,可藉由周知之方法,例如活性白土處理等,對芝麻素萃取物 (或芝麻素濃縮物)進行無臭無味處理。 The sesamin used in the present invention is not limited by the form, the production method, and the like. For example, when sesamin is used as the sesamin, a sesamin extract (called a sesamin extract or concentrate) extracted from a sesame oil by a known method (for example, the method described in JP-A-4-9331) can be used. ), or directly use commercially available sesame oil (liquid). However, when sesame oil is used, since the content of sesamin is extremely low (generally less than 1%), when the desired sesamin is to be blended in order to obtain the physiological action of sesamin, the volume of the unit dose of the formulated composition is too large. Will cause difficulty in ingestion. In particular, after formulation for oral administration, there is an obstacle to ingestion due to an excessively large amount of the preparation (tablet, capsule, etc.). Therefore, it is preferable to use a sesamin extract (or sesamin concentrate) derived from sesame oil from the viewpoint that the amount of intake is small. In addition, due to the unique flavor of sesame oil, poor sensory evaluation may be obtained, and the sesamin extract may be obtained by a known method such as active clay treatment. (or sesamin concentrate) for odorless and odorless treatment.

因此,芝麻素類,以使用藉由將芝麻油等來自食品素材進行萃取及/或純化後,使所得之芝麻素類含有濃度增加之芝麻素類濃縮物為佳。濃縮程度可根據所使用的芝麻素類之種類及摻混組成物之形態,適當地加以設定,一般係以使用將芝麻素類之總量濃縮為1w/w%以上之芝麻素類濃縮物為佳。芝麻素類濃縮物中之芝麻素類總含量以濃縮(純化)為20w/w%以上更佳,50w/w%以上,70w/w%以上,進而90w/w%以上者最佳。 Therefore, the sesamin-based concentrate is preferably obtained by extracting and/or purifying the obtained sesamin-containing material from a food material, and then obtaining the sesamin-containing concentrate having an increased concentration. The degree of concentration can be appropriately set depending on the type of sesamin used and the form of the blended composition, and generally, a sesamin concentrate obtained by concentrating the total amount of sesamin into 1 w/w% or more is used. good. The total sesamin content in the sesamin concentrate is preferably 20 w/w% or more, more preferably 50 w/w% or more, 70 w/w% or more, and further preferably 90 w/w% or more.

芝麻素類之含量可使用HPLC法等周知之任一種方法進行測定。有關HPLC法可參考例如特開2009-155312號公報中記載之方法等。 The content of the sesamin can be measured by any one of known methods such as HPLC. For the HPLC method, for example, the method described in JP-A-2009-155312, and the like can be referred to.

(γ-米糠醇以及米胚芽油) ( γ -mysterol and rice germ oil)

可促進芝麻素類之體內吸收的有效成分之一係γ-米糠醇。已知γ-米糠醇具有降低血液中中性脂質作用(Geriant.med.19,1812-1840,1981)、調節內分泌/自律神經作用(日藥理誌,75(4),399-403,1979)、保護胃黏膜作用(日藥理誌,84(6),537-542,1984)等各種生理作用,經純化者已被認可作為高血脂症治療劑及身心症(更年期障礙、過敏性大腸激躁症)之治療劑等醫藥品。本發明中使用之γ-米糠醇係指阿魏酸經酯鍵結與三萜烯醇或固醇結合者之總稱。前述之三萜烯醇可舉出例如環木菠蘿烯醇、24-亞甲基環木菠蘿烷醇、環木菠蘿烷醇、環布來醇等, 固醇可舉例如菜油固醇、黃豆固醇、β-榖固醇等。本發明中,可單獨使用該等化合物,亦可以混合物形式使用。γ-米糠醇之定量法,可適當地使用UV吸光度法及HPLC法等周知之方法。例如,如「類醫藥品原料規格」及「化學性合成品以外之食品添加物自主規格」記載般,使檢體溶解於庚烷中,使用於315nm附近吸收之極大波長,藉由測定吸光度,可進行定量。 One of the active ingredients which can promote the absorption of sesamin in the body is γ -methanol. It is known that γ -methanol has a role in lowering neutral lipids in the blood (Geriant. med. 19, 1812-1840, 1981) and regulating endocrine/autonomic nervous effects (Japanese Medicine, 75(4), 399-403, 1979). It protects the gastric mucosa (Japanese Medicine, 84 (6), 537-542, 1984) and other physiological effects. It has been approved as a therapeutic agent for hyperlipemia and psychosis (menopausal disorders, allergic bowel irritation). Medicines such as therapeutic agents. The γ -mysterol used in the present invention is a generic term for a combination of ferulic acid ester bond with triterpene alcohol or sterol. Examples of the triterpene alcohol include cyclocarenol, 24-methylenecycloartanol, cycloartanol, cyclodextrol, and the like. The sterol may, for example, be vegetable sterol or soybean solid. Alcohol, β-steroids, and the like. In the present invention, these compounds may be used singly or in the form of a mixture. As a method of quantifying γ -methanol, a well-known method such as a UV absorbance method or an HPLC method can be suitably used. For example, as described in "Standards for Pharmaceutical Raw Materials" and "Independent Specifications for Food Additives Other than Chemically Synthetic Products", the sample is dissolved in heptane and used to measure the absorbance at a maximum wavelength absorbed near 315 nm. Can be quantified.

已知糙米、玉米、大麥等中含有γ-米糠醇。γ-米糠醇亦含於自糙米萃取之油脂的米糠油中。 It is known that brown rice, corn, barley, and the like contain γ -methanol. Gamma -mysterol is also contained in rice bran oil from the oil extracted from brown rice.

另外,γ-米糠醇亦含於促進芝麻素類之體內吸收的有效成分之一之米胚芽油中。米胚芽油係自米的胚芽所萃取的油脂,一般認為米胚芽油中含有的γ-米糠醇約1.0~1.5w/w%(該濃度係以含γ-米糠醇重量之米胚芽油之總重量為標準)。米胚芽油之含有量可使用周知之任一種方法進行測定。例如,米胚芽油之含量可利用米胚芽油或米胚芽油濃縮物中特有的固醇之含量,以及各種固醇的含有比例作為指標而進行測定。具體而言,由於米胚芽油,與游離型固醇相比,結合型固醇含量較多,因此可以固醇組成為基礎,判斷某組成物中是否含有米胚芽油。另外,由於米胚芽油中菜油固醇與黃豆固醇之含量較高,可將該等之含有量,作為為了測定米胚芽油含量之指標。 Further, γ -methanol is also contained in rice germ oil which is one of active ingredients which promotes absorption of sesamin in the body. The rice germ oil is a fat extracted from the germ of rice. It is generally considered that the γ -mysterol contained in the rice germ oil is about 1.0 to 1.5 w/w% (this concentration is the total amount of rice germ oil containing the weight of γ -methanol). The weight is standard). The content of the rice germ oil can be measured by any of the known methods. For example, the content of the rice germ oil can be measured by using the content of the sterol which is peculiar to the rice germ oil or the rice germ oil concentrate, and the content ratio of various sterols as an index. Specifically, since rice germ oil has a large amount of bound sterol compared with free sterol, it can be judged whether or not a certain composition contains rice germ oil based on the sterol composition. In addition, since the content of the vegetable oil sterol and the soybean sterol in the rice germ oil is high, the content of these may be used as an index for determining the content of the rice germ oil.

本發明所使用的γ-米糠醇以及米胚芽油,未因其來源及形態、製造方法等而有任何限制。 The γ -mysterol and rice germ oil used in the present invention are not limited by the source, form, production method and the like.

例如,γ-米糠醇可直接使用市售的米胚芽油等,但 如上所述般,米胚芽油中含有的γ-米糠醇量並不高。因此,為使以後述之比例摻混γ-米糠醇以及米胚芽油,僅摻混該二種並不充分。因此之故,取代該二種,或以追加的形式,以使用γ-米糠醇含量高者為佳,例如以使用來自米糠油及米胚芽油等之γ-米糠醇濃縮物為佳。使用γ-米糠醇濃縮物時,γ-米糠醇濃縮物中γ-米糠醇含量,以總量而言,以2w/w%以上為佳,30w/w%以上更佳(該等之濃度係以含γ-米糠醇重量之濃縮物之總重量為標準)。該等γ-米糠醇濃縮物可為以工業方式,使用有機溶劑自米糠油以及米胚芽油中萃取,或利用樹脂處理後進行純化後可得,例如,可購入米胚芽油γ 30(築野食品工業股份有限公司)、γ-米糠醇、OrizadorimuV-50、米糠油、糙米胚芽油(ORYZA油化股份有限公司)。 For example, γ -mysterol can be directly used as a commercially available rice germ oil, but as described above, the amount of γ -mysterol contained in the rice germ oil is not high. Therefore, in order to blend γ -mysterol and rice germ oil in the ratio described later, it is not sufficient to merely blend the two. Accordingly, therefore, the two kinds of substituted or added in the form of using gamma] - meters high alcohol content is preferred, for example using gamma] from rice bran and rice germ oil - A furfuryl alcohol rice concentrate better. When the γ -mysterol concentrate is used, the γ -mysterol content in the γ -mysterol concentrate is preferably 2 w/w% or more in terms of the total amount, more preferably 30 w/w% or more (these concentrations are Based on the total weight of the concentrate containing gamma -mysterol. The γ -mysterol concentrate can be obtained by industrially extracting from rice bran oil and rice germ oil using an organic solvent, or after purification by treatment with a resin, for example, rice germ oil γ 30 can be purchased. Food Industry Co., Ltd.), γ -methanol, Orizadorimu V-50, rice bran oil, brown rice germ oil (ORYZA Oil Chemical Co., Ltd.).

米胚芽油目前有使用例如含有1.2~1.5%之γ-米糠醇(該濃度係以含γ-米糠醇之量之米胚芽油之總重量為標準)ORYZA Oil S-1(一丸自然美健公司)、含有1.0~1.5%之γ-米糠醇(該濃度係以含γ-米糠醇之量之米胚芽油之總重量為標準)米胚芽油PRO-15(築野食品工業股份有限公司)等名稱於市面販售。 Rice germ oil is currently used, for example, containing 1.2 to 1.5% of γ -mysterol (this concentration is based on the total weight of rice germ oil containing γ -mysterol) ORYZA Oil S-1 (Yumaru Natural Beauty Co., Ltd.) Having a 1.0-1.5% γ -mycohol (this concentration is based on the total weight of rice germ oil containing γ -mysterol), such as rice germ oil PRO-15 (Tsino Food Industry Co., Ltd.) It is sold in the market.

(含芝麻素類與γ-米糠醇及米胚芽油之組成物) (Constituents containing sesamin and γ -mysterol and rice germ oil)

根據本發明,當組合使用芝麻素類、γ-米糠醇以及米胚芽油時,可達成提高芝麻素類之體內吸收性。因此,於可有效率地發揮其生理活性的同時,藉由各成分所具有 的生理作用,可期待對於增進健康之效果。 According to the present invention, when sesamin, gamma -mysterol, and rice germ oil are used in combination, it is possible to improve the in vivo absorption of sesamin. Therefore, the physiological activity of each component can be exhibited efficiently, and the effect of improving health can be expected by the physiological action of each component.

本發明之含芝麻素類、γ-米糠醇以及米胚芽油之組成物(飲食品、醫藥組成物等)中各成分之摻混量以及摻混比例,如後所述,於可促進芝麻素類之體內吸收,可有效率地發揮其生理活性的範圍內適當選擇為佳。 The blending amount and blending ratio of each component in the composition (food and beverage, pharmaceutical composition, etc.) of the sesamin-containing, gamma -mysterol, and rice germ oil of the present invention can promote sesamin as described later. It is preferred that the absorption in the body can be appropriately selected within the range in which physiological activity can be exerted efficiently.

本發明之組成物中,若為期待可促進芝麻素類之體內吸收效果時,所含有的γ-米糠醇之總重量,相對於γ-米糠醇之總重量與米胚芽油重量之合計量之比例,以1:4~1:66為佳,1:8.7~1:62,1:20~1:60更佳,1:25~1:55,1:32~1:54或1:32.4~53.2,更佳係1:32~1:49。且,所使用的米胚芽油中含有γ-米糠醇時,與本發明有關記載之米胚芽油之重量,在規定相同的範圍內,並非含有γ-米糠醇重量之總量,係意指自總量中去掉γ-米糠醇之重量。 In the composition of the present invention, when it is expected to promote the in vivo absorption effect of sesamin, the total weight of γ -mysterol contained is the total amount of γ -mysterol and the weight of the rice germ oil. Proportion, preferably 1:4~1:66, 1:8.7~1:62, 1:20~1:60 is better, 1:25~1:55, 1:32~1:54 or 1:32.4 ~53.2, better system 1:32~1:49. Further, when the rice germ oil to be used contains γ -mysterol, the weight of the rice germ oil described in the present invention is not in the same range as the weight of the γ -mysterol, and means The weight of γ -methanol was removed from the total amount.

另外,以所含芝麻素類之總重量為1時,γ-米糠醇之總重量以0.3以上為佳,更佳係0.4以上,0.6以上,0.69以上,0.8以上,1.0以上更佳。並未特別限制該值之上限,例如可為5.0以下,更佳係3.0以下,1.6以下,1.5以下,1.4以下,1.39以下,1.2以下,1.1以下,進而更佳為1.06以下。本發明係包含該等上限值以及下限值之全部之組合。以芝麻素類之總重量為1時,γ-米糠醇較佳之總重量範圍之例如下所述:0.3~5.0,0.3~3.0,0.3~1.6,0.3~1.5,0.3~1.4,0.3~1.39,0.3~1.2,0.3~1.1,0.3~1.06; 0.4~5.0,0.4~3.0,0.4~1.6,0.4~1.5,0.4~1.4,0.4~1.39,0.4~1.2,0.4~1.1,0.4~1.06;0.6~5.0,0.6~3.0,0.6~1.6,0.6~1.5,0.6~1.4,0.6~1.39,0.6~1.2,0.6~1.1,0.6~1.06;0.69~5.0,0.69~3.0,0.69~1.6,0.69~1.5,0.69~1.4,0.69~1.39,0.69~1.2,0.69~1.1,0.69~1.06;0.8~5.0,0.8~3.0,0.8~1.6,0.8~1.5,0.8~1.4,0.8~1.39,0.8~1.2,0.8~1.1,0.8~1.06;1.0~5.0,1.0~3.0,1.0~1.6,1.0~1.5,1.0~1.4,1.0~1.39,1.0~1.2,1.0~1.1,1.0~1.06。特別適合的範圍為例如0.69~1.39,0.69~1.06。 Further, when the total weight of the sesamin-containing compound is 1, the total weight of γ -methanol is preferably 0.3 or more, more preferably 0.4 or more, 0.6 or more, 0.69 or more, 0.8 or more, and more preferably 1.0 or more. The upper limit of the value is not particularly limited, and may be, for example, 5.0 or less, more preferably 3.0 or less, 1.6 or less, 1.5 or less, 1.4 or less, 1.39 or less, 1.2 or less, 1.1 or less, and still more preferably 1.06 or less. The invention includes all combinations of such upper and lower limits. When the total weight of the sesamin-class is 1, the preferred total weight range of γ-mysterol is as follows: 0.3 to 5.0, 0.3 to 3.0, 0.3 to 1.6, 0.3 to 1.5, 0.3 to 1.4, 0.3 to 1.39, 0.3~1.2, 0.3~1.1, 0.3~1.06; 0.4~5.0, 0.4~3.0, 0.4~1.6, 0.4~1.5, 0.4~1.4, 0.4~1.39, 0.4~1.2, 0.4~1.1, 0.4~1.06; 0.6~ 5.0, 0.6~3.0, 0.6~1.6, 0.6~1.5, 0.6~1.4, 0.6~1.39, 0.6~1.2, 0.6~1.1, 0.6~1.06; 0.69~5.0, 0.69~3.0, 0.69~1.6, 0.69~1.5, 0.69~1.4, 0.69~1.39, 0.69~1.2, 0.69~1.1, 0.69~1.06; 0.8~5.0, 0.8~3.0, 0.8~1.6, 0.8~1.5, 0.8~1.4, 0.8~1.39, 0.8~1.2, 0.8~ 1.1, 0.8~1.06; 1.0~5.0, 1.0~3.0, 1.0~1.6, 1.0~1.5, 1.0~1.4, 1.0~1.39, 1.0~1.2, 1.0~1.1, 1.0~1.06. A particularly suitable range is, for example, 0.69 to 1.39, 0.69 to 1.06.

有關摻混量,本發明之組成物中無論組成物之全重量,可摻混之芝麻素類量以1~100mg為佳,1~50mg更佳,3~30mg最佳。γ-米糠醇則可摻混1~100mg為佳,1~60mg更佳,3~30mg最佳。米胚芽油以1~5000mg,10~1000mg更佳,30~500mg之程度摻混最佳。 Regarding the blending amount, the amount of the sesamin compound which can be blended in the composition of the present invention is preferably from 1 to 100 mg, more preferably from 1 to 50 mg, and most preferably from 3 to 30 mg. Γ -methanol can be blended with 1~100mg, preferably 1~60mg, and 3~30mg. Rice germ oil is best blended with 1~5000mg, 10~1000mg, and 30~500mg.

無論組成物之全重量,本發明之組成物中之芝麻素類典型的總摻合比例以1w/w%以上,1~50w/w%更佳,1~10w/w%最佳。另外,γ-米糠醇典型的總摻合比例,相對於組成物全量以0.1~50w/w%,0.5~30w/w%更佳,1~10w/w%最佳。米胚芽油典型的總摻合比例,相對於組成物全量以5~99w/w%,20~98w/w%更佳,50~95w/w%最佳。 The total blending ratio of sesamin in the composition of the present invention is preferably 1 w/w% or more, more preferably 1 to 50 w/w%, and most preferably 1 to 10 w/w%, regardless of the total weight of the composition. Further, the typical total blending ratio of γ -mysterol is preferably 0.1 to 50 w/w%, more preferably 0.5 to 30 w/w%, and most preferably 1 to 10 w/w%, based on the total amount of the composition. The typical total blending ratio of rice germ oil is 5~99w/w%, 20~98w/w% is better, and 50~95w/w% is the best relative to the total amount of the composition.

另外,本發明組成物之形態為液劑時,芝麻素類典型 的總摻合比例以0.001w/w%以上,0.001~0.5w/w%更佳,0.001~0.05w/w%最佳,γ-米糠醇典型的總摻合比例,相對於組成物全量以0.0001~0.1w/w%,0.0005~0.05w/w%更佳,0.001~0.02w/w%最佳,米胚芽油典型的總摻合比例,相對於組成物全量以0.05~5w/w%,0.1~2.5w/w%更佳,0.2~1w/w%最佳。 Further, when the form of the composition of the present invention is a liquid preparation, a typical total blending ratio of sesamin is 0.001 w/w% or more, more preferably 0.001 to 0.5 w/w%, and most preferably 0.001 to 0.05 w/w%. The typical total blending ratio of γ -methanol is 0.0001~0.1w/w%, 0.0005~0.05w/w% is better, 0.001~0.02w/w% is best, and rice germ oil is typical. The total blending ratio is preferably 0.05 to 5 w/w%, more preferably 0.1 to 2.5 w/w%, and most preferably 0.2 to 1 w/w%, relative to the total amount of the composition.

並未特別限制本發明組成物之形態及攝取路徑。然而,本發明中以期望增進健康為目的而攝取時,以經口用組成物之形式進行攝取為佳。 The form and the ingestion route of the composition of the present invention are not particularly limited. However, in the present invention, it is preferred to take it in the form of an oral composition when it is ingested for the purpose of improving health.

本發明之組成物,於不會損及其效果的範圍內,除芝麻素類、γ-米糠醇以及米胚芽油之外,亦可摻混其他任一種期望之成分。例如維生素E,維生素C等維生素類、礦物質類、荷爾蒙、營養成分、香料等生理活性成分之外,亦可適當地摻混於製劑化時摻混的乳化劑、等張化劑、緩衝劑、溶解輔助劑、防腐劑、安定化劑、抗氧化劑等。 In the composition of the present invention, in addition to sesamin, gamma -mysterol, and rice germ oil, any other desired component may be blended in a range that does not impair the effect. For example, vitamin E, vitamin C and other vitamins, minerals, hormones, nutrients, spices and other physiologically active ingredients, may also be suitably blended in the formulation of the emulsifier, isotonic agent, buffer , dissolution aids, preservatives, stabilizers, antioxidants, etc.

由於本發明之組成物具有優異的抗氧化作用,可使用為抗氧化劑,亦即可使用為目的為於生體內發揮抗氧化作用之組成物。抗氧化劑之使用係例如與消除生體內的活性氧、改善肝功能、抑制生體內過氧化脂質之生成、或改善熱量代謝,以及與下述疾病或狀態之預防或防止相關連;皮膚的皺紋、皮膚的斑點、肌膚的鬆弛、疲勞、代謝症候群、糖尿病、動脈硬化、高血壓、癌症、發炎或老化。因此,本發明之抗氧化劑係可有效應用於該等用途。 Since the composition of the present invention has an excellent antioxidant action, it can be used as an antioxidant, and can be used as a composition for exhibiting an antioxidant action in a living body. The use of antioxidants is, for example, associated with elimination of active oxygen in the living body, improvement of liver function, inhibition of the production of lipid peroxides in the body, or improvement of caloric metabolism, and prevention or prevention of diseases or conditions described below; wrinkles of the skin, Spots on the skin, sagging of the skin, fatigue, metabolic syndrome, diabetes, arteriosclerosis, hypertension, cancer, inflammation or aging. Therefore, the antioxidant of the present invention can be effectively applied to such applications.

體內吸收促進劑、體內吸收促進方法 In vivo absorption enhancer, in vivo absorption promotion method

如上所述,藉由組合使用芝麻素類、γ-米糠醇以及米胚芽油,可使芝麻素類之體內吸收性顯著地被增強。因此,本發明從另一面相而言,係含有以γ-米糠醇以及米胚芽油為有效成分之芝麻素類之體內吸收促進劑。另外,本發明亦有關含有以γ-米糠醇以及米胚芽油為有效成分之組成物,用於製造芝麻素類之促進體內吸收劑之使用。另外,本發明從另一面相而言,係用於促進芝麻素類之體內吸收之方法,亦為有關包含投予該當芝麻素類、γ-米糠醇以及米胚芽油之方法。投予對象係具有該等促進體內吸收之需要,包含人類等哺乳動物。 As described above, by using sesamin, γ -mysterol, and rice germ oil in combination, the in vivo absorption of sesamin can be remarkably enhanced. Therefore, the present invention contains, in another aspect, an in vivo absorption enhancer of sesamin-containing γ -mysterol and rice germ oil as an active ingredient. Further, the present invention relates to a composition for promoting the in vivo absorption of a composition comprising γ -mysterol and rice germ oil as an active ingredient for producing sesamin. Further, the present invention is a method for promoting in vivo absorption of sesamin from the other surface, and is also a method comprising administering the sesamin, gamma -mysterol, and rice germ oil. The subject to be administered has such a need to promote absorption in the body, and includes mammals such as humans.

該促進體內吸收劑、組成物以及方法中,芝麻素類、γ-米糠醇以及米胚芽油之使用比例、摻混率、摻混量、攝取量等,可以與含有芝麻素類、γ-米糠醇以及米胚芽油之組成物有關之上述數值為基礎而適當地加以決定。所使用之芝麻素類、γ-米糠醇以及米胚芽油之種類亦相同。 In the body-absorbing absorbent, composition, and method, the use ratio, blending ratio, blending amount, and intake amount of sesamin, γ -mysterol, and rice germ oil may be combined with sesamin-containing and γ -mysterol. The above values based on the composition of the rice germ oil are appropriately determined based on the above values. The types of sesamin, gamma -mysterol, and rice germ oil used are also the same.

飲食品以及醫藥品 Food and beverages and pharmaceuticals

本發明之組成物以及促進體內吸收劑,適合提供於飲食品(功能性食品、健康輔助品、營養功能食品、特別用途食品、特定保健用食品、營養輔助食品、飲食療法用食品、健康食品、營養補充品等)以及醫藥品之形態。該等 飲食品以及醫藥品中,包含含芝麻素類、γ-米糠醇以及米胚芽油之飲食組成物以及醫藥組成物,以及含有或經添加該當組成物之飲食品以及醫藥品。另外,本發明亦包含含有或經添加含γ-米糠醇以及米胚芽油作為有效成分之芝麻素類之促進體內吸收劑之飲食品或醫藥品。 The composition of the present invention and the absorption promoting agent in the body are suitably supplied to foods and drinks (functional foods, health supplements, nutritional functional foods, special purpose foods, specific health foods, nutritional supplement foods, diet therapy foods, health foods, nutrition). Supplements, etc.) and the form of pharmaceuticals. These foods and drinks and pharmaceuticals include a dietary composition containing sesamin, gamma -mysterol, and rice germ oil, and a pharmaceutical composition, and a food or beverage and a pharmaceutical containing or adding the composition. Further, the present invention also includes a food or drink or a pharmaceutical preparation containing an in vivo absorption agent containing sesamin containing γ -mysterol and rice germ oil as an active ingredient.

另外,飲食品以及醫藥品,亦可作為寵物的飼料進行加工之寵物食品及動物飼料等,以及動物用醫藥品。 In addition, foods and beverages and pharmaceuticals can also be used as pet food, animal feed, and animal foods.

含有芝麻素類、γ-米糠醇以及米胚芽油之飲食品以及醫藥品,被認為可使用於目的為獲得芝麻素類所具有的降低血中膽固醇作用以及降低血中中性脂質作用、改善肝功能作用、去除活性氧作用、阻礙△5不飽和化酵素作用、抑制過氧化脂質生成作用、抗高血壓作用、防止爛醉作用、抑制乳癌作用等各種具有功效的生理作用。另外,含γ-米糠醇以及米胚芽油之芝麻素類之促進體內吸收劑之飲食品以及醫藥品,可被使用於目的為使芝麻素類有效率地發揮上述各種生理作用。 Foods and beverages containing sesamin, gamma -mysterol, and rice germ oil, and pharmaceuticals, are considered to be useful for the purpose of obtaining blood cholesterol lowering action and lowering blood neutral lipid action and improving liver in order to obtain sesamin Functional effects, removal of reactive oxygen species, inhibition of Δ5 desaturase, inhibition of lipid peroxidation, antihypertensive effects, prevention of detoxification, inhibition of breast cancer, and other physiological effects. In addition, foods and beverages and pharmaceuticals for promoting the in vivo absorption of sesamin-containing γ -methanol and rice germ oil can be used for the purpose of causing sesamin to efficiently exhibit various physiological actions as described above.

將本發明之組成物提供為飲食品時,其形態可以錠劑、膠囊劑、粉末劑、顆粒劑、飲料劑(包含溶液劑以及懸濁液劑)等健康食品之形態提供,亦可以清涼飲料、茶飲料、優格及乳酸菌飲料等乳製品、調味料、加工食品、甜點類、零食(例如口香糖、糖果、果凍)之形態提供,但並未限定於該等項目。 When the composition of the present invention is provided as a food or drink, the form may be provided in the form of a health food such as a tablet, a capsule, a powder, a granule, a drink (including a solution and a suspension), or a refreshing drink. Milk, beverages, yoghurt and lactic acid bacteria beverages are provided in the form of dairy products, seasonings, processed foods, desserts, snacks (eg chewing gum, candy, jelly), but are not limited to such items.

另外,將本發明之組成物利用為醫藥品時,其投予形態可為經口投予,亦可利用為注射劑等形態進行投予,各 種適合投予之製劑可適當地使用周知者。例如,適合用於經口投予之製劑,包含錠劑、膠囊劑、散劑、顆粒劑、溶液劑、懸濁液劑、糖漿劑等,但未限定於該等劑型。 Further, when the composition of the present invention is used as a pharmaceutical, the administration form may be oral administration, or may be administered in the form of an injection or the like, each of which may be administered. A formulation suitable for administration can be suitably used by a well-known person. For example, a preparation suitable for oral administration includes a tablet, a capsule, a powder, a granule, a solution, a suspension, a syrup, and the like, but is not limited to the dosage forms.

將芝麻素類、γ-米糠醇以及米胚芽油個別製劑化,再將該等於幾乎同時間,或於服用其中一種製劑後,於其效果持續的期間內再服用另一個製劑,可獲得本發明所希望的芝麻素類之促進體內吸收作用。因此,可將γ-米糠醇以及米胚芽油共同製劑,或個別含有芝麻素類之促進體內吸收劑,與含有芝麻素類組成物之試劑組等,亦包含於本發明之範圍。試劑組中個別所含之各成分,可同時攝取,亦可逐次或個別地進行攝取。 The invention is obtained by separately formulating sesamin, γ -mysterol and rice germ oil, and then taking another preparation at a time equal to or at the same time, after taking one of the preparations, and taking another preparation for the duration of the effect. The desired sesamin-like substances promote absorption in the body. Therefore, a co-formulation of γ -methanol and rice germ oil, a body-inducing agent containing sesamin alone, a reagent group containing a sesamin-based composition, and the like are also included in the scope of the present invention. Each component contained in the reagent group may be ingested at the same time, or may be ingested sequentially or individually.

為明確化而記載時,本說明書中以上限值與下限值表示之數值範圍,亦即「下限值~上限值」係包含該等下限值以及上限值。例如以「1~2」表示之範圍,包含1以及2。 In the description of the clarification, the numerical range indicated by the upper limit and the lower limit in the present specification, that is, the "lower limit to the upper limit" includes the lower limit and the upper limit. For example, the range indicated by "1~2" includes 1 and 2.

[實施例] [Examples]

以下藉由試驗例以及實施例更具體說明本發明,但本發明並未該等例示而有所限制。 The present invention will be more specifically described by the following examples and examples, but the invention is not limited thereto.

實施例1. 利用腸管外翻模式之吸收性檢討 Example 1. Absorption review using the bowel valgus pattern <實驗方法> <Experimental method>

使SD系雄性大鼠(7週齡)於試驗環境下進行馴化後,用於實驗。於麻醉下開腹並將其放血後,立刻自幽門 摘出約15cm的小腸(主要是空腸),並分割為2部分。於單側綁上繩子,並使內側反轉至外側,充滿調整液(內液:NaCl 140mM,CaCl2 0.1mM,MgCl2 0.5mM,D-mannose 40mM,Ascorbic acid 0.8mM,10mM Tris,pH7.4)之後,再於另一側綁上繩子,製作為5cm的外翻腸管。於0.5ml之對照溶液或試驗溶液中,添加含有膽酸鈉與白蛋白之調整液4.5ml後,進行3分鐘之超音波處理製作為乳化狀,並將其作為外液。將外翻腸管浸入各外液中,混合後於37℃下進行培育。1小時後取出外翻腸管,回收內液並測定重量。取20μl之內液,以50%甲醇稀釋10倍,進行離心分離後將上清液以過濾器過濾後,測定其中芝麻素混合物之濃度。吸收量係利用濃度乘以回收液量而計算。芝麻素混合物之測定可參考過去之報告(特開2009-155312號等),使用HPLC實施測定。 SD male rats (7 weeks old) were acclimated in the test environment and used for experiments. Immediately after anesthesia was opened and blood was exsanguin, a small intestine (mainly jejunum) of about 15 cm was taken from the pylorus and divided into two parts. Tied the rope on one side and reversed the inside to the outside, filled with the adjustment solution (internal solution: NaCl 140 mM, CaCl 2 0.1 mM, MgCl 2 0.5 mM, D-mannose 40 mM, Ascorbic acid 0.8 mM, 10 mM Tris, pH 7. 4) After that, the rope was tied to the other side to make a 5 cm valgus intestine. To 0.5 ml of the control solution or the test solution, 4.5 ml of an adjustment solution containing sodium cholate and albumin was added, and then subjected to ultrasonic treatment for 3 minutes to prepare an emulsified form, which was used as an external solution. The everted intestinal tube was immersed in each external solution, mixed, and then incubated at 37 °C. After 1 hour, the everted intestinal tube was taken out, and the internal liquid was recovered and the weight was measured. 20 μl of the inner solution was taken, diluted 10 times with 50% methanol, centrifuged, and the supernatant was filtered through a filter, and the concentration of the sesamin mixture was measured. The amount of absorption is calculated by multiplying the concentration by the amount of recovered liquid. For the measurement of the mixture of the sesamin, the measurement can be carried out using HPLC using the above-mentioned report (Japanese Patent Laid-Open No. 2009-155312, etc.).

對照群係使用100mg之芝麻素混合物(芝麻素:表芝麻素=1:1),250mg之米胚芽油濃縮物(米胚芽油γ 30S:含30% γ-米糠醇,含70%米胚芽油,築野食品工業股份有限公司),4250mg之橄欖油(Nakaraitesuku股份有限公司)加熱混合均勻者,另外試驗群係使用100mg之芝麻素混合物(芝麻素:表芝麻素=1:1),250mg之米胚芽油濃縮物(米胚芽油γ 30S:含30% γ-米糠醇,含70%米胚芽油,築野食品工業股份有限公司),4250mg之米胚芽油(米胚芽油PRO-15:1.5% γ-米糠醇,含98.5%米胚芽油,築野食品工業股份有限公司)加熱混合均勻者。亦即,投 予對照群之組成物中,γ-米糠醇:(γ-米糠醇+米胚芽油)之重量比係1:3.3。投予試驗群之組成物中,γ-米糠醇:(γ-米糠醇+米胚芽油)之重量比係1:32.4。對照群、試驗群均以n=4實施。 The control group used a mixture of 100 mg of sesamin (sesame: episesamin = 1:1), 250 mg of rice germ oil concentrate (rice germ oil γ 30S: containing 30% γ -mysterol, containing 70% rice germ oil) , Chikuno Food Industry Co., Ltd.), 4250mg of olive oil (Nakaraitesuku Co., Ltd.) heated and mixed evenly, and the test group used 100mg of sesamin mixture (sesame: episesamin = 1:1), 250mg Rice germ oil concentrate (rice germ oil γ 30S: containing 30% γ -mysterol, containing 70% rice germ oil, Chino Food Industry Co., Ltd.), 4250mg rice germ oil (rice germ oil PRO-15: 1.5 % γ -myristyl alcohol, containing 98.5% rice germ oil, Chino Food Industry Co., Ltd.) heated and evenly mixed. That is, the weight ratio of γ -methanol: ( γ -mysterol + rice germ oil) to the composition of the control group was 1:3.3. In the composition of the test group, the weight ratio of γ -methanol: ( γ -mysterol + rice germ oil) was 1:32.4. The control group and the test group were all performed with n=4.

<結果> <Result>

結果示於圖1。比較培育1小時後內液中的芝麻素以及表芝麻素之吸收量,對照群芝麻素為16.19μg,表芝麻素為16.23μg,試驗群芝麻素為24.29μg,表芝麻素為23.89μg,芝麻素以及表芝麻素同樣變為約1.5倍,確認吸收量顯著增加。自上述結果可明確得知,組合使用芝麻素類、γ-米糠醇以及米胚芽油時,進而藉由以特定比例使用γ-米糠醇以及米胚芽油,可顯著促進芝麻素類之體內吸收。特別藉由使γ-米糠醇之重量之相對於γ-米糠醇以及米胚芽油之合計重量之比例,較對照群之比例之1:3.3更為降低,可獲得顯著的促進體內吸收效果。 The results are shown in Figure 1. The absorption amount of sesamin and episesamin in the inner solution was compared after 1 hour of incubation. The control group was 16.19 μg of sesamin, 16.23 μg of episesamin, 24.29 μg of test group sesamin, and 23.89 μg of episemin. The selenium and the episesamin were also about 1.5 times, and it was confirmed that the absorption amount was remarkably increased. As is clear from the above results, the combined use of sesamin, gamma] - when m furfuryl alcohol and rice germ oil, and further by using a specific ratio gamma] - m rice germ oil and alcohol, can significantly promote the absorption of sesamin-class compounds in vivo. In particular by making γ - m the weight of furfuryl alcohol with respect to γ - m and the ratio of total alcohol of the weight of rice germ oil, compared with the control group the ratio of 1: 3.3 is more reduced, can be obtained in vivo absorption promoting significant effect.

實施例2. 配方例 Example 2. Formulation example (製劑例1)顆粒劑 (Formulation Example 1) granules

將上述物質均勻混合後,加入100ml之10%羥丙基纖維素/乙醇溶液,依據常用方法進行混合、壓出、乾燥後得顆粒劑。 After uniformly mixing the above materials, 100 ml of a 10% hydroxypropylcellulose/ethanol solution was added, and mixed, pressed, and dried according to a usual method to obtain granules.

(製劑例2)膠囊劑 (Formulation Example 2) capsule

將依上述成分所製成之膠囊劑皮中,利用常用方法填充下述所示組成物,獲得每粒360mg之軟膠囊。 The following composition was filled in the capsule skin made of the above ingredients by a usual method to obtain a soft capsule of 360 mg per capsule.

(製劑例3)飲料劑 (Formulation Example 3) Beverage agent

混合上述成分,加入水使之成為10公升。該飲料劑每次飲用約100ml。 The above ingredients were mixed, and water was added to make it 10 liters. The beverage is consumed about 100 ml each time.

(製劑例4)飲料劑 (Formulation Example 4) Beverage agent

混合上述成分,加入水使之成為10公升。該飲料劑每次飲用約100ml。 The above ingredients were mixed, and water was added to make it 10 liters. The beverage is consumed about 100 ml each time.

實施例3. 藉由動物實驗檢討吸收性以及抗氧化能力-1 Example 3. Evaluation of absorption and antioxidant capacity by animal experiment-1 <實驗方法> <Experimental method>

自東方生物服務(OrientalBioService)公司購入10隻SD系雄性大鼠(7週齡),於試驗環境下進行馴化後1週後,分為對照群5隻,實驗群5隻。經絕食一晚後,於對照群以80mg之芝麻素混合物(芝麻素:表芝麻素=1:1),100mg之米胚芽油濃縮物(米胚芽油γ 30S:含30% γ-米糠醇,含70%米胚芽油,築野食品工業股份有限公司),1700mg之橄欖油(Nakaraitesuku股份有限公司)加熱混合均勻者,另外試驗群以80mg之芝麻素混合物(芝麻素:表芝麻素=1:1),100mg之米胚芽油濃縮物(米胚芽油γ 30S:含30% γ-米糠醇,含70%米胚芽油,築野食品工業股份有限公司),1700mg之米胚芽油(米胚芽油PRO-15:1.5% γ-米糠醇,含98.5%米胚芽油,築野食品工業股份有限公司)加熱混合均勻者,以每1kg體重用量為2ml,使用餵食管進行經口投予。γ-米糠醇:(γ-米糠醇+米胚芽油)之重量比於對照群係1:3.3,於試驗群係1:32.4。於投予前,以及投予開始之1、2、3、6、9、24小時後,自 尾靜脈使用肝素採血管採取血液,並藉由離心分離操作(8000rpm,10min)獲得血漿檢體,測定血漿之抗氧化能力。 Ten SD male rats (7 weeks old) were purchased from Oriental BioService, and one week after acclimation in the experimental environment, they were divided into 5 control groups and 5 experimental groups. After a hunger strike for one night, a mixture of 80 mg of sesamin in the control group (sesamin: episesamin = 1:1), 100 mg of rice germ oil concentrate (rice germ oil γ 30S: containing 30% γ -mysterol, 70% rice germ oil, Chino Food Industry Co., Ltd.), 1700mg of olive oil (Nakaraitesuku Co., Ltd.) heated and mixed evenly, and the test group with 80mg of sesamin mixture (sesame: episesamin = 1: 1), 100mg of rice germ oil concentrate (rice germ oil γ 30S: containing 30% γ -mysterol, containing 70% rice germ oil, Chino Food Industry Co., Ltd.), 1700mg rice germ oil (rice germ oil) PRO-15: 1.5% γ -methanol, containing 98.5% rice germ oil, Chino Food Industry Co., Ltd.), heated and mixed evenly, 2 ml per 1 kg of body weight, using a feeding tube for oral administration. The weight ratio of γ -mysterol: ( γ -mysterol + rice germ oil) was 1:3.3 in the control group and 1:32.4 in the test group. Blood samples were taken from the tail vein using heparin blood collection tubes before administration, and 1, 2, 3, 6, 9, and 24 hours after the start of administration, and plasma samples were obtained by centrifugation (8000 rpm, 10 min). The antioxidant capacity of plasma was measured.

血漿之抗氧化能力測定係使用ORAC(Oxygen Radical Absorbance Capacity法,氧自由基吸收能力)(參照文獻Free Radic.Biol.Med.14(3),303-311(1993)、J Agric Food Chem.49(10),4619-4626(2001)、JAgric Food Chem.50(7),1815-1821(2002)、J Agric Food Chem.53(10),4290-4302(2005)等)。高ORAC值係表示具有高抗氧化能力。 The antioxidant capacity of plasma is determined by ORAC (Oxygen Radical Absorbance Capacity method, oxygen radical absorption capacity) (Reference Radi. Biol. Med. 14 (3), 303-311 (1993), J Agric Food Chem. (10), 4619-4626 (2001), JAgric Food Chem. 50 (7), 1815-1821 (2002), J Agric Food Chem. 53 (10), 4290-4302 (2005), etc.). A high ORAC value indicates a high antioxidant capacity.

<結果> <Result>

計算每隻動物投予前之血液ORAC值(μmol TE/L),與開始投予後採血檢體之血液ORAC值(μmol TE/L)之差。將該值作為⊿ORAC值表示。圖2係表示⊿ORAC值之AUC。自圖2可確認與對照群相比,試驗群之⊿ORAC值之AUC顯著上升。自以上結果,可明確得知藉由使γ-米糠醇之重量之相對於γ-米糠醇以及米胚芽油之合計重量之比例,較對照群之比例之1:3.3更為降低,可使抗氧化能力顯著上升。由於已知芝麻素類顯示具有在生體內的抗氧化作用,認為該抗氧化能力的提高,係證實促進芝麻素類之體內吸收。 The difference between the blood ORAC value (μmol TE/L) before administration of each animal and the blood ORAC value (μmol TE/L) of the blood sampling sample after the start of administration was calculated. This value is expressed as the ⊿ORAC value. Figure 2 shows the AUC of the ⊿ORAC value. From Figure 2, it was confirmed that the AUC of the ORAC value of the test group significantly increased compared with the control group. From the above result, by making clear that γ - m the weight of furfuryl alcohol with respect to γ - m and the ratio of total alcohol of the weight of rice germ oil, compared with the control group the ratio of 1: 3.3 is more reduced, enables anti The oxidizing power is significantly increased. Since sesamin is known to have an antioxidant action in the living body, it is considered that the improvement of the antioxidant ability is confirmed to promote the in vivo absorption of sesamin.

實施例4. 藉由動物實驗檢討吸收性以及抗氧化能力-2 Example 4. Evaluation of absorption and antioxidant capacity by animal experiments-2 <實驗方法> <Experimental method>

自東方生物服務(OrientalBioService)公司購入10隻SD系雄性大鼠(7週齡),於試驗環境下進行馴化後1週後,分為對照群5隻,實驗群5隻。經絕食一晚後,於對照群以80mg之芝麻素混合物(芝麻素:表芝麻素=1:1),1218mg之米胚芽油(米胚芽油PRO-15:1.5% γ-米糠醇,含98.5%米胚芽油,築野食品工業股份有限公司),3282mg之橄欖油(Nakaraitesuku股份有限公司)加熱混合均勻者,另外試驗群以80mg之芝麻素混合物(芝麻素:表芝麻素=1:1),60mg之米胚芽油濃縮物(米胚芽油γ 30S:含30% γ-米糠醇,含70%米胚芽油,築野食品工業股份有限公司),4440mg之米胚芽油(米胚芽油PRO-15:1.5% γ-米糠醇,含98.5%米胚芽油,築野食品工業股份有限公司)加熱混合均勻者,以每1kg體重用量為5ml,使用餵食管進行經口投予。γ-米糠醇:(γ-米糠醇+米胚芽油)之重量比於對照群係1:67,於試驗群係1:53.2。於投予前,以及投予開始之1、3、6、9、24小時後,自尾靜脈使用肝素採血管採取血液,並藉由離心分離操作(8000rpm,10min)獲得血漿檢體,測定血漿之抗氧化能力。血漿之抗氧化能力測定係採用與實施例3相同之方法實施。 Ten SD male rats (7 weeks old) were purchased from Oriental BioService, and one week after acclimation in the experimental environment, they were divided into 5 control groups and 5 experimental groups. After a hunger strike for one night, a mixture of 80 mg of sesamin in the control group (sesamin: episesamin = 1:1), 1218 mg of rice germ oil (rice germ oil PRO-15: 1.5% gamma -mysterol, containing 98.5 % rice germ oil, Chino Food Industry Co., Ltd.), 3282mg of olive oil (Nakaraitesuku Co., Ltd.) heated and mixed evenly, and the test group was 80mg of sesamin mixture (sesame: episesamin = 1:1) , 60mg rice germ oil concentrate (rice germ oil γ 30S: containing 30% γ -mysterol, containing 70% rice germ oil, Chino Food Industry Co., Ltd.), 4440mg rice germ oil (rice germ oil PRO- 15: 1.5% γ -methanol, containing 98.5% rice germ oil, Chino Food Industry Co., Ltd.), heating and mixing evenly, using 5 ml per 1 kg of body weight, using a feeding tube for oral administration. γ - m furfuryl :( γ - rice + rice germ oil alcohol) weight ratio of 1:67 to control formations, formations in Test 1: 53.2. Before the administration, and 1, 3, 6, 9, and 24 hours after the start of the administration, blood was taken from the tail vein using heparin blood collection tubes, and plasma samples were obtained by centrifugation (8000 rpm, 10 min) to determine plasma. Its antioxidant capacity. The antioxidant capacity of plasma was measured in the same manner as in Example 3.

<結果> <Result>

圖3係表示⊿ORAC值(定義如上所述)之AUC。自圖3可確認與對照群相比,試驗群之⊿ORAC值之AUC顯著上升。自以上結果,可明確得知藉由使γ-米糠醇之重量 之相對於γ-米糠醇以及米胚芽油之合計重量之比例,較對照群之比例之1:67更為提高,可使抗氧化能力顯著上升。認為該抗氧化能力的提高,係證實促進芝麻素類之體內吸收。 Figure 3 is a graph showing the AUC of the ⊿ORAC value (as defined above). From Figure 3, it was confirmed that the AUC of the ORAC value of the test group significantly increased compared with the control group. From the above result, by making clear that γ - m the weight of furfuryl alcohol with respect to γ - m and the ratio of total alcohol of the weight of rice germ oil, compared with the control group the ratio of 1:67 is more improved anti can The oxidizing power is significantly increased. It is considered that the improvement of the antioxidant ability is confirmed to promote the in vivo absorption of sesamin.

Claims (14)

一種組成物,其係含有至少一種芝麻素類、至少一種γ-米糠醇、及米胚芽油(rice germ oil)之組成物,其特徵為:該γ-米糠醇之總重量:(該γ-米糠醇之總重量與該米胚芽油之重量的合計量)=1:4~1:66,當該米胚芽油內含γ-米糠醇時,該米胚芽油之重量係從內含γ-米糠醇之該米胚芽油之總重量去除該米胚芽油所含有之γ-米糠醇重量的重量,該芝麻素類為芝麻素及/或表芝麻素,使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上,該γ-米糠醇的總摻合比例,相對於該組成物全量為0.1~50w/w%。 A composition comprising at least one sesamin, at least one gamma-mysterol, and a rice germ oil, characterized by: a total weight of the gamma-mysterol: (the γ- The total weight of rice sterol and the weight of the germ oil of the rice) = 1 : 4 ~ 1: 66, when the rice germ oil contains γ-mysterol, the weight of the rice germ oil is from the internal γ- The total weight of the rice germ oil of rice sterol removes the weight of the γ-mysterol contained in the rice germ oil, and the sesamin is sesamin and/or episesamin, and the total weight of the aforementioned sesamin is 1 The total weight of the γ-mysterol is 0.3 or more, and the total blending ratio of the γ-mysterol is 0.1 to 50 w/w% based on the total amount of the composition. 一種組成物,其係含有至少一種芝麻素類、至少一種γ-米糠醇、及米胚芽油(rice germ oil)之液劑型態的組成物,其特徵為:該γ-米糠醇之總重量:(該γ-米糠醇之總重量與該米胚芽油之重量的合計量)=1:4~1:66,當該米胚芽油內含γ-米糠醇時,該米胚芽油之重量係從內含γ-米糠醇之該米胚芽油之總重量去除該米胚芽油所含有之γ-米糠醇重量的重量,該芝麻素類為芝麻素及/或表芝麻素,使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上,該γ-米糠醇的總摻合比例,相對於該 組成物全量為0.0001~0.1w/w%。 A composition comprising a liquid dosage form of at least one sesamin, at least one gamma-mysterol, and rice germ oil, characterized by a total weight of the gamma-mysterol : (the total weight of the γ-mysterol and the weight of the rice germ oil) = 1: 4 ~ 1: 66, when the rice germ oil contains γ-mysterol, the weight of the rice germ oil Removing the weight of the γ-mysterol contained in the rice germ oil from the total weight of the rice germ oil containing γ-mysterol, the sesamin is sesamin and/or episesamin, and the sesamin When the total weight is 1, the total weight of the γ-mysterol is 0.3 or more, and the total blending ratio of the γ-mysterol is relative to the The total amount of the composition is 0.0001 to 0.1 w/w%. 如請求項1或2之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:20~1:60。 The composition of claim 1 or 2, wherein the total weight of the γ-mysterol: (the total weight of the aforementioned γ-mysterol and the total weight of the aforementioned rice germ oil) = 1:20 to 1:60. 如請求項3之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:25~1:55。 The composition of claim 3, wherein the total weight of the γ-mysterol: (the total weight of the γ-mysterol and the weight of the aforementioned rice germ oil) is 1:25 to 1:55. 如請求項4之組成物,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:32~1:49。 The composition of claim 4, wherein the total weight of the γ-mysterol: (the total weight of the aforementioned γ-mysterol and the weight of the aforementioned rice germ oil) = 1:32 to 1:49. 如請求項1或2之組成物,其係經口用。 The composition of claim 1 or 2 is used orally. 如請求項1或2之組成物,其係飲食物。 The composition of claim 1 or 2 is a food or drink. 如請求項1或2之組成物,其係抗氧化劑。 The composition of claim 1 or 2 which is an antioxidant. 一種使用,其特徵為含有至少一種γ-米糠醇及米胚芽油作為有效成分之組成物用於製造至少一種芝麻素類之促進體內吸收劑之使用,前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:4~1:66,當該米胚芽油內含γ-米糠醇時,該米胚芽油之重量係從內含γ-米糠醇之該米胚芽油之總重量去除該米胚芽油所含有之γ-米糠醇重量的重量,該芝麻素類為芝麻素及/或表芝麻素,使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上,該γ-米糠醇的總摻合比例,相對於該 組成物全量為0.1~50w/w%。 A use characterized by the use of at least one gamma-mysterol and rice germ oil as an active ingredient for the manufacture of at least one sesamin-promoting in vivo absorbent, the total weight of the aforementioned gamma-mysterol: (previously The total weight of γ-mysterol and the weight of the above-mentioned rice germ oil is 1=4~1:66. When the rice germ oil contains γ-mysterol, the weight of the rice germ oil is from the inside. The total weight of the rice germ oil of γ-mysterol is removed by weight of the weight of γ-mysterol contained in the rice germ oil, and the sesamin is sesamin and/or episesamin, and the total weight of the aforementioned sesamin When it is 1, the total weight of the γ-mysterol is 0.3 or more, and the total blending ratio of the γ-mysterol is relative to the ratio The total amount of the composition is 0.1 to 50 w/w%. 一種使用,其特徵為含有至少一種γ-米糠醇及米胚芽油作為有效成分之液劑型態的組成物用於製造至少一種芝麻素類之促進體內吸收劑之使用,前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:4~1:66,當該米胚芽油內含γ-米糠醇時,該米胚芽油之重量係從內含γ-米糠醇之該米胚芽油之總重量去除該米胚芽油所含有之γ-米糠醇重量的重量,該芝麻素類為芝麻素及/或表芝麻素,使前述芝麻素類之總重量為1時,前述γ-米糠醇之總重量為0.3以上,該γ-米糠醇的總摻合比例,相對於該組成物全量為0.0001~0.1w/w%。 Use of a liquid dosage form comprising at least one gamma-mysterol and rice germ oil as an active ingredient for the manufacture of at least one sesamin-promoting agent, the gamma-mysterol Total weight: (the total weight of the aforementioned γ-mysterol and the weight of the aforementioned rice germ oil) = 1:4 to 1:66, when the rice germ oil contains γ-mysterol, the rice germ oil The weight is obtained by removing the weight of the γ-mysterol contained in the rice germ oil from the total weight of the rice germ oil containing γ-mysterol, and the sesamin is sesamin and/or episesamin, and the sesame is obtained. When the total weight of the saccharide is 1, the total weight of the γ-mysterol is 0.3 or more, and the total blending ratio of the γ-mysterol is 0.0001 to 0.1 w/w% based on the total amount of the composition. 如請求項9或10之使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:20~1:60。 The use of claim 9 or 10, wherein the total weight of the aforementioned γ-mysterol: (the total weight of the aforementioned γ-mysterol and the weight of the aforementioned rice germ oil) = 1:20 to 1:60. 如請求項11之使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:25~1:55。 The use of claim 11, wherein the total weight of the γ-mysterol: (the total weight of the aforementioned γ-mysterol and the weight of the aforementioned rice germ oil) = 1:25 to 1:55. 如請求項12之使用,其中前述γ-米糠醇之總重量:(前述γ-米糠醇之總重量與前述米胚芽油之重量的合計量)=1:32~1:49。 The use of claim 12, wherein the total weight of the aforementioned γ-mysterol: (the total weight of the aforementioned γ-mysterol and the weight of the aforementioned rice germ oil) = 1:32 to 1:49. 如請求項9或10之使用,其中前述促進體內吸收劑係經口用。 The use of claim 9 or 10, wherein the aforementioned in vivo absorption of the absorbent is oral.
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