WO2013187391A1 - COMPOSITION COMPRENANT UN COMPOSÉ DE DÉSAMINE, UN γ-ORIZANOL ET DE L'HUILE DE GERME DE RIZ - Google Patents

COMPOSITION COMPRENANT UN COMPOSÉ DE DÉSAMINE, UN γ-ORIZANOL ET DE L'HUILE DE GERME DE RIZ Download PDF

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WO2013187391A1
WO2013187391A1 PCT/JP2013/066033 JP2013066033W WO2013187391A1 WO 2013187391 A1 WO2013187391 A1 WO 2013187391A1 JP 2013066033 W JP2013066033 W JP 2013066033W WO 2013187391 A1 WO2013187391 A1 WO 2013187391A1
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oryzanol
sesamin
germ oil
rice germ
composition
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PCT/JP2013/066033
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English (en)
Japanese (ja)
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悠 一本松
佳子 小野
菜美乃 冨森
大輔 竹本
俊明 末安
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サントリーホールディングス株式会社
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Priority to JP2014521336A priority Critical patent/JP6157463B2/ja
Priority to CN201380031469.5A priority patent/CN104394864B/zh
Publication of WO2013187391A1 publication Critical patent/WO2013187391A1/fr
Priority to HK15105560.2A priority patent/HK1204936A1/xx

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/115—Fatty acids or derivatives thereof; Fats or oils
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Definitions

  • the present invention relates to in vivo absorption promoters of sesamin and compositions such as foods and drinks or pharmaceutical compositions using them.
  • the present invention also relates to the use of the composition as an antioxidant.
  • Sesamin is a kind of lignan compound contained in sesame.
  • sesamin and its stereoisomer episesamin have a blood cholesterol lowering action and a blood neutral lipid lowering action, a liver function improving action, an active oxygen scavenging action, a ⁇ 5 desaturase inhibiting action, a lipid peroxide production.
  • Various physiological activities such as inhibitory action, antihypertensive action, sickness prevention action, breast cancer inhibitory action have been reported (Patent Document 1).
  • lignan compounds including sesamin are hardly soluble in water and are only slightly soluble in organic solvents that can be used for medicine or food. Due to such poor solubility, lignan compounds have a problem that they are difficult to be absorbed in vivo.
  • Patent Documents 1 and 2 As a method for improving the in vivo absorbability of lignan compounds including sesamins, for example, methods using an emulsion have been proposed (Patent Documents 1 and 2). However, there are not many reports of examples in which the in vivo absorbability of sesamin is improved by simply combining with other compounds in a simpler manner.
  • An object of the present invention is to provide a new means for promoting in-vivo absorption of sesamins, which can solve such problems.
  • the present inventor has found that when sesamin is combined with ⁇ -oryzanol and rice germ oil, the absorption of sesamin in the body can be promoted. This effect can be prominent when ⁇ -oryzanol and rice germ oil are used in a specific ratio.
  • the present invention includes, but is not limited to: 1.
  • the composition according to 1, wherein the total weight of the ⁇ -oryzanol: (the total amount of the total weight of the ⁇ -oryzanol and the weight of the rice germ oil) 1: 20 to 1:60. 2a. 3.
  • the in-vivo absorption enhancer or use according to 11, wherein the total weight of the ⁇ -oryzanol: (the total amount of the total weight of the ⁇ -oryzanol and the weight of the rice germ oil) 1: 25 to 1:55.
  • the absorbability of sesamin in the body can be improved.
  • the effect can be remarkable when the amount of the latter two components is set to a specific ratio. Therefore, the physiological activity can be efficiently exhibited without increasing the dose of sesamin.
  • the present invention can remarkably enhance the antioxidant action of a composition containing sesamin, ⁇ -oryzanol and rice germ oil. Therefore, this invention also provides the antioxidant which can exhibit the outstanding antioxidant effect
  • ⁇ -oryzanol is known to have various physiological actions such as blood neutral lipid lowering action, endocrine / autonomic nerve regulating action, gastric mucosa protecting action and the like. Furthermore, sesamin and ⁇ -oryzanol are extremely safe because they are derived from plants. Therefore, the present invention not only improves the absorbability of sesamin compounds, but also provides a food and drink product and a pharmaceutical composition that can be expected to have a useful physiological effect of ⁇ -oryzanol and that can be consumed safely and continuously. .
  • FIG. 1 is a graph showing the amount of sesamin and episesamin absorbed in the intestinal tract.
  • FIG. 2 is a graph showing the AUC of the ⁇ ORAC value.
  • FIG. 3 is a graph showing the AUC of the ⁇ ORAC value.
  • sesamin The sesamin of the present invention is a general term for a series of compounds including sesamin and its analogs.
  • the sesamin analog include episesamin and dioxabicyclo [3.3.0] octane derivatives described in JP-A-4-9331.
  • Specific examples of sesamin can include sesamin, sesaminol, episesaminol, sesamorin and the like, and these stereoisomers or racemates can be used alone or in combination, but in the present invention, , Sesamin and / or episesamin can be suitably used.
  • metabolites of sesamin compounds (for example, described in JP-A No. 2001-139579) are sesamin analogs contained in the sesamin compounds of the present invention as long as the effects of the present invention are exhibited, and are used in the present invention. Can do.
  • sesamin used in the present invention is not limited at all by its form, production method and the like.
  • sesamin extracted from sesame oil by a known method for example, the method described in JP-A-4-9331
  • sesamin extract or concentrate is usually used.
  • commercially available sesame oil (liquid state) can also be used as it is.
  • sesame oil liquid state
  • the sesamin content is low (usually less than 1%), so when trying to formulate the sesamin necessary to obtain the physiological effects of sesamin, per unit dosage of the formulated composition The volume can become too large, which can cause inconveniences.
  • the dosage form (tablets, capsules, etc.) becomes too large, which causes problems in ingestion. Therefore, it is preferable to use a sesamin extract (or sesamin concentrate) from sesame oil from the viewpoint that the amount of intake may be small.
  • the sesamin extract (or sesamin concentrate) may be made tasteless and odorless by a known means such as activated clay treatment.
  • a sesamin concentrate obtained by improving the content of sesamin by extraction and / or purification from a food-derived material such as sesame oil.
  • the degree of concentration may be appropriately set depending on the type of sesamin used and the form of the composition to be blended.
  • a sesamin concentrate concentrated so that the total amount of sesamin is 1 w / w% or more is used.
  • the total sesamin content in the sesamin concentrate is more preferably 20 w / w% or more, further preferably 50 w / w% or more, more preferably 70 w / w% or more, and concentration to 90 w / w% or more (purification). What is done is optimal.
  • the content of sesamin can be measured using any known method such as HPLC.
  • HPLC method for example, the method described in JP2009-155531A can be referred to.
  • ⁇ -oryzanol and rice germ oil One of the effective ingredients for promoting in vivo absorption of sesamin is ⁇ -oryzanol.
  • ⁇ -Oryzanol has blood neutral lipid lowering action (Geriant.med. 19, 1812-1840, 1981), endocrine / autonomic nerve regulating action (Japanese Pharmacology, 75 (4), 399-403, 1979), Various physiological effects such as gastric mucosal protective action (Nippon Pharmacological Journal, 84 (6), 537-542, 1984) are known, and purified products are used to treat hyperlipidemia and psychosomatic disorders (menopause, It is approved as a medicine for treating irritable bowel syndrome.
  • the ⁇ -oryzanol used in the present invention is a generic name for ferulic acid obtained by ester-linking triterpene alcohol or sterol.
  • triterpene alcohol examples include cycloartol, 24-methylenecycloartanol, cycloartanol, and cyclopranol.
  • sterol examples include campesterol, stigmasterol, ⁇ -sitosterol, and the like. It can be illustrated. In the present invention, these compounds can be used alone or as a mixture.
  • a method for quantifying ⁇ -oryzanol a known method such as a UV absorbance method or an HPLC method can be appropriately used.
  • the sample is dissolved in heptane and the absorbance is measured at the maximum absorption wavelength near 315 nm, as described in the “Quasi-drug raw material standard” and “Food additive other than chemically synthesized products”. This can be quantified.
  • ⁇ -Oryzanol is known to be contained in brown rice, corn, barley and the like. ⁇ -oryzanol is also contained in rice bran oil, which is an oil extracted from brown rice.
  • ⁇ -oryzanol is also contained in rice germ oil, which is another component effective for promoting in vivo absorption of sesamins.
  • Rice germ oil is oil extracted from rice germ, and usually contains about 1.0 to 1.5 w / w% of ⁇ -oryzanol (this concentration is the amount of rice including the weight of ⁇ -oryzanol). (Based on the total weight of the germ oil).
  • the content of rice germ oil can be measured using any known method.
  • the content of rice germ oil can be measured using the content of sterols characteristically contained in rice germ oil or rice germ oil concentrate and the content ratio of various sterols as an index.
  • rice germ oil contains more bound sterols than free sterols, it may be possible to determine whether a composition contains rice germ oil based on the sterol composition. Moreover, since the content of campesterol and stigmasterol in rice germ oil is relatively high, these contents may be used as an index for measuring the content of rice germ oil.
  • ⁇ -Oryzanol and rice germ oil used in the present invention are not limited at all by the origin, form, production method and the like.
  • ⁇ -oryzanol For example, commercially available rice germ oil or the like can be used as it is for ⁇ -oryzanol, but as described above, the content of ⁇ -oryzanol is not high. Therefore, it is not sufficient to add ⁇ -oryzanol and rice germ oil in a proportion as described later. Therefore, instead of or in addition, it is preferable to use one having a high ⁇ -oryzanol content, for example, a ⁇ -oryzanol concentrate from rice bran oil, rice germ oil or the like.
  • the total ⁇ -oryzanol content in the ⁇ -oryzanol concentrate is preferably 2 w / w% or more, more preferably 30 w / w% or more (these concentrations are ⁇ -Based on the total weight of the concentrate including the weight of oryzanol).
  • a concentrate of ⁇ -oryzanol is industrially obtained by extracting from rice bran oil or rice germ oil with an organic solvent or purifying after resin treatment.
  • rice germ oil gamma 30 (Tsukino) Food Industry Co., Ltd.)
  • ⁇ -oryzanol, oryzadorim V-50 rice bran oil, brown rice germ oil (Oryza Oil Co., Ltd.).
  • Rice germ oil contains, for example, oryzal oil S-1 (1.2% to 1.5% ⁇ -oryzanol (this concentration is based on the total amount of rice germ oil including the amount of ⁇ -oryzanol)). Ichimaru Falcos), rice germ oil PRO-15 containing 1.0 to 1.5% ⁇ -oryzanol (this concentration is based on the total amount of rice germ oil including the amount of ⁇ -oryzanol) No. Food Industry Co., Ltd.).
  • composition containing sesamin, ⁇ -oryzanol and rice germ oil Composition containing sesamin, ⁇ -oryzanol and rice germ oil
  • the combination of sesamin, ⁇ -oryzanol and rice germ oil can improve the in vivo absorbability of sesamin. And while being able to exhibit the physiological activity efficiently, health promotion can be aimed at by the physiological effect of each component.
  • the amount and ratio of each component in the composition containing the sesamin of the present invention, ⁇ -oryzanol and rice germ oil are as follows. May be selected as appropriate within the range in which the bioactivity is promoted and the physiological activity is efficiently exhibited.
  • the ratio of the total weight of ⁇ -oryzanol to the total weight of ⁇ -oryzanol and the weight of rice germ oil, if expected to enhance the absorption of sesamin in the body Is from 1: 4 to 1:66, preferably from 1: 8.7 to 1:62, more preferably from 1:20 to 1:60, more preferably from 1:25 to 1:55, more preferably 1:32. To 1:54 or 1: 32.4 to 53.2, more preferably 1:32 to 1:49.
  • the weight of the rice germ oil described in relation to the present invention is the total amount including the weight of ⁇ -oryzanol unless otherwise specified. Without the weight of ⁇ -oryzanol from the total amount.
  • the total weight of ⁇ -oryzanol when the total weight of sesamin contained is 1 is preferably 0.3 or more, more preferably 0.4 or more, more preferably 0.6 or more, more preferably 0.69 or more, more preferably 0.8 or more, and even more preferably 1.0 or more.
  • it is preferably 5.0 or less, more preferably 3.0 or less, more preferably 1.6 or less, more preferably 1.5 or less, more preferably 1.4 or less, more preferably Is 1.39 or less, more preferably 1.2 or less, more preferably 1.1 or less, more preferably 1.06 or less.
  • the present invention includes all combinations of these upper and lower limits.
  • Examples of the preferred total weight range of ⁇ -oryzanol when the total weight of sesamin is 1 are 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 to 1.2, 0.3 to 1.1, 0.3 to 1.06; 0.4 to 5.0, 0.4 to 3.0, 0.4 to 1.6, 0.4 to 1.5, 0.4 to 1.4, 0.4 to 1.39, 0. 4 to 1.2, 0.4 to 1.1, 0.4 to 1.06; 0.6 to 5.0, 0.6 to 3.0, 0.6 to 1.6, 0.6 to 1.5, 0.6 to 1.4, 0.6 to 1.39, 0.
  • sesamin is blended in an amount of about 1 to 100 mg, preferably 1 to 50 mg, more preferably about 3 to 30 mg, depending on the total weight of the composition.
  • ⁇ -oryzanol can be blended in an amount of about 1 to 100 mg, preferably 1 to 60 mg, more preferably about 3 to 30 mg.
  • Rice germ oil can be blended in an amount of about 1 to 5000 mg, preferably 10 to 1000 mg, more preferably about 30 to 500 mg.
  • the typical total mixing ratio of sesamin in the composition of the present invention is 1 w / w% or more, preferably 1 to 50 w / w%, more preferably 1 to 10 w / w%.
  • the typical total blending ratio of ⁇ -oryzanol is 0.1 to 50 w / w%, preferably 0.5 to 30 w / w%, more preferably 1 to 10 w / w% with respect to the total amount of the composition. is there.
  • a typical total blending ratio of rice germ oil is 5 to 99 w / w%, preferably 20 to 98 w / w%, more preferably 50 to 95 w / w% with respect to the total amount of the composition.
  • the typical total blending ratio of sesamin is 0.001 w / w% or more, preferably 0.001 to 0.5 w / w%. More preferably, it is 0.001 to 0.05 w / w%, and the typical total blending ratio of ⁇ -oryzanol is 0.0001 to 0.1 w / w%, preferably 0.
  • the typical total blending ratio of rice germ oil is 0.05 to 5 w / w based on the total amount of the composition %, Preferably 0.1 to 2.5 w / w%, more preferably 0.2 to 1 w / w%.
  • the form and intake route of the composition of the present invention are not particularly limited. However, in the present invention, when ingested for the purpose of promoting health, it is preferably ingested as an oral composition.
  • composition of the present invention may contain any desired component in addition to sesamins, ⁇ -oryzanol, and rice germ oil as long as the effect is not impaired.
  • vitamins such as vitamin E and vitamin C, minerals, hormones, nutritional ingredients, physiologically active ingredients such as fragrances, emulsifiers, tonicity agents (isotonic agents), buffers, Solubilizing agents, preservatives, stabilizers, antioxidants and the like can be appropriately blended.
  • the composition of the present invention can be used as an antioxidant, that is, a composition for exerting an antioxidant action in vivo due to its excellent antioxidant action.
  • the use of antioxidants is, for example, for eliminating active oxygen in vivo, improving liver function, suppressing lipid peroxide production in vivo, improving energy metabolism, or preventing or preventing the following diseases or conditions: Can lead: skin wrinkles, skin blemishes, skin sag, fatigue, metabolic syndrome, diabetes, arteriosclerosis, hypertension, cancer, inflammation, or aging. Therefore, the antioxidant of the present invention is also effective in these applications.
  • the present invention is an in vivo absorption enhancer of sesamin containing ⁇ -oryzanol and rice germ oil as active ingredients.
  • the present invention also relates to the use of a composition containing ⁇ -oryzanol and rice germ oil as active ingredients for the production of an in vivo absorption enhancer of sesamins.
  • the present invention also relates to a method for promoting in vivo absorption of sesamins, the method comprising administering the sesamins, ⁇ -oryzanol, and rice germ oil.
  • Subjects to be administered include mammals such as humans in need of such enhanced absorption in the body.
  • the use ratio, blending ratio, blending amount, intake amount, etc. of sesamin, ⁇ -oryzanol and rice germ oil in the in vivo absorption enhancer, composition and method include sesamin, ⁇ -oryzanol and rice germ oil. It can determine suitably based on the above-mentioned numerical value regarding the composition to do.
  • the types of sesamin, ⁇ -oryzanol and rice germ oil used are the same.
  • Food / beverage products and pharmaceuticals are used for food / beverage products (functional foods, health supplements, functional nutrition foods, special-purpose foods, foods for specified health use, dietary supplements, diet foods, health It is preferable to provide foods, supplements, etc.) and pharmaceuticals.
  • Such foods and drinks and pharmaceuticals include food and drink compositions and pharmaceutical compositions containing sesamins, ⁇ -oryzanol and rice germ oil, and foods and drinks and pharmaceuticals containing or added to the composition. Also included are foods and drinks and pharmaceuticals that contain or add sesamin absorption enhancers containing ⁇ -oryzanol and rice germ oil as active ingredients.
  • the food and drink and the medicine may be pet food processed as pet food, animal feed, and veterinary medicine.
  • Food / beverage products and pharmaceuticals containing sesamin, ⁇ -oryzanol and rice germ oil have blood cholesterol lowering action, blood neutral lipid lowering action, liver function improving action, active oxygen scavenging action, ⁇ 5 desaturase inhibiting action
  • sesamin can be used to obtain various physiological actions considered to be effective, such as lipid peroxide production inhibitory action, antihypertensive action, sickness prevention action, breast cancer inhibitory action and the like.
  • foods and drinks and pharmaceuticals which are sesamin in vivo absorption promoters containing ⁇ -oryzanol and rice germ oil can be used to allow sesamins to efficiently exhibit the various physiological functions as described above.
  • composition of the present invention is provided as a food or drink
  • the form is provided in the form of health food such as tablets, capsules, powders, granules, drinks (including solutions and suspensions). It can also be provided in the form of soft drinks, tea drinks, dairy products such as yogurt and lactic acid bacteria drinks, seasonings, processed foods, desserts, confectionery (eg gum, candy, jelly), It is not limited to these.
  • the administration form may be oral administration, administration may be in the form of injections, etc., as long as a known formulation suitable for each administration is appropriately used.
  • formulations suitable for oral administration include, but are not limited to, tablets, capsules, powders, granules, solutions, suspensions, syrups and the like.
  • sesamin, ⁇ -oryzanol and rice germ oil are formulated individually, and they are taken almost simultaneously, or after taking one preparation, while taking the other preparation,
  • the in vivo absorption promoting action of sesamins intended by the present invention can be obtained.
  • a kit containing a sesamin in vivo absorption enhancer and a sesamin-containing composition containing ⁇ -oryzanol and rice germ oil together or separately is also intended by the present invention.
  • Each component separately contained in the kit may be taken at the same time, or may be taken sequentially or separately.
  • the numerical range represented by the upper limit value and the lower limit value in this specification that is, “lower limit value to upper limit value” includes the lower limit value and the upper limit value.
  • the range represented by “1-2” includes 1 and 2.
  • Example 1 Examination of absorbability by inversion intestinal model ⁇ Experimental method> SD male rats (7 weeks old) were acclimated in the test environment and used in the experiments. After laparotomy and blood removal under anesthesia, the small intestine (mainly jejunum) of about 15 cm was immediately removed from the pylorus and divided into two. One side is tied with a thread, the outside and inside are inverted, and the adjustment solution (inner 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. Satisfying 4) and tied the other side to produce a 5 cm inverted intestinal tract.
  • the adjustment solution inner 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. Sat
  • rice germ oil rice germ oil PRO-15: ⁇ -oryzanol 1.5%, rice germ oil 98.5% , Tsukino Food Industry Co., Ltd.
  • 4250 mg heated and mixed to be uniform. That is, in the composition administered to the control group, the weight ratio of ⁇ -oryzanol: ( ⁇ -oryzanol + rice germ oil) was 1: 3.3. In the composition administered to the test group, the weight ratio of ⁇ -oryzanol: ( ⁇ -oryzanol + rice germ oil) was 1: 32.4.
  • Example 2 Formulation Example (Formulation Example 1) Granule Sesamin 0.75g 10g rice germ oil containing ⁇ -oryzanol (containing 25%) Tocopherol acetate 50g Silica anhydride 20g 110g corn starch After uniformly mixing the above, 100 ml of 10% hydroxypropylcellulose / ethanol solution was added, kneaded as usual, extruded and dried to obtain granules.
  • Example 3 Examination of absorbability and antioxidant capacity by animal test -1 ⁇ Method of experiment> Ten SD male rats (7 weeks old) were purchased from Oriental Bioservice, and acclimated in the test environment for 1 week, and then divided into 5 control groups and 5 test groups.
  • the weight ratio of ⁇ -oryzanol: ( ⁇ -oryzanol + rice germ oil) was 1: 3.3 in the control group and 1: 32.4 in the test group.
  • blood was collected from the tail vein with a heparin blood collection tube, and a plasma sample was obtained by centrifugation (8000 rpm, 10 min). The oxidation ability was measured.
  • ORAC Oxygen Radical Absorbance Capacity method
  • FIG. 2 shows the AUC of the ⁇ ORAC value. From FIG. 2, it was confirmed that the AUC of the ⁇ ORAC value of the test group was significantly increased as compared with the control group. From the above, it is clear that the antioxidant capacity is remarkably increased by reducing the ratio of the weight of ⁇ -oryzanol to the total weight of ⁇ -oryzanol and rice germ oil from the ratio of 1: 3.3 in the control group. It became. Since sesamin is known to exhibit an antioxidant action in vivo, this increase in antioxidant capacity is considered to support the promotion of in vivo absorption of sesamin.
  • Example 4 Examination of absorbability and antioxidant capacity by animal test-2 ⁇ Method of experiment>
  • the weight ratio of ⁇ -oryzanol: ( ⁇ -oryzanol + rice germ oil) was 1:67 in the control group and 1: 53.2 in the test group.
  • blood was collected from the tail vein with a heparin blood collection tube, and a plasma sample was obtained by centrifugation (8000 rpm, 10 min). Was measured.
  • Plasma antioxidant capacity was measured in the same manner as in Example 3.
  • FIG. 3 shows the AUC of the ⁇ ORAC value (the definition is as described above). From FIG. 3, it was confirmed that the AUC of the ⁇ ORAC value of the test group was significantly increased as compared with the control group. From the above, it has been clarified that the antioxidant capacity is remarkably increased by increasing the ratio of the weight of ⁇ -oryzanol to the total weight of ⁇ -oryzanol and rice germ oil from the ratio of 1:67 in the control group. It was. This increase in antioxidant capacity is thought to support the promotion of sesamin absorption in the body.

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Abstract

L'invention concerne une combinaison de composé de sésamine, d'γ-orizanol et d'huile de germe de riz.
PCT/JP2013/066033 2012-06-14 2013-06-11 COMPOSITION COMPRENANT UN COMPOSÉ DE DÉSAMINE, UN γ-ORIZANOL ET DE L'HUILE DE GERME DE RIZ WO2013187391A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2014521336A JP6157463B2 (ja) 2012-06-14 2013-06-11 セサミン類とγ−オリザノールと米胚芽油とを含有する組成物
CN201380031469.5A CN104394864B (zh) 2012-06-14 2013-06-11 含有芝麻素类、γ-谷维素和米胚芽油的组合物
HK15105560.2A HK1204936A1 (en) 2012-06-14 2015-06-11 Composition comprising sesamin compound, orizanol and rice germ oil

Applications Claiming Priority (2)

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JP2012135034 2012-06-14
JP2012-135034 2012-06-14

Publications (1)

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WO2013187391A1 true WO2013187391A1 (fr) 2013-12-19

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JP (1) JP6157463B2 (fr)
CN (1) CN104394864B (fr)
HK (1) HK1204936A1 (fr)
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WO (1) WO2013187391A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015093484A1 (fr) * 2013-12-16 2015-06-25 サントリーホールディングス株式会社 Composition à teneur élevée en sésamine
JP2019014697A (ja) * 2017-07-11 2019-01-31 株式会社アンチエイジング・プロ ポリフェノール吸収促進用組成物、ポリフェノール体内吸収性向上方法、及び経口摂取用組成物
JP2019196340A (ja) * 2018-05-10 2019-11-14 亀井　淳三 セサミノールとシクロデキストリンとの包接複合体及びその製造方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016152846A1 (fr) * 2015-03-23 2016-09-29 サントリーホールディングス株式会社 Composition destinée à améliorer le rythme circadien

Citations (7)

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Publication number Priority date Publication date Assignee Title
JPH06227977A (ja) * 1993-02-01 1994-08-16 Suntory Ltd 活性酸素消去剤
JPH06340889A (ja) * 1993-05-31 1994-12-13 Tokyo Yushi Kogyo Kk オリザノール類を豊富に含んだ、こめ油の製造法
JPH07255393A (ja) * 1994-03-24 1995-10-09 Chikuno Shokuhin Kogyo Kk 米飯品質改良剤
WO2006070856A1 (fr) * 2004-12-28 2006-07-06 Suntory Limited Compositions de sesamine/episesamine
JP2007124917A (ja) * 2005-11-01 2007-05-24 Chikuno Shokuhin Kogyo Kk オリザノールを豊富に含んだ米油の製造法及びその用途
JP2009073749A (ja) * 2007-09-19 2009-04-09 Suntory Ltd セサミン類とγ−オリザノールとを含有する組成物
WO2010074220A1 (fr) * 2008-12-26 2010-07-01 サントリーホールディングス株式会社 Composition contenant des sésamines et de l'épigallocatéchine gallate

Family Cites Families (1)

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Publication number Priority date Publication date Assignee Title
TWI406867B (zh) * 2005-09-30 2013-09-01 Suntory Holdings Ltd And a method for producing a high content of episesamin

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06227977A (ja) * 1993-02-01 1994-08-16 Suntory Ltd 活性酸素消去剤
JPH06340889A (ja) * 1993-05-31 1994-12-13 Tokyo Yushi Kogyo Kk オリザノール類を豊富に含んだ、こめ油の製造法
JPH07255393A (ja) * 1994-03-24 1995-10-09 Chikuno Shokuhin Kogyo Kk 米飯品質改良剤
WO2006070856A1 (fr) * 2004-12-28 2006-07-06 Suntory Limited Compositions de sesamine/episesamine
JP2007124917A (ja) * 2005-11-01 2007-05-24 Chikuno Shokuhin Kogyo Kk オリザノールを豊富に含んだ米油の製造法及びその用途
JP2009073749A (ja) * 2007-09-19 2009-04-09 Suntory Ltd セサミン類とγ−オリザノールとを含有する組成物
WO2010074220A1 (fr) * 2008-12-26 2010-07-01 サントリーホールディングス株式会社 Composition contenant des sésamines et de l'épigallocatéchine gallate

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015093484A1 (fr) * 2013-12-16 2015-06-25 サントリーホールディングス株式会社 Composition à teneur élevée en sésamine
JP2019014697A (ja) * 2017-07-11 2019-01-31 株式会社アンチエイジング・プロ ポリフェノール吸収促進用組成物、ポリフェノール体内吸収性向上方法、及び経口摂取用組成物
JP2019196340A (ja) * 2018-05-10 2019-11-14 亀井　淳三 セサミノールとシクロデキストリンとの包接複合体及びその製造方法
JP7079931B2 (ja) 2018-05-10 2022-06-03 淳三 亀井 セサミノールとシクロデキストリンとの包接複合体及びその製造方法

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HK1204936A1 (en) 2015-12-11
CN104394864B (zh) 2016-10-05
CN104394864A (zh) 2015-03-04
JP6157463B2 (ja) 2017-07-05
TWI603732B (zh) 2017-11-01
JPWO2013187391A1 (ja) 2016-02-04
TW201410238A (zh) 2014-03-16

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