JP2024002801A - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP2024002801A JP2024002801A JP2022102222A JP2022102222A JP2024002801A JP 2024002801 A JP2024002801 A JP 2024002801A JP 2022102222 A JP2022102222 A JP 2022102222A JP 2022102222 A JP2022102222 A JP 2022102222A JP 2024002801 A JP2024002801 A JP 2024002801A
- Authority
- JP
- Japan
- Prior art keywords
- oral composition
- aminobutyric acid
- blood pressure
- polymethoxyflavone
- weight
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 67
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims abstract description 100
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 claims abstract description 50
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims abstract description 50
- 229930182496 polymethoxyflavone Chemical group 0.000 claims abstract description 38
- 239000011720 vitamin B Chemical group 0.000 claims abstract description 19
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- 229930003270 Vitamin B Chemical group 0.000 claims abstract description 8
- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 claims description 20
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- 150000003839 salts Chemical class 0.000 claims description 17
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Landscapes
- Coloring Foods And Improving Nutritive Qualities (AREA)
- General Preparation And Processing Of Foods (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
本発明は、γ－アミノ酪酸を含み、優れた血圧降下作用を有する経口組成物に関する。 The present invention relates to an oral composition containing γ-aminobutyric acid and having an excellent antihypertensive effect.
高血圧症は、代表的な生活習慣病の一つであり、心臓病、脳卒中、動脈硬化等の重篤な症状を引き起こす危険因子である。また、日本人では、若年から中年の男性を中心に、肥満（特に、内臓肥満）を伴う高血圧症の者が増加している。このような肥満を伴う高血圧症は、メタボリックシンドロームに進行し易いため、早期の対策が必要になる。 Hypertension is one of the typical lifestyle-related diseases and is a risk factor that causes serious symptoms such as heart disease, stroke, and arteriosclerosis. Furthermore, in the Japanese population, the number of people suffering from hypertension accompanied by obesity (particularly visceral obesity) is increasing, mainly among young to middle-aged men. Hypertension associated with obesity is likely to progress to metabolic syndrome, so early countermeasures are required.
高血圧の予防又は改善には、塩分の摂取制限による食事療法が有効であるが、かかる食事療法では、長期間継続しなければ効果発現が認められ難く、長期的な塩分の摂取制限にはストレスを伴うことがあるという欠点がある。そこで、血圧降下作用を有する成分を有する経口組成物の摂取によって、高血圧の予防又は改善を図ることが注目されている。 Dietary therapy that restricts salt intake is effective in preventing or improving high blood pressure, but it is difficult to see the effects of such dietary therapy unless it is continued for a long period of time, and long-term salt intake restriction requires stress. There are disadvantages that may come with it. Therefore, attention has been focused on preventing or improving hypertension by ingesting an oral composition containing a component having a blood pressure lowering effect.
従来、γ－アミノ酪酸には血圧降下作用があることが報告されており、γ－アミノ酪酸を含む経口組成物が、高血圧の予防又は改善用途に使用されている。また、従来、γ－アミノ酪酸の血圧降下作用を向上させた経口組成物についても検討されている。例えば、特許文献１には、γ－アミノ酪酸を含むアスパラガス抽出組成物は、γ－アミノ酪酸単独の場合に比べて、優れた血圧降下作用を有することが記載されている。また、特許文献２には、γ－アミノ酪酸とテアニンを５．５：４．５乃至３：７の重量比で併用することによって、血圧降下作用を相乗的に向上させ得ることが記載されている。 It has been reported that γ-aminobutyric acid has a hypotensive effect, and oral compositions containing γ-aminobutyric acid have been used to prevent or improve hypertension. Furthermore, oral compositions with improved antihypertensive effects of γ-aminobutyric acid have also been studied. For example, Patent Document 1 describes that an asparagus extract composition containing γ-aminobutyric acid has a superior blood pressure lowering effect compared to γ-aminobutyric acid alone. Further, Patent Document 2 describes that the blood pressure lowering effect can be synergistically improved by using γ-aminobutyric acid and theanine in a weight ratio of 5.5:4.5 to 3:7. There is.
経口組成物の機能性に対する要求特性は年々高まっており、血圧降下作用の更なる向上、製剤処方の多様化等に対応するために、γ－アミノ酪酸を含み、優れた血圧降下作用を有する経口組成物の新たな処方の開発が望まれている。 The functional requirements for oral compositions are increasing year by year, and in order to further improve blood pressure lowering effects and diversify drug formulations, oral compositions that contain γ-aminobutyric acid and have excellent blood pressure lowering effects are needed. The development of new formulations of compositions is desired.
本発明の目的は、γ－アミノ酪酸を含み、優れた血圧降下作用を有する経口組成物を提供することである。 An object of the present invention is to provide an oral composition containing γ-aminobutyric acid and having an excellent antihypertensive effect.
γ－アミノ酪酸は、副交感神経を優位にすることにより血圧降下作用を示すことが知られている。一方、ポリメトキシフラボンには、交感神経を優位にすることにより脂肪を燃焼させる作用が知られているが、それ自体は血圧降下作用を有していない。つまり、γ－アミノ酪酸とポリメトキシフラボンでは、自律神経に対して相反する作用を示すため、従来の知見からは、γ－アミノ酪酸とポリメトキシフラボンを併用すると、γ－アミノ酪酸による血圧降下作用を低下させることが懸念される。 γ-aminobutyric acid is known to exhibit a blood pressure lowering effect by making parasympathetic nerves dominant. On the other hand, polymethoxyflavone is known to have the effect of burning fat by making the sympathetic nervous system dominant, but it does not itself have a blood pressure lowering effect. In other words, since γ-aminobutyric acid and polymethoxyflavone show opposing effects on autonomic nerves, conventional knowledge suggests that when γ-aminobutyric acid and polymethoxyflavone are used together, the blood pressure lowering effect of γ-aminobutyric acid There is a concern that this may lead to a decline in
これに対して、本発明者は、経口組成物において、γ－アミノ酪酸と、ポリメトキシフラボンと、ビタミンＢ類とを組み合わせて含有させることにより、これらの成分の相乗効果によって、γ－アミノ酪酸が有する血圧降下作用が飛躍的に向上することを見出した。γ－アミノ酪酸とポリメトキシフラボンでは自律神経に対して相反する作用があることを踏まえると、前記３種の成分を併用することにより、γ－アミノ酪酸が有する血圧降下作用が飛躍的に向上することは、極めて意外な知見である。 In contrast, the present inventor has found that by containing γ-aminobutyric acid, polymethoxyflavone, and vitamin B in combination in an oral composition, γ-aminobutyric acid It was found that the blood pressure lowering effect of the drug was dramatically improved. Considering that γ-aminobutyric acid and polymethoxyflavone have opposing effects on autonomic nerves, the combined use of the above three components dramatically improves the blood pressure lowering effect of γ-aminobutyric acid. This is an extremely surprising finding.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項１． γ－アミノ酪酸、ポリメトキシフラボン、及びビタミンＢ類を含有する、経口組成物。
項２． 前記ポリメトキシフラボンとして、ポリメトキシフラボンを含有するブラックジンジャー抽出物を含む、項１に記載の経口組成物。
項３． 前記ビタミンＢ類が、パントテン酸、パントテン酸の塩、及びビタミンＢ2よりなる群から選択される少なくとも１種である、項１又は２に記載の経口組成物。
項４． 更に、カルニチン及び／又はその塩を含有する、項１～３のいずれかに記載の経口組成物。
項５． 血圧降下用の経口組成物である、項１～４のいずれかに記載の経口組成物。
That is, the present invention provides the inventions of the following aspects.
Item 1. An oral composition containing γ-aminobutyric acid, polymethoxyflavone, and B vitamins.
Item 2. Item 2. The oral composition according to Item 1, wherein the polymethoxyflavone is a black ginger extract containing polymethoxyflavone.
Item 3. Item 3. The oral composition according to item 1 or 2 , wherein the vitamin B is at least one selected from the group consisting of pantothenic acid, a salt of pantothenic acid, and vitamin B2.
Item 4. Item 4. The oral composition according to any one of Items 1 to 3, further comprising carnitine and/or a salt thereof.
Item 5. Item 5. The oral composition according to any one of Items 1 to 4, which is an oral composition for lowering blood pressure.
本発明の経口組成物では、γ－アミノ酪酸と、ポリメトキシフラボンと、ビタミンＢ類とを併用することにより、これらの相乗効果によって、格段に優れた血圧降下作用を備えさせることができる。また、ポリメトキシフラボンには、交感神経を優位にすることにより脂肪を燃焼させる作用があることが知られているので、本発明の経口組成物では、優れた血圧降下作用と共に、脂肪を燃焼させる作用も期待できるので、高血圧と肥満の双方に対する予防又は改善が期待できる。 In the oral composition of the present invention, by using γ-aminobutyric acid, polymethoxyflavone, and B vitamins in combination, the synergistic effect of these can provide an extremely excellent antihypertensive effect. In addition, polymethoxyflavone is known to have the effect of burning fat by making sympathetic nerves dominant, so the oral composition of the present invention has an excellent antihypertensive effect as well as a fat burning effect. Since it is also expected to have beneficial effects, it can be expected to prevent or improve both hypertension and obesity.
本発明の経口組成物は、γ－アミノ酪酸、ポリメトキシフラボン、及びビタミンＢ類を含むことを特徴とする。以下、本発明の経口組成物について詳述する。 The oral composition of the present invention is characterized by containing γ-aminobutyric acid, polymethoxyflavone, and B vitamins. The oral composition of the present invention will be described in detail below.
［(A)γ－アミノ酪酸］
本発明の経口組成物は、γ－アミノ酪酸を含有する。γ－アミノ酪酸は、副交感神経を優位にすることにより血圧降下作用を発揮することが知られている成分である。
[(A) γ-aminobutyric acid]
The oral composition of the present invention contains γ-aminobutyric acid. γ-aminobutyric acid is a component known to exert a blood pressure lowering effect by making parasympathetic nerves dominant.
本発明で使用されるγ－アミノ酪酸は、γ－アミノ酪酸を含む植物からの抽出、微生物醗酵、酵素合成、化学合成等のいずれの製造方法で得られたものであってもよい。 The γ-aminobutyric acid used in the present invention may be obtained by any production method such as extraction from plants containing γ-aminobutyric acid, microbial fermentation, enzymatic synthesis, or chemical synthesis.
また、本発明で使用されるγ－アミノ酪酸は、精製された状態のものであってもよく、また、γ－アミノ酪酸を含む植物抽出物、γ－アミノ酪酸が産生された発酵物及びその抽出物等の状態のものであってもよい。 Furthermore, the γ-aminobutyric acid used in the present invention may be in a purified state, or may be a plant extract containing γ-aminobutyric acid, a fermented product in which γ-aminobutyric acid is produced, or a fermented product thereof. It may be in the form of an extract or the like.
本発明の経口組成物におけるγ－アミノ酪酸の含有量については、経口組成物の形態、１日当たりの摂取・投与量等に応じて適宜設定すればよいが、例えば、１～５０重量％、好ましくは２～３０重量％、より好ましくは２～１０重量％が挙げられる。 The content of γ-aminobutyric acid in the oral composition of the present invention may be appropriately set depending on the form of the oral composition, daily intake/dosage, etc., but is preferably 1 to 50% by weight, for example. is 2 to 30% by weight, more preferably 2 to 10% by weight.
［ポリメトキシフラボン］
本発明の経口組成物は、ポリメトキシフラボンを含有する。ポリメトキシフラボンとは、２個以上のメトキシ基を含むフラボンである。
[Polymethoxyflavone]
The oral composition of the present invention contains polymethoxyflavone. Polymethoxyflavone is a flavone containing two or more methoxy groups.
本発明で使用されるポリメトキシフラボンにおけるメトキシ基の数については、特に制限されないが、例えば、２～７個、好ましくは２～５個が挙げられる。 The number of methoxy groups in the polymethoxyflavone used in the present invention is not particularly limited, but may be, for example, 2 to 7, preferably 2 to 5.
本発明で使用されるポリメトキシフラボンの種類については、特に制限されないが、例えば、５，７－ジメトキシフラボン、３，５，７－トリメトキシフラボン、５，７，４’－トリメトキシフラボン、３，５，７，４’－テトラメトキシフラボン、５，７，３’，４’－テトラメトキシフラボン、３，５，７，３’，４’－ペンタメトキシフラボン、５，６，７，８，４'－ペンタメトキシフラボン、５，６，７，３'，４'－ペンタメトキシフラボン、５，６，７，８，３'，４'－ヘキサメトキシフラボン、３，５，６，７，３'，４'－ヘキサメトキシフラボン、３，５，６，７，８，３'，４'－ヘプタメトキシフラボン等が挙げられる。これらのポリメトキシフラボンは、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。 The type of polymethoxyflavone used in the present invention is not particularly limited, but examples include 5,7-dimethoxyflavone, 3,5,7-trimethoxyflavone, 5,7,4'-trimethoxyflavone, 3 , 5,7,4'-tetramethoxyflavone, 5,7,3',4'-tetramethoxyflavone, 3,5,7,3',4'-pentamethoxyflavone, 5,6,7,8, 4'-pentamethoxyflavone, 5,6,7,3',4'-pentamethoxyflavone, 5,6,7,8,3',4'-hexamethoxyflavone, 3,5,6,7,3 Examples include ',4'-hexamethoxyflavone, 3,5,6,7,8,3',4'-heptamethoxyflavone, and the like. These polymethoxyflavones may be used alone or in combination of two or more.
ポリメトキシフラボンの由来については、特に制限されないが、好適な一例として、ブラックジンジャー由来のポリメトキシフラボンが挙げられる。ブラックジンジャー由来のポリメトキシフラボンとしては、具体的には、５，７－ジメトキシフラボン、３，５，７－トリメトキシフラボン、５，７，４’－トリメトキシフラボン、３，５，７，４’－テトラメトキシフラボン、５，７，３’，４’－テトラメトキシフラボン、及び３，５，７，３’，４’－ペンタメトキシフラボンが挙げられる。 The origin of polymethoxyflavone is not particularly limited, but a suitable example is polymethoxyflavone derived from black ginger. Specifically, the polymethoxyflavone derived from black ginger includes 5,7-dimethoxyflavone, 3,5,7-trimethoxyflavone, 5,7,4'-trimethoxyflavone, 3,5,7,4 Examples include '-tetramethoxyflavone, 5,7,3',4'-tetramethoxyflavone, and 3,5,7,3',4'-pentamethoxyflavone.
本発明で使用されるポリメトキシフラボンは、精製された状態のものであってもよく、また、ポリメトキシフラボンを含む植物抽出物の状態のものであってもよい。ポリメトキシフラボンを含む植物抽出物の好適な一例として、ブラックジンジャー抽出物が挙げられる。 The polymethoxyflavone used in the present invention may be in a purified state, or may be in the form of a plant extract containing polymethoxyflavone. A suitable example of a plant extract containing polymethoxyflavone is black ginger extract.
ブラックジンジャーとは、別名は黒ショウガ、学名はケンペリア・パルウィフローラ（Ｋａｅｍｐｆｅｒｉａ ｐａｒｖｉｆｌｏｒａ）であり、ショウガ科（Ｚｉｎｇｉｂｅｒａｃｅａｅ）バンウコン属（Ｋａｅｍｐｆｅｒｉａ）に属する植物である。抽出原料として使用されるブラックジンジャーの部位としては、例えば、花、蕾、種子、種皮、茎、葉、枝、枝葉、根、根茎等が挙げられる。これらの中でも、好ましくは、根茎が挙げられる。これらの原料部位は、１種単独で使用してもよく、２種以上を組み合わせて使用してもよい。また、これらの抽出原料は、必要に応じて、粉砕、切断、蒸熱、揉捻、乾燥、焙煎等の前処理に供されていてもよい。 Black ginger, also known as black ginger and scientific name Kaempferia parviflora, is a plant belonging to the family Zingiberaceae and the genus Kaempferia. Parts of black ginger used as extraction raw materials include, for example, flowers, buds, seeds, seed coats, stems, leaves, branches, foliage, roots, rhizomes, and the like. Among these, rhizomes are preferred. These raw material parts may be used alone or in combination of two or more. Moreover, these extraction raw materials may be subjected to pretreatment such as crushing, cutting, steaming, rolling, drying, and roasting, as necessary.
ポリメトキシフラボンを含むブラックジンジャー抽出物を得るための抽出処理は、通常の植物エキスの製造に使用される一般的な抽出手法であればよい。また、抽出原料として使用されるブラックジンジャーの部位は、生の状態であってもよいが、必要に応じて、粉砕、切断、蒸熱、揉捻、乾燥、焙煎等の前処理に供されていてもよい。 The extraction treatment for obtaining the black ginger extract containing polymethoxyflavone may be any general extraction method used in the production of normal plant extracts. In addition, the parts of black ginger used as extraction raw materials may be in a raw state, but if necessary, they may be subjected to pretreatment such as crushing, cutting, steaming, rolling, drying, and roasting. Good too.
抽出処理は、溶媒抽出処理、超臨界抽出処理、水蒸気蒸留処理等によって行うことができる。これらの中でも、好ましくは溶媒抽出処理が挙げられる。 The extraction process can be performed by solvent extraction process, supercritical extraction process, steam distillation process, etc. Among these, preferred is solvent extraction treatment.
溶媒抽出処理に使用される抽出溶媒は、ポリメトキシフラボンを抽出可能なものを適宜選択すればよいが、例えば、水；メタノール、エタノール、ｎ－プロパノール、イソプロパノール、ｎ－ブタノール等の炭素数１～４の低級１価アルコール；プロピレングリコール、１，３－ブチレングリコール等の多価アルコール；これらの混合溶媒等が挙げられる。これらの抽出溶媒の中でも、好ましくは、水、低級１価アルコール、及びこれらの混合溶媒、より好ましくは水、エタノール、及びこれらの混合溶媒、更に好ましくは水とエタノールの混合溶媒が挙げられる。抽出溶媒として、水と低級１価アルコールの混合溶媒を使用する場合、水と低級１価アルコールとの比率については、特に制限されないが、水：低級１価アルコールの重量比が、１：９９～９０：１０、好ましくは５：９５～７０：３０、より好ましくは５：９５～６０：４０、更に好ましくは５：９５～５０：５０が挙げられる。 The extraction solvent used in the solvent extraction process may be appropriately selected from those capable of extracting polymethoxyflavone, but examples include water; 4 lower monohydric alcohols; polyhydric alcohols such as propylene glycol and 1,3-butylene glycol; mixed solvents thereof, and the like. Among these extraction solvents, preferably water, lower monohydric alcohol, and a mixed solvent thereof, more preferably water, ethanol, and a mixed solvent thereof, still more preferably a mixed solvent of water and ethanol. When a mixed solvent of water and lower monohydric alcohol is used as the extraction solvent, the ratio of water and lower monohydric alcohol is not particularly limited, but the weight ratio of water:lower monohydric alcohol is 1:99 to 1:99. Examples include 90:10, preferably 5:95 to 70:30, more preferably 5:95 to 60:40, and even more preferably 5:95 to 50:50.
溶媒抽出処理は、抽出溶媒中にブラックジンジャーの原料部位を浸漬又は還流させて行えばよい。抽出処理後に固液分離により固形物を除去することにより、植物の抽出液が得られる。得られたブラックジンジャーの抽出液は、そのままブラックジンジャー抽出物として使用してもよいが、必要に応じて、一部又は全ての溶媒を除去して濃縮物又は乾燥物として使用してもよい。 The solvent extraction process may be performed by immersing or refluxing the raw material part of black ginger in the extraction solvent. After the extraction process, solid matter is removed by solid-liquid separation to obtain a plant extract. The obtained black ginger extract may be used as it is as a black ginger extract, but if necessary, part or all of the solvent may be removed and used as a concentrate or dry product.
本発明の経口組成物におけるポリメトキシフラボンの含有量については、経口組成物の形態、１日当たりの摂取・投与量等に応じて適宜設定すればよいが、例えば、０．５～６０重量％、好ましくは１～３０重量％、より好ましくは１～２０重量％が挙げられる。なお、本明細書におけるポリメトキシフラボンの含有量に関する記載は、ポリメトキシフラボンを含む植物抽出物を使用する場合は、当該植物抽出物に含まれるポリメトキシフラボン量に換算した値である。 The content of polymethoxyflavone in the oral composition of the present invention may be appropriately set depending on the form of the oral composition, daily intake/dosage, etc., but for example, 0.5 to 60% by weight, Preferably it is 1 to 30% by weight, more preferably 1 to 20% by weight. Note that, when a plant extract containing polymethoxyflavone is used, the description regarding the content of polymethoxyflavone in this specification is a value converted to the amount of polymethoxyflavone contained in the plant extract.
本発明の経口組成物において、γ－アミノ酪酸とポリメトキシフラボンとの比率としては、例えば、γ－アミノ酪酸１００重量部当たり、ポリメトキシフラボンが０．１～１００００重量部、好ましくは１～１０００重量部、より好ましくは１０～３５０重量部、更に好ましくは４０～８０重量部が挙げられる。 In the oral composition of the present invention, the ratio of γ-aminobutyric acid to polymethoxyflavone is, for example, 0.1 to 10,000 parts by weight, preferably 1 to 1,000 parts by weight of polymethoxyflavone per 100 parts by weight of γ-aminobutyric acid. Parts by weight, more preferably 10 to 350 parts by weight, still more preferably 40 to 80 parts by weight.
［ビタミンＢ類］
本発明の経口組成物は、ビタミンＢ類を含有する。本発明で使用されるビタミンＢ類の種類については、特に制限されないが、例えば、パントテン酸、ビタミンＢ2（リボフラビン、リボフラビン酢酸エステル等）、チアミン、ピリドキシン、ピリドキサール、ピリドキサミン、アデノシルコバラミン、メチルコバラミン、スルフィトコバラミン、ヒドロキソコバラミン、シアノコバラミンナイアシン、葉酸、ビオチン、ニコチン酸、及びこれらの塩等が挙げられる。これらのビタミンＢ類は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。
[Vitamin B]
The oral composition of the present invention contains B vitamins. The types of B vitamins used in the present invention are not particularly limited, but include, for example, pantothenic acid, vitamin B 2 (riboflavin, riboflavin acetate, etc.), thiamine, pyridoxine, pyridoxal, pyridoxamine, adenosylcobalamin, methylcobalamin. , sulfitocobalamin, hydroxocobalamin, cyanocobalamin niacin, folic acid, biotin, nicotinic acid, and salts thereof. These B vitamins may be used alone or in combination of two or more.
これらのビタミンＢ類の中でも、より一層効果的に血圧降下作用を向上させるという観点から、好ましくは、パントテン酸、パントテン酸の塩、及びビタミンＢ2の少なくとも１種、より好ましくは、パントテン酸及び／又はその塩とビタミンＢ2との組み合わせが挙げられる。 Among these B vitamins, from the viewpoint of more effectively improving the blood pressure lowering effect, at least one of pantothenic acid, a salt of pantothenic acid, and vitamin B 2 is preferred, and more preferably pantothenic acid and /or a combination of its salt and vitamin B2 .
ビタミンＢ類として、パントテン酸及び／又はその塩とビタミンＢ2とを組み合わせて使用する場合、これらの比率としては、例えば、パントテン酸及び／又はその塩の総量１００重量部当たり、ビタミンＢ2が総量で０．１～１００００重量部、好ましくは１～１０００重量部、より好ましくは１０～２００重量部、更に好ましくは２０～８０重量部が挙げられる。 When using a combination of pantothenic acid and/or its salt and vitamin B 2 as vitamin B, the ratio of these is, for example, 100 parts by weight of the total amount of pantothenic acid and/or its salt . The total amount is 0.1 to 10,000 parts by weight, preferably 1 to 1,000 parts by weight, more preferably 10 to 200 parts by weight, and still more preferably 20 to 80 parts by weight.
本発明の経口組成物におけるビタミンＢ類の含有量については、経口組成物の形態、１日当たりの摂取・投与量等に応じて適宜設定すればよいが、例えば、２～８０重量％、好ましくは３～５０重量％、より好ましくは５～３０重量％が挙げられる。 The content of B vitamins in the oral composition of the present invention may be appropriately set depending on the form of the oral composition, daily intake/dosage, etc., but for example, 2 to 80% by weight, preferably 3 to 50% by weight, more preferably 5 to 30% by weight.
本発明の経口組成物において、γ－アミノ酪酸とビタミンＢ類との比率としては、例えば、γ－アミノ酪酸１００重量部当たり、ビタミンＢ類が１～１００００重量部、より好ましくは１０～１０００重量部、更に好ましくは１００～４００重量部が挙げられる。 In the oral composition of the present invention, the ratio of γ-aminobutyric acid to vitamin B is, for example, 1 to 10,000 parts by weight, more preferably 10 to 1,000 parts by weight of vitamin B per 100 parts by weight of γ-aminobutyric acid. parts, more preferably 100 to 400 parts by weight.
［カルニチン及び／又はその塩］
本発明の経口組成物には、前述する成分に加えて、カルニチン及び／又はその塩を含んでいてもよい。カルニチンとは、リジンとメチオニンから合成されるビタミン様物質である。
[Carnitine and/or its salt]
The oral composition of the present invention may contain carnitine and/or a salt thereof in addition to the above-mentioned components. Carnitine is a vitamin-like substance synthesized from lysine and methionine.
本発明では、カルニチンとして、Ｌ－カルニチン、Ｄ－カルニチン、レボカルニチン、及びＤＬ－カルニチンのいずれを使用してもよいが、好ましくはＬ－カルニチン、ＤＬ－カルニチン、より好ましくはＬ－カルニチンが挙げられる。 In the present invention, as carnitine, any of L-carnitine, D-carnitine, levocarnitine, and DL-carnitine may be used, but L-carnitine, DL-carnitine, and more preferably L-carnitine are preferred. It will be done.
カルニチンの塩としては、可食性のものであることを限度として特に制限されないが、例えば、塩化物塩；ナトリウム塩、カリウム塩、カルシウム塩、マグネシウム塩、亜鉛塩等の金属塩；アンモニウム塩；酢酸塩、プロピオン酸塩、乳酸塩、酒石酸塩、クエン酸塩、コハク酸塩、マレイン酸塩、フマル酸塩等の有機酸塩；塩酸塩、硫酸塩、リン酸塩等の無機酸塩等が挙げられる。 Carnitine salts are not particularly limited as long as they are edible, but include, for example, chloride salts; metal salts such as sodium salts, potassium salts, calcium salts, magnesium salts, and zinc salts; ammonium salts; acetic acid salts. Organic acid salts such as salt, propionate, lactate, tartrate, citrate, succinate, maleate, fumarate; inorganic acid salts such as hydrochloride, sulfate, phosphate, etc. It will be done.
本発明の経口組成物にカルニチン及び／又はその塩を含有させる場合、その含有量については、経口組成物の形態、１日当たりの摂取・投与量等に応じて適宜設定すればよいが、例えば、２～８０重量％、好ましくは４～６０重量％、より好ましくは８～４０重量％が挙げられる。 When the oral composition of the present invention contains carnitine and/or its salt, the content may be determined as appropriate depending on the form of the oral composition, daily intake/dosage, etc. 2 to 80% by weight, preferably 4 to 60% by weight, more preferably 8 to 40% by weight.
本発明の経口組成物にカルニチン及び／又はその塩を含有させる場合、γ－アミノ酪酸とカルニチン及び／又はその塩との比率としては、例えば、γ－アミノ酪酸１００重量部当たり、カルニチン及び／又はその塩が総量で１～１０００００重量部、より好ましくは１０～１００００重量部、更に好ましくは１００～１０００重量部が挙げられる。 When the oral composition of the present invention contains carnitine and/or its salt, the ratio of γ-aminobutyric acid to carnitine and/or its salt is, for example, per 100 parts by weight of γ-aminobutyric acid, carnitine and/or The total amount of the salt is 1 to 100,000 parts by weight, more preferably 10 to 10,000 parts by weight, and even more preferably 100 to 1,000 parts by weight.
［その他の成分］
本発明の経口組成物は、前述する成分に加えて、他の栄養成分や薬理成分を含有していてもよい。このような栄養成分や薬理成分としては、食品や内服用医薬品に使用可能なものであれば特に制限されないが、例えば、ビタミン（ビタミンＢ類以外）、アミノ酸、ミネラル、糖質、脂肪酸、香料、調味剤、植物エキス、抗酸化剤、血糖降下剤、抗コレステロール剤、免疫賦活剤等が挙げられる。これらの成分は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。また、これらの成分の含有量については、使用する添分の種類や経口組成物の用途等に応じて適宜設定される。
[Other ingredients]
In addition to the above-mentioned components, the oral composition of the present invention may contain other nutritional components and pharmacological components. Such nutritional and pharmacological ingredients are not particularly limited as long as they can be used in foods and internal medicines, but include, for example, vitamins (other than B vitamins), amino acids, minerals, carbohydrates, fatty acids, fragrances, Examples include seasonings, plant extracts, antioxidants, hypoglycemic agents, anticholesterol agents, and immunostimulants. These components may be used alone or in combination of two or more. Further, the content of these components is appropriately set depending on the types of additives used, the intended use of the oral composition, and the like.
更に、本発明の経口組成物は、所望の製剤形態に調製するために、必要に応じて前述する成分の他に、基剤や添加剤等が含まれていてもよい。このような基剤及び添加剤としては、食品や内服用医薬品に使用可能なものであれば特に制限されないが、例えば、賦形剤、崩壊剤、滑沢剤、結合剤、増粘剤、低級アルコール、固形油、高級アルコール、水溶性高分子、界面活性剤、多価アルコール、ｐＨ調整剤、緩衝剤、酸化防止剤、防腐剤、キレート剤、水等が挙げられる。これらは、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。また、これらの基剤や添加剤の含有量については、使用する成分の種類や経口組成物の用途等に応じて適宜設定される。 Furthermore, in order to prepare the oral composition of the present invention into a desired dosage form, in addition to the above-mentioned components, the oral composition may contain a base, additives, etc. as necessary. Such bases and additives are not particularly limited as long as they can be used in foods and internal medicines, but include excipients, disintegrants, lubricants, binders, thickeners, and lower grade Examples include alcohol, solid oil, higher alcohol, water-soluble polymer, surfactant, polyhydric alcohol, pH adjuster, buffer, antioxidant, preservative, chelating agent, water, and the like. These may be used alone or in combination of two or more. Further, the contents of these bases and additives are appropriately set depending on the types of components used, the intended use of the oral composition, and the like.
[剤型・製剤形態]
本発明の経口組成物の剤型については、経口摂取又は経口投与が可能であることを限度として特に制限されず、固体状、半固体状、又は液体状のいずれであってもよく、経口組成物の種類や用途に応じて適宜設定すればよい。
[Dosage form/formulation]
The dosage form of the oral composition of the present invention is not particularly limited as long as it can be taken orally administered, and may be solid, semi-solid, or liquid. It may be set as appropriate depending on the type and purpose of the object.
本発明の経口組成物の製剤形態については、経口摂取又は経口投与が可能であることを限度として特に制限されないが、具体的には、飲食品及び内服用医薬品が挙げられる。 The formulation form of the oral composition of the present invention is not particularly limited as long as it can be taken orally administered, and specific examples thereof include food and drinks and internal medicines.
本発明の経口組成物を飲食品の製剤形態にする場合、前述する成分を、そのまま又は他の食品素材や添加成分と組み合わせて所望の形態に調製すればよい。このような飲食品としては、一般の飲食品の他、特定保健用食品、栄養補助食品、機能性表示食品、病者用食品等が挙げられる。これらの飲食品の形態として、特に制限されないが、具体的には、カプセル剤（ソフトカプセル剤、ハードカプセル剤）、錠剤（コーティング錠を含む）、顆粒剤、散剤、ゼリー剤等のサプリメント；栄養ドリンク、果汁飲料、炭酸飲料、乳酸飲料等の飲料；団子、アイス、シャーベット、グミ、キャンディー等の嗜好品等が例示される。これらの飲食品の中でも、好ましくはサプリメント、より好ましくは錠剤、カプセル剤、顆粒剤、散剤が挙げられる。 When the oral composition of the present invention is made into a food or drink formulation, the above-mentioned components may be prepared into a desired form as is or in combination with other food materials or additive components. Examples of such foods and drinks include general foods and drinks, as well as foods for specified health uses, nutritional supplements, foods with functional claims, foods for the sick, and the like. The forms of these foods and drinks are not particularly limited, but specifically include supplements such as capsules (soft capsules, hard capsules), tablets (including coated tablets), granules, powders, and jelly; nutritional drinks; Examples include beverages such as fruit juice drinks, carbonated drinks, and lactic acid drinks; luxury goods such as dumplings, ice creams, sherbet, gummies, and candies. Among these foods and beverages, supplements are preferred, and tablets, capsules, granules, and powders are more preferred.
本発明の経口組成物を内服用医薬品の製剤形態にする場合、前述する成分を、そのまま又は他の添加成分と組み合わせて所望の形態に調製すればよい。このような内服用医薬品としては、具体的には、カプセル剤（ソフトカプセル剤、ハードカプセル剤）、錠剤（コーティング錠を含む）、顆粒剤、散剤、ゼリー剤、シロップ剤、液剤等が挙げられる。これらの内服用医薬品の中でも、好ましくは、錠剤、カプセル剤、顆粒剤、散剤が挙げられる。 When the oral composition of the present invention is made into a pharmaceutical preparation for internal use, the above-mentioned components may be prepared as is or in combination with other additive components to form a desired form. Specific examples of such internal medicines include capsules (soft capsules, hard capsules), tablets (including coated tablets), granules, powders, jellies, syrups, liquids, and the like. Among these medicines for internal use, tablets, capsules, granules, and powders are preferred.
［用途］
本発明の経口組成物の用途については、特に制限されないが、γ－アミノ酪酸の血圧降下作用を増強して発揮できるので、血圧降下用の経口組成物として好適に使用できる。本明細書において、血圧降下用の経口組成物とは、対象者の血圧を降下させる目的、又は対象者における血圧上昇を抑制する目的で使用される経口組成物を指す。また、高血圧は、高血圧症、メタボリックシンドローム、心筋梗塞、狭心症、脳梗塞等の疾患又は症状の危険因子になっているので、本発明の経口組成物は、これらの疾患又は症状の予防又は改善目的で使用することができる。
[Application]
The use of the oral composition of the present invention is not particularly limited, but it can enhance and exhibit the blood pressure lowering effect of γ-aminobutyric acid, so it can be suitably used as an oral composition for lowering blood pressure. As used herein, an oral composition for lowering blood pressure refers to an oral composition used for the purpose of lowering a subject's blood pressure or suppressing an increase in blood pressure in a subject. Furthermore, since hypertension is a risk factor for diseases or symptoms such as hypertension, metabolic syndrome, myocardial infarction, angina pectoris, and cerebral infarction, the oral composition of the present invention can be used to prevent or treat these diseases or symptoms. May be used for improvement purposes.
また、本発明の経口組成物に含まれるポリメトキシフラボンには、交感神経を優位にすることにより脂肪を燃焼させる作用があり、本発明の経口組成物は、血圧降下作用と共に脂肪燃焼作用も発揮し得るので、肥満の予防又は改善、内臓脂肪又は体脂肪の低減、メタボリックシンドロームの予防又は改善等の目的で使用することもできる。 In addition, the polymethoxyflavone contained in the oral composition of the present invention has the effect of burning fat by making sympathetic nerves dominant, and the oral composition of the present invention also exhibits a fat burning effect as well as a blood pressure lowering effect. Therefore, it can also be used for the purposes of preventing or improving obesity, reducing visceral fat or body fat, preventing or improving metabolic syndrome, etc.
［摂取又は服用量］
本発明の経口組成物の摂取又は服用量については、特に限定されず、製剤形態、用途等に応じて適宜設定されるが、例えば、成人の場合、１日当たりのγ－アミノ酪酸の摂取又は服用量が、５～５０ｍｇ程度、好ましくは１０～３０ｍｇ程度となるように設定すればよい。
[Intake or dose]
The intake or dosage of the oral composition of the present invention is not particularly limited and may be set appropriately depending on the formulation form, use, etc. For example, in the case of adults, the intake or dosage of γ-aminobutyric acid per day The amount may be set to be about 5 to 50 mg, preferably about 10 to 30 mg.
以下に実施例を示して本発明をより具体的に説明するが、本発明はこれらに限定されるものではない。 EXAMPLES The present invention will be explained in more detail with reference to Examples below, but the present invention is not limited thereto.
試験例１：血圧降下作用の評価
１．試験材料及び方法
（１）実験動物
高血圧症を自然発症するモデルラット（ＳＨＲ／Ｉｚｍ、雄、１３週齢；日本エスエルシー株式会社）を使用した。
Test Example 1: Evaluation of blood pressure lowering effect
1. Test materials and methods (1) Experimental animals A model rat (SHR/Izm, male, 13 weeks old; Japan SLC Co., Ltd.) that spontaneously develops hypertension was used.
（２）飼育条件
温度１８～２８度、湿度３０～８０％ＲＨ、照明時間１２時間／日（7～19時）の環境下で、１ケージに１匹を収容して飼育した。
(2) Breeding conditions One animal per cage was bred in an environment with a temperature of 18 to 28 degrees, humidity of 30 to 80% RH, and lighting time of 12 hours/day (7:00 to 19:00).
（３）飼料及び飲料
固形飼料ＭＦ（オリエンタル酵母工業株式会社）をケージ蓋の給餌部に入れて自由に摂取させた。また、オートクレーブ滅菌済みの給水瓶に水道水を充填し、ノズルより自由摂取させた。
（４）検体
表１に示す検体を調製した。
(4) Specimen Specimens shown in Table 1 were prepared.
（５）被験体の投与及び血圧測定
馴化期間中の一般状態に異常を認めなかったラットについて、血圧測定を実施し、各群の平均血圧と体重の測定値が均等になるように、対照群、比較例１の検体投与群、及び実施例１の検体投与群の３群（１群６匹）に分けた。対照群には、生理食塩水を経口投与した。比較例１の検体投与群のラットには、比較例１の検体０．５ｍｇを生理食塩水５ｍＬに溶解させた溶液を、検体投与量が０．５ｍｇ／ｋｇ体重（γ－アミノ酪酸の投与量が０．５ｍｇ／ｋｇ体重）となるように経口投与した。実施例１の検体投与群のラットには、実施例１の検体６．９ｍｇを生理食塩水５ｍＬに溶解させた溶液を、検体投与量が６．９ｍｇ／ｋｇ体重（γ－アミノ酪酸の投与量が０．５ｍｇ／ｋｇ体重）となるように経口投与した。
(5) Administration of subjects and blood pressure measurement Blood pressure measurements were carried out on rats that showed no abnormality in general condition during the acclimatization period. The animals were divided into three groups (6 animals per group): a sample administration group of Comparative Example 1, and a sample administration group of Example 1. Physiological saline was orally administered to the control group. The rats in the sample administration group of Comparative Example 1 were given a solution of 0.5 mg of the sample of Comparative Example 1 dissolved in 5 mL of physiological saline at a sample dose of 0.5 mg/kg body weight (dose of γ-aminobutyric acid). was orally administered at a concentration of 0.5 mg/kg body weight). The rats in the sample administration group of Example 1 received a solution of 6.9 mg of the sample of Example 1 dissolved in 5 mL of physiological saline at a sample dose of 6.9 mg/kg body weight (dose of γ-aminobutyric acid). was orally administered at a concentration of 0.5 mg/kg body weight).
検体投与直前、検体投与後４、８及び２４時間後に、非観血式血圧計を用いて血圧測定を行った。検体投与後の各時点での血圧値から検体投与直前の血圧値を差し引いた値を血圧変化値（ΔｍｍＨｇ）として求めた。 Immediately before administration of the sample, and 4, 8, and 24 hours after administration of the sample, blood pressure was measured using a non-invasive sphygmomanometer. The value obtained by subtracting the blood pressure value immediately before administration of the sample from the blood pressure value at each time point after administration of the sample was determined as a blood pressure change value (ΔmmHg).
（６）統計解析
血圧変化値は平均±標準誤差（平均値±標準偏差）で表記した。血圧変化値についてそれぞれ多群間比較を行った。血圧変化値について等分散の測定（Ｂａｒｔｌｅｔｔ検定、両側）を行った結果、検体投与後４及び２４時間の時点では等分散であったため、Ｄｕｎｎｅｔｔ検定を実施し、検体投与後８時間の時点では不等分散であったため、Ｓｔｅｅｌ－Ｄｗａｓｓ検定及びＳｔｅｅｌ検定（両側）を行った。いずれの場合も有意水準を５％とした。
(6) Statistical analysis Blood pressure change values were expressed as mean ± standard error (mean ± standard deviation). Multigroup comparisons were made for blood pressure changes. As a result of measuring equal variance for blood pressure change values (Bartlett test, two-tailed), it was found that the variance was equal at 4 and 24 hours after administration of the sample, so a Dunnett test was performed, and no difference was found at 8 hours after administration of the sample. Since the variances were equal, Steel-Dwass test and Steel test (two-tailed) were performed. In both cases, the significance level was set at 5%.
２．試験結果
結果を表２及び図１に示す。γ－アミノ酪酸を単独で含む検体（比較例１）を投与した群は、投与から８時間後に僅かな血圧降下が認められるに止まっていた。これに対して、γ－アミノ酪酸とポリメトキシフラボンを含む検体（実施例１）を投与した群は、投与から４時間後には血圧降下が認められ、８時間後には対照群に比べて有意な血圧降下が認められた。
また、実施例１の検体から、Ｌ－カルニチンを除外した検体についても、前記と同様に試験（γ－アミノ酪酸の投与量が０．５ｍｇ／ｋｇ体重となるように設定）したところ、実施例１の検体投与群と同様に、優れた血圧降下効果が認められた。一方、実施例１の検体から、パントテン酸カルシウム、リボフラビン、及びＬ－カルニチンを除外した検体についても、前記と同様に試験（γ－アミノ酪酸の投与量が０．５ｍｇ／ｋｇ体重となるように設定）したところ、血圧変化値の経時変化は対照群と略同じであった。また、実施例１の検体から、パントテン酸カルシウム及びリボフラビンを除外した検体についても、前記と同様に試験（γ－アミノ酪酸の投与量が０．５ｍｇ／ｋｇ体重となるように設定）したところ、血圧変化値の経時変化は対照群と略同じであった。更に、ブラックジンジャー抽出物を単独で３．７ｍｇ／ｋｇ体重となるように投与して前記と同様に試験したところ、血圧変化値の経時変化は対照群と略同じであった。また、パントテン酸カルシウム０．７ｍｇ／ｋｇ体重とリボフラビン０．３ｍｇ／ｋｇ体重を同時投与して前記と同様に試験したところ、血圧変化値の経時変化は対照群と略同じであった。 In addition, when the sample from Example 1 except for L-carnitine was tested in the same manner as above (the dose of γ-aminobutyric acid was set to be 0.5 mg/kg body weight), it was found that Similar to sample administration group 1, an excellent blood pressure lowering effect was observed. On the other hand, the sample from Example 1 excluding calcium pantothenate, riboflavin, and L-carnitine was tested in the same manner as above (the dose of γ-aminobutyric acid was 0.5 mg/kg body weight). (setting), the time-course changes in blood pressure values were approximately the same as in the control group. In addition, a sample from Example 1 excluding calcium pantothenate and riboflavin was also tested in the same manner as above (the dose of γ-aminobutyric acid was set to be 0.5 mg/kg body weight). The change in blood pressure over time was almost the same as in the control group. Furthermore, when black ginger extract was administered alone at a dose of 3.7 mg/kg body weight and tested in the same manner as above, the change in blood pressure over time was approximately the same as in the control group. Further, when 0.7 mg/kg body weight of calcium pantothenate and 0.3 mg/kg body weight of riboflavin were administered simultaneously and tested in the same manner as above, the change in blood pressure over time was approximately the same as in the control group.
以上の結果から、γ－アミノ酪酸とポリメトキシフラボンとビタミンＢ類を組み合わせて使用することにより、これらの相乗効果によって、γ－アミノ酪酸の血圧降下作用が飛躍的に向上することが明らかとなった。 From the above results, it is clear that the synergistic effect of using γ-aminobutyric acid, polymethoxyflavone, and B vitamins in combination dramatically improves the blood pressure lowering effect of γ-aminobutyric acid. Ta.
処方例
表３に示した経口組成物（錠剤）を調製し、錠剤を粉砕し試験例１と同様の方法で、血圧降下作用を評価したところ、処方例１～５のいずれの経口組成物においても、血圧降下効果が認められた。
Prescription Example The oral compositions (tablets) shown in Table 3 were prepared, the tablets were crushed, and the blood pressure lowering effect was evaluated in the same manner as in Test Example 1. A blood pressure lowering effect was also observed.
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