JP2021097637A - Oral composition - Google Patents
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- JP2021097637A JP2021097637A JP2019231400A JP2019231400A JP2021097637A JP 2021097637 A JP2021097637 A JP 2021097637A JP 2019231400 A JP2019231400 A JP 2019231400A JP 2019231400 A JP2019231400 A JP 2019231400A JP 2021097637 A JP2021097637 A JP 2021097637A
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- monacolin
- lactone
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- 239000000203 mixture Substances 0.000 title claims abstract description 45
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims abstract description 81
- 229920001353 Dextrin Polymers 0.000 claims abstract description 30
- 239000004375 Dextrin Substances 0.000 claims abstract description 30
- 235000019425 dextrin Nutrition 0.000 claims abstract description 30
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims description 74
- 235000013305 food Nutrition 0.000 claims description 14
- 238000006243 chemical reaction Methods 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 8
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract description 20
- 239000008280 blood Substances 0.000 abstract description 9
- 210000004369 blood Anatomy 0.000 abstract description 9
- 230000000694 effects Effects 0.000 abstract description 7
- 229940026314 red yeast rice Drugs 0.000 description 7
- 239000000654 additive Substances 0.000 description 6
- 239000000843 powder Substances 0.000 description 6
- 239000003826 tablet Substances 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- 150000002596 lactones Chemical class 0.000 description 5
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 4
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 230000000996 additive effect Effects 0.000 description 4
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- 229940079593 drug Drugs 0.000 description 4
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- 229920002472 Starch Polymers 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 150000001298 alcohols Chemical class 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 235000013361 beverage Nutrition 0.000 description 2
- 235000015872 dietary supplement Nutrition 0.000 description 2
- 239000008157 edible vegetable oil Substances 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 235000012041 food component Nutrition 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 235000001727 glucose Nutrition 0.000 description 2
- 239000007902 hard capsule Substances 0.000 description 2
- 235000015110 jellies Nutrition 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 239000007901 soft capsule Substances 0.000 description 2
- 239000013589 supplement Substances 0.000 description 2
- IVLXQGJVBGMLRR-UHFFFAOYSA-N 2-aminoacetic acid;hydron;chloride Chemical compound Cl.NCC(O)=O IVLXQGJVBGMLRR-UHFFFAOYSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- VCTWQBQEFPBQGT-ZXVDENEASA-N CC[C@H](C)C(O[I]1[C@](C)([C@@H](CC[C@H](C[C@H](CC(C)=O)O)O)[C@@H](C)CC2)C2=CCC1)=O Chemical compound CC[C@H](C)C(O[I]1[C@](C)([C@@H](CC[C@H](C[C@H](CC(C)=O)O)O)[C@@H](C)CC2)C2=CCC1)=O VCTWQBQEFPBQGT-ZXVDENEASA-N 0.000 description 1
- 240000004160 Capsicum annuum Species 0.000 description 1
- 235000008534 Capsicum annuum var annuum Nutrition 0.000 description 1
- 235000007862 Capsicum baccatum Nutrition 0.000 description 1
- 229920001661 Chitosan Polymers 0.000 description 1
- 229920002245 Dextrose equivalent Polymers 0.000 description 1
- 239000004278 EU approved seasoning Substances 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920002774 Maltodextrin Polymers 0.000 description 1
- 239000005913 Maltodextrin Substances 0.000 description 1
- 244000113306 Monascus purpureus Species 0.000 description 1
- 235000002322 Monascus purpureus Nutrition 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
- 108090000854 Oxidoreductases Proteins 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- -1 and for example Substances 0.000 description 1
- 229940127226 anticholesterol agent Drugs 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000001728 capsicum frutescens Substances 0.000 description 1
- 235000014171 carbonated beverage Nutrition 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000010411 cooking Methods 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000011194 food seasoning agent Nutrition 0.000 description 1
- 235000015203 fruit juice Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000002304 glucoses Chemical class 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 229940126904 hypoglycaemic agent Drugs 0.000 description 1
- 235000015243 ice cream Nutrition 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229960004844 lovastatin Drugs 0.000 description 1
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 229930185723 monacolin Natural products 0.000 description 1
- 229940057059 monascus purpureus Drugs 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000010865 sewage Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
Landscapes
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
本発明は、ラクトン型モナコリンＫを含み、体内でラクトン型モナコリンＫを酸型モナコリンＫに効率的に変換できる経口組成物に関する。 The present invention relates to an oral composition containing lactone-type monacolin K, which can efficiently convert lactone-type monacolin K to acid-type monacolin K in the body.
モナコリンＫ（ロバスタチンと称されることもある）は、紅麹によって産生される化合物であり、体内のコレステロール合成酵素であるＨＭＧ−ＣｏＡレダクターゼを阻害する作用があり、血中コレステロールを低下できることが知られている。 Monacolin K (sometimes called lovastatin) is a compound produced by red yeast rice and is known to have the effect of inhibiting HMG-CoA reductase, which is a cholesterol synthase in the body, and can lower blood cholesterol. Has been done.
従来、モナコリンＫを配合した様々な経口組成物に応用することが検討告されている。例えば、特許文献１には、紅麹及び／又は紅麹エキスを主体として、これにキトサンを混入してなる紅麹健康補助食品が、血圧降下や汚血浄化等に有効であることが開示されている。また、特許文献２には、モナコリンＫを含有する食用油脂が、血中コレステロール濃度を低下させる調理・加工用の食用油脂として有用であることが開示されている。特許文献３には、モナコリンＫを１ｍｇ以上含有する紅楸ドリンクによって、飲料として１日に必要なモナコリンＫを一時に摂取可能になることが開示されている。 Conventionally, it has been studied and announced that it may be applied to various oral compositions containing monacolin K. For example, Patent Document 1 discloses that a red yeast rice health supplement containing red yeast rice and / or red yeast rice extract mixed with chitosan is effective for lowering blood pressure, purifying sewage, and the like. ing. Further, Patent Document 2 discloses that an edible oil / fat containing monacolin K is useful as an edible oil / fat for cooking / processing that lowers a blood cholesterol concentration. Patent Document 3 discloses that a red pepper drink containing 1 mg or more of monacolin K makes it possible to temporarily ingest monacolin K, which is necessary for one day as a beverage.
モナコリンＫには、以下に示すラクトン型と酸型が存在し、これらは相互に変換可能であることが知られている。また、モナコリンＫは、生体内において、酸型が活性を示し、ラクトン型では不活性であることが知られている（非特許文献１）。
一方、紅麹等を用いて製造されるモナコリンＫは、７０〜９０％程度がラクトン型（即ち、不活性型）であり、モナコリンＫ摂取による血中コレステロール低下効果を有効に奏させるには、生体内でモナコリンＫをラクトン型から酸型に効率的に変換させることが重要になる。しかしながら、従来、生体内でモナコリンＫをラクトン型から酸型に効率的に変換させるための製剤技術については報告されていない。 On the other hand, about 70 to 90% of monacolin K produced by using red yeast rice or the like is a lactone type (that is, an inactive type), and in order to effectively exert the blood cholesterol lowering effect by ingesting monacolin K, it is necessary. It is important to efficiently convert monacolin K from the lactone type to the acid type in the living body. However, conventionally, no formulation technique for efficiently converting monacolin K from a lactone type to an acid type in a living body has been reported.
本発明の目的は、ラクトン型モナコリンＫを含み、体内でラクトン型モナコリンＫを酸型モナコリンＫに効率的に変換でき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 lactone-type monacolin K, which can efficiently convert lactone-type monacolin K to acid-type monacolin K in the body.
本発明者は、前記課題を解決すべく鋭意検討を行ったところ、ラクトン型モナコリンＫと共にデキストリンを含む経口組成物は、体内でラクトン型モナコリンＫを酸型モナコリンＫに効率的に変換でき、モナコリンＫによる血中コレステロール低下効果を効率的に奏させ得ることを見出した。本発明は、かかる知見に基づいて、更に検討を重ねることにより完成したものである。 As a result of diligent studies to solve the above problems, the present inventor has found that an oral composition containing dextrin together with lactone-type monacolin K can efficiently convert lactone-type monacolin K to acid-type monacolin K in the body, and monacolin. It has been found that the blood cholesterol lowering effect of K can be effectively exerted. The present invention has been completed by further studies based on such findings.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項１． ラクトン型モナコリンＫ、及びデキストリンを含む、経口組成物。
項２． ラクトン型モナコリンＫ １重量部当たり、デキストリンを１〜１０００００重量部含む、項１に記載の経口組成物。
項３． 飲食品である、項１又は２に記載の経口組成物。
項４． ラクトン型モナコリンＫの酸型モナコリンＫへの変換効率を向上させる方法であって、経口組成物中で、ラクトン型モナコリンＫとデキストリンを共存させる、方法。
That is, the present invention provides the inventions of the following aspects.
Item 1. An oral composition comprising a lactone-type monacolin K and dextrin.
Item 2. Item 2. The oral composition according to Item 1, which contains 1 to 100,000 parts by weight of dextrin per 1 part by weight of lactone-type monacolin K.
Item 3. Item 2. The oral composition according to Item 1 or 2, which is a food or drink.
Item 4. A method for improving the conversion efficiency of lactone-type monacolin K to acid-type monacolin K, wherein lactone-type monacolin K and dextrin coexist in an oral composition.
本発明によれば、体内で、ラクトン型モナコリンＫ（不活性型）を酸型モナコリンＫ（活性型）に効率的に変換できるので、モナコリンＫによるＨＭＧ−ＣｏＡレダクターゼ阻害作用を効率的に発揮させ、優れた血中コレステロール低下効果を奏することができる。 According to the present invention, lactone-type monacolin K (inactive form) can be efficiently converted to acid-type monacolin K (active form) in the body, so that the HMG-CoA reductase inhibitory action of monacolin K can be efficiently exerted. , Can exert an excellent blood cholesterol lowering effect.
１．経口組成物
本発明の経口組成物は、ラクトン型モナコリンＫ及びデキストリン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。
1. 1. Oral Composition The oral composition of the present invention is characterized by containing lactone-type monacolin K and dextrin. Hereinafter, the oral composition of the present invention will be described in detail.
［ラクトン型モナコリンＫ］
本発明の経口組成物は、ラクトン型モナコリンＫを含有する。ラクトン型モナコリンＫ自体は、ＨＭＧ−ＣｏＡレダクターゼの阻害作用が低く、血中コレステロールの低下効果が微弱であるが、本発明によれば、体内で酸型モナコリンＫに効率的に変換させることができる。
[Lactone-type monacolin K]
The oral composition of the present invention contains a lactone-type monacolin K. Lactone-type monacolin K itself has a low inhibitory effect on HMG-CoA reductase and has a weak effect of lowering blood cholesterol, but according to the present invention, it can be efficiently converted to acid-type monacolin K in the body. ..
ラクトン型モナコリンＫは、紅麹菌株モナスカス・ピローサス等のモナコリンＫ産生菌を用いて製楸する方法等の公知の製造方法で得ることができる。 The lactone-type monacolin K can be obtained by a known production method such as a method for producing monacolin K-producing bacteria such as Monascus purpureus and Pirosus.
また、ラクトン型モナコリンＫは、酸型モナコリンＫと混合された状態のものを使用してもよく、また紅麹のエキス、紅麹の粉末化物等の状態のものを使用してもよい。 Further, the lactone-type monacolin K may be used in a state of being mixed with the acid-type monacolin K, or may be in a state of a red yeast rice extract, a powdered red yeast rice, or the like.
本発明の経口組成物におけるラクトン型モナコリンＫの含有量については、配合される他の成分の含有量、経口組成物の形態や用途、１回当たりの摂取量等に応じて適宜設定すればよいが、例えば、０．００１〜１０重量％、好ましくは０．０１〜９．５重量％、より好ましくは０．１〜９．５重量％、更に好ましくは０．１〜９．１重量％が挙げられる。 The content of lactone-type monacolin K in the oral composition of the present invention may be appropriately set according to the content of other components to be blended, the form and use of the oral composition, the amount of intake per dose, and the like. However, for example, 0.001 to 10% by weight, preferably 0.01 to 9.5% by weight, more preferably 0.1 to 9.5% by weight, still more preferably 0.1 to 9.1% by weight. Can be mentioned.
［デキストリン］
本発明の経口組成物は、デキストリンを含有する。本発明において、デキストリンは、体内でラクトン型モナコリンＫが酸型モナコリンＫに変換されるのを促進する役割を果たす。
[dextrin]
The oral composition of the present invention contains dextrin. In the present invention, dextrin plays a role in promoting the conversion of lactone-type monacolin K to acid-type monacolin K in the body.
本発明で使用されるデキストリンは、直鎖状、分岐鎖状、又は環状のいずれであってもよいが、好ましくは鎖状が挙げられる。また、本発明で使用されるデキストリンにおいて、グルコース間の結合様式としては、例えば、α−１，４結合、α−１，６結合、β−１，２結合、β−１，３結合、β−１，４結合、β−１，６結合等のいずれであってもよく、単一の結合様式のみを含むものであっても、また、２種以上の結合様式方式を含むものであってもよい。体内における酸型モナコリンＫへの変換効率をより一層向上させるという観点から、好ましくはα−１，４結合及びα−１，６結合のいずれか少なくとも一方を有するデキストリンが挙げられる。 The dextrin used in the present invention may be linear, branched or cyclic, but is preferably chain. Further, in the dextrin used in the present invention, as the binding mode between glucoses, for example, α-1,4 bond, α-1,6 bond, β-1,2 bond, β-1,3 bond, β It may be any of -1,4 bond, β-1,6 bond, etc., it may contain only a single binding mode, or it may contain two or more binding modes. May be good. From the viewpoint of further improving the conversion efficiency to acid-type monacolin K in the body, dextrin having at least one of α-1,4 bond and α-1,6 bond is preferable.
本発明において、「デキストリン」は、狭義のデキストリン及びマルトデキストリンを指しており、分子量が大きい難消化性デキストリンや焙焼デキストリンは包含されない。本発明で使用されるデキストリンのＤＥについては、１〜２０であればよいが、体内における酸型モナコリンＫへの変換効率をより一層向上させるという観点から、好ましくは１〜１５、より好ましくは１〜１０、更に好ましくは２〜８、特に好ましくは６〜８が挙げられる。本発明において、デキストリンのＤＥとは、澱粉の分解程度を示す指標であるデキストロース当量であり、ソモギ変法（澱粉糖関連工業分析法１１〜１３頁、澱粉糖技術部会編、食品化学新聞社発行）により測定される値である。 In the present invention, "dextrin" refers to dextrin and maltodextrin in a narrow sense, and does not include indigestible dextrin or roasted dextrin having a large molecular weight. The DE of the dextrin used in the present invention may be 1 to 20, but is preferably 1 to 15, more preferably 1 from the viewpoint of further improving the conversion efficiency to acid-type monacolin K in the body. 10, more preferably 2 to 8, and particularly preferably 6 to 8. In the present invention, DE of dextrin is a dextrose equivalent which is an index indicating the degree of decomposition of starch, and is a modified Somogi method (starch sugar-related industrial analysis method, pp. 11 to 13, edited by Starch Sugar Technology Subcommittee, published by Food Chemistry Newspaper). ) Is the value measured by.
本発明において、デキストリンは、１種の構造のものを単独で使用してもよく、また２種以上の構造のものを組み合わせて使用してもよい。 In the present invention, the dextrin may be used alone or in combination of two or more types.
本発明の経口組成物におけるデキストリンの含有量については、配合されるラクトン型モナコリンＫの含有量、経口組成物の形態や用途、１回当たりの摂取量等に応じて適宜設定すればよいが、例えば、５〜９９．９９５重量％、好ましくは１０〜９９重量％、より好ましくは２０〜９５重量％、更に好ましくは３０〜９０重量％が挙げられる。 The content of dextrin in the oral composition of the present invention may be appropriately set according to the content of the lactone-type monacolin K to be blended, the form and use of the oral composition, the amount of intake per dose, and the like. For example, 5 to 99.995% by weight, preferably 10 to 99% by weight, more preferably 20 to 95% by weight, still more preferably 30 to 90% by weight.
また、本発明の経口組成物におけるラクトン型モナコリンＫとデキストリンの比率としては、例えば、ラクトン型モナコリンＫ１重量部当たり、デキストリンが１〜１０００００重量部、好ましくは１０〜２００００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、特に好ましくは３００〜１０００重量部が挙げられる。 The ratio of lactone-type monacolin K to dextrin in the oral composition of the present invention is, for example, 1 to 100,000 parts by weight, preferably 10 to 20,000 parts by weight, more preferably 10 parts by weight of dextrin per 1 part by weight of lactone-type monacolin K. Examples thereof include 10000 parts by weight, more preferably 100 to 1000 parts by weight, and particularly preferably 300 to 1000 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、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]
The oral composition of the present invention may contain other nutritional components and pharmacological components in addition to the above-mentioned components. Such nutritional components and pharmacological components are not particularly limited as long as they can be used in foods and oral medicines, and for example, vitamins, amino acids, minerals, sugars, fatty acids, flavors, seasonings, plant extracts, etc. Examples thereof include antioxidants, hypoglycemic agents, anticholesterol agents, immunostimulators and the like. These components may be used alone or in combination of two or more. The content of these components is appropriately set according to the type of additive used, the 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。 Further, the oral composition of the present invention may contain a base, an additive and the like in addition to the above-mentioned components, if necessary, in order to prepare it into a desired pharmaceutical form. Such bases and additives are not particularly limited as long as they can be used in foods and oral medicines, and are, for example, excipients, disintegrants, lubricants, binders, thickeners, and lower grades. Examples thereof include alcohols, solid oils, higher alcohols, water-soluble polymers, surfactants, polyhydric alcohols, pH adjusters, buffers, antioxidants, preservatives, chelating agents, water and the like. These may be used individually by 1 type, and may be used in combination of 2 or more type. The contents of these bases and additives are appropriately set according to the type of ingredients used, the 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 form]
The dosage form of the oral composition of the present invention is not particularly limited as long as it can be orally ingested or orally administered, and may be solid, semi-solid, or liquid, and the oral composition. It may be set appropriately according to the type and use 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 pharmaceutical form of the oral composition of the present invention is not particularly limited as long as it can be orally ingested or orally administered, and specific examples thereof include foods and drinks and oral 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 formed into a pharmaceutical form, the above-mentioned components may be prepared as they are or in combination with other food materials or additive components into a desired form. Examples of such foods and drinks include general foods and drinks, foods for specified health use, dietary supplements, foods with functional claims, foods for the sick, and the like. The form of these foods and drinks is not particularly limited, but specifically, supplements such as capsules (soft capsules, hard capsules), tablets (including coated tablets), granules, powders, jellies, etc.; nutritional drinks, Beverages such as fruit juice drinks, carbonated drinks, and lactic acid drinks; luxury products such as dumplings, ice cream, sherbet, gummy, and candy are exemplified. Among these foods and drinks, supplements are preferable, and tablets, capsules, granules and powders are more preferable.
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 form for internal use, the above-mentioned components may be prepared as they are or in combination with other additive components into a desired form. Specific examples of such an internal medicine include capsules (soft capsules, hard capsules), tablets (including coated tablets), granules, powders, jellies, syrups, liquids and the like. Among these oral medicines, tablets, capsules, granules and powders are preferable.
［用途］
本発明の経口組成物は、体内でラクトン型モナコリンＫを効率的に酸型モナコリンＫに変換させて、ＨＭＧ−ＣｏＡレダクターゼ阻害作用、及び血中コレステロール低下作用を効率的に発現させるので、ＨＭＧ−ＣｏＡレダクターゼ阻害用途や血中コレステロール低下用途に使用することができる。
[Use]
The oral composition of the present invention efficiently converts lactone-type monacolin K into acid-type monacolin K in the body to efficiently express the HMG-CoA reductase inhibitory action and the blood cholesterol lowering action, and thus HMG- It can be used for CoA reductase inhibitory use and blood cholesterol lowering use.
［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日当たりのラクトン型モナコリンＫの摂取又は服用量が、０．１〜１０ｍｇ程度、好ましくは０．５〜１０ｍｇ程度となるように設定すればよい。
[Intake or dosage]
The ingestion or dosage of the oral composition of the present invention is not particularly limited and is appropriately set according to the formulation form, use and the like. For example, in the case of an adult, ingestion or administration of lactone-type monacolin K per day. The amount may be set to be about 0.1 to 10 mg, preferably about 0.5 to 10 mg.
２．ラクトン型モナコリンＫの酸型モナコリンＫへの変換効率向上方法
本発明は、更に、ラクトン型モナコリンＫの酸型モナコリンＫへの変換効率向上方法であって、経口組成物中で、ラクトン型モナコリンＫとデキストリンを共存させる方法を提供する。
2. Method for improving conversion efficiency of lactone-type monacolin K to acid-type monacolin K The present invention further provides a method for improving the conversion efficiency of lactone-type monacolin K to acid-type monacolin K in an oral composition. And provide a method for coexistence of dextrins.
本方法において、ラクトン型モナコリンＫ及びデキストリンの種類、含有量、これらの比率、経口組成物に配合可能な他の成分、経口組成物の剤形、形態、用途等については、前記「１．経口組成物」の欄に記載の通りである。 In this method, the types and contents of lactone-type monacolin K and dextrin, their ratios, other components that can be blended in the oral composition, the dosage form, form, use, etc. of the oral composition are described in the above-mentioned "1. Oral". As described in the "Composition" column.
次に、本発明を実施例により、更に詳細に説明するが、本発明は、これらの例によってなんら限定されるものではない。 Next, the present invention will be described in more detail by way of examples, but the present invention is not limited to these examples.
試験例１
１．５ｍｌ容のマイクロチューブに、ラクトン型モナコリンＫ（東京化成工業株式会社）１ｍｇ、表１に示す各検体１０ｍｇ、１００ｍｇ又は３００ｍｇ、及び人工胃液（１００ｍＭグリシン−塩酸溶液、ｐＨ２．２）０．１ｍｌをこの順に添加し、２５℃で１時間保温した。試験開始時と１時間保温後の液について、ＨＰＬＣにて酸型モナコリンＫ量を定量し、下記算出式に従って、酸型モナコリンＫへの変換率を算出した。
In a 1.5 ml microtube, 1 mg of lactone-type monacolin K (Tokyo Chemical Industry Co., Ltd.), 10 mg, 100 mg or 300 mg of each sample shown in Table 1, and artificial gastric juice (100 mM glycine-hydrochloric acid solution, pH 2.2) 0. 1 ml was added in this order and kept warm at 25 ° C. for 1 hour. The amount of acid-type monacolin K was quantified by HPLC for the liquid at the start of the test and after being kept warm for 1 hour, and the conversion rate to acid-type monacolin K was calculated according to the following formula.
結果を表１に示す。ラクトン型モナコリンＫと、片栗粉、グルコース又は結晶セルロースを共存させた場合には、ラクトン型モナコリンＫから酸型モナコリンＫへの変換がやや促進されていたが、酸型モナコリンＫへの変換率はいずれも２％を下回っていた。これに対して、ラクトン型モナコリンＫとデキストリンを共存させた場合には、ラクトン型モナコリンＫから酸型モナコリンＫへの変換が飛躍的に促進されていた。即ち、以上の結果から、ラクトン型モナコリンＫとデキストリンを含む経口組成物は、胃内でラクトン型モナコリンＫを酸型モナコリンＫに効率的に変換させ得ることが明らかとなった。本効果は、出発原料が同種の成分や賦形剤として汎用される原料の中でも、デキストリン特有の効果であることが示された。 The results are shown in Table 1. When lactone-type monacolin K and potato starch, glucose, or crystalline cellulose were allowed to coexist, the conversion of lactone-type monacolin K to acid-type monacolin K was slightly promoted, but the conversion rate to acid-type monacolin K will eventually increase. Was also below 2%. On the other hand, when lactone-type monacolin K and dextrin coexisted, the conversion of lactone-type monacolin K to acid-type monacolin K was dramatically promoted. That is, from the above results, it was clarified that the oral composition containing lactone-type monacolin K and dextrin can efficiently convert lactone-type monacolin K to acid-type monacolin K in the stomach. It was shown that this effect is peculiar to dextrin among the raw materials whose starting materials are generally used as the same kind of ingredients and excipients.
製造例
表２に示す組成の粉末剤を調製した。得られた粉末剤を人工胃液に添加すると、ラクトン型モナコリンＫから酸型モナコリンＫに効率的に変換されることが確認された。
Production Example A powder having the composition shown in Table 2 was prepared. It was confirmed that when the obtained powder was added to artificial gastric juice, lactone-type monacolin K was efficiently converted to acid-type monacolin K.
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