JP2020196672A - Vitamin B12-containing composition - Google Patents

Vitamin B12-containing composition Download PDF

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JP2020196672A
JP2020196672A JP2019102033A JP2019102033A JP2020196672A JP 2020196672 A JP2020196672 A JP 2020196672A JP 2019102033 A JP2019102033 A JP 2019102033A JP 2019102033 A JP2019102033 A JP 2019102033A JP 2020196672 A JP2020196672 A JP 2020196672A
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vitamin
weight
composition
fatty acid
sorbitan fatty
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美穂 金本
Miho Kanemoto
美穂 金本
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Kobayashi Pharmaceutical Co Ltd
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Kobayashi Pharmaceutical Co Ltd
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Priority to JP2019102033A priority Critical patent/JP2020196672A/en
Priority to CN202080034923.2A priority patent/CN113811314A/en
Priority to PCT/JP2020/019747 priority patent/WO2020241374A1/en
Publication of JP2020196672A publication Critical patent/JP2020196672A/en
Priority to JP2023207968A priority patent/JP2024023610A/en
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Abstract

To provide a composition which contains a vitamin B12 and in which the decomposition of the vitamin B12 due to light exposure is suppressed.SOLUTION: A polyoxyethylene sorbitan fatty acid ester is added to a vitamin B12-containing composition and the content of the polyoxyethylene sorbitan fatty acid ester is controlled to 10 pts.wt. or less per part by weight of the vitamin B12. Thus, the decomposition of the vitamin B12 can be suppressed even if the composition is exposed to light under severe conditions and an extremely remarkable effect of photostabilizing the vitamin B12 can be achieved.SELECTED DRAWING: None

Description

本発明は、ビタミンB12類を含み、光暴露によるビタミンB12類の分解が抑制されている組成物に関する。 The present invention includes a vitamin B 12 compounds, to compositions which decomposition of vitamin B 12 compound by light exposure is inhibited.

ビタミンB12類は、水溶性ビタミンの一種であり、生命を維持するために不可欠な栄養素である。ビタミンB12類は、ビタミンB12類欠乏症、巨赤芽球性貧血、広節裂頭条虫症、悪性貧血、吸収不全症候群、眼精疲労、栄養性貧血、妊娠性貧血、神経痛等の症状の予防又は改善、肌荒れ改善等に有効であることが知られており、飲食品、口腔ケア製品、医薬品、化粧料等で使用されている。一方、ビタミンB12類は、光暴露により分解され易いことが知られており、ビタミンB12類を含む製品を実用化する上では、ビタミンB12類に対して光安定性を備えさせることが不可欠になっている。 Vitamin B 12 is a kind of water-soluble vitamin and is an essential nutrient for sustaining life. Vitamin B 12 is a symptom of vitamin B 12 deficiency, megaloblastic anemia, fish tapeworm, pernicious anemia, malabsorption syndrome, eye fatigue, nutritional anemia, gestational anemia, nerve pain, etc. It is known to be effective for prevention or improvement of skin irritation, improvement of rough skin, etc., and is used in foods and drinks, oral care products, pharmaceuticals, cosmetics, etc. On the other hand, vitamin B 12 compound, it tends to be decomposed by light exposure are known, the practical use of products containing vitamin B 12 compound may be caused to comprise a light stable against vitamin B 12 compound It has become indispensable.

従来、ビタミンB12類に光安定性を備えさせる製剤技術について種々報告されている。例えば、特許文献1には、ビタミンB12、及びブタノールを含む製剤が、ビタミンB12に光安定性を付与できることが開示されている。また、特許文献2には、ビタミンB12、及び特定のフェニルプロペンカルボニル構造を有するビタミン安定剤を含むビタミン組成物が、ビタミンB12に光安定性を付与できることが開示されている。また、特許文献3には、ビタミンB12にシクロデキストリン又はその誘導体を添加することによって、ビタミンB12に光安定化が図られることが開示されている。 Conventionally, various preparation techniques for making vitamin B 12s have photostability have been reported. For example, Patent Document 1 discloses that a preparation containing vitamin B 12 and butanol can impart photostability to vitamin B 12 . Further, Patent Document 2, vitamin compositions comprising vitamin stabilizer comprising a vitamin B 12, and the particular phenylpropenoic carbonyl structure, it is disclosed that can be imparted to light stability to vitamin B 12. Further, Patent Document 3, by the addition of cyclodextrin or a derivative thereof to vitamin B 12, it is disclosed that the light stabilizing vitamin B 12 is achieved.

このように、従来、ビタミンB12類の光安定化を図る製剤技術については検討されているものの、近年、製品の多様化や品質向上に対する要望が向上しており、このような要望に追従するために、ビタミンB12類の光安定化を図る新たな技術の開発が望まれている。 As described above, although the formulation technology for photostabilizing vitamin B 12s has been studied in the past, the demand for product diversification and quality improvement has been increasing in recent years, and it follows such demand. Therefore, it is desired to develop a new technology for photostabilizing vitamin B 12s .

国際公開第2008/113483号International Publication No. 2008/113483 特開2007−125018号公報JP-A-2007-125018 特開平4−49239号公報Japanese Unexamined Patent Publication No. 4-49239

本発明の目的は、ビタミンB12類を含み、光暴露によるビタミンB12類の分解が抑制されている組成物を提供することである。 An object of the present invention includes a vitamin B 12 compound is to provide a composition which decomposition of vitamin B 12 compound by light exposure is inhibited.

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、ビタミンB12類を含む組成物にポリオキシエチレンソルビタン脂肪酸エステルを含有させ、且つビタミンB12類1重量部に対してポリオキシエチレンソルビタン脂肪酸エステルが10重量部以下となるように設定することにより、過酷な条件で光暴露を行ってもビタミンB12類の分解を抑制でき、ビタミンB12類に対する光安定化効果が格段顕著に奏されることを見出した。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。 The present inventors have was subjected to solve intensive study of the problem, a composition comprising a vitamin B 12 compound is a polyoxyethylene sorbitan fatty acid esters, and polyoxy against vitamin B 12 compound 1 part by weight by sorbitan fatty acid ester is set to be equal to or less than 10 parts by weight, even when the light exposure under severe conditions can inhibit the decomposition of vitamin B 12 compound, remarkably conspicuous light stabilizing effect on vitamin B 12 compound I found that it was played by. 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. ビタミンB12類及びポリオキシエチレンソルビタン脂肪酸エステルを含有し、且つビタミンB12類1重量部当たりポリオキシエチレンソルビタン脂肪酸エステルが10重量部以下である、ビタミンB12類含有組成物。
項2. 更にビタミンE類を含有する、項1に記載のビタミンB12類含有組成物。
項3. ビタミンB12類1重量部当たりビタミンE類が0.00125〜1000重量部である、項2に記載のビタミンB12類含有組成物。
項4. 水性組成物である、項1〜3のいずれかに記載のビタミンB12類含有組成物。
That is, the present invention provides the inventions of the following aspects.
Item 1. Containing vitamin B 12 acids and polyoxyethylene sorbitan fatty acid esters, and vitamin B 12 compound 1 part by weight per polyoxyethylene sorbitan fatty acid ester is less than 10 parts by weight, vitamin B 12 analog-containing composition.
Item 2. Item 2. The composition containing vitamin B 12s , which further contains vitamin Es.
Item 3. Item 2. The composition containing vitamin B 12 according to Item 2, wherein the amount of vitamin E per part by weight of vitamin B 12 is 0.00125 to 1000 parts by weight.
Item 4. Item 2. The composition containing vitamin B 12 according to any one of Items 1 to 3, which is an aqueous composition.

本発明によれば、光暴露によるビタミンB12類の分解を抑制できるので、ビタミンB12類を含む各種製品の保存安定性を向上させることが可能になる。 According to the present invention, since the decomposition of vitamin B 12s due to light exposure can be suppressed, it is possible to improve the storage stability of various products containing vitamin B 12s .

1.ビタミンB 12 類含有組成物
本発明のビタミンB12類含有組成物は、ビタミンB12類及びポリオキシエチレンソルビタン脂肪酸エステルを含有し、且つビタミンB12類1重量部当たりポリオキシエチレンソルビタン脂肪酸エステルが10重量部以下であることを特徴とする。以下、本発明のビタミンB12類含有組成物について、詳述する。
1. 1. Vitamin B 12 compounds containing composition of vitamin B 12 analog-containing composition the present invention contains a vitamin B 12 acids and polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid ester per and vitamin B 12 compound 1 part by weight It is characterized in that it is 10 parts by weight or less. Hereinafter, the vitamin B 12- containing composition of the present invention will be described in detail.

[ビタミンB12類]
ビタミンB12類とは、ビタミンB12(シアノコバラミン)、その誘導体、及びそれらの塩を指す。本発明で使用されるビタミンB12類の種類については、飲食品、口腔ケア製品、医薬品、化粧料等の製品に配合可能であることを限度として特に制限されない。例えば、ビタミンB12の誘導体としては、メチルコバラミン、ヒドロキソコバラミン、アデノシルコバラミン、アクアコバラミン等が挙げられる。また、ビタミンB12及びその誘導体の塩としては、例えば、酢酸塩、トリフルオロ酢酸塩、酪酸塩、パルミチン酸塩、ステアリン酸塩、フマル酸塩、マレイン酸塩、コハク酸塩、マロン酸塩、乳酸塩、酒石酸塩、クエン酸塩等のカルボン酸塩;メタンスルホン酸塩、トルエンスルホン酸塩、トシル酸塩等の有機スルホン酸塩;塩酸塩、硫酸塩、硝酸塩、リン酸塩等の無機酸塩;メチルアミン、トリエチルアミン、トリエタノールアミン等の有機アミン塩;ナトリウム塩、カリウム塩等のアルカリ金属塩;カルシウム、マグネシウム等のアルカリ土類金属塩;アンモニウム塩等が挙げられる。
[Vitamin B 12 ]
Vitamin B 12s refer to vitamin B 12 (cyanocobalamin), its derivatives, and salts thereof. For the types of vitamin B 12 compound for use in the present invention is not particularly limited as limit the food products, oral care products, pharmaceuticals, can be formulated into products of cosmetics. For example, derivatives of vitamin B 12 include methylcobalamin, hydroxocobalamin, adenosylcobalamin, aquacobalamin and the like. Examples of salts of Vitamin B 12 and its derivatives include acetate, trifluoroacetate, butyrate, palmitate, stearate, fumarate, maleate, succinate, malonate, and the like. Carbolates such as lactates, tartrates and citrates; organic sulfonates such as methanesulfonates, toluenesulfonates and tosylates; inorganic acids such as hydrochlorides, sulfates, nitrates and phosphates Salts; organic amine salts such as methylamine, triethylamine, triethanolamine; alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium and magnesium; ammonium salts and the like.

これらのビタミンB12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。 These vitamin B 12s may be used alone or in combination of two or more.

これらのビタミンB12類の中でも、好ましくはシアノコバラミンが挙げられる。 Among these vitamin B 12 compounds, preferably include cyanocobalamin.

本発明のビタミンB12類含有組成物におけるビタミンB12類の濃度については、当該ビタミンB12類含有組成物の形状や製品形態等に応じて適宜設定すればよいが、例えば、0.0001〜0.2重量%、好ましくは0.0002〜0.02重量%、より好ましくは0.0002〜0.002重量%が挙げられる。 The concentration of vitamin B 12 rocks in vitamin B 12 analog-containing composition of the present invention may be appropriately set according to the shape and product forms like of the vitamin B 12 analog-containing composition, but for example, 0.0001 0.2% by weight, preferably 0.0002 to 0.02% by weight, more preferably 0.0002 to 0.002% by weight.

[ポリオキシエチレンソルビタン脂肪酸エステル]
本発明のビタミンB12類含有組成物は、ビタミンB12類の光安定化を図るために、ビタミンB12類1重量部に対して10重量部以下となる比率でポリオキシエチレンソルビタン脂肪酸エステルを含有する。
[Polyoxyethylene sorbitan fatty acid ester]
Vitamin B 12 compounds containing composition of the present invention, in order to light stabilization of vitamin B 12 compound, a polyoxyethylene sorbitan fatty acid esters in a ratio of 10 parts by weight or less with respect to vitamin B 12 compound 1 part by weight contains.

ポリオキシエチレンソルビタン脂肪酸エステルとは、脂肪酸とソルビタンとのモノエステル、ジエステル、又はトリエステルであるソルビタン脂肪酸エステルにエチレンオキサイドが縮合している化合物である。ポリオキシエチレンソルビタン脂肪酸エステルを構成する脂肪酸の炭素数としては、例えば、8〜30、好ましくは10〜22、より好ましくは12〜18が挙げられる。また、ポリオキシエチレンソルビタン脂肪酸エステルに縮合されているエチレンオキサイドの平均付加モル数としては、例えば、6〜160、好ましくは6〜60、より好ましくは6〜30が挙げられる。ポリオキシエチレンソルビタン脂肪酸エステルとしては、具体的には、ポリソルベート20(ポリオキシエチレン(20)ソルビタンモノパルミテート)、ポリソルベート40(ポリオキシエチレン(20)ソルビタンモノラウレート)、ポリソルベート60(ポリオキシエチレン(20)ソルビタンモノステアレート)、ポリソルベート65(ポリオキシエチレン(20)ソルビタントリステアレート)、ポリソルベート80(ポリオキシエチレン(20)ソルビタンモノオレエート)、ポリソルベート85(ポリオキシエチレン(20)ソルビタントリオレエート)、ステアリン酸PEG−6ソルビタン、イソステアリン酸PEG−20ソルビタン、オレイン酸PEG−6ソルビタン、ポリソルベート85等が挙げられる。 The polyoxyethylene sorbitan fatty acid ester is a compound in which ethylene oxide is condensed with a sorbitan fatty acid ester which is a monoester, a diester, or a triester of a fatty acid and sorbitan. Examples of the carbon number of the fatty acid constituting the polyoxyethylene sorbitan fatty acid ester include 8 to 30, preferably 10 to 22, and more preferably 12 to 18. The average number of moles of ethylene oxide condensed on the polyoxyethylene sorbitan fatty acid ester is, for example, 6 to 160, preferably 6 to 60, and more preferably 6 to 30. Specific examples of the polyoxyethylene sorbitan fatty acid ester include polysorbate 20 (polyoxyethylene (20) sorbitan monopalmitate), polysorbate 40 (polyoxyethylene (20) sorbitan monolaurate), and polysorbate 60 (polyoxyethylene). (20) sorbitan monostearate), polysorbate 65 (polyoxyethylene (20) sorbitan tristearate), polysorbate 80 (polyoxyethylene (20) sorbitan monooleate), polysorbate 85 (polyoxyethylene (20) sorbitan trioleate). Ate), PEG-6 sorbitan stearate, PEG-20 sorbitan isostearate, PEG-6 sorbitan oleate, polysorbate 85 and the like.

これらのポリオキシエチレンソルビタン脂肪酸エステルは、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。 These polyoxyethylene sorbitan fatty acid esters may be used alone or in combination of two or more.

これらのポリオキシエチレンソルビタン脂肪酸エステルの中でも、より一層効果的にビタミンB12類の光安定化を図るという観点から、好ましくはポリソルベート80が挙げられる。 Among these polyoxyethylene sorbitan fatty acid esters, from the viewpoint of more effectively achieving the photostability of the vitamin B 12 compounds, preferably polysorbates 80.

本発明のビタミンB12類含有組成物において、ビタミンB12類とポリオキシエチレンソルビタン脂肪酸エステルとを共存させる際の両者の比率としては、ビタミンB12類100重量部当たり、ポリオキシエチレンソルビタン脂肪酸エステルが10重量部以下であればよいが、好ましくは1〜10重量部、より好ましくは2.5〜10重量部が挙げられる。 In the composition containing vitamin B 12 of the present invention, the ratio of both vitamin B 12 and polyoxyethylene sorbitan fatty acid ester when coexisting with them is as follows: polyoxyethylene sorbitan fatty acid ester per 100 parts by weight of vitamin B 12 It may be 10 parts by weight or less, but preferably 1 to 10 parts by weight, more preferably 2.5 to 10 parts by weight.

また、本発明のビタミンB12類含有組成物におけるポリオキシエチレンソルビタン脂肪酸エステルの濃度については、前記比率を充足する範囲で適宜設定すればよいが、例えば、0.001〜0.1重量%、好ましくは0.0025〜0.1重量%、より好ましくは0.005〜0.1重量%が挙げられる。 The concentration of the polyoxyethylene sorbitan fatty acid ester in the composition containing vitamin B 12 of the present invention may be appropriately set within a range that satisfies the above ratio, and is, for example, 0.001 to 0.1% by weight. It is preferably 0.0025 to 0.1% by weight, more preferably 0.005 to 0.1% by weight.

[ビタミンE類]
本発明のビタミンB12類含有組成物には、ビタミンB12類及びポリオキシエチレンソルビタン脂肪酸エステルに加えてビタミンE類を含有していてもよい。このようにビタミンE類を更に含有させることにより、より一層効果的にビタミンB12類の光安定化を図ることが可能になる。
[Vitamin E]
The vitamin B 12- containing composition of the present invention may contain vitamin E in addition to vitamin B 12 and polyoxyethylene sorbitan fatty acid ester. By thus further contain vitamin E, the more it can be more effectively reduced the photostability of the vitamin B 12 compound.

ビタミンE類とは、ビタミンE(トコフェロール、トコトリエノール)、及びその誘導体を指す。本発明で使用されるビタミンE類の種類については、飲食品、口腔ケア製品、医薬品、化粧料等の製品に配合可能であることを限度として特に制限されない。例えば、トコフェロール及びトコトリエノールは、α−、β−、γ−、及びδ−のいずれであってもよく、またd体又はdl体のいずれであってもよい。また、例えば、ビタミンEの誘導体としては、酢酸トコフェロール、コハク酸トコフェロール、リノール酸トコフェロール、リノレイン酸トコフェロール、ニコチン酸トコフェロール、(リノール酸/オレイン酸)トコフェロール等のトコフェロール有機酸エステル等が挙げられる。 Vitamin E refers to vitamin E (tocopherol, tocotrienol) and its derivatives. The types of vitamin E used in the present invention are not particularly limited as long as they can be blended in products such as foods and drinks, oral care products, pharmaceuticals, and cosmetics. For example, tocopherols and tocotrienols may be any of α-, β-, γ-, and δ-, and may be either d-form or dl-form. In addition, for example, as a derivative of vitamin E, tocopherol organic acid esters such as tocopherol acetate, tocopherol succinate, tocopherol linoleate, tocopherol linoleate, tocopherol nicotinate, and tocopherol (linoleic acid / oleic acid) can be mentioned.

これらのビタミンE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。 These vitamin Es may be used alone or in combination of two or more.

これらのビタミンE類の中でも、より一層効果的にビタミンB12類の光安定化を図るという観点から、好ましくはトコフェロールの誘導体、より好ましくはトコフェロール酢酸エステルが挙げられる。 Among these vitamin E, from the viewpoint of more effectively achieving the photostability of the vitamin B 12 compound, preferably derivatives of tocopherol, or more preferably tocopherol acetate.

本発明のビタミンB12類含有組成物にビタミンE類を含有させる場合、ビタミンB12類とビタミンE類との比率としては、例えば、ビタミンB12類1重量部当たり、ビタミンE類が0.00125〜1000重量部、好ましくは0.025〜250重量部、より好ましくは2.5〜250重量部が挙げられる。 When the vitamin B 12- containing composition of the present invention contains vitamin E, the ratio of vitamin B 12 to vitamin E is, for example, 0. Vitamin E per 1 part by weight of vitamin B 12 . 00125 to 1000 parts by weight, preferably 0.025 to 250 parts by weight, and more preferably 2.5 to 250 parts by weight.

また、本発明のビタミンB12類含有組成物にビタミンE類を含有させる場合、ビタミンB12類含有組成物におけるビタミンE類の濃度としては、例えば、0.00025〜0.1重量%、好ましくは0.0005〜0.05重量%、より好ましくは0.0005〜0.005重量%が挙げられる。 When the vitamin B 12- containing composition of the present invention contains vitamin E, the concentration of vitamin E in the vitamin B 12- containing composition is, for example, 0.00025 to 0.1% by weight, preferably 0.00025 to 0.1% by weight. Is 0.0005 to 0.05% by weight, more preferably 0.0005 to 0.005% by weight.

[キレート剤]
本発明のビタミンB12類含有組成物は、更にキレート剤を含有してもよい。本発明で使用されるキレート剤の種類については、飲食品、口腔ケア製品、医薬品、化粧料等の製品に配合可能であることを限度として特に制限されないが、例えば、エデト酸、クエン酸、コハク酸、及びこれら塩等が挙げられる。塩の形態としては、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩等が挙げられる。これらのキレート剤は、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。
[Chelating agent]
The vitamin B 12- containing composition of the present invention may further contain a chelating agent. The type of chelating agent used in the present invention is not particularly limited as long as it can be blended in products such as foods and drinks, oral care products, pharmaceuticals, cosmetics, etc., but for example, edetic acid, citric acid, and succinic acid. Acids, salts thereof and the like can be mentioned. Examples of the salt form include alkali metal salts such as sodium salt and potassium salt. These chelating agents may be used alone or in combination of two or more.

これらのキレート剤の中でも、好ましくはエデト酸及びその塩、より好ましくはエデト酸ナトリウムが挙げられる。 Among these chelating agents, edetic acid and a salt thereof are preferable, and sodium edetate is more preferable.

また、本発明のビタミンB12類含有組成物においてキレート剤を含有させる場合、ビタミンB12類含有組成物におけるキレート剤の濃度については、特に制限されないが、例えば、0.001〜0.3重量%、好ましくは0.005〜0.1重量%、より好ましくは0.01〜0.1重量%が挙げられる。 When the chelating agent is contained in the vitamin B 12- containing composition of the present invention, the concentration of the chelating agent in the vitamin B 12- containing composition is not particularly limited, but is, for example, 0.001 to 0.3 weight. %, preferably 0.005 to 0.1% by weight, more preferably 0.01 to 0.1% by weight.

[多価アルコール]
本発明のビタミンB12類含有組成物は、更に多価アルコールを含有してもよい。本発明で使用される多価アルコールの種類としては、例えば、エチレングリコール、1,3−ブチレングリコール、プロピレングリコール、イソプレングリコール、ジエチレングリコール、ジプロピレングリコール、ポリプロピレングリコール、グリセリン等が挙げられる。これらの多価アルコールは、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。
[Multivalent alcohol]
The vitamin B 12- containing composition of the present invention may further contain a polyhydric alcohol. Examples of the type of polyhydric alcohol used in the present invention include ethylene glycol, 1,3-butylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polypropylene glycol, glycerin and the like. These polyhydric alcohols may be used alone or in combination of two or more.

これらの多価アルコールの中でも、好ましくプロピレングリコールが挙げられる。 Among these polyhydric alcohols, propylene glycol is preferably mentioned.

また、本発明のビタミンB12類含有組成物に多価アルコールを含有させる場合、ビタミンB12類含有組成物における多価アルコールの濃度については、特に制限されないが、例えば、0.01〜10重量%、好ましくは0.1〜5重量%、より好ましくは0.1〜1重量%が挙げられる。 When the vitamin B 12- containing composition of the present invention contains a polyhydric alcohol, the concentration of the polyhydric alcohol in the vitamin B 12- containing composition is not particularly limited, but is, for example, 0.01 to 10 weight. %, preferably 0.1 to 5% by weight, more preferably 0.1 to 1% by weight.

[その他の成分]
本発明のビタミンB12類含有組成物には、前記成分の他に、当該ビタミンB12類含有組成物の形状や製品形態に応じて、各種の薬理成分、食品素材、添加剤等の成分を含有させてもよい。このような成分は、ビタミンB12類含有組成物の形状や製品形態に応じて使用可能なものを適宜選定すればよいが、例えば、水、薬理成分、清涼化剤、界面活性剤(ポリオキシエチレンソルビタン脂肪酸エステル以外)、油脂類、ロウ類、炭化水素類、脂肪酸類、高級アルコール類、エステル類、水溶性高分子、金属石鹸、1価低級アルコール類、pH調整剤、緩衝剤、酸化防止剤、紫外線防止剤、防腐剤、香料、粉体、増粘剤、色素等が挙げられる。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。これらの成分の濃度については、使用する成分の種類や組成物の形状及び製品形態等に応じて適宜設定される。
[Other ingredients]
In addition to the above-mentioned components, the vitamin B 12- containing composition of the present invention contains various pharmacological components, food materials, additives and other components according to the shape and product form of the vitamin B 12- containing composition. It may be contained. Such components may be suitably selected usable in accordance with the shape and product forms of vitamin B 12 analog-containing composition, for example, water, the pharmaceutical agent, cooling agent, surfactant (polyoxy (Other than ethylene sorbitan fatty acid esters), fats and oils, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, metal soaps, monohydric lower alcohols, pH adjusters, buffers, antioxidants Examples include agents, UV inhibitors, preservatives, fragrances, powders, thickeners, pigments and the like. These components may be used alone or in combination of two or more. The concentration of these components is appropriately set according to the type of component used, the shape of the composition, the product form, and the like.

[ビタミンB12類含有組成物の形状・製品形態等]
本発明のビタミンB12類含有組成物は、水性組成物又は非水性組成物のいずれであってもよい。一般的にビタミンB12類は水性組成物中で光暴露により分解され易くなる傾向があるが、本発明によれば、水性組成物中でも光暴露によるビタミンB12類の分解を効果的に抑制できる。このような本発明の効果を鑑みると、本発明のビタミンB12類含有組成物の好適な例として水性組成物が挙げられる。
Shape-product forms such as vitamin B 12 analog-containing composition]
The vitamin B 12- containing composition of the present invention may be either an aqueous composition or a non-aqueous composition. In general, vitamin B 12s tend to be easily decomposed by light exposure in an aqueous composition, but according to the present invention, the decomposition of vitamin B 12s by light exposure can be effectively suppressed even in an aqueous composition. .. In view of such effects of the present invention, an aqueous composition can be mentioned as a suitable example of the vitamin B 12- containing composition of the present invention.

水性組成物とは、水を含有する組成物である。水性組成物における水の濃度としては、具体的には、50量%以上、好ましくは50〜99.99重量%、より好ましくは50〜99.8重量%が挙げられる。水性組成物の形状としては、例えば、液状、ゲル状、ペースト状等が挙げられる。 The aqueous composition is a composition containing water. Specific examples of the concentration of water in the aqueous composition include 50% by weight or more, preferably 50 to 99.99% by weight, and more preferably 50 to 99.8% by weight. Examples of the shape of the aqueous composition include liquid, gel, and paste.

ビタミンB12類含有組成物が水性組成物である場合、そのpHとしては、例えば、4.0〜8.0、好ましくは5.0〜7.7、より好ましくは5.5〜7.0が挙げられる。 When the vitamin B 12- containing composition is an aqueous composition, the pH thereof is, for example, 4.0 to 8.0, preferably 5.0 to 7.7, and more preferably 5.5 to 7.0. Can be mentioned.

また、非水性組成物とは、配合成分の吸湿によって不可避的に含まれる水を除いて、水が実質的に配合されていない組成物である。非水性組成物の形状としては、例えば、粉末状、顆粒状、錠剤状、丸剤状、軟膏状等が挙げられる。 Further, the non-aqueous composition is a composition in which water is substantially not blended, except for water which is inevitably contained due to moisture absorption of the blending component. Examples of the shape of the non-aqueous composition include powder, granule, tablet, pill, ointment and the like.

本発明のビタミンB12類含有組成物の製品形態については、特に制限されず、例えば、飲食品、口腔ケア製品、医薬品、化粧料等が挙げられる。 The product form of the composition containing vitamin B 12 of the present invention is not particularly limited, and examples thereof include foods and drinks, oral care products, pharmaceuticals, and cosmetics.

飲食品としては、例えば、清涼飲料水、酒類、栄養ドリンク、コーヒー、茶、牛乳、果汁飲料、清涼飲料等の飲料;錠剤、顆粒剤、粉剤、ゼリー剤、散剤、懸濁剤、シロップ剤、カプセル剤(ソフトカプセル剤、ハードカプセル剤)等のサプリメント;チーズ、ウインナー、ソーセージ、ハム、魚介加工品等の副菜;アイスクリーム、クッキー、ケーキ、ゼリー、プリン、キャンディー、チューインガム、ヨーグルト、グミ、チョコレート、ビスケット等の菓子類等が挙げられる。 Foods and drinks include, for example, soft drinks, alcoholic beverages, nutritional drinks, coffee, tea, milk, fruit juice drinks, soft drinks and other beverages; tablets, granules, powders, jellies, powders, suspending agents, syrups, etc. Supplements such as capsules (soft capsules, hard capsules); side dishes such as cheese, wieners, sausages, hams, processed seafood; ice cream, cookies, cakes, jellies, puddings, candies, chewing gum, yogurt, gummies, chocolate, Examples include confectionery such as biscuits.

口腔ケア製品としては、例えば、練歯磨剤、粉歯磨剤、液体歯磨剤等の歯磨剤;歯用クリーム;マウスウォッシュ、含嗽剤等の洗口剤;口腔用パスタ剤、マウススプレー、口腔内崩壊性フィルム、ゲル、トローチ、タブレット、チュアブル、口腔用軟膏剤等が挙げられる。 Oral care products include, for example, dentifrices such as dentifrices, powdered dentifrices, and liquid dentifrices; tooth creams; mouthwashes such as mouthwashes and mouthwashes; oral pasta agents, mouth sprays, and oral disintegration. Examples include sex films, gels, troches, tablets, chewables, oral ointments and the like.

医薬品としては、例えば、散剤、顆粒剤、錠剤、カプセル剤、丸剤、液剤等の内服用の医薬品;輸液、注射剤等の皮下、血管内又は腹腔内投与用の医薬品;液剤(ローション剤、スプレー剤、エアゾール剤、及び乳液剤を含む)、水溶性軟膏剤、油脂性軟膏剤、クリーム剤、フォーム剤、ジェル剤、貼付剤、点眼剤、洗眼剤等の皮膚又は粘膜用の医薬品等が挙げられる。 Examples of pharmaceuticals include powders, granules, tablets, capsules, pills, liquids and the like for internal use; subcutaneous, intravascular or intraperitoneal administration of infusions, injections and the like; liquids (lotions, lotions, etc.) (Including sprays, aerosols, and emulsions), water-soluble ointments, oily ointments, creams, foams, gels, patches, eye drops, eye wash, and other skin or mucous medicines. Can be mentioned.

化粧料としては、例えば、軟膏、クリーム、乳液、化粧水、ローション、パック、ゲル等の基礎化粧料;ファンデーション、アイシャドウ、口紅、頬紅等のメークアップ化粧料等が挙げられる。 Examples of cosmetics include basic cosmetics such as ointments, creams, milky lotions, lotions, lotions, facial masks, and gels; make-up cosmetics such as foundations, eye shadows, lipsticks, and blushers.

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。 The present invention will be described in more detail with reference to Examples below, but the present invention is not limited thereto.

試験例1
表1に示す組成の水性組成物を調製した。500ml容の透明容器(ポリエチレンテレフタレート製)に得られた水性組成物500mlを充填し、昼間に直射日光が当たる室内(南側の窓から10cm離れた場所)に35日間静置した。35日間の静置後に、水性組成物の外観を目視にて観察し、以下の判定基準に従って、シアノコバラミンの保存安定性を判定した。なお、シアノコバラミンはピンク色の色調を呈し、分解されると退色するため、本試験において、退色が多い程、シアノコバラミンの分解が進んでいることを示している。
<シアノコバラミンの保存安定性>
◎ :製造直後に比べて、色調が同等である。
○ :製造直後に比べて、僅かに退色が認められるが許容範囲内である。
× :製造直後に比べて、明らかに退色が認められ許容できない。
××:退色が著しく、ほぼ無色になっている。
Test Example 1
An aqueous composition having the composition shown in Table 1 was prepared. A 500 ml transparent container (made of polyethylene terephthalate) was filled with 500 ml of the obtained aqueous composition, and allowed to stand in a room exposed to direct sunlight in the daytime (a place 10 cm away from the window on the south side) for 35 days. After standing for 35 days, the appearance of the aqueous composition was visually observed, and the storage stability of cyanocobalamin was determined according to the following criteria. It should be noted that cyanocobalamin exhibits a pink color tone and fades when decomposed. Therefore, in this test, it is shown that the more fading, the more the decomposition of cyanocobalamin progresses.
<Cyanocobalamin storage stability>
⊚: The color tone is the same as that immediately after manufacturing.
◯: Slight fading is observed as compared with immediately after production, but it is within the permissible range.
X: Color fading is clearly observed and unacceptable as compared with immediately after production.
XX: Fading is remarkable and it is almost colorless.

結果を表1に示す。この結果、水性組成物中で、シアノコバラミン及びポリソルベート80を共存させても、シアノコバラミン1重量部当たりポリソルベート80が10重量部超である場合には、光暴露によるシアノコバラミンの分解を抑制できていなかった。これに対して、水性組成物中でシアノコバラミンと共にポリソルベート80を共存させ、且つシアノコバラミン1重量部当たりポリソルベート80が10重量部以下の場合には、光暴露によるシアノコバラミンの分解を抑制できることが確認された。また、水性組成物中でシアノコバラミンと、シアノコバラミン1重量部当たり10重量部以下のポリソルベート80と共に、トコフェロール酢酸エステルを含有させた場合には、光暴露によるシアノコバラミンの分解を格段効果的に抑制できることも明らかとなった。 The results are shown in Table 1. As a result, even if cyanocobalamin and polysorbate 80 coexisted in the aqueous composition, when the polysorbate 80 per 1 part by weight of cyanocobalamin was more than 10 parts by weight, the decomposition of cyanocobalamin by light exposure could not be suppressed. On the other hand, it was confirmed that when polysorbate 80 coexists with cyanocobalamin in the aqueous composition and the polysorbate 80 per 1 part by weight of cyanocobalamin is 10 parts by weight or less, the decomposition of cyanocobalamin by light exposure can be suppressed. It is also clear that when cyanocobalamin and tocopherol acetic acid ester are contained together with polysorbate 80 of 10 parts by weight or less per 1 part by weight of cyanocobalamin in the aqueous composition, the decomposition of cyanocobalamin by light exposure can be suppressed remarkably effectively. It became.

Figure 2020196672
Figure 2020196672

処方例
表2に示す組成の水性組成物を調製した。得られた水性組成物を、前記試験例1と同様の方法でシアノコバラミンの保存安定性を評価したところ、いずれも、光暴露によるシアノコバラミンの分解を効果的に抑制できていた。
Formulation Examples An aqueous composition having the composition shown in Table 2 was prepared. When the storage stability of cyanocobalamin was evaluated for the obtained aqueous composition by the same method as in Test Example 1, the decomposition of cyanocobalamin due to light exposure could be effectively suppressed in each case.

Figure 2020196672
Figure 2020196672

Claims (4)

ビタミンB12類及びポリオキシエチレンソルビタン脂肪酸エステルを含有し、且つビタミンB12類1重量部当たりポリオキシエチレンソルビタン脂肪酸エステルが10重量部以下である、ビタミンB12類含有組成物。 Containing vitamin B 12 acids and polyoxyethylene sorbitan fatty acid esters, and vitamin B 12 compound 1 part by weight per polyoxyethylene sorbitan fatty acid ester is less than 10 parts by weight, vitamin B 12 analog-containing composition. 更にビタミンE類を含有する、請求項1に記載のビタミンB12類含有組成物。 The composition containing vitamin B 12 according to claim 1, further containing vitamin E. ビタミンB12類1重量部当たりビタミンE類が0.00125〜1000重量部である、請求項2に記載のビタミンB12類含有組成物。 The composition containing vitamin B 12 according to claim 2, wherein the amount of vitamin E per part by weight of vitamin B 12 is 0.00125 to 1000 parts by weight. 水性組成物である、請求項1〜3のいずれかに記載のビタミンB12類含有組成物。 The composition containing vitamin B 12 according to any one of claims 1 to 3, which is an aqueous composition.
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