JP2019055927A - Solid composition containing coenzyme q10 - Google Patents
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- JP2019055927A JP2019055927A JP2017182003A JP2017182003A JP2019055927A JP 2019055927 A JP2019055927 A JP 2019055927A JP 2017182003 A JP2017182003 A JP 2017182003A JP 2017182003 A JP2017182003 A JP 2017182003A JP 2019055927 A JP2019055927 A JP 2019055927A
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- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 title claims abstract description 91
- 239000008247 solid mixture Substances 0.000 title claims abstract description 63
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 claims abstract description 90
- 235000017471 coenzyme Q10 Nutrition 0.000 claims abstract description 90
- 229940110767 coenzyme Q10 Drugs 0.000 claims abstract description 90
- 239000000203 mixture Substances 0.000 claims abstract description 34
- 239000007788 liquid Substances 0.000 claims abstract description 28
- 239000002245 particle Substances 0.000 claims abstract description 24
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 22
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 20
- 239000000230 xanthan gum Substances 0.000 claims abstract description 18
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- KCYQMQGPYWZZNJ-BQYQJAHWSA-N hydron;2-[(e)-oct-1-enyl]butanedioate Chemical compound CCCCCC\C=C\C(C(O)=O)CC(O)=O KCYQMQGPYWZZNJ-BQYQJAHWSA-N 0.000 claims description 5
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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- QNTNKSLOFHEFPK-UPTCCGCDSA-N ubiquinol-10 Chemical compound COC1=C(O)C(C)=C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)C(O)=C1OC QNTNKSLOFHEFPK-UPTCCGCDSA-N 0.000 description 2
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- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
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- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
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- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
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- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
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- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
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- BECPQYXYKAMYBN-UHFFFAOYSA-N casein, tech. Chemical compound NCCCCC(C(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(CC(C)C)N=C(O)C(CCC(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(C(C)O)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(COP(O)(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(N)CC1=CC=CC=C1 BECPQYXYKAMYBN-UHFFFAOYSA-N 0.000 description 1
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- Medicinal Preparation (AREA)
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Abstract
Description
本発明は、コエンザイムＱ１０を高含量で含有するコエンザイムＱ１０含有固形組成物に関する。詳細には、脂溶性のコエンザイムＱ１０を高含量で含みながら、水性液体に容易に分散が可能で、しかも固形の形態で長期間保管することが可能なコエンザイムＱ１０含有組成物に関する。 The present invention relates to a coenzyme Q10-containing solid composition containing a high content of coenzyme Q10. Specifically, the present invention relates to a coenzyme Q10-containing composition that can be easily dispersed in an aqueous liquid and can be stored in a solid form for a long period of time while containing a high content of fat-soluble coenzyme Q10.
コエンザイムＱ１０は、ユビデカレノンまたは補酵素Ｑ１０とも呼ばれ、高等動物に存在する補酵素の１種である。コエンザイムＱ１０は、補酵素として生物活性をもつだけでなく、酸素利用効率を改善させる作用を有するビタミン様作用物質として知られている。コエンザイムＱ１０は、エネルギー産生や抗酸化等の作用を有し、種々の健康機能に関与するとされている。臨床的に狭心症、心不全、虚血性心疾患、筋ジストロフィーの症状改善に用いられ、高血圧、動脈硬化、心臓病、糖尿病、癌等に効果があるとされ、疲労回復や運動機能回復等にも有効であると報告されている。このようにコエンザイムＱ１０は高い生理活性を有し、且つ生体内に存在するため、安全性の高い物質である。 Coenzyme Q10 is also called ubidecalenone or coenzyme Q10, and is one type of coenzyme present in higher animals. Coenzyme Q10 is known as a vitamin-like substance having not only biological activity as a coenzyme but also an effect of improving oxygen utilization efficiency. Coenzyme Q10 has actions such as energy production and antioxidants, and is considered to be involved in various health functions. It is clinically used to improve symptoms of angina pectoris, heart failure, ischemic heart disease, muscular dystrophy, and is effective for hypertension, arteriosclerosis, heart disease, diabetes, cancer, etc. It is reported to be effective. Thus, coenzyme Q10 is a highly safe substance because it has high physiological activity and exists in vivo.
しかし、コエンザイムＱ１０は融点の低い親油性固体であり、水に難溶性であるため、取扱いにくく、また経口摂取しても吸収性に非常に劣る成分である。また、コエンザイムＱ１０は光や熱によって分解しやすく、安定性も低い成分である。 However, Coenzyme Q10 is a lipophilic solid having a low melting point and is hardly soluble in water, so it is difficult to handle and is a component that is very poorly absorbed even when taken orally. Coenzyme Q10 is a component that is easily decomposed by light and heat and has low stability.
そのため、コエンザイムＱ１０の安定性や吸収性を高めたり、含有量を高めた組成物に関する技術が提案されている。特許文献１には、コエンザイムＱ１０、リゾレシチン、グリセリン及び水を含有し、油脂を含有しない液状組成物が記載されている。この技術はコエンザイムＱ１０の吸収性が高められているが、液体組成物であるため、取扱い性に劣るものであった。特許文献２には、コエンザイムＱ１０を、オクテニルコハク酸澱粉とデキストリンからなる水溶性物質及びグリセリンを含有する水性液体中で分散・乳化した、コエンザイムＱ１０含有液体組成物、並びにこれを乾燥したコエンザイムＱ１０含有固形組成物が記載されている。特許文献２では、コエンザイムＱ１０の最大含有量５２％の実施例が示されている。この技術はコエンザイムＱ１０の安定性や吸収性が高く、液状でも固形状でも用い得る優れたものであるが、より簡便にコエンザイムＱ１０を高含有化する技術を本発明者らは検討した。 Therefore, techniques relating to compositions with increased stability and absorbability of coenzyme Q10 and increased content have been proposed. Patent Document 1 describes a liquid composition containing coenzyme Q10, lysolecithin, glycerin and water, but not containing fats and oils. Although this technology has improved the absorbability of coenzyme Q10, it is a liquid composition and therefore is inferior in handleability. Patent Document 2 discloses a coenzyme Q10-containing liquid composition in which coenzyme Q10 is dispersed and emulsified in an aqueous liquid containing a water-soluble substance composed of octenyl succinic acid starch and dextrin and glycerin, and a solid containing coenzyme Q10. A composition is described. Patent Document 2 shows an example in which the maximum content of coenzyme Q10 is 52%. Although this technique has high stability and absorbability of coenzyme Q10 and is excellent in use in liquid or solid form, the present inventors have examined a technique for increasing the content of coenzyme Q10 more easily.
特許文献３には、コエンザイムＱ１０のようなキノン骨格を有する化合物と抗酸化剤とを含有し、このいずれかが被覆された状態で共存する組成物が記載されている。しかしこの技術では、吸収性が悪いコエンザイムＱ１０の結晶を被覆しただけのものであり、吸収性は高くないものであった。特許文献４には、還元型補酵素Ｑ１０と、油脂、脂肪酸、ワックス及び界面活性剤から選択される１種以上を含有する液状組成物が記載されている。しかしこの技術は、還元型補酵素Ｑ１０の酸化を抑制することを目的としており、吸収性や含有量という点では劣るものであった。 Patent Document 3 describes a composition containing a compound having a quinone skeleton such as coenzyme Q10 and an antioxidant and coexisting in a state where any of these is coated. However, in this technique, the absorbability is not high because it is only coated with crystals of coenzyme Q10 having poor absorbability. Patent Document 4 describes a liquid composition containing reduced coenzyme Q10 and at least one selected from fats and oils, fatty acids, waxes and surfactants. However, this technique aims to suppress oxidation of reduced coenzyme Q10, and is inferior in terms of absorbability and content.
固形組成物中に脂溶性のコエンザイムＱ１０を高い含有量で含み、かつその固形組成物が水性液体に良く分散するものであれば、コエンザイムＱ１０の吸収性を高めることができる上、取扱い性の点からも、容易に小型で安定な製剤にすることができ、また食品や飼料にも均一に混合できる等の多くの利点がある。
本発明の課題は、脂溶性のコエンザイムＱ１０を高含量で含みながら、水性液体への分散性の高いコエンザイムＱ１０含有組成物を提供することである。
As long as the solid composition contains fat-soluble coenzyme Q10 in a high content and the solid composition is well dispersed in an aqueous liquid, the absorbability of coenzyme Q10 can be increased, and handling characteristics Therefore, there are many advantages such that it can be easily made into a small and stable preparation and can be uniformly mixed with food and feed.
An object of the present invention is to provide a composition containing coenzyme Q10 having a high dispersibility in an aqueous liquid while containing a high content of fat-soluble coenzyme Q10.
上記の課題は、以下の組成物によって解決することができる。
１．コエンザイムＱ１０、乳化剤及びキサンタンガムを含有する固形組成物であって、該固形組成物を水に分散した際の平均粒子径が１〜５０μｍである固形組成物。
２．前記乳化剤が、オクテニルコハク酸澱粉とショ糖脂肪酸エステルから選択される１種以上である上記１の固形組成物。
３．コエンザイムＱ１０を組成物中に６０〜９０質量％で含有するものである、上記１又は２の固形組成物。
４．キサンタンガムを組成物中に０．３〜５質量％で含有するものである、上記１〜３の固形組成物。
５．乳化剤を組成物中に８〜５０質量％で含有するものである、上記１〜４の固形組成物。
６．コエンザイムＱ１０、乳化剤及びキサンタンガムを含む混合物を水性液体の存在下に分散後、乾燥する固形組成物の製造方法であって、該固形組成物を有する固形組成物を水に再分散した際の平均粒子径が１〜５０μｍである固形組成物の製造方法。
The above problems can be solved by the following composition.
1. A solid composition containing coenzyme Q10, an emulsifier and xanthan gum, wherein the solid composition has an average particle size of 1 to 50 µm when dispersed in water.
2. The solid composition according to 1 above, wherein the emulsifier is at least one selected from octenyl succinic acid starch and sucrose fatty acid ester.
3. The solid composition according to 1 or 2 above, wherein the composition contains Coenzyme Q10 at 60 to 90% by mass.
4). Solid composition of said 1-3 which is what contains xanthan gum in a composition at 0.3-5 mass%.
5. Solid composition of said 1-4 which is what contains an emulsifier in 8-50 mass% in a composition.
6). A method for producing a solid composition in which a mixture containing coenzyme Q10, an emulsifier and xanthan gum is dispersed in the presence of an aqueous liquid and then dried, and the average particle when the solid composition having the solid composition is redispersed in water The manufacturing method of the solid composition whose diameter is 1-50 micrometers.
本発明のコエンザイムＱ１０含有固形組成物は、コエンザイムＱ１０を極めて高含量で含みながら、水性液体に対する分散性が高い。そのため、錠剤等のサプリメントや医薬品の形態で摂取する際も、小型の製剤で十分量を摂取可能である。また一般的な食品や飼料の形態で摂取する場合でも、固形組成物の配合量を少量とすることができるため、食品や飼料の風味、食感に悪影響を与えることが無く、自然に摂取することができる。
また、本発明のコエンザイムＱ１０含有固形組成物は、水性液体に対する分散性が高い結果、コエンザイムＱ１０の吸収性が良くなるという利点がある。
さらに、本発明のコエンザイムＱ１０含有固形組成物は、分散性が高いため、粒子の凝集や粒子径の増大が抑制される結果、安定性が高く、固形の形態で長期間保管することが可能である。
The coenzyme Q10-containing solid composition of the present invention is highly dispersible in an aqueous liquid while containing a very high content of coenzyme Q10. Therefore, even when taking in the form of supplements such as tablets or pharmaceuticals, a sufficient amount can be taken in a small preparation. Even when ingested in the form of general food or feed, the amount of the solid composition can be reduced so that it does not adversely affect the flavor and texture of the food and feed and is naturally ingested. be able to.
In addition, the coenzyme Q10-containing solid composition of the present invention has the advantage that the absorbability of coenzyme Q10 is improved as a result of its high dispersibility in aqueous liquids.
Furthermore, since the coenzyme Q10-containing solid composition of the present invention has high dispersibility, it is highly stable and can be stored for a long time in a solid form as a result of suppressing particle aggregation and particle size increase. is there.
本発明のコエンザイムＱ１０含有固形組成物は、コエンザイムＱ１０、乳化剤及びキサンタンガムを含有しており、常温（日本工業規格では２０℃±１５℃）で水性液体に分散した際の平均粒子径が１〜５０μｍである。この固形組成物は、好ましくは、コエンザイムＱ１０、乳化剤及びキサンタンガムを含む混合物を水性液体の存在下に均一に分散後、乾燥することによって製造することができる。 The coenzyme Q10-containing solid composition of the present invention contains coenzyme Q10, an emulsifier and xanthan gum, and has an average particle size of 1 to 50 μm when dispersed in an aqueous liquid at room temperature (20 ° C. ± 15 ° C. in Japanese Industrial Standards). It is. This solid composition can be preferably produced by uniformly dispersing a mixture containing coenzyme Q10, an emulsifier and xanthan gum in the presence of an aqueous liquid and then drying.
本発明のコエンザイムＱ１０含有固形組成物において、水性液体に分散した際の平均粒子径とは、固形組成物を質量基準で１０〜１００倍量の水性液体に投入し、機械を用いた乳化や分散工程を行わずとも実現できる分散粒子の平均粒子径を指す。例えば高圧乳化機のような装置を用いれば、コエンザイムＱ１０を一時的に微粒に分散することは可能であるが、本発明のコエンザイムＱ１０含有固形組成物は、そのような操作を必要とせず、例えばマグネチックスターラー等によって、普通に攪拌するだけで、簡便に水性液体に分散
した状態を得ることができる。なお、本発明において平均粒子径とは、湿式法のレーザー回折・散乱法により算出された粒径のメジアン径（Ｄ５０）をいう。
In the coenzyme Q10-containing solid composition of the present invention, the average particle size when dispersed in an aqueous liquid refers to emulsification or dispersion using a machine by charging the solid composition into 10 to 100 times the amount of aqueous liquid on a mass basis The average particle diameter of the dispersed particles that can be realized without performing the process. For example, if a device such as a high-pressure emulsifier is used, it is possible to temporarily disperse coenzyme Q10 into fine particles, but the coenzyme Q10-containing solid composition of the present invention does not require such an operation. With a magnetic stirrer or the like, it is possible to easily obtain a state dispersed in an aqueous liquid simply by stirring. In the present invention, the average particle diameter means a median diameter (D50) of a particle diameter calculated by a wet method of laser diffraction / scattering.
本発明の固形組成物中におけるコエンザイムＱ１０の含有量は、所望の摂取量、固形組成物の形態に応じて適宜決められるが、簡便に摂取するとの本発明の効果を得るためには、固形組成物１００質量％に対して６０〜９０質量％の範囲であり、好ましくは７０〜８５質量％の範囲である。 The content of coenzyme Q10 in the solid composition of the present invention is appropriately determined according to the desired intake amount and the form of the solid composition, but in order to obtain the effect of the present invention with simple intake, the solid composition It is the range of 60-90 mass% with respect to 100 mass% of things, Preferably it is the range of 70-85 mass%.
本発明で用いる乳化剤としては、脂溶性物質を水性液体に分散・乳化できるものの中から適宜選択して用いることができ、好ましくは食品に適用可能な乳化剤を用いると、簡便に摂取可能な固形組成物を得ることができる。乳化剤としては、グリセリン脂肪酸エステル、ショ糖脂肪酸エステル、モノグリセリド等の合成界面活性剤、乳化能を有する澱粉、加工澱粉、レシチン、サポニン、カゼイン等が挙げられる。これらの中でも、高含有量のコエンザイムＱ１０を水性液体に分散可能な状態で安定的に保存する効果の点で、ショ糖脂肪酸エステル及びエステル化澱粉から選択される１種以上を用いることが好ましい。エステル化澱粉としては、酢酸、リン酸、コハク酸、オクテニルコハク酸等で澱粉をエステル化したものが例示できる。エステル化澱粉としては、オクテニルコハク酸澱粉が最も好ましい。また、澱粉の原料澱粉としては、タピオカ澱粉、馬鈴薯澱粉、コーンスターチ、ワキシーコーンスターチ、米澱粉、小麦澱粉等の澱粉類が挙げられる。 The emulsifier used in the present invention can be appropriately selected from those that can disperse and emulsify a fat-soluble substance in an aqueous liquid, preferably a solid composition that can be easily ingested when an emulsifier applicable to foods is used. You can get things. Examples of the emulsifier include synthetic surfactants such as glycerin fatty acid ester, sucrose fatty acid ester and monoglyceride, starch having modified ability, modified starch, lecithin, saponin, casein and the like. Among these, it is preferable to use at least one selected from sucrose fatty acid esters and esterified starch in terms of the effect of stably storing a high content of coenzyme Q10 in a state dispersible in an aqueous liquid. Examples of the esterified starch include those obtained by esterifying starch with acetic acid, phosphoric acid, succinic acid, octenyl succinic acid and the like. As the esterified starch, octenyl succinic acid starch is most preferred. Examples of the starch material starch include starches such as tapioca starch, potato starch, corn starch, waxy corn starch, rice starch, and wheat starch.
本発明の固形組成物中における乳化剤の含有量は、コエンザイムＱ１０の含有量によっても異なるが、固形組成物１００質量％に対して８〜５０質量％の範囲であり、好ましくは１０〜３５質量％の範囲である。 The content of the emulsifier in the solid composition of the present invention varies depending on the content of coenzyme Q10, but is in the range of 8 to 50% by mass, preferably 10 to 35% by mass with respect to 100% by mass of the solid composition. Range.
本発明で用いるキサンタンガムは、安定した粘性を示して、コエンザイムＱ１０と乳化剤とが乳化した乳化物の安定性に寄与する。食品や医薬品として利用されているキサンタンガムはいずれも使用できる。本発明の固形組成物中におけるキサンタンガムの含有量は、コエンザイムＱ１０の含有量によっても異なるが、固形組成物の全質量に対して０．３〜５質量％の範囲であり、好ましくは０．４〜２質量％の範囲である。 The xanthan gum used in the present invention exhibits a stable viscosity and contributes to the stability of an emulsion obtained by emulsifying coenzyme Q10 and an emulsifier. Any xanthan gum used as a food or medicine can be used. The content of xanthan gum in the solid composition of the present invention varies depending on the content of coenzyme Q10, but is in the range of 0.3 to 5% by mass, preferably 0.4%, based on the total mass of the solid composition. It is the range of -2 mass%.
本発明の固形組成物には、上記の乳化剤及びキサンタンガムを含んでいれば、本発明の効果を妨げない限り、その他の増粘剤やゲル化剤を含んでいてもよい。増粘剤やゲル化剤の例には、例えば、ペクチン、グアーガム、アラビアガム、タマリンドガム、カラギーナン、プロピレングリコール、カルボキシメチルセルロース、寒天等が挙げられる。その他の増粘剤やゲル化剤の添加量は、その種類により異なるが、一般的には組成物の質量に基づき１０質量％以下程度である。 If the above-mentioned emulsifier and xanthan gum are included in the solid composition of the present invention, other thickeners and gelling agents may be included as long as the effects of the present invention are not hindered. Examples of thickeners and gelling agents include pectin, guar gum, gum arabic, tamarind gum, carrageenan, propylene glycol, carboxymethyl cellulose, agar and the like. The amount of the other thickener or gelling agent added varies depending on the type, but is generally about 10% by mass or less based on the mass of the composition.
本発明の固形組成物には、コエンザイムＱ１０の安定化を目的として、さらに有機酸を含んでいてもよい。有機酸の例には、例えばクエン酸、コハク酸、フマル酸、乳酸、グルコン酸、リンゴ酸、酒石酸およびこれらの塩が挙げられる。有機酸の添加量は、その種類により異なるが、一般的には組成物の質量に基づき１０質量％以下程度である。 The solid composition of the present invention may further contain an organic acid for the purpose of stabilizing Coenzyme Q10. Examples of organic acids include citric acid, succinic acid, fumaric acid, lactic acid, gluconic acid, malic acid, tartaric acid and their salts. The addition amount of the organic acid varies depending on the type, but is generally about 10% by mass or less based on the mass of the composition.
本発明のコエンザイムＱ１０含有固形組成物の調製方法は、脂溶性成分を分散又は乳化するなどして微細化して固形化する公知の方法を採用することができる。そのような方法としては、特許第４８４２８２４号公報に記載の方法を例示することができる。即ち、コエンザイムＱ１０を予め融点以上に加熱して溶融し、これを乳化剤及びキサンタンガムを含有する水性液体中に分散・乳化して均一なコエンザイムＱ１０乳化液を形成させる。具体的には、乳化剤及びキサンタンガムの水性溶液を調製し、好ましくは加温した状態で、予め加熱・融解したコエンザイムＱ１０を導入し、次いで公知の手段、例えば高圧乳化機を使用して、分散・乳化させることにより、均一なコエンザイムＱ１０乳化液を形成させ
ることができる。これらの工程は、コエンザイムＱ１０の融点より高い温度、例えば４５〜９０℃、好ましくは５０〜７０℃で実施するのが好ましい。また、予め加温（４５〜９０℃、好ましくは５０〜７０℃）した水性溶液に、コエンザイムＱ１０の結晶粉末を直接添加・分散し、該溶液中で融解させ、次いで乳化させてもよい。この方法は、作業性を効率化し、原材料の損失を抑制できるために好ましい。さらに、コエンザイムＱ１０の分散・乳化処理に際して、コエンザイムＱ１０を油脂や食用油に溶解または混合してもよく、水性溶液の調製時にコエンザイムＱ１０の安定化の目的で有機酸を添加してもよい。
As a method for preparing the coenzyme Q10-containing solid composition of the present invention, a known method in which a fat-soluble component is dispersed or emulsified to be solidified and solidified can be employed. As such a method, a method described in Japanese Patent No. 4842824 can be exemplified. That is, coenzyme Q10 is previously heated to a melting point or higher and melted, and this is dispersed and emulsified in an aqueous liquid containing an emulsifier and xanthan gum to form a uniform coenzyme Q10 emulsion. Specifically, an aqueous solution of an emulsifier and xanthan gum is prepared, preferably in a heated state, pre-heated and melted coenzyme Q10 is introduced, and then dispersed or dispersed using a known means such as a high-pressure emulsifier. By emulsifying, a uniform coenzyme Q10 emulsion can be formed. These steps are preferably performed at a temperature higher than the melting point of Coenzyme Q10, for example, 45 to 90 ° C, preferably 50 to 70 ° C. Alternatively, the coenzyme Q10 crystal powder may be directly added to and dispersed in an aqueous solution preheated (45 to 90 ° C., preferably 50 to 70 ° C.), melted in the solution, and then emulsified. This method is preferable because the workability is improved and the loss of raw materials can be suppressed. Further, during the dispersion / emulsification treatment of coenzyme Q10, coenzyme Q10 may be dissolved or mixed in oil or edible oil, and an organic acid may be added for the purpose of stabilizing coenzyme Q10 when preparing an aqueous solution.
上記、コエンザイムＱ１０乳化液は、平均粒子径として０．２〜２０μｍになるまで分散・乳化処理を行うことが好ましい。コエンザイムＱ１０乳化液の粒子径を前記範囲とすることで、本発明のコエンザイムＱ１０含有固形組成物を水性液体に均一に分散することができる。 The coenzyme Q10 emulsion is preferably subjected to a dispersion / emulsification treatment until the average particle size becomes 0.2 to 20 μm. By setting the particle diameter of the coenzyme Q10 emulsion to the above range, the coenzyme Q10-containing solid composition of the present invention can be uniformly dispersed in an aqueous liquid.
上記のようにして得られたコエンザイムＱ１０乳化液は、次いで、固形化して本発明のコエンザイムＱ１０含有固形組成物とする。固形組成物の大きさは任意の大きさとすることができるが、水性液体に対する分散しやすさからは、粉末状の形態とすることが好ましい。固形化する手段としては、食品および医薬製剤の製造において慣用される任意の乾燥・固形化手段を用いることができる。例えば、噴霧乾燥法、流動層造粒法、攪拌造粒法、凍結乾燥法等が挙げられる。これらの中では、粉末化が容易との観点からは、噴霧乾燥法が好ましい。 The coenzyme Q10 emulsion obtained as described above is then solidified to obtain the coenzyme Q10-containing solid composition of the present invention. Although the magnitude | size of a solid composition can be made into arbitrary magnitude | sizes, it is preferable to set it as a powder form from the ease of disperse | distributing with respect to an aqueous liquid. As a means for solidifying, any drying / solidifying means commonly used in the production of foods and pharmaceutical preparations can be used. For example, a spray drying method, a fluidized bed granulation method, a stirring granulation method, a freeze drying method and the like can be mentioned. Among these, the spray drying method is preferable from the viewpoint of easy powdering.
噴霧乾燥法は、スプレードライ、スプレークール等の市販の装置を用いて行うことができる。噴霧乾燥の際、必要に応じて担体を加え、これに吸着または担持させて固形化してもよいが、担体の性質による影響を受けて水性液体に分散しにくくなるおそれがあるため、水溶性の担体を用いるのが好ましい。水溶性の担体としては、例えば、デキストリン、マルトデキストリン、還元麦芽糖、ソルビトールなどが挙げられる。 The spray drying method can be performed using a commercially available apparatus such as spray drying or spray cool. At the time of spray drying, a carrier may be added if necessary and adsorbed or supported to be solidified, but it may be difficult to disperse in an aqueous liquid due to the influence of the properties of the carrier. It is preferable to use a carrier. Examples of the water-soluble carrier include dextrin, maltodextrin, reduced maltose, sorbitol and the like.
本発明のコエンザイムＱ１０含有固形組成物は、そのまま摂取することもできるが、これを医薬品、食品、化粧料および飼料に配合して用いてもよい。本発明のコエンザイムＱ１０含有固形組成物はコエンザイムＱ１０を高含量で安定して含んでおり、医薬品や食品に少量の添加でも有効量のコエンザイムＱ１０を配合することができる。 The coenzyme Q10-containing solid composition of the present invention can be ingested as it is, but it may be used in combination with pharmaceuticals, foods, cosmetics and feeds. The coenzyme Q10-containing solid composition of the present invention stably contains a high content of coenzyme Q10, and an effective amount of coenzyme Q10 can be blended with a small amount of pharmaceutical or food.
本発明のコエンザイムＱ１０含有固形組成物を医薬品に配合する場合、その形態は、錠剤、粉末剤、カプセル剤等を選択でき、常法の製剤方法により、医薬品とすることができる。その際、必要に応じて、医薬品製造に用いられる賦形剤、滑沢剤、流動化剤、安定化剤、ハードカプセル、ソフトカプセル等を利用することができる。 When the coenzyme Q10-containing solid composition of the present invention is blended with a pharmaceutical product, the form can be selected from tablets, powders, capsules and the like, and can be made into a pharmaceutical product by a conventional formulation method. At that time, excipients, lubricants, fluidizing agents, stabilizers, hard capsules, soft capsules and the like used for pharmaceutical production can be used as necessary.
本発明のコエンザイムＱ１０含有固形組成物を食品に配合する場合、固形の形態のコエンザイムＱ１０を配合できるものであれば制限なく、サプリメント、健康食品、機能性食品はもちろん、一般的な食品にも配合することができる。サプリメント、健康食品、機能性食品としては、上記した医薬品の製剤方法がそのまま採用できる。一般的な食品としては、パン類、スパゲティ、うどん等の麺類、クッキー、チョコレート、キャンディ、せんべい等の菓子類、ふりかけ、ソース、バター等のスプレッド類等が挙げられる。これらの形態では、その製造原料として本発明のコエンザイムＱ１０含有固形組成物を用いることで、簡便に配合することができる。 When the coenzyme Q10-containing solid composition of the present invention is blended into food, there is no limitation as long as coenzyme Q10 in a solid form can be blended, and it is blended in supplements, health foods, functional foods, and general foods as well. can do. As supplements, health foods, and functional foods, the above-described pharmaceutical preparation methods can be employed as they are. Examples of common foods include breads, spaghetti, noodles such as udon, confectionery such as cookies, chocolate, candy, and rice crackers, spreads such as sprinkles, sauces, and butter. In these forms, the coenzyme Q10-containing solid composition of the present invention can be simply blended as the production raw material.
本発明のコエンザイムＱ１０含有固形組成物を化粧料に配合する場合、固形の形態のコエンザイムＱ１０を配合できるものであれば制限なく、石鹸、洗顔剤、歯磨き、ゼリー状化粧料、クリーム状化粧料等に配合することができる。 When the coenzyme Q10-containing solid composition of the present invention is blended in cosmetics, there is no limitation as long as the solid form of coenzyme Q10 can be blended, soap, facial cleanser, toothpaste, jelly cosmetic, cream cosmetic, etc. Can be blended.
本発明のコエンザイムＱ１０含有固形組成物を飼料に配合する場合も、固形の形態のコエンザイムＱ１０を配合できるものであれば、ペレット状や缶詰等、各種の資料に配合することができる。 Even when the coenzyme Q10-containing solid composition of the present invention is blended in a feed, it can be blended into various materials such as pellets and canned foods as long as the coenzyme Q10 in a solid form can be blended.
本発明のコエンザイムＱ１０含有固形組成物における、コエンザイムＱ１０の１日当たりの摂取量は、年齢、体重や健康状態により異なるが通常、成人で５〜３００ｍｇ、好ましくは１０〜１００ｍｇ程度である。本発明のコエンザイムＱ１０含有固形組成物をそのまま摂取する場合、上記１日量を都度計量して摂取してもよいし、予め１日量や１回量を小分けしておいてもよい。本発明のコエンザイムＱ１０含有固形組成物を医薬品、食品、化粧料、飼料に配合する場合も、上記１日量を参考にして配合量を決定すればよい。 The daily intake of coenzyme Q10 in the coenzyme Q10-containing solid composition of the present invention varies depending on age, body weight and health condition, but is usually about 5 to 300 mg, preferably about 10 to 100 mg for adults. When the coenzyme Q10-containing solid composition of the present invention is ingested as it is, the above-mentioned daily amount may be measured and ingested, or the daily amount or once amount may be subdivided in advance. Even when the coenzyme Q10-containing solid composition of the present invention is blended with pharmaceuticals, foods, cosmetics, and feeds, the blending amount may be determined with reference to the daily dose.
以下、実施例によって本発明を詳細に説明するが、本発明はこれらの実施例に限定されるものではない。 EXAMPLES Hereinafter, although an Example demonstrates this invention in detail, this invention is not limited to these Examples.
（実施例１〜１０、比較例１〜７）
表１〜３の配合で、各コエンザイムＱ１０含有固形組成物を製造した。まずコエンザイムＱ１０以外の成分を精製水に加え、６５℃まで加温した。ここにコエンザイムＱ１０粉末（日清ファルマ製）を添加し、さらに高圧ホモジナイザー（三和機械社製；処理圧力５０ＭＰａ、３回）を通過させ、乳化液を得た。次いで、この乳化液を１３０℃に加熱した熱気流中に噴出し、噴霧乾燥して粉末状のコエンザイムＱ１０含有固形組成物を製造した。
(Examples 1-10, Comparative Examples 1-7)
Each coenzyme Q10 containing solid composition was manufactured with the composition of Tables 1-3. First, components other than coenzyme Q10 were added to purified water and heated to 65 ° C. Coenzyme Q10 powder (manufactured by Nisshin Pharma) was added thereto, and further passed through a high-pressure homogenizer (manufactured by Sanwa Kikai Co., Ltd .; treatment pressure 50 MPa, 3 times) to obtain an emulsion. Next, this emulsion was sprayed into a hot air stream heated to 130 ° C. and spray-dried to produce a powdered coenzyme Q10-containing solid composition.
（試験例１）
実施例１〜１０、比較例１〜７の製造の際、乳化の可否（〇：可能、×：不可能）を判断した。また、得られた乳化液の平均粒子径をマイクロトラックＭＴ３０００II（マイクロトラック・ベル社製）を用いてＤ５０として測定し、さらに
乳化液の均一性を、１０サンプルを目視にて下記判断基準にてスコア化した。また、乳化液を噴霧乾燥した際の粉末化の可否（〇：粉末になる、×：粉末にならない）を判断した。これらの結果を表１〜３に示す。
(Test Example 1)
During the production of Examples 1 to 10 and Comparative Examples 1 to 7, whether emulsification was possible (O: possible, X: impossible) was determined. Moreover, the average particle diameter of the obtained emulsion was measured as D50 using Microtrac MT3000II (manufactured by Microtrac Bell Co.), and the uniformity of the emulsion was visually determined on the basis of the following criteria. Scored. Moreover, the propriety of the powderization at the time of spray-drying the emulsion was determined (O: powdered, x: powderless). These results are shown in Tables 1-3.
（試験例２）
実施例１〜１０、比較例１〜７のコエンザイムＱ１０含有固形組成物０．２ｇを５０ｍＬの精製水に常温で加え、マグネチックスターラーで７００ｒｐｍ、２０分間撹拌して分散させ、１時間静置した。その分散液の均一性を、下記判断基準にてスコア化した。また、分散液の平均粒子径をマイクロトラックＭＴ３０００II（マイクロトラック・ベル社製）を用いてＤ５０として測定した。これらの
結果を表１〜３に示す。
(Test Example 2)
0.2 g of coenzyme Q10-containing solid compositions of Examples 1 to 10 and Comparative Examples 1 to 7 were added to 50 mL of purified water at room temperature, and stirred and dispersed with a magnetic stirrer at 700 rpm for 20 minutes, and allowed to stand for 1 hour. . The uniformity of the dispersion was scored according to the following criteria. The average particle size of the dispersion was measured as D50 using Microtrac MT3000II (manufactured by Microtrac Bell). These results are shown in Tables 1-3.
（乳化液の均一性の評価）
５：均一性が非常に高く、時間が経過しても油層と水層が全く分離しない
４：均一性が高く、時間が経過しても油層と水層がほとんど分離しない
３：均一性は普通で、時間が経過すると油層と水層がわずかに分離する
２：均一性が低く、時間が経過すると油層と水層が分離する
１：均一性が非常に低く、短い時間で油層と水層が分離する
（分散液の均一性の評価）
５：水への分散性が非常に高く、微細で均一な分散液が得られる
４：水への分散性が高く、微細でほぼ均一な分散液が得られる
３：水への分散性が普通であり、わずかに凝集した粒子がみられる
２：水への分散性が低く、凝集した粒子がみられる
１：水への分散性が非常に低く、凝集粒子や水との分離がみられる
(Evaluation of uniformity of emulsion)
5: The uniformity is very high, and the oil layer and the water layer do not separate at all even after a lapse of time 4: The uniformity is high, and the oil layer and the water layer hardly separate even after a lapse of time 3: The uniformity is normal The oil layer and the water layer are slightly separated over time. 2: The uniformity is low, and the oil layer and the water layer are separated over time. 1: The uniformity is very low, and the oil layer and the water layer are separated in a short time. Separation (Evaluation of dispersion uniformity)
5: Dispersibility in water is very high and a fine and uniform dispersion can be obtained. 4: Dispersibility in water is high and a fine and almost uniform dispersion can be obtained. 3: Dispersibility in water is normal. Slightly agglomerated particles are observed 2: Dispersibility in water is low, agglomerated particles are observed 1: Dispersibility in water is very low, and separation from aggregated particles and water is observed
上の結果は、アラビアガム、ペクチン、ヒドロキシプロピルセルロースのような増粘剤やゲル剤を用いても、キタンタンガムを用いない場合は、所望の均一な分散性を示す組成物を得ることができないことを示している。特に、比較例3はキサンタンガムを用いなかったため、分散液の粒子径は満たしたものの、分散液の均一性に劣るものであった。 The above results show that even when thickeners and gels such as gum arabic, pectin, and hydroxypropylcellulose are used, a composition that exhibits the desired uniform dispersibility cannot be obtained without using chitantan gum. Is shown. Particularly, since Comparative Example 3 did not use xanthan gum, the particle size of the dispersion liquid was satisfied, but the uniformity of the dispersion liquid was poor.
上の結果は、コエンザイムＱ１０の量が多すぎる場合には、所望の粒子径で均一な分散性を示す組成物を得られにくい場合があることを示している。なお、比較例５の配合でも、分散・乳化処理の方法を適宜変更することで、所望の組成物を得ることが可能である。 The above results indicate that if the amount of coenzyme Q10 is too large, it may be difficult to obtain a composition having a desired particle size and uniform dispersibility. Even in the blending of Comparative Example 5, it is possible to obtain a desired composition by appropriately changing the method of dispersion / emulsification treatment.
上の結果は、キサンタンガムの量が少なすぎる場合や多すぎる場合には、所望の粒子径で均一な分散性を示す組成物を得られにくい場合があることを示している。なお、比較例６や７の配合でも、分散・乳化処理の方法を適宜変更することで、所望の組成物を得ることが可能である。 The above results indicate that when the amount of xanthan gum is too small or too large, it may be difficult to obtain a composition exhibiting uniform dispersibility at a desired particle size. In addition, also in the blending of Comparative Examples 6 and 7, a desired composition can be obtained by appropriately changing the method of dispersion / emulsification treatment.
（比較例８〜９）
配合は実施例１又は３と同様にして、ただし高圧ホモジナイザーの通過回数を表４のように変更して組成物を製造し、試験例１、２と同様に評価した。その結果を表４に示す。なお、表４には、対比のため実施例1、３の結果を再掲する。
(Comparative Examples 8-9)
The composition was the same as in Example 1 or 3, except that the composition was prepared by changing the number of passes through the high-pressure homogenizer as shown in Table 4 and evaluated in the same manner as in Test Examples 1 and 2. The results are shown in Table 4. In Table 4, the results of Examples 1 and 3 are shown again for comparison.
上の結果は、同一の組成であっても、本発明で規定する平均粒子径ではない場合、均一な分散性を示す組成物を得られないことを示している。 The above results show that even if the composition is the same, a composition exhibiting uniform dispersibility cannot be obtained if the average particle diameter is not specified in the present invention.
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| WO2016024344A1 (en) * | 2014-08-13 | 2016-02-18 | 日清ファルマ株式会社 | Livestock production method and livestock-growth promoting method |
| US20160081927A1 (en) * | 2014-09-18 | 2016-03-24 | Virun, Inc. | Pre-spray emulsions and powders containing non-polar compounds |
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| JP2003055203A (en) * | 2001-08-10 | 2003-02-26 | Nisshin Pharma Inc | Ubiquinone-containing preparation |
| WO2006022187A1 (en) * | 2004-08-24 | 2006-03-02 | Nisshin Pharma Inc. | Coenzyme q10-containing composition |
| WO2008053920A1 (en) * | 2006-10-31 | 2008-05-08 | Kaneka Corporation | Physiologically active substance-containing granular composition and method of producing the same |
| WO2009001786A1 (en) * | 2007-06-22 | 2008-12-31 | Kaneka Corporation | Composition containing physiologically active substance |
| KR20100038578A (en) * | 2008-10-06 | 2010-04-15 | (주)아모레퍼시픽 | Cosmetic formulations of granule type and preparation method of the same |
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| US20160081927A1 (en) * | 2014-09-18 | 2016-03-24 | Virun, Inc. | Pre-spray emulsions and powders containing non-polar compounds |
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