Poorly water-soluble substances contain preparations

Abstract

To effectively blend a poorly water-soluble component with a low degree of solubility with a water-containing processed food containing water.SOLUTION: The present invention relates to a poorly water-soluble substance-containing preparation in which a water-diluted liquid prepared by diluting using water with a 10-100000-fold dilution factor has an average emulsified particle diameter of 60 nm or less, or a water-diluted liquid prepared by diluting using water with a 10-100000-fold dilution factor has an average dispersed particle diameter of 150 nm or less.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a formulation containing a poorly water-soluble substance that can effectively add and blend a poorly water-soluble substance to a processed food containing water.

Background Art

[0002] Dietary nutritional components represented by vitamins are roughly classified into two components: water-soluble and water-insoluble. On the other hand, since processed foods such as beverages contain a large amount of water, it is easy to blend water-soluble components such as vitamin C. However, for poorly water-soluble components such as vitamin E, coenzyme Q10, curcumin, and astaxanthin, if they are blended in their original state, floating separation and precipitation will occur, so formulation processing such as emulsification and dispersion is required. Regarding the stability of the emulsified and dispersed state, as known by Stokes' equation, it is inversely proportional to the square of the particle diameter of the component. Therefore, for the stable blending of poorly water-soluble substances into processed foods, formulation processing with a smaller particle diameter is required. Furthermore, Desai et al. discussed the effective uptake of minute emulsified particles into cells using emulsified particles of bovine serum albumin (Non-Patent Document 1), and a similar effect is expected for poorly water-soluble substances.

[0003] Regarding the micronization of such poorly water-soluble substances, techniques for micronizing poorly water-soluble substances such as curcumin and coenzyme Q10 by combining polyhydric alcohols with emulsifiers such as polyglycerol fatty acid esters, sugar esters, and lecithin have been disclosed. However, the specifically shown particle diameters are either the particle diameters of the undiluted solution that do not reflect the blending state in processed foods, or even in the case of dilutions considering blending, they are both 100 nm or more in the emulsion system and 200 nm or more in the dispersion system, and neither can be said to be a sufficient micronization technique (Patent Documents 1 to 3). 。

[0004] Furthermore, technologies have been published that combine polyglycerin fatty acid esters, sugar esters, lecithin, and monoglycerides to micronize emulsified coenzyme Q10 particles to 65.5 nm (Patent Document 4), and technologies that use thickening polysaccharides such as ghatti gum to micronize curcuminoids to 190 nm (Patent Document 5). However, neither of these technologies considered their use in processed foods, or their stability after incorporation was insufficient, making them inadequate as micronization technologies.

[0005] Furthermore, formulation technologies that solubilize poorly water-soluble substances using amphiphilic solvents such as polysorbates, polyethylene glycols, and alcohols have also been published. However, these only mention particle size in the solubilized formulations and either do not consider their incorporation into processed foods, or they investigate formulations at high concentrations of around 20%, which cannot be considered practical formulations (Patent Documents 6-8). 。 [Prior art documents] [Non-patent literature]

[0006] [Non-Patent Document 1] MP Desai et al, Pharmaceutical Res. 14, 1568 (1997) [Patent Documents]

[0007] [Patent Document 1] Japanese Patent Publication No. 2009-201371 [Patent Document 2] Special Publication No. 2006-134970 [Patent Document 3] Japanese Patent Publication No. 2013-56858 [Patent Document 4] Japanese Patent Publication No. 2008-245588 [Patent Document 5] Japanese Patent Publication No. 2014-118391 [Patent Document 6] Special Publication No. 2012-510466 [Patent Document 7] Japanese Patent Publication No. 2016-505579 [Patent Document 8] Japanese Patent Publication No. 2016-34918 [Overview of the Initiative] [Problems that the invention aims to solve]

[0008] The object of the present invention is to provide a formulation containing poorly water-soluble substances that can effectively incorporate poorly water-soluble components into processed foods containing water. [Means for solving the problem]

[0009] To solve the above problems, the present inventors conducted diligent studies and found that, in the case of a formulation containing a poorly water-soluble substance in a dispersion system, a formulation containing a poorly water-soluble substance in which the average dispersed particle size of the aqueous dilution is 150 nm or less, and in particular, a formulation containing one or more emulsifiers exhibiting an HLB of 10 to 16 and / or water and a polyhydric alcohol as a continuous phase, can effectively incorporate poorly water-soluble components into processed foods containing water, thus completing the present invention.

[0010] In other words, the present invention relates to a formulation containing poorly water-soluble substances, which is a dispersion formulation containing a poorly water-soluble substance, characterized in that the average dispersed particle size of the aqueous dilution obtained by diluting the formulation with water at a dilution ratio of 10 to 100,000 times is 150 nm or less. In particular, it relates to a formulation containing poorly water-soluble substances which contains one or more emulsifiers exhibiting an HLB of 10 to 16 and / or water and a polyhydric alcohol as a continuous phase. Compared to conventional formulation technologies for poorly water-soluble substances, it has superior appearance compatibility and permeability in processed foods containing water, and is a novel technology that enables the effective addition and blending of poorly water-soluble substances in the field of processed foods containing water. [Effects of the Invention]

[0011] This invention offers excellent compatibility in terms of appearance and permeability in processed foods containing water, enabling the effective addition and blending of poorly water-soluble substances in the field of processed foods containing water.

[0012] The poorly water-soluble substances used in the present invention are not particularly limited in type as long as they are used as food or food additives, but examples include curcuminoids, and one or more of these can be used.

[0013] The content of the poorly water-soluble substance in the formulation containing the poorly water-soluble substance of the present invention is preferably 0.05 to 40% by weight, more preferably 0.1 to 35% by weight, and even more preferably 0.2 to 30% by weight, relative to the total amount of the formulation. If the amount is less than 0.05% by weight, the effect of the formulation is insufficient, and if it exceeds 40% by weight, the viscosity of the formulation becomes high, which is undesirable.

[0014] Furthermore, one embodiment of the poorly water-soluble substance-containing formulation of the present invention is a dispersion-type formulation containing a poorly water-soluble substance, which is normally used after dilution. The formulation is diluted with water to a dilution ratio of 10 to 100,000 times, preferably 20 to 50,000 times, and the average dispersed particle size of the aqueous dilution is 150 nm or less. In the case of a dispersion system, if the particle size exceeds 150 nm, the effect of incorporating it into processed foods decreases, which is undesirable. The average dispersed particle size can be measured by laser light scattering.

[0015] Any type of emulsifier used in food can be used in this invention. Examples include polyglycerol esters, monoglycerol esters, sugar esters, sorbitan esters, lecithins, and thickening polysaccharides. These can be added individually or in combination of two or more, and among them, emulsifiers exhibiting an HLB of 10 to 16 are preferred. Types with an HLB of less than 10 or greater than 16 may not exhibit sufficient emulsification and dispersibility and are therefore undesirable. Here, HLB represents the hydrophilic-hydrophobic balance used in the field of surfactants, and for example, the following calculation formula (Kawakami formula) can be used. HLB = 7 + 11.7 log(M W / M O ) Here, M W is the molecular weight of the hydrophilic group, and M O is the molecular weight of the hydrophobic group. Also, the HLB values described in catalogs etc. may be used.

[0016] The content of the emulsifier used in the present invention is preferably 0.01 to 40% by weight, more preferably 0.1 to 35% by weight, and still more preferably 0.5 to 30% by weight with respect to the whole preparation. If the blending amount is less than 0.01% by weight, the effect of emulsification and dispersion is not sufficient, and if it exceeds 40% by weight, problems such as an increase in the viscosity of the preparation or a limitation in the blending amount of poorly water-soluble substances occur, which is not preferable.

[0017] In the preparation containing a poorly water-soluble substance of the present invention, the continuous phase is an aqueous phase component (aqueous solvent), and preferably water. At that time, it is preferable to add a polyhydric alcohol to the aqueous phase component for the purpose of adjusting the interfacial tension and assisting the dissolution of the emulsifier.

[0018] Any kind of polyhydric alcohols can be used as long as they are used in foods. For example, propylene glycol, glycerin, maltitol, reduced starch syrup, lactitol, palatinite, erythritol, mannitol, sorbitol, etc. can be mentioned, and these can be added alone or in combination of two or more. Among them, glycerin is most preferable for ensuring the fluidity of the composition.

[0019] The content of the polyhydric alcohol used in the present invention is preferably 0.01 to 70% by weight, more preferably 0.05 to 65% by weight, and still more preferably 0.1 to 60% by weight with respect to the whole preparation. If the blending amount is less than 0.01% by weight, a stable preparation may not be obtained, and if it exceeds 70% by weight, problems such as a limitation in the blending amount of poorly water-soluble substances occur, which is not preferable.

[0020] The formulation containing poorly water-soluble substances of the present invention may contain known food or food additive ingredients, as long as they do not impair the effects of the present invention. For example, oils, alcohols, waxes, etc., may be used as base components, and preservatives, fragrances, chelating agents, antioxidants, specific gravity adjusters, viscosity adjusters, etc., may be used as additive components.

[0021] The machinery used for manufacturing the formulation containing poorly water-soluble substances of the present invention is not particularly limited, and machines such as mixers, agitators, dispersers, homomixers, homogenizers, high-pressure homogenizers, ultra-high-pressure homogenizers, ball mills, colloid mills, planetary mills, and wet OB mills can be used individually or in combination.

[0022] The method for producing the formulation containing poorly water-soluble substances of the present invention is not necessarily limited, but one preferred method is to first emulsify and disperse the poorly water-soluble substance and the other components of the formulation in a continuous phase using a homomixer, homogenizer, ultrasound, etc. (for example, homogenization treatment is performed using a homomixer at 4000 to 6000 rpm for 30 to 60 minutes), and then to subsequently perform high-pressure homogenization treatment by repeating the operation 4 to 10 times under conditions of 30 to 70 MPa. By using this method, a formulation containing poorly water-soluble substances that exhibits a dispersed phase with the average particle size specified in the present invention when diluted with water can be efficiently produced.

[0023] The form of the formulation containing poorly water-soluble substances of the present invention is not particularly limited as long as the effects of the present invention are not impaired. In conventional preparation methods, it often takes the form of a liquid formulation, but it can also be used after mixing with excipients and converting it into a powder by spray drying or freeze-drying. [Examples]

[0024] The present invention will now be described in detail with reference to examples, but the present invention is not limited to these examples.

[0025] [Example 1, Comparative Example 1] In this example and comparative example, Decaglyn 1-SV (product name Decaglycerin Monostearate, manufactured by Nikko Chemicals) was used as the polyglycerin fatty acid ester, and SLP Paste Lyso (manufactured by Tsuji Oil Co., Ltd.) was used as the lecithin.

[0026] [Preparation Example: Preparation of Turmeric Extract] 1 kg of dried turmeric rhizomes were crushed in a hammer mill, and then 10 times the amount of ethanol was added and the mixture was immersed overnight in a cool, dark place. After immersion, the solution was filtered off and the solvent was removed using a rotary evaporator. 10 times the amount of water was added to the resulting extract and stirred thoroughly, after which the precipitate was filtered off and collected. This precipitate was thoroughly dried in a 70°C oven and then ground in a ball mill to obtain 130 g of turmeric extract containing 95% curcuminoids. 。

[0027] [Example 1, Comparative Example 1: Turmeric extract preparation] Comparative Example 1 was prepared by using the turmeric extract containing 95% curcuminoids in the composition shown in Table 1 and homogenizing it using a homomixer at 6000 rpm for 30 minutes. For the example, the turmeric extract was further ground using a planetary ball mill with 2 mm zirconia beads, 0.3 mm zirconia beads, and 0.03 mm zirconia beads to obtain the turmeric extract preparation of Example 1.

[0028] [Particle size measurement] Each formulation from Example 1 and Comparative Example 1 was diluted in water to a concentration of 0.1%, and the average particle size (nm) was measured by laser light scattering.

[0029] [Visual evaluation of dispersion] The appearance of the aqueous dilutions of Example 1 and Comparative Example 1 was examined and evaluated according to the following criteria. ◎: High transparency, and preferably very little influence on appearance from the solvent, water. ○: It is transparent and has little influence on appearance due to the solvent, water. △: Turbidity is noticeable, affecting the appearance due to the solvent, water. ×: Clearly cloudy, significantly affecting appearance.

[0030] [Table 1]

[0031] As is clear from Table 1, when the formulation is a dispersion system, Example 1, in which the average particle size of the aqueous dilution is 150 nm or less, showed little influence on the transparency of the dilution water and demonstrated good compatibility.

[0032] [Examples 2 Comparative example 2 [Evaluation of the coloring properties of pickled radish] Each of the formulations from Example 1 and Comparative Example 1 was added at a concentration of 1% to a commercially available pickling base, and these were then used in the respective Examples. 2 Comparative example 2 Then, the radishes, cut with a knife, were soaked in each solution, and their coloring was visually inspected, which clearly indicated that the example was different. 2 This method resulted in faster coloring and demonstrated better penetration into the radish tissue.

Claims

1. A dispersion formulation containing a poorly water-soluble substance, wherein the average dispersed particle size of the aqueous dilution obtained by diluting the formulation with water at a dilution ratio of 10 to 100,000 times is 150 nm or less. It contains one or more emulsifiers exhibiting an HLB of 10 to 16, The amount of the emulsifier is 0.01 to 40% by weight relative to the entire formulation. The continuous phase contains water and polyhydric alcohols. A food-grade preparation containing poorly water-soluble substances, characterized in that the polyhydric alcohol content is 0.01 to 70% by weight of the entire preparation.

2. The food preparation containing a poorly water-soluble substance according to claim 1, characterized in that the poorly water-soluble substance is curcuminoids and the polyhydric alcohol is glycerin.

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