JP2020058297A - Creatine-containing water dispersible powdery composition and method for producing the same - Google Patents

Abstract

To provide a creatine-containing water dispersible powdery composition in which the water dispersibility of creatine is good and which can be provided in a dosage form that is difficult to provide in the prior art, namely, in a form of beverage and powdered beverage and thus providing a high convenience when used as a supplement, and a method for producing the same.SOLUTION: Provided is a creatine-containing water dispersible powdery composition which contains an emulsifier by 0.1 to 10 pts.wt. for 100 pts.mass of creatine and in which a part or all of the surface of creatine is covered with the emulsifier.SELECTED DRAWING: None

Description

  The present invention relates to a creatine-containing water-dispersible powdery composition having improved creatine water dispersibility and increased ingestion efficiency, and a method for producing the same.

  Creatine is a substance involved in ATP resynthesis in the living body, and there are many reports that creatine causes an increase in exercise performance when ingested. It has also been suggested to have an effect of strengthening muscles, and it is well known as being actually taken by many athletes.

  Creatine is a substance that is synthesized in vivo and is contained in a relatively large amount in meat and fish (5 g / 1 kg). However, a large amount of intake (20 g / day) is required to exert the above-mentioned effects, and if this is ingested only with food, the nutritional balance will be disturbed. Therefore, a method of orally ingesting creatine as a supplement has attracted attention. However, if creatine is directly ingested as a crystal as it is, it cannot be said to be easily ingested orally because it has a gritty texture.

  Therefore, it is considered that creatine is not taken as it is but is dissolved in a drink and taken. However, creatine is a substance that is sparingly soluble in water and oil (solubility is about 10 g / L, 10 ° C water), and a sufficient amount of creatine cannot be dissolved even when added to a beverage. Creatine may precipitate during storage.

  Furthermore, especially under acidic conditions, creatine is apt to undergo a structural change to creatinine, and as a result, it becomes a substance that does not bring about the effect of improving exercise performance. Therefore, if an acidic beverage containing creatine is prepared in advance, creatine may change to creatinine over time, and the effect of creatine may not be enjoyed. That is, the creatine-containing acidic beverage is not suitable for long-term storage in terms of the effect of creatine.

  Therefore, as a powdered beverage, a method of ingesting creatine by adding creatine to water immediately before drinking to prepare an aqueous solution of creatine, and drinking this can be considered. With this method, it is not necessary to worry about the change from creatine to creatinine because the time lapse between adding creatine to water and ingesting it is short.

  However, as described above, since creatine is poorly soluble in water, almost all the amount of creatine precipitates even when added to water, and the creatine is susceptible to discomfort due to roughness and undissolved residue. Furthermore, it is expected that the absorption efficiency into the living body will be poor. Therefore, from the viewpoint of convenience of creatine intake and improvement of creatine absorption efficiency, development of a creatine-containing composition having good water dispersibility is expected.

  Under these circumstances, various preparations have been proposed for creatine in order to make it easier to take creatine. For example, in Patent Document 1, since creatine has a low solubility, it has a gritty texture, and when creatine is finely pulverized into granules or tablets, there is a phenomenon that teeth are clogged when chewed. Therefore, a method for producing a food or pharmaceutical product in the form of granules and compression tablets, which is free from roughness even at a high dose and has few teeth, has been reported by containing creatine having a particle size of 5 μm to 200 μm.

  Further, in Patent Document 2, in order to provide creatine having excellent absorbability to living bodies and having high water solubility, creatine is dispersed in a non-aqueous solvent and then crushed by applying a bead mill having a bead size of 1 mm or less. The obtained finely divided creatine having an average particle diameter of 2 μm or less is reported.

Japanese Patent No. 3892610 JP-A-2007-39408

  However, in the preparation of creatine shown in Patent Document 1, the dosage form is granules and tablets, and there is no mention of water solubility, dispersibility and absorbability into living bodies.

  Further, in the creatine fine powder disclosed in Patent Document 2, the solubility thereof is 21 g / L (10 ° C. water), and the necessary amount of creatine which is considered to obtain the above-mentioned effect of creatine is Ingestion with a beverage in which fine powder is dissolved requires ingestion of a large amount of beverage. In addition, in the production of the fine powder, a large amount of a solvent such as ethanol is used, so that it is not realistic from the viewpoint of actual production.

  As described above, the conventional techniques relating to creatine preparations are not sufficient in water dispersibility of creatine, and are not particularly satisfactory in terms of convenience when used as a powdered beverage. Regarding the dosage form of creatine preparations, the form of powdered drink to be dripped after adding water etc. is as a dosage form that efficiently and quickly supplements creatine for muscle strengthening and suppression of muscle decomposition, especially in sports scenes. Since it is particularly useful, it is expected to provide a creatine formulation in the form of a powdered beverage.

  Therefore, the present invention has good water dispersibility of creatine, and since it can be provided in a dosage form which was difficult to provide by the conventional technique, that is, a beverage and a powdered beverage, it is used as a supplement. It is an object of the present invention to provide a creatine-containing water-dispersible powdery composition and a method for producing the same, which is highly convenient for use.

  The present inventor, as a result of intensive research to solve the above problems, after dissolving creatine in hot water together with an emulsifier, by spray drying, it was found that to obtain a powder with enhanced water dispersibility, the present The invention was completed.

The present invention relates to the following [1] to [6].
[1] Creatine-containing water-dispersible powdery composition, characterized by containing 0.1 to 10 parts by weight of an emulsifier with respect to 100 parts by mass of creatine, and coating a part or all of the surface of creatine with the emulsifier. Stuff.
[2] The water-dispersible powdery composition according to the above [1], wherein the emulsifier is one or more selected from the group consisting of glycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, and lecithins. .
[3] The water-dispersible powdery composition according to the above [1] or [2], wherein the water-dispersible powdery composition has an average particle diameter of 40 μm or less.
[4] A food or drink, a drug or a quasi drug, comprising the water-dispersible powdery composition according to any one of [1] to [3].
[5] The food and drink, the drug or the quasi drug according to the above [4], wherein the dosage form is a drink or a powdered drink.
[6] To 100 parts by mass of creatine, 0.1 to 10 parts by mass of an emulsifier and 500 to 2000 parts by mass of water are added and mixed, and heated in a range of 80 to 100 ° C. to be dissolved to prepare an aqueous solution. 1 step,
A second step of obtaining a fine powder by spray drying the aqueous solution, the method for producing a creatine-containing water-dispersible powdery composition.

  The present invention, because the water dispersibility of creatine is sufficiently improved, water or water-based solvent, creatine particles are stably dispersed when dispersed in a beverage, precipitation or aggregation is less likely to occur, therefore, creatine. Is easily ingested, and absorbability into the body is improved. In addition, since it can be provided in the form of a drink or a powdered drink that is a dosage form capable of efficiently and quickly supplementing creatine, the convenience of using it as a supplement can be greatly enhanced.

One minute after the powders obtained in Examples 1 to 9 and Comparative Examples 1 and 2 were added to water and sufficiently shaken to disperse (Examples 1 to 5 from the upper left, Examples from the lower left 6 to 9 and Comparative Examples 1 and 2) are explanatory views. It is a figure which shows the change of the precipitation amount with time progress after disperse | distributing in the fine powder obtained in Examples 1-9 in water. It is explanatory drawing which shows the state after 120 minutes passed after disperse | distributing the fine powder obtained in Examples 1-9 in water (Examples 1-5 from an upper stage left, Examples 6-9 from a lower stage left).

  Hereinafter, the present invention will be described in detail. First, the composition of the present invention will be described. As described above, the composition of the present invention is characterized by containing 0.1 to 10 parts by weight of an emulsifier with respect to 100 parts by weight of creatine, and coating a part or all of the surface of creatine with the emulsifier. It is a water-dispersible powdery composition containing creatine.

  In the present invention, creatine (1-methylguanidinoacetic acid) strictly refers to creatine monohydrate, but includes creatine salts such as anhydrides and creatine phosphate. Generally commercially available products may be used, and the types and properties thereof are not particularly limited. In addition, creatine or creatine salt may be used alone, or creatine and creatine salt may be used in combination. It may be a combination of two or more kinds of creatine and / or a salt thereof obtained by various methods, or may be a combination of two or more kinds of creatine salts. In the living body, creatine is a substance synthesized from arginine, glycine and methionine, and there is no deficiency in normal diet. However, creatine tends to be deficient in athletes who perform high-intensity exercise and patients who rehabilitate due to insufficient nutrition due to illness or injury.

  One of the characteristics of the composition of the present invention is that it contains 0.1 to 10 parts by mass of an emulsifier with respect to 100 parts by mass of creatine. By adding an emulsifier, the water dispersibility of creatine can be further enhanced. If it is more than 10 parts by mass, the creatine that has precipitated over time will solidify, making it difficult to re-disperse it. Further, in the case of production by spray drying, creatine will be generated in the pipe during liquid transfer to the spray dryer. Since the tendency to recrystallize and solidify becomes stronger, there may be a problem in actual production. On the other hand, if the amount is less than 0.1 part by mass, the amount is too small to obtain good water dispersibility. When the proportion of emulsifier increases, it becomes difficult for the precipitation phase to re-disperse when dispersed in water, but the rate of precipitation is reduced, and dissolution and recrystallization when heat is applied tend to be suppressed. To be From this, it is advisable to determine the blending ratio within the above range according to the final application. Further, in consideration of this, the amount of the emulsifier is preferably 0.1 to 9 parts by mass. Furthermore, it is more desirable that the amount of the emulsifier is 3 to 9 parts by mass, more preferably 5 to 9 parts by mass, relative to 100 parts by mass of creatine, in addition to the water dispersibility, the water dispersion stability is improved. The water dispersibility means the degree to which particles are suspended or suspended in water, and the water dispersion stability means the degree to which the dispersed state does not change with time in water.

  The type of the emulsifier is not limited as long as it does not impair the effects of the present invention. They may be used alone or in combination of two or more. Examples of the emulsifier include glycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, lecithins, gum arabic, modified starch and the like. Among these, sucrose fatty acid ester is particularly preferably used.

  Further, an excipient may be used separately from creatine and the emulsifier. For example, dextrin, maltodextrin, starch and lactose which do not have an emulsifying action can be used.

  The composition of the present invention has creatine as a core, and a part or all of the surface thereof is coated with the emulsifier. In order to coat creatine with the emulsifier, any method may be used as long as the effects of the present invention can be obtained, but as described below, creatinine and the aqueous solution in which the emulsifier is completely dissolved are spray-dried. The coating method is preferable in that the target product can be obtained easily and surely.

  The average particle diameter of the composition of the present invention is preferably 40 μm or less, and more preferably 20 μm or less. The smaller the finer particles, the more the water dispersibility increases, but if it is larger than 40 μm, the water dispersibility cannot be said to be good. The average particle size can be measured by dispersing the composition in ethanol and using a laser diffraction / scattering method.

  The composition of the present invention may be used as it is as a final product, or may have a component other than the above as an active ingredient of creatine. That is, the present composition can be used as an additive for food and drink, medicine, and quasi drugs.

  The base and other additives used in that case are not particularly limited as long as the object of the present invention is not impaired, and may be selected according to the dosage form and end use of the final product.

  The composition of the present invention can be ingested as a composition powder as it is, but can also be used in the form of a powdered beverage or a beverage to be dripped after being added to an aqueous solvent such as water. When the composition of the present invention is used as a powdered beverage, it is easy to ingest because the composition of the present invention is quickly and uniformly dispersed when added to an aqueous solvent such as water, and can be stored for a long time without change over time. it can. Further, when the composition of the present invention is used as a beverage, the composition is difficult to recrystallize during heating after dispersing the composition of the present invention in an aqueous solvent, that is, a precipitate is formed even after a sterilization step. It has a characteristic that it hardly occurs. These dosage forms are particularly useful as a dosage form for efficiently and quickly supplementing with creatine in order to increase exercise performance and strengthen muscles, especially in sports scenes. In addition, it can be molded into a desired shape and the like and provided in various dosage forms.

  The composition of the present invention has improved absorbability into the living body due to finer particles. Therefore, even if the intake is less than the conventionally required intake, there is a possibility of exhibiting the same effect as the conventional one.

  In the composition of the present invention, the water dispersibility is remarkably improved. Therefore, for example, by blending with a powdered beverage, it can be easily dispersed in water, maintain a uniform dispersed state over time, can be drunk without causing discomfort, and a product with enhanced absorbability can be proposed. .

  Next, the manufacturing method of the present invention will be described. The composition of the present invention described above may be produced by any method as long as the effects of the present invention can be obtained. However, the production method of the present invention, that is, 100 parts by mass of creatine, 0 emulsifier is used. 1 to 10 parts by mass and 500 to 2000 parts by mass of water are added and mixed, and the mixture is heated to a temperature in the range of 80 to 100 ° C. to be dissolved to prepare an aqueous solution, and by spray drying the aqueous solution. And a second step of obtaining a fine powder having an average particle size of 40 μm or less, the average particle size is smaller than that of other manufacturing methods (for example, pulverization), Is preferred in that the target product having high properties and high water dispersion stability can be simply and reliably obtained.

  In the first step, 500 to 2000 parts by mass, preferably 600 to 1000 parts by mass of water is added and mixed with a predetermined amount of creatine and the emulsifier. If it is less than 500 parts by mass, it will be difficult to sufficiently dissolve creatine, and there is a risk that creatine will be recrystallized during sending to a spray dryer described later, while if it exceeds 2000 parts by mass, creatine will be It becomes difficult to sufficiently coat the above with the emulsifier.

  In addition, in the first step, when creatine, the emulsifier, and water are mixed, the mixture is heated to a temperature in the range of 80 to 100 ° C, preferably 85 to 95 ° C to dissolve the creatine to prepare an aqueous solution. This aqueous solution becomes the spray liquid that is the target of spray drying in the second step. Since this spray solution needs to completely dissolve creatine and the emulsifier, as described above, creatine, the emulsifier, and water are mixed at 80 to 100 ° C. In this case, if the temperature is lower than 80 ° C., it becomes difficult to sufficiently dissolve creatine, while if the temperature exceeds 100 ° C., creatine may be destroyed by heat because it is weak against heat. The creatine and emulsifier are as described above. The heating time in the above temperature range is 60 minutes or less, preferably 30 minutes or less. If the heating time is longer than 60 minutes, the activity of creatine may decrease.

  In the second step, the aqueous solution (spray solution) prepared in the first step is spray-dried to obtain a fine powder, that is, the composition of the present invention. This composition has creatine as a core and the emulsifier fixed to the surface thereof. Spray drying is a method of dissolving a substance to be powdered in a solvent, spraying it at a high temperature to remove the solvent, and instantaneously drying it to obtain a powder. A generally known spray dryer may be used as a device for performing spray drying in the present invention. No special additional equipment is required, and conditions for spraying on the device side may be adjusted according to each device.

  It is desirable that the aqueous solution be spray-dried immediately after its preparation. Also, keep the temperature warm during the spraying process so that the liquid temperature does not drop as much as possible. Specifically, it is preferable to carry out the spray drying treatment while maintaining the liquid temperature at 80 to 100 ° C, preferably 85 to 95 ° C. When the liquid temperature is lower than 80 ° C., creatine may be recrystallized during the feeding to the spray dryer, while when it is higher than 100 ° C., heat may destroy the creatine.

  The manufacturing method of the present invention is characterized by performing the above-mentioned spray drying treatment. In the method of using a pulverizer such as a pin mill or a hammer mill, instead of spray drying treatment, it is not possible to refine the creatine crystals to an average particle size or less required for the performance of the present invention, and an emulsifier on the surface of the creatine as a core. Since the particles cannot be properly attached, the water dispersibility which is the effect of the present invention may not be sufficiently obtained. Alternatively, it takes time to miniaturize and is not suitable for actual manufacturing.

  The smaller the finer particles, the more the water dispersibility increases, but in order to obtain sufficient water dispersibility, the average particle size of the fine powder obtained by spray drying is preferably 40 μm or less, More preferably, it is 20 μm or less.

  The manufacturing method of the present invention may further include other steps, if necessary, in addition to the first step and the second step. For example, a step of adding a food material and / or a food additive to the aqueous solution and mixing them can be added.

  Hereinafter, the present invention will be described in more detail with reference to Examples. The present invention is not limited to these.

[Examples 1 to 9 and Comparative Examples 1 and 2]
1. Difference in water dispersibility depending on the micronization method Creatine (manufactured by Phyto Pharma Co., Ltd.) and sucrose fatty acid ester (manufactured by Mitsubishi Chemical Foods Co., Ltd.) as an emulsifier were blended at a ratio shown in Table 1, and added to 700 parts by mass of water. , Sealed state, heated at 90 ° C. for 30 minutes to completely dissolve. After that, spray-drying treatment was promptly performed to obtain fine powders (Examples 1 to 5). In addition, creatine (manufactured by Phyto Pharma Co., Ltd.) and the emulsifier (manufactured by Mitsubishi Chemical Foods Co., Ltd.) were blended in a ratio shown in Table 1, and pulverized by a free pulverizer to obtain powders (Examples 6 to 9). It was
On the other hand, as a comparative object, untreated creatine (manufactured by Phyto Pharma Co., Ltd.) which has not been crushed is used as Comparative Example 1. Further, creatine (manufactured by Phyto Pharma Co., Ltd.) and the emulsifier (manufactured by Mitsubishi Chemical Foods Co., Ltd.) were blended in a ratio shown in Table 1 and mixed well to obtain a powder (Comparative Example 2).
The powders obtained in Examples 1 to 9 and Comparative Examples 1 and 2 were dispersed in ethanol, and the average particle size was measured by the laser diffraction scattering method (see Table 1).
In order to compare the water dispersibility of the powders obtained in Examples 1 to 9 and Comparative Examples 1 and 2, 5 g of each powder obtained in Examples 1 to 9 and Comparative Examples 1 and 2 was added to 50 g of water, and After 1 minute of shaking and dispersion, the state was visually observed and shown in FIG. 1 (Examples 1 to 5 from the upper left, Examples 6 to 9 from the lower left, Comparative Examples 1 and 2). .

(result)
As can be seen from FIG. 1, in Examples 1 to 9, uniform and good water dispersibility was observed, whereas in Comparative Examples 1 and 2, precipitation was observed in a short time, and uniform and good water dispersion was observed. No sex was observed. In addition, Examples 1 to 5 subjected to the spray drying treatment have a smaller average particle diameter than Examples 6 to 9 subjected to the pulverization treatment with a free pulverizer, and it is possible to realize higher improvement in water dispersibility. Was done. Example 4 and Examples 7 and 8 were different from each other in water dispersibility, although there was no big difference in the average particle size. That is, it was proved that not only simply reducing the particle diameter but also performing spray drying treatment can realize higher improvement in water dispersibility.

2. Difference in Water Dispersion Stability Furthermore, in order to evaluate the water dispersion stability of the fine powders obtained in Examples 1 to 9, changes in the amount of precipitation with the passage of time after being dispersed in water are shown in FIG. . The value of “height of creatine dispersed phase / height of liquid surface” is expressed in percentage, which is shown on the vertical axis of FIG. 2 and the elapsed time is shown on the horizontal axis. The smaller the above value is, the more the precipitation is advanced and the dispersion stability is low. In addition, the photographs showing the state after 120 minutes have passed since the fine powders obtained in Examples 1 to 9 were dispersed in water (Examples 1 to 5 from the upper left, Examples 6 to 9 from the lower left) are illustrated. Shown in 3.

(result)
As can be seen from the results shown in FIG. 2, the fine powders obtained in Examples 1 to 5 show the above range of 47 to 100% even after 120 minutes, and exhibit high water dispersion stability. Was confirmed. On the other hand, Examples 6 to 9 prepared by the pulverization treatment had lower aqueous dispersion stability than Examples 1 to 5 prepared by the spray drying treatment. In addition, among Examples 1 to 5, Example 5 exhibits the highest water dispersion stability, then Example 4 exhibits the highest water dispersion stability, and Example 1 exhibits the lowest water dispersion stability. did. The fine powders obtained in Examples 4 and 5 have larger average particle diameters than those obtained in Example 2, and the fine powders obtained in Example 3 have the same average particle diameters as those obtained in Example 2. From the fact that they are the same, it was found that not only the particle size was simply reduced, but also the compounding amount of the emulsifier had a great influence on the water dispersion stability.

Claims (6)

  A creatine-containing water-dispersible powdery composition, which comprises 0.1 to 10 parts by weight of an emulsifier with respect to 100 parts by mass of creatine, and is obtained by coating a part or all of the surface of creatine with the emulsifier.   The water-dispersible powdery composition according to claim 1, wherein the emulsifier is one or more selected from the group consisting of glycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, and lecithin.   The water-dispersible powdery composition according to claim 1, wherein the water-dispersible powdery composition has an average particle diameter of 40 μm or less.   A food or drink, a pharmaceutical product, or a quasi drug, comprising the water-dispersible powdery composition according to any one of claims 1 to 3.   The food or drink, the drug or the quasi drug according to claim 4, wherein the dosage form is a drink or a powdered drink. With respect to 100 parts by mass of creatine, 0.1 to 10 parts by mass of an emulsifier and 500 to 2000 parts by mass of water are added and mixed, and heated in a range of 80 to 100 ° C. to be dissolved to prepare an aqueous solution. ,
A second step of obtaining a fine powder by spray drying the aqueous solution, the method for producing a creatine-containing water-dispersible powdery composition.

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