JPS6245842B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a method for producing a rapidly soluble biotin preparation in water, which comprises spray-drying an aqueous solution containing biotin, dextrin with a starch decomposition rate of 10 to 25% (hereinafter referred to as dextrin), and ammonia. . Biotin is generally used as a feed additive for livestock, farmed fish, etc. It is also used medicinally to prevent and treat skin diseases. Since biotin is sparingly soluble in water, it is not possible to adopt an addition method that achieves highly uniform blending of biotin into feed by dissolving biotin in water and spraying it onto feed, which is extremely inconvenient in use. Furthermore, when urgently administering biotin to livestock, it is usually dissolved in drinking water or liquid feed, but biotin cannot be administered in this way because it is sparingly soluble in water. Furthermore, they have the disadvantage of poor absorption rate during administration, slow onset of effects, and insufficient bioavailability. Therefore, in order to overcome the above-mentioned inconveniences and drawbacks in use, we have intensively investigated various methods for increasing the solubility of biotin in water. It was found that the solubility of biotin in water was significantly enhanced by spray drying an aqueous solution containing biotin, dextrin, and ammonia. Normally, the intermediate products produced during the hydrolysis of starch to maltose or dextrose are collectively called dextrins, but in the case of dextrins with a starch decomposition rate of 10% or less, their dissolution rate in water is slow and they tend to age easily, resulting in a clear aqueous solution. I can't get it. In addition, in the case of dextrin with a starch decomposition rate of 25% or more, the dissolution rate in water becomes faster, but the dextrin becomes extremely hygroscopic and easily colored. In order to obtain a practically valuable water-soluble biotin preparation, which is the object of the present invention, the starch decomposition rate must be 10 to 10.
They discovered that it was necessary to use 25% dextrin and completed the present invention. The biotin preparation obtained by the method of the present invention not only enhances the solubility of biotin in water, but also has a fast dissolution rate of the preparation itself in water, making it easy to use by dissolving it in drinking water or liquid feed. Biotin is uniformly dispersed and contained in each particle, and the particle size is small and spherical, so it has excellent fluidity and is easy to mix uniformly into feed, making it extremely effective in practice. . Generally known methods for decomposing starch include roasting, acid-added roasting, acid decomposition, and enzymatic decomposition, but the high-temperature liquefaction method can decompose starch into a homogeneous state because the conditions are extremely mild. It is advantageous to use enzyme-modified dextrin according to the invention. The method of the invention is carried out by dissolving biotin, dextrin and ammonia as described above and then spray drying this aqueous solution in a manner known per se. At this time, when only biotin is dissolved in an aqueous solution containing ammonia and then spray-dried, no enhancement of solubility in water is observed and the addition of dextrin is necessary. The blending ratio of biotin and dextrin is not particularly limited, but in actual products it is usually in the range of 1:40 to 1:100. On the other hand, it is desirable that biotin be completely dissolved in the spray-drying solution, and for this purpose it is necessary to add ammonia. The amount of ammonia added is sufficient as long as it dissolves the biotin, usually 0.1% as a 28% ammonia aqueous solution.
The liquid property of the aqueous solution that is spray-dried after adding W/V or more is
It is convenient to adjust the pH to 5-9. The method of adding biotin, dextrin, and ammonia is not particularly limited, but usually a method of adding biotin to an aqueous ammonia solution and then adding dextrin, a method of adding a mixture of dextrin and biotin to an aqueous ammonia solution, or a method of adding a mixture of dextrin and biotin to an aqueous ammonia solution. A method of adding ammonia after dispersing it in water is used. As detailed above, according to the method of the present invention, biotin that is poorly soluble in water can be provided as a rapidly soluble biotin preparation that is extremely effective in practice. The method of the present invention will be explained in detail below with reference to Examples. Example 1 Biotin 10g, dextrin (starch decomposition rate
17%) 490g 28% ammonia aqueous solution 0.25%
Add to water 2 containing W/V and heat to 60-70°C to dissolve. Spray this liquid using a mini spray dryer (Yamato Scientific Co., Ltd.)
Co., Ltd. under the following operating conditions, a preparation containing 2% W/W biotin in the form of spherical particles with a particle size of 5 to 40 microns and good fluidity was obtained. Operating conditions Γ Chamber temperature: 130 to 140℃ Γ Chamber vacuum: 30 mmH ₂ O Γ Atomization pressure: 2.5 Kg/cm ² Reference example 1 10 g of biotin and 490 g of dextrin with a starch decomposition rate of 7% are mixed with 28% ammonia aqueous solution at 0.25% W/
Add to water 2 containing V and heat to 60 to 70°C to dissolve. This liquid was spray-dried under the same operating conditions as in Example 1 to obtain a formulation containing 2% W/W biotin. Reference example 2 10g of biotin and 490g of dextrin with a starch decomposition rate of 35% and 28% ammonia aqueous solution at 0.25%
The mixture was added to water 2 containing W/V and heated to 60 to 70°C to dissolve it, and then spray-dried under the same operating conditions as in Example 1 to obtain a formulation containing 2% W/W of biotin. Reference example 3 10g of biotin and dextrin (starch decomposition rate
17%) was weighed and mixed for 30 minutes using a V-type mixer to obtain a preparation containing 2% W/W biotin. Reference example 4 Biotin 10g 28% ammonia aqueous solution 0.25%
It was added to water 2 containing W/V and heated to 60 to 70°C to dissolve, and then spray-dried under the same operating conditions as in Example 1. Reference example 5 10g of biotin and dextrin (starch decomposition rate
Add 490 g of 17%) to water 2, heat to 60-70°C, and stir to obtain a uniformly dispersed suspension. This suspension was spray dried under the same operating conditions as in Example 1. Next, Table 1 shows the dissolution rate in water of the biotin preparation obtained by the method of the present invention, and Table 2 shows the results of comparison with the reference example in terms of the solubility of biotin in water. The dissolution rate of the biotin preparations in water was measured by weighing 100 ml of water in a beaker, adding 10 g of each preparation while stirring with a magnetic stirrer, and measuring the time until it dissolved clearly. Furthermore, the solubility of biotin in water was measured at room temperature, and biotin was quantified using high performance liquid chromatography.

【table】

[Table] From the results in Table 1, when using dextrin with a low starch decomposition rate, the dissolution rate in water is slow;
In the case of dextrin with a high rate of starch decomposition, the dissolution rate in water was fast, but there was also a tendency for the dissolved solution to become slightly colored over time. On the other hand, as is clear from Table 2, in order to increase the solubility of biotin in water, it is necessary to spray dry an aqueous solution containing biotin, dextrin, and ammonia. Example 2 Biotin 10g 28% ammonia aqueous solution 0.5%
In addition to water 2 containing W/V, 490 g of dextrin (starch decomposition rate 15%) was added to 60-70 g.
After heating to 0.degree. C. for dissolution, spray drying was performed under the same operating conditions as in Example 1 to obtain a preparation containing 2% W/W biotin in the form of spherical particles with a particle size of 5 to 40 microns. This preparation had a fast dissolution rate in water, little hygroscopicity over time, and good fluidity. On the other hand, the solubility of biotin in water was 14 mg/ml. Example 3 Biotin 10g, dextrin (starch decomposition rate
20%) 990g 28% ammonia aqueous solution 0.1%W/
The mixture was added to 10% of water containing V and dissolved by heating to 60-70°C, and then spray-dried under the same operating conditions as in Example 1 to obtain a formulation containing 1% W/W of biotin. Example 4 Biotin 10g and dextrin (starch decomposition rate
12%) 490g and then dispersed in water 2,
Next, add 10g of 28% ammonia aqueous solution to 60-70%
The mixture was heated to 0.degree. C. to dissolve, and then spray-dried under the same operating conditions as in Example 1 to obtain a preparation containing 2% W/W biotin.

Claims (1)

[Scope of Claims] 1. A method for producing a water-soluble biotin preparation, which comprises spray-drying an aqueous solution containing biotin, dextrin with a starch decomposition rate of 10 to 25%, and ammonia. 2. The method for producing a biotin preparation according to claim 1, wherein the ratio of biotin to dextrin with a starch decomposition rate of 10 to 25% is 1:40 to 1:100. 3 An aqueous solution containing biotin, dextrin with a starch decomposition rate of 10 to 25%, and ammonia has a pH of 5 to
9. The method for producing a biotin preparation according to claim 1.