JPH0678229B2 - Process for producing hard granules containing vitamin C - Google Patents

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a method for producing high unit vitamin C-containing hard granules, and a hard granule produced by the method.

[0002]

2. Description of the Related Art Vitamin C (ascorbic acid) is used for the treatment of vitamin C deficiency such as scurvy, treatment of drug poisoning and adrenocortical dysfunction, formation of bone matrix during fracture, or spots, freckles, inflammation, etc. It is also effective for removing pigment deposits and is used in a wide range of fields including pharmaceuticals, foods and cosmetics. In particular, the therapeutic effect of high unit vitamin C has been attracting attention.

[0003]

However, since vitamin C has a strong sourness, the amount that can be taken at one time is limited. That is, although the maximum dose for adults according to the Ministry of Health and Welfare is 2000 mg / day, the maximum dose that can be taken at one time is 300 mg, which makes high-unit vitamin C treatment difficult. In particular, in the case of severely ill patients, the elderly and children, it was not possible to take a sufficient amount.

[0004]

[Means for Solving the Problems] The inventors of the present invention have conducted extensive studies for the purpose of obtaining a vitamin C product in a dosage form that enables high doses of vitamin C to be taken. As a result, the granules obtained by granulating in the presence of a certain amount of water and ethanol and then drying have a low solubility in the mouth, and therefore, even if they contain a high concentration of vitamin C, they have a sour taste. Although not allowed, it was found that the physiological activity of vitamin C was maintained as it was, and the present invention was completed.

That is, according to the present invention, vitamin C, which is rotating at a high speed,
The mixing ratio was 9 in the granulating mixture containing the sweetener and the sizing agent.
A method for producing vitamin C-containing hard granules, which comprises granulating a mixture of 5: 0.5 to 5: 5 ethanol and water while dripping, and then evaporating ethanol and water in the granules. Is.

The raw material for producing the hard granules of the present invention is selected from the raw materials usually used for producing vitamin C granules. In particular, starch can be mentioned as a sizing agent that can be used in the method of the present invention. Examples of the sweetener include aspartame, glycyrrhizin, steviaside, saccharin and the like. However, it is not limited to these. According to the method of the present invention, the vitamin C content in the granulation mixture can be increased to a high concentration of up to about 80-90%, if desired. The mixture ratio of the mixture is
As long as the desired vitamin C concentration can be achieved, it can be appropriately selected within a range that does not hinder granulation.
For example, vitamin C: sizing agent: sweetener about 9: about 0.7:
Hard granules can be obtained by mixing in a ratio of about 0.3. The preferred blending ratio is about 8.1: about 1.6: about 0.3, but is not limited thereto. Granulation with such a mixture gives granules whose surface is coated with a sweetener.

In the method of the present invention, a commercially available high speed mixer is used. The rotation speed varies depending on the rotation speed of the machine, but normally, the agitator: about 100 to 500 rpm.
p. m. Chopper: about 100 to 1200 r. p.
m. Preferably, the agitator is about 200 rpm and the chopper is about 200 rpm. The water / ethanol mixture is added dropwise while rotating the granulation mixture at such high speed. The mixing ratio of water and ethanol is about 0.5: by weight.
9.5 to about 5: 5, preferably about 1: 9 to 3: 7, particularly preferably 1: 9 are suitable. Further, the addition amount to the granulation mixture can be about 10 to 25% by weight, preferably about 15% by weight. The size of the granule is appropriately selected according to the purpose, but when used as a medicinal raw material, a particle size range of about 16 to 80 mesh will be suitable.

The granules are then dried to a water content of about 0-5%, preferably about 3%. The drying method is not particularly limited, but it is preferable to use a vibration fluidized vacuum dryer. In this case, preferably under a reduced pressure of 70 cmHg,
Drying at a temperature of about 60 to 100 ° C., preferably about 80 ° C. gives hard granules in about 3 hours.

[0009]

The hard granules produced by the method of the present invention are about 80-
Despite containing a high concentration of 90% by weight of vitamin C, the solubility in the mouth is low, so that strong acidity is not felt when taken. Therefore, by mixing this as a vitamin C raw material, a high unit vitamin C-containing pharmaceutical composition can be produced. Further, since it is coated with a suitable high-concentration sweetener, it is easy to take and can be used as it is for high-unit vitamin C treatment.

The present invention is described in detail below with reference to examples, but the present invention is not limited thereto.

Example 1 Vitamin C (ascorbic acid) 40.5 kg, aspartame (sweetener) and sizing agent 9 kg are put into a high speed mixer (FS-GS-50 type: Fukae Industry Co., Ltd.). Number of rotations of high speed mixer (Agitator: about 2
(00 rpm / min; chopper: about 200 rpm / min) while mixing with water and ethanol (weight ratio 1: 9)
7.5 kg are added dropwise in about 5 to 15 minutes. About 2 minutes after the end of dropping, the number of rotations of the high speed mixer is readjusted (agitator: about 200 rpm / minute; chopper: about 200 rpm / minute).

Next, the wet granules were placed in a vibrating fluidized vacuum dryer (VH-60V-Dryer: Chuo Koki Co., Ltd.), the jacket was heated to 80 ° C. and 3 to 10 speed was applied.
It is dried under reduced pressure at about 70 cmHg while vibrating. About 8
Time treatment gives granules with a water content of about 3%. The vitamin C content in the final product was about 80%. The hard granules thus produced have the surface coated with a high concentration sweetener. When I put it in my mouth, there was no sourness, and I felt only sweetness.

[Effect] The hard granules according to the method of the present invention are
Despite the high concentration of Vitamin C, it does not cause a sour taste in the mouth and can be easily taken by anyone. Therefore, it can be clinically applied as a component of a high unit vitamin C-containing pharmaceutical composition or as a single agent because the surface is coated with a sweetener in various situations. As described above, according to the present invention, it is possible to give a large amount of vitamin C to all people.

Claims (5)

[Claims] 1. A granulation mixture containing vitamin C, a sweetener and a sizing agent, which is rotating at a high speed, having a mixing ratio of 9.5: 0.5 to.
A method for producing vitamin C-containing hard granules, which comprises granulating while a 5: 5 mixture of ethanol and water is added dropwise, and then evaporating water and ethanol in the granules. 2. The method of claim 1, wherein the content of vitamin C in the granulation mixture is about 80 to about 90% by weight. 3. A mixing ratio of ethanol and water of 9: 1 to 7:
3. The method of claim 1 or 2 which is 3. 4. Ethanol and water mixture in a total weight of 1
The method according to any one of claims 1 to 3, wherein 0 to 25% by weight is added. 5. Vitamin C hard granules produced by the method according to claim 1.