JPH11243907A - Production of tablet preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a tablet preparation that can improve the fluidity of powder without using lubricant, the taste quality, hardness and moisture absorption, and is useful for food products, medicines and the like, by directly compressing xylitol powder coated with a lipid that is solid at room temperature. SOLUTION: Xylitol particles are coated with a lipid that is solid at room temperature such as hardened tallow oil, preferably in an amount of 0.1-6.0 wt.%, and the coated xylitol powder is directly compressed to prepare the objective tablets. The resultant lipid-coated xylitol powder is mixed with a sugar alcohol selected from the group consisting of sorbitol, maltitol, mannitol, lactitol, palatinit, erythritol and their mixtures and they are directly compressed into the objective tablets.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD OF THE INVENTION

[0002] The present invention relates to a method for producing a tablet containing xylitol.

[0003]

2. Description of the Related Art

In recent years, as a method for producing tablets, a direct compression method that does not require a granulating operation has been tending to be used because it is economically advantageous because the process can be simplified.

On the other hand, xylitol does not cause caries because it is not assimilated by oral bacteria, and it is metabolized independently of insulin in the body, so that it does not raise blood sugar levels.
Further, since it is a chemically stable sugar alcohol having a strong cooling sensation, it is used as a sweetener, a diluent and the like in many foods and pharmaceuticals.

However, xylitol has a problem that it is extremely difficult to form a tablet by the direct compression method, or even if it can be formed, satisfactory tablet hardness cannot be obtained.

As a method for solving this problem, Japanese Patent Laid-Open No.
Japanese Patent Application Laid-Open No. 2-102467 describes a method of directly compressing a mixture containing about 10 to 80% by weight of xylitol and about 10 to 80% by weight of a polyhydric alcohol such as sorbitol.

In this method, a mixed powder obtained by mixing xylitol in a dry state with a polyhydric alcohol such as sorbitol is directly compressed, but in order to obtain a sufficient tablet hardness, the same weight as xylitol or xylitol is used. It is necessary to mix higher weight polyhydric alcohol,
As a result, the cool feeling and refreshing taste of xylitol cannot be imparted to the tablet.

In addition, despite the fact that xylitol powder itself has almost no hygroscopicity, tablets formed from a mixed powder mixed with a polyhydric alcohol such as sorbitol powder easily absorb moisture during storage and deliquesce. .

In addition, a method of directly compressing a granulated xylitol powder by spraying a sorbitol solution onto the xylitol powder (JP-A-2-15035), partially melting a powder containing xylitol as a main component, A method of directly compressing a powder obtained by extrusion (Japanese Patent Laid-Open No.
Further, a method of directly compressing granules obtained by spray-drying a binder such as polydextrose or hydrogenated starch hydrolyzate onto xylitol powder using a granulating device (Japanese Patent Application Laid-Open No. 6-503080). Publication).

However, in any of the methods, the powder processed directly by using a heating extruder or a granulating device such as a spray granulator or an extruder is directly compression-molded as a raw material, and the processing operation is complicated. However, the method is not always satisfactory because a large amount of energy is required for evaporating water in the sprayed aqueous solution and melting the powder.

An object of the present invention is to solve these problems and to provide a method for directly compression-molding a xylitol tablet having sufficient hardness and stable during storage.

[0013]

[Means for Solving the Problems]

The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, by directly compressing a xylitol powder coated with a solid lipid at room temperature, a tablet having a sufficient hardness can be obtained. In addition, the obtained tablets were found to be stable for long-term storage, and the present invention was completed.

That is, means for solving the problems of the present invention are as follows. First, there is a method for producing tablets by directly compressing a xylitol powder coated with a solid lipid at room temperature. Second, the method for producing a tablet according to the first aspect, wherein the lipid in the xylitol powder coated with the lipid is 0.1 to 6.0% by weight. Thirdly, the lipid-coated xylitol powder is mixed with a sugar alcohol powder selected from the group consisting of sorbitol, maltitol, mannitol, lactitol, palatinit, erythritol and a mixture thereof, and then directly compressed. 2
The method for producing a tablet according to the above. Fourthly, the method for producing a tablet according to the third aspect, wherein the sugar alcohol powder is a powder coated with a lipid that is solid at room temperature. Fifth, sorbitol, maltitol, mannitol, xylitol powder
This is a method for producing a tablet in which a mixed powder obtained by adding a sugar alcohol powder selected from the group consisting of lactitol, palatinit, erythritol and a mixture thereof is coated at room temperature with a solid lipid and then directly compressed. Sixth
The method according to claim 5, wherein the lipid in the mixed powder coated with the solid lipid at room temperature is 0.1 to 6.0% by weight.

The lipid which can be used for coating in the present invention includes:
A lipid that is solid at room temperature, preferably a lipid having a melting point of 40 ° C. or higher, more preferably a lipid having a melting point of 50 ° C. or higher, for example, tallow hydrogenated oil, rapeseed hydrogenated oil, palm hydrogenated oil,
Hardened soybean oils, waxes such as carnauba wax and beeswax, fatty acids such as stearic acid and palmitic acid, metal soaps such as calcium stearate, sterols such as cholesterol and fucosterol, fatty acid esters of glycerin and the like can be used and are appropriately selected.

Also, fats and oils having a melting point of 40 ° C. or less can be used as long as they are appropriately mixed with the above-mentioned lipids and the mixed lipid has a melting point of 40 ° C. or more. However, when a lipid having a melting point of 40 ° C. or less is used, a powder suitable for direct tableting with fluidity cannot be obtained, and when a tablet is formed using the obtained powder, It is not preferable because the surface of the tablet becomes sticky.

As a method of coating the lipid on the xylitol powder or sugar alcohol powder, a known mixer, ball mill, electric mortar, high efficiency powder mixing device, or the like is used to mix the xylitol powder or sugar alcohol powder with the solid lipid powder. A method of contacting and colliding powders with each other to coat them can be used. At this time, by previously mixing the lipid with xylitol powder or sugar alcohol powder,
A more uniform coating can be achieved. Further, it is also possible to spray and coat a molten fat or oil while stirring with the above-mentioned apparatus or fluidized bed granulator.

In the present invention, the amount of lipid in the xylitol powder coated with lipid is adjusted to preferably 0.1 to 6.0% by weight, more preferably 1.0 to 4.0% by weight. When the lipid amount exceeds 6.0% by weight, a punch is formed during the production of the tablet, and not only the lipid is released and sticky on the surface of the prepared tablet, but also the cooling sensation inherent in xylitol is excellent. It is not preferable because the taste quality is impaired. If the lipid content is less than 0.1% by weight, it is difficult to uniformly coat the surface of the xylitol powder with the lipid, and the expected effect cannot be obtained.

As the sugar alcohol to be mixed with the xylitol powder in the present invention, any one of sorbitol, maltitol, mannitol, lactitol, palatinit, erythritol and a mixture thereof is selected. Tablets with sufficient hardness can be obtained.

The mixing ratio of xylitol and the sugar alcohol other than xylitol can be freely selected in such a ratio as to maintain the excellent taste and non-caries properties of xylitol.

The xylitol powder and the sugar alcohol powder other than xylitol mixed in the present invention can be coated directly with solid lipids at room temperature and then mixed directly for tableting. The mixed powder obtained by coating the solid with lipid at room temperature after mixing the powder can also be directly compressed. Further, a sugar alcohol powder other than xylitol, which is not coated with lipid, may be mixed with a xylitol powder coated with lipid, which is solid at room temperature, and directly compressed.

Sorbitol, maltitol, mannitol, lactitol, palatinit,
When coating a mixed powder obtained by adding a sugar alcohol powder selected from the group consisting of erythritol and a mixture thereof with a solid lipid at room temperature, in order to maintain the cool feeling of xylitol and prevent sticking The lipid content in the mixed powder after coating is preferably adjusted to 0.1 to 6.0% by weight, more preferably 1.0 to 4.0% by weight.

In the production of the tablet of the present invention, a sweetener, a flavor, a lubricant, a binder, a bulking agent, a coloring agent, a medicine, a preservative and the like can be freely added according to the purpose. Further, bone powder, tribasic calcium phosphate, diatomaceous earth and the like can be added in the step of coating with lipid for the purpose of improving the fluidity of the powder as the raw material of the tablet and preventing the powder from scattering and caking. .

[0025]

【Example】

The present invention will be described in more detail with reference to Comparative Examples and Examples.

However, in the following comparative examples and examples,
% Means weight% unless otherwise specified.

The tablets were formed using a rotary tableting machine 8F3 manufactured by Kikusui Seisakusho Co., Ltd., with a 10 mmφ, 14R punch, an upper punch position of 3.0 mm, and a tablet weight of 0.5 g / tablet. The hardness of the prepared tablets was measured using a Kiya tablet hardness tester manufactured by Kiya Seisakusho Co., Ltd. or a tablet hardness tester TH-203CP manufactured by Toyama Sangyo Co., Ltd., and the measurement results of 5 tablets for each tablet were measured. Was taken as the hardness of the tablet.

The hygroscopicity of the tablets is determined by precisely weighing one tablet of each tablet in a weighing bottle, and then adjusting the temperature and humidity of the tablet (Ettac Co., Ltd., F
X210P) at a temperature of 30 ° C. and a relative humidity of 80%
Was measured over time, the moisture absorption was calculated by the following equation, and the average value of six tablets was taken as the moisture absorption of the tablet.

Amount of moisture absorption (%) = [{(weight at the time of measurement) − (weight before the test)} / (weight before the test)] × 100

In Comparative Examples and Examples, the sugar alcohol powders shown in Table 1 were used.

[0032]

[Table 1]

[0033]

[Comparative Example 1]

D was added to 97 g of xylitol powder as a lubricant.
3 g of KD F-20W (manufactured by Daiichi Kogyo Seiyaku Co., Ltd.) was mixed, and a tablet was formed using the obtained mixed powder as a raw material. The fluidity of the mixed powder was poor and was not suitable for tableting. Also,
The hardness of the molded tablet was as small as only 3.4 kg and easily disintegrated.

[0035]

[Comparative Example 2]

DKD F-20W as a lubricant was added to 48.5 g of xylitol powder and 48.5 g of maltitol powder.
3 g (manufactured by Daiichi Kogyo Seiyaku Co., Ltd.) was mixed, and tablets were formed using the obtained mixed powder as a raw material. Although tableting was possible, the fluidity of the mixed powder was poor and not suitable for tableting.

[0037]

Embodiment 1

To 150 g of xylitol powder was added a fine powder of soybean hardened oil (manufactured by NOF Corporation, average particle size 8.6 μm, melting point 6).
(4.6 ° C.), 4.6 g of the mixture was added, and the mixture was treated for 5 minutes using a Nara hybridization system (manufactured by Nara Machinery Co., Ltd.) to coat the xylitol powder with hydrogenated soybean oil. Tablets were formed using the obtained xylitol powder coated with hardened soybean oil as a raw material. The fluidity of the xylitol powder coated with soy hydrogenated oil was good and the tableting operation was easy. The hardness of the molded tablet was 6.8 kg, which was sufficiently improved as compared with Comparative Example 1. 3. Even if the molded tablet is stored for 7 days at 30 ° C./80% relative humidity,
Only 93% absorbed moisture and did not deliquesce.

[0039]

Embodiment 2

A tablet was formed under the same conditions as in Example 1 except that the weight of the hardened soybean oil fine powder was 7.9 g. Example 1
Like the soybean-hardened oil-coated xylitol powder prepared in
The fluidity of the powder was good and the tableting operation was easy. The hardness of the molded tablet is 11.4 kg, and the moisture absorption when stored for 7 days at 30 ° C./80% relative humidity is 3.84%.
It improved, and there was no deliquescence.

[0041]

Embodiment 3

A mixture of 50 g of xylitol powder coated with soybean hardened oil prepared in the same manner as in Example 2 and 47.5 g of maltitol powder not coated with lipid was used to form a tablet using the resulting mixed powder as a raw material. did. The fluidity of the obtained mixed powder was good and the tableting operation was easy. The hardness of the formed tablet was 14.5 kg.

[0043]

Embodiment 4

50 g of xylitol powder coated with hardened soybean oil prepared in the same manner as in Example 2 and 150 g of maltitol powder in advance were mixed with finely ground soybean oil (Nippon Oil & Fats Co., Ltd.)
Maltitol powder coated with lipids by adding 7.9 g of an average particle size of 8.6 μm and a melting point of 63.6 ° C.) and treating for 5 minutes using a Nara hybridization system (manufactured by Nara Machinery Co., Ltd.). 50 g were mixed, and a tablet was formed using the obtained mixed powder as a raw material. The fluidity of the obtained mixed powder was very good. The hardness of the molded tablet was 20.9 kg.

[0045]

Embodiment 5

Carnauba wax (produced by Noda Wax Co., Ltd., manufactured by pulverizing a product having a melting point of 83.7 ° C. to an average particle size of 15.4 μm) in 150 g of xylitol powder 7.9
g, and the mixture was treated for 10 minutes using a vertical granulator (manufactured by Powrex Corporation) to coat the xylitol powder with carnauba wax. 50 g of xylitol powder coated with the obtained carnauba wax
And 47.5 g of sorbitol powder not coated with lipid
Were mixed, and tablets were formed using the obtained mixed powder as a raw material. The fluidity of the obtained mixed powder was good. Also,
The hardness of the formed tablet was 22.4 kg.

[0047]

Embodiment 6

[0048] 50 g of xylitol powder coated with soybean hardened oil prepared in the same manner as in Example 1 and 150 g of sorbitol powder in advance were mixed with soybean hardened oil fine powder (Nippon Oil & Fats Co., Ltd.)
(Average particle size: 8.6 μm, melting point: 63.6 ° C.) and treated with a Nara hybridization system for 5 minutes to give lipid-coated sorbitol powder 5
0 g were mixed, and tablets were formed using the obtained mixed powder as a raw material. The fluidity of the obtained mixed powder was very good. The hardness of the formed tablet was 26.1 kg.

[0049]

Embodiment 7

A mixed powder 200 obtained by uniformly mixing 100 g of xylitol powder and 100 g of maltitol powder.
Then, 10.5 g of soybean hardened oil fine powder was added to the resulting mixture and treated for 10 minutes using a high-speed mixer (manufactured by Fukae Kogyo Co., Ltd.) to prepare a xylitol / maltitol mixed powder coated with lipid. Next, xylitol coated with lipid
Tablets were formed using the maltitol mixed powder as a raw material. The fluidity of the obtained mixed powder was very good. Also,
The hardness of the formed tablet was 19.5 kg.

[0051]

【The invention's effect】

According to the present invention, a xylitol tablet having improved taste and hardness can be formed by a direct compression method. Further, in the present invention, it is not necessary to add a lubricant, particularly when the amount of lipid used for coating is large. According to the present invention, the energy consumption is low in the preparation stage of the powder to be directly compressed, and the tablet processing cost can be reduced. Furthermore, the fluidity of the powder used as the raw material for tablet molding can be improved, the scattering of the powder can be prevented, and the tableting operation can be facilitated.

──────────────────────────────────────────────────続 き Continuation of the front page (51) Int.Cl. ⁶ Identification code FI A61K 47/14 A61K 47/14 D (72) Inventor Mutsuro Kawamoto 3-27-3-503, Kameari, Katsushika-ku, Tokyo (72) Inventor Naoki Okamoto 186-2, Onemoto, Matsudo-shi, Chiba (72) Inventor Abejima ritual 3-3-5-1, Fujimi, Fukiage-cho, Kitadachi-gun, Saitama -2-8

Claims (6)

[Claims] 1. A method for producing a tablet, wherein a xylitol powder coated with a lipid which is solid at room temperature is directly compressed. 2. The method according to claim 1, wherein the lipid in the xylitol powder coated with the lipid is 0.1 to 6.0% by weight. 3. The method of claim 1, wherein the lipid-coated xylitol powder is mixed with a sugar alcohol powder selected from the group consisting of sorbitol, maltitol, mannitol, lactitol, palatinit, erythritol and a mixture thereof, and then directly compressed. Or a method for producing a tablet according to 2. 4. The method according to claim 3, wherein the sugar alcohol powder is a powder coated with a lipid that is solid at room temperature. 5. A mixed powder obtained by adding a sugar alcohol powder selected from the group consisting of sorbitol, maltitol, mannitol, lactitol, palatinit, erythritol and a mixture thereof to a xylitol powder, and adding a solid lipid at room temperature A method for producing a tablet, which is directly compressed after being coated with. 6. The method according to claim 5, wherein the lipid in the mixed powder coated with the lipid solid at room temperature is 0.1 to 6.0% by weight.