JPS61145111A - Production of tablet - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to a method for manufacturing tablets by a dry direct compression method. The present invention relates to a method for obtaining tablets that have good compressibility and excellent properties such as compression moldability and hardness.

Conventional techniques and their problems Conventionally, when tablets are manufactured by a dry direct compression method using tablet materials containing powders with poor moldability such as acetaminophen powder and ascorbic acid powder, it is necessary to improve the compression moldability of the tablets. For this purpose, it is known to mix fine powder of a binder such as polyethylene glycol, gelatin, dextrin, cellulose, etc. with the tablet raw material (Japanese Patent Publication No. 15755/1983). Additionally, in order to improve the moldability of powders with poor moldability, it has also been proposed to further pulverize microcrystalline cellulose, knead it with powder with poor moldability, and apply spread coating to the powder. (Special Publication No. 46-8718).

However, the former method requires the use of a large amount of fine binder powder, resulting in disadvantages in terms of manufacturing process, cost, quality, etc. In addition, the latter method has the problem that it is difficult to uniformly coat the ultrafine cellulose powder, resulting in variations in the quality of the obtained tablets.

Summary of the Invention In view of the above circumstances, the present inventors have conducted various studies on improving the moldability of powders with poor moldability.
A powder tablet in which the surface of one or more of the powder tablet components is coated with an aqueous solution of a water-soluble polymer substance having a concentration of 1 to 15% (weight: fiit%, the same hereinafter) with the above amount of water-soluble polymer substance. By spray coating the coating to a concentration of 0.1 to 5% of the ingredient amount and drying it, even if only a small amount of water-soluble polymer material is used as a binder, the water-soluble polymer material can be coated on the surface of the powdered tablet ingredients. When a water-soluble polymer substance coated powder is obtained which is uniformly coated with a substance and has excellent moldability, and this coated powder is mixed with tablet material and tableted by a dry direct compression method,
The present invention was based on the discovery that it is possible to obtain tablets with good compressibility, excellent properties such as compression moldability and hardness.

The present invention will be explained in more detail below.

Structure of the Invention The method for manufacturing a tablet according to the present invention comprises coating the surface of one or more types of powder tableting components with an aqueous solution of a water-soluble polymer substance having a concentration of 1 to 15%. Spray coating is applied to the desired amount of powder tableting ingredients to be 0.1 to 5%, and this is dried to obtain a water-soluble polymer coated powder, and the tablet raw material mixed with this coating powder is dry-directly compressed into tablets. Tablets are obtained by compression according to the law.

In this case, there are no restrictions on the type of water-soluble polymeric substance, such as gelatin, pectin, polyacrylic acid, polyacrylate, polyvinyl alcohol, polyvinylpyrrolidone,
Polyvinylpyrrolidone-vinyl acetate copolymer,?
Liethylene oxide, sodium carboxymethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose, alginate, xanthan gum, gum arabic, gum tragacanth, gum karaya,
One or more types selected from synthetic, semi-synthetic, and natural water-soluble polymer substances such as caradanan, methyl vinyl ether/maleic anhydride copolymer, etc. can be used, but in the present invention, polyvinylpicolidone, hydroxypropyl It is particularly preferred to use one or more of cellulose, methylcellulose, gum arabic and caradanan.

In addition, as mentioned above, the aqueous solution of the water-soluble polymeric substance needs to have a concentration of 1 to 15%, and if the concentration is lower than 1%, it will take one hour to spray and dry. It takes a long time, which reduces manufacturing efficiency and
The cost will also be higher.

In addition, if the concentration is higher than 10%, the viscosity of the aqueous solution will increase, making it necessary to increase the spray pressure, making it difficult to coat the powder surface uniformly, and secondary agglomeration may occur, so it must be ground. Therefore, the manufacturing process becomes complicated and it becomes difficult to obtain tablets of uniform quality. Note that the most preferable concentration of the water-soluble polymeric substance is 1 to 5%.

In the present invention, an aqueous solution of the water-soluble polymeric substance described above is sprayed onto one or more powder tableting ingredients, and the surface of the tabletting ingredients is coated with the water-soluble polymeric substance. It is preferable to carry out this method for powdered tablet components that have poor moldability. Such ingredients include acetaminophen, ascorbic acid, and the like. In this case, when two or more of these components are used as tablet material, only one of these components may be coated, or two or more of these components may be coated. In addition, it is preferable that the average particle size of these powder components to be coated is 150μ to 840μ.

The coating amount of the water-soluble polymer substance on the surface of the powder tablet component to be coated needs to be 0.1 to 5% of the component to be coated, as described above, and the coating amount is 0.1% to 5% of the component to be coated. If it is less than 1%, the moldability of the powder will not be improved, and if it is more than 5%, the disintegration properties of the tablet will be poor and a large amount of disintegrant will be required, resulting in high costs. The coating amount is preferably in the range of 1 to 3.
%.

There are no restrictions on the method and conditions for spraying the water-soluble polymer substance aqueous solution onto the powder tablet component and drying it, and known methods and conditions can be employed.

In the present invention, the powder coated with the above-mentioned water-soluble polymer substance is mixed with other tablet materials, and tablets are manufactured using the powder by a dry direct compression method using conventional equipment and methods.

In this case, there are no limitations on the other ingredients of the tablet material, including excipients,
Disintegrants, lubricants, active ingredients, etc. can be added as appropriate.

As described in detail of the invention, according to the method for manufacturing tablets according to the present invention, even if the tablet material contains powder tableting components with poor formability, one or both of the powder tableting components can be used. By coating the above surface with a water-soluble polymeric substance, the moldability is improved, and therefore, tablets can be obtained that have excellent tabletting properties and good properties such as compression moldability and hardness. Moreover, according to the present invention, even if only a small amount of water-soluble polymer substance (binder) is used, the light surface of the powder tablet component can be uniformly coated with the water-soluble polymer substance. Problems such as high costs and variations in tablet quality due to non-uniformity of coating do not occur.

Next, examples and comparative examples will be shown to specifically explain the present invention.

[Examples 1 to 5, Comparative Examples 1 to 5] Three to nine parts of acetaminophen powder was placed in a fluidized bed granulator with a capacity of 51, and hydroxypropylcellulose (RPC) klA! was added at the concentration shown in Table 1. Each 7 cetaminophene powder A- coated with hydroxypropyl cellulose was spray coated with an aqueous solution dissolved in O water at an intake temperature of 70°C and an exhaust temperature of 50°C.
E (product of the present invention) obtained. Note that the amount of hydroxypropyl cellulose coated on the acetamin 7ene powder is as shown in the first coating.

Table 1 Next, each of the above powders A to E was uniformly mixed with the following components to obtain each tablet material, and then this material was compressed by a dry direct tableting method to give Examples 1 to 50 tablets. The hardness and capping rate of these tablets were investigated using a proprietary method. In addition, for comparison, the same procedure as Examples 1 to 5 was performed except that the acetaminophen powder was not coated with the dihydroxypropyl cellulose powder and the hydroxypropyl cellulose powder was simply mixed with the acetaminophen powder in the amount shown in Table 2. Tablets of Comparative Examples 1 to 5 were manufactured using the method described above, and the tablet hardness and capping rate were similarly examined. Furthermore, control tablets in which hydroxypropyl cellulose was not coated or mixed with acetaminophen powder were prepared in the same manner, and the same measurements were performed. The results are shown in Table 2. Two components: Acetaminophenone + Hydroxypropylcellulose 29.3% Aspirin
47.9# Caffeine
11.5# Magnesium stearate 0
．． 21 total
100゜0I (1) Hardness 2 tablet breaking strength measuring machine (2) Capping rate 2 tablet abrasion tester, 10 pieces, 5
According to the results in Table 2, it was found that the tablets of the examples containing acetaminophen powder coated with hydroxypropyl cellulose had moderate hardness and were unlikely to cause capping. . On the other hand, all of the tablets containing powdered hydroxypropylcellulose were capped, and problems such as chipping occurred during tablet compression. Furthermore, due to poor moldability, tablets with appropriate hardness could not be obtained.

[Example 6] Volume t5J? Put 3 kg of acetaminophen powder into a fluidized bed granulator, and add to it an aqueous solution of 6011 hydroxypropyl cellulose dissolved in 1 ml of water (hydroxypropyl cellulose concentration 6%), total intake temperature 70°C, exhaust temperature 50°C. Spray coating was carried out under the following conditions to obtain a powder coated with 2 parts of hydroxypropylcellulose per weight of acetaminophen.

Next, at 1.53 hours of the above powder, 2.5 kg of aspirin,
Caffeine 0.6 kg, excipients such as starch o, 55
After uniformly mixing 0.01 kg of magnesium stearate to obtain a tablet material, this material was compressed by a dry direct tableting method to produce tablets.

[Example 7] 1.5 kg of ascorbic acid powder was placed in a fluidized bed granulator with a capacity of 3 mm, and an aqueous solution of 759 polyvinylpyrrolidone dissolved in 675 mm water (polyvinylpyrrolidone concentration 1 os) was added to the inlet air temperature. Spray coating was carried out under conditions of 55° C. and exhaust temperature of 45° C. to obtain a powder coated with 5% polyvinylpyrrolidone based on the weight of ascorbic acid.

9. to 0.85 of the above powder. Avicel 0.1 to 9. A tablet material was obtained by uniformly mixing 0.045 kp of corn starch and 0.005 k19 of talc, and then this material was compressed by a dry direct compression method to produce tablets.

The tablets of Examples 6 and 7 had excellent compression moldability and moderate hardness.

Claims (1)

[Claims] 1. An aqueous solution of a water-soluble polymeric substance having a concentration of 1 to 15% by weight is coated on the surface of one or more types of powder tableting ingredients by 0.1 of the amount of the powder tableting ingredients to be coated with the above-mentioned amount of water-soluble polymeric substance.
Spray coat to ~5% by weight, dry this to obtain a water-soluble polymer coated powder, and tablet material mixed with this coating powder is compressed using a dry direct compression method to obtain tablets. A method for manufacturing a tablet, characterized by: