JPH0587487B2 - - Google Patents

Description

[Detailed description of the invention]

INDUSTRIAL APPLICATION FIELD The present invention relates to a method for producing acetaminophene-containing tablets by a dry direct compression method. More specifically, the present invention relates to a method for producing acetaminophene-containing tablets by a dry direct compression method. The present invention relates to a method for producing acetaminophene-containing tablets that have good tablet properties and excellent properties such as compression moldability and hardness. Conventional Technology and Problems to be Solved by the Invention Conventionally, when tablets are manufactured by a dry direct compression method using a tablet material containing acetaminophene powder, which has poor moldability, polyethylene is used to improve the compression moldability of the tablet. It is known to mix fine powder of binders such as glycol, gelatin, dextrin, cellulose, etc. with tablet raw materials (Japanese Patent Publication No. 1973-
No. 15755). In addition, in order to improve the moldability of powders with poor moldability, it has been proposed to further pulverize microcrystalized cellulose, knead this with powder with poor moldability, and spread and coat the powder. (Special Publication No. 46-8718). However, the former method requires the use of a large amount of fine binder powder, which is disadvantageous in terms of manufacturing process, cost, quality, etc. Furthermore, the latter method has the problem that it is difficult to uniformly coat the ultrafine cellulose powder onto the powder, resulting in variations in the quality of the obtained tablets. Means and Effects for Solving the Problems In view of the above circumstances, the present inventors conducted various studies on improving the moldability of acetaminophene powder, which has poor moldability, and found that
By spray coating an aqueous solution of hydroxypropylcellulose at a concentration of Even when a small amount of hydroxypropyl cellulose is not used as a hydroxypropyl cellulose, the surface of the acetaminophene powder is uniformly coated with hydroxypropyl cellulose, and a water-soluble polymer coated acetaminophene powder with excellent moldability can be obtained. It has been discovered that when aminophen powder is mixed with tablet material and the mixture is compressed using a dry direct compression method, tablets with good compressibility and excellent properties such as compression moldability and hardness can be obtained. However, the present invention has been completed. The present invention will be explained in more detail below. In the method for manufacturing tablets according to the present invention, a 1 to 15% concentration hydroxypropylcellulose aqueous solution is applied to the surface of acetaminophen powder so that the amount of hydroxypropylcellulose is equal to the amount of acetaminophen powder.
Spray coating to 0.1-5%,
This is dried to obtain hydroxypropyl cellulose-coated acetaminophene powder, and the tablet material mixed with this coated acetaminophen powder is compressed by a dry direct compression method to obtain acetaminophen-containing tablets. In addition, as mentioned above, the aqueous solution of hydroxypropyl cellulose needs to have a concentration of hydroxypropyl cellulose of 1 to 15%, and if the concentration is lower than 1%, a long spraying time and drying time are required. Manufacturing efficiency is reduced and costs are also increased. 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 will occur, so it must be crushed. A process is required to
Therefore, the manufacturing process becomes complicated and it becomes difficult to obtain tablets of uniform quality. In addition, the more preferable concentration of hydroxypropylcellulose is 1 to
It is 5%. In the present invention, the aqueous solution of hydroxypropylcellulose described above is sprayed onto acetaminophene powder, and the surface of the acetaminophene powder is coated with hydroxypropylcellulose. In this case, the average particle size of the acetaminophene powder is preferably 150μ to 840μ. As mentioned above, the amount of hydroxypropylcellulose coated on the acetaminophene powder needs to be 0.1 to 5% relative to the acetaminophen powder, and if the coating amount is less than 0.1%, the moldability of the powder will improve. No, 5%
If the amount is larger than this, the disintegration properties of the tablet will be poor and a large amount of disintegrant will be required, resulting in high cost. In addition,
A more preferable range of coating amount is 1 to 3%. There are no restrictions on the method and conditions for spraying the acetaminophene powder with an aqueous hydroxypropyl cellulose solution and drying it, and any known spraying, drying method, or conditions may be used. In the present invention, the hydroxypropylcellulose-coated acetaminophene powder is mixed with other tablet materials, and tablets are manufactured using the same by a dry direct compression method using conventional equipment and methods. In this case, there are no limitations on other ingredients of the tablet material;
Excipients, disintegrants, lubricants, active ingredients, etc. can be added as appropriate. Effects of the Invention As explained above, according to the tablet manufacturing method of the present invention, even if the tablet material contains acetaminophen powder with poor moldability, the surface of the acetaminophen powder has hydroxypropyl cellulose. The coating improves its moldability,
Therefore, it is possible to obtain acetaminophene-containing tablets that have excellent tabletability and good properties such as compression moldability and hardness. Moreover, according to the present invention, even if only a small amount of hydroxypropylcellulose (binder) is used, the surface of the acetaminophene powder can be uniformly coated with hydroxypropylcellulose, which eliminates the high cost associated with using a large amount of binder and the coating process. Problems such as variations in tablet quality due to non-uniformity 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] 3 kg of acetaminophene powder was placed in a fluidized bed granulator with a capacity of 5, and hydroxypropylcellulose (HPC) was added to it at the concentration shown in Table 1 in 1 part of water. The aqueous solution dissolved in
Acetaminophene powders A to E (products of the present invention) each coated with hydroxypropylcellulose by spray coating under the conditions of ℃
I got it. The amount of hydroxypropylcellulose coated on the acetaminophene powder is shown in Table 1.

[Table] Next, each of the above powders A to E was uniformly mixed with the following components to obtain each tablet material, and this material was compressed by a dry direct tableting method to form the tablets of Examples 1 to 5. The hardness and capping rate of these tablets were examined using the following method. In addition, for comparison, Examples 1 to 3 were used except that the acetaminophene powder was not coated with hydroxypropyl cellulose, and the hydroxypropyl cellulose powder was simply mixed with the acetaminophene powder in the amount shown in Table 2.
Tablets of Comparative Examples 1 to 5 were manufactured in the same manner as in Example 5, and the tablet hardness and capping ratio were similarly examined. Furthermore, control tablets were produced in the same manner, in which hydroxypropyl cellulose was not coated with acetaminophene powder, and in which this was not mixed.
Similar measurements were made. The results are shown in Table 2. Ingredients Acetaminophen + 29.3% Hydroxypropyl cellulose aspirin 47.9〃 Caffeine 11.5〃 Magnesium stearate 0.2〃 Corn starch 11.1〃 Total 100.0〃 Hardness/capping rate measurement method (1) Hardness: Tablet breaking strength measuring device (2) Capping rate: Tablet Friability tester, 10 pieces,
5 minutes

[Example 6]

3 kg of acetaminophene powder was placed in a fluidized bed granulator with a capacity of 5, and an aqueous solution of 60 g of hydroxypropyl cellulose dissolved in 1 part of water (hydroxypropyl cellulose concentration: 6%) was added at an intake temperature of 70°C and an exhaust temperature of 50°C. Spray coating at ℃ condition, 2% based on the weight of acetaminophene
A powder coated with hydroxypropylcellulose was obtained. Next, 1.53 kg of the above powder, 2.5 kg of aspirin, 0.6 kg of caffeine, 0.58 kg of excipients such as starch, and 0.01 kg of magnesium stearate were uniformly mixed to obtain a tablet material, and this material was directly compressed into tablets using a dry method. Tablets were manufactured by compression method. The tablet of Example 6 had excellent compression moldability and moderate hardness. Next, an experimental example will be shown in which the effect of using hydroxypropyl cellulose as a water-soluble polymer material for coating acetaminophene powder is compared with that of using other water-soluble polymer materials. [Experimental example] 3 kg of acetaminophene powder (average particle size 500 μm) was placed in a fluidized granulator with a capacity of 5, and various water-soluble polymers shown in Table 3 were added to it in the same manner as in Examples 1 to 5. substance to acetaminophen
The 0.1 to 5% sprayed mixture was mixed with the following ingredients, and this was compressed into tablets with a diameter of 11 mm and a compression pressure of 1.5 tons, and the hardness and capping rate of the resulting tablets were measured in the same manner as in Examples 1 to 5. . The results are shown in Table 3. Ingredients Acetaminophene + 30% Water-soluble polymeric substance anhydrous caffeine 10〃 Crystalline cellulose 44〃 Corn starch 15〃 Magnesium stearate 1〃 Total 100.0%

【table】

[Table] As is clear from the results in Table 3, among the water-soluble polymeric substances used to coat acetaminophene, hydroxypropyl cellulose has the most remarkable effect in terms of capping incidence and hardness of acetaminophene-containing tablets. It is recognized that On the other hand, other water-soluble polymer substances have no effect at low coating amounts, and increasing the coating amount reduces the occurrence of capping. , it is necessary to prepare an aqueous solution of a water-soluble polymer substance with a high concentration and therefore a high viscosity, which may cause problems in terms of spray operability, etc., and in practice, it is difficult to adjust the water solubility at a high concentration (especially gum arabic and sodium carboxymethylcellulose). It is also conceivable to repeat coatings using aqueous solutions of low concentration and therefore low viscosity, but this method increases production time and costs. Note that gelatin is temperature-dependent, and if it is kept in a high-temperature solution for a long time, it will hydrolyze and gelatinize when cooled, making it impossible to perform reliable film coating, which is not practical. Therefore, hydroxypropylcellulose is found to be most suitable.

Claims (1)

[Claims] 1 Spray coat an aqueous solution of hydroxypropyl cellulose with a concentration of 1 to 15% by weight on the surface of acetaminophene powder so that the amount of hydroxypropylcellulose is 0.1 to 5% by weight of the amount of acetaminophene powder, and dry it to coat the surface of the acetaminophene powder. A method for producing an acetaminophene-containing tablet, which comprises obtaining a propylcellulose-coated acetaminophene powder and compressing a tablet material mixed with the coated acetaminophene powder by a dry direct compression method to obtain a tablet.