Medicinal tablets

Abstract

To provide a medicinal tablet that minimizes changes in appearance, bitterness, and odor, while maintaining high palatability and convenience, without complicating the manufacturing process or reducing productivity. [Solution] The pharmaceutical tablet of this embodiment contains ibuprofen, amino acids selected from amino acids or their salts, and polyvinyl alcohols. The pharmaceutical tablet of this embodiment has the following composition when the ratio of ibuprofen is (A), the ratio of amino acids is (B), and the ratio of polyvinyl alcohols is (C): A:B:C = 100:30~231:2~93.

Description

Technical Field

[0001] This embodiment relates to a pharmaceutical tablet containing ibuprofen.

Background Art

[0002] Ibuprofen, which is used as an antipyretic and analgesic component, has a characteristic bitterness and odor. Therefore, pharmaceutical tablets containing ibuprofen as a main component contain additives for reducing the characteristic bitterness and odor. In addition, pharmaceutical tablets obtained by adding amino acids to ibuprofen have the characteristic that the appearance of the tablets changes over time, such as discoloration. Therefore, in order to reduce the change in appearance, it is known to coat the surface of the tablets with various materials (see Patent Documents 1 and 2).

[0003] However, when various additives are added to tablets in order to reduce bitterness and odor or reduce changes in appearance, the tablets become larger and the number of tablets to be taken increases. Therefore, there is a problem that the convenience decreases, such as a decrease in the ease of taking. In addition, when the surface of the tablets is coated in order to reduce the change in the appearance of the tablets, an additional process is required, resulting in a problem of complication of the working process and a decrease in productivity.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0005] Therefore, an object of the present invention is to provide a pharmaceutical tablet that suppresses the effects of changes in appearance, bitterness, and odor without causing complication of the working process and a decrease in productivity, and has high ease of taking and convenience.

Means for Solving the Problems

[0006] To solve the above problems, the pharmaceutical tablet of this embodiment contains ibuprofen, amino acids selected from amino acids or their salts, and polyvinyl alcohols. Furthermore, when the proportion of ibuprofen in the pharmaceutical tablet of this embodiment is (A), the proportion of the amino acids is (B), and the proportion of the polyvinyl alcohols is (C), A:B:C = 100:30~231:2~93.

[0007] The inventors of this invention have discovered that by adding polyvinyl alcohols in addition to amino acids to a pharmaceutical tablet containing ibuprofen as the main ingredient, changes in appearance, bitterness, and odor can be suppressed. In other words, in this embodiment, the properties of the pharmaceutical tablet can be changed by adding polyvinyl alcohols without requiring additional work processes. Therefore, changes in appearance, bitterness, and odor can be suppressed without complicating the work process or reducing productivity, thereby improving palatability and convenience. [Brief explanation of the drawing]

[0008] [Figure 1] A schematic diagram showing the composition and evaluation results of an example of a pharmaceutical tablet according to one embodiment. [Figure 2] A schematic diagram showing the composition and evaluation results of examples and comparative examples of pharmaceutical tablets according to one embodiment. [Modes for carrying out the invention]

[0009] The pharmaceutical tablets of this embodiment will be described below. The pharmaceutical tablets of this embodiment contain ibuprofen, amino acids, and polyvinyl alcohols. Ibuprofen is the main ingredient that exerts the efficacy of the pharmaceutical tablets. The amino acids are not limited to individual amino acids, but may also be salts of amino acids with alkali metals or alkaline earth metals. In the pharmaceutical tablets of this embodiment, the amino acids are selected from glycine, aspartic acid, or arginine. In this case, the amino acids may be individual glycine, aspartic acid, or arginine, or salts of glycine, aspartic acid, or arginine. The polyvinyl alcohols are additives of this embodiment and are selected from either polyvinyl alcohol or polyvinyl alcohol-acrylic acid-methyl methacrylate copolymer. The degree of saponification of the polyvinyl alcohol is arbitrary and may be fully saponified or partially saponified.

[0010] In this embodiment, when the ratio of ibuprofen is (A), the ratio of amino acids is (B), and the ratio of polyvinyl alcohols is (C), A:B:C = 100:30~231:2~93 Thus, in this embodiment, the main components, ibuprofen, amino acids, and polyvinyl alcohols, are blended in a predetermined ratio. The blending ratio is determined based on the mass of each component.

[0011] In addition to the above, the pharmaceutical tablets of this embodiment may also contain a cellulose derivative. The cellulose derivative is an additive of this embodiment and is selected from either low-substituted hydroxypropyl cellulose or crystalline cellulose. The cellulose derivative preferably has an average particle size of 20 μm or less. When a cellulose derivative is added to the pharmaceutical tablets of this embodiment, when the blending ratio of the cellulose derivative is (D), A:B:C:D = 100:30~231:2~93:5~74 Thus, in this embodiment, when a cellulose derivative is added to the main components, the blending ratios of ibuprofen, amino acids, polyvinyl alcohols, and cellulose derivatives are set within a predetermined range.

[0012] In addition to the above, the pharmaceutical tablets of this embodiment may contain, as needed, one or more of the following: other active ingredients, appropriate amounts of excipients, binders, disintegrants, lubricants, colorants, flavoring agents, and fragrances. Other active ingredients may include, for example, antipyretic and analgesic components, hypnotic and sedative components, vitamins, amino acids, gastric mucosal protective components, caffeine, and antacids.

[0013] (Examples and Comparative Examples) The pharmaceutical tablets of this embodiment will be described in detail below based on the examples and comparative examples shown in Figures 1 and 2. First, the method for preparing the pharmaceutical tablets of this embodiment will be described. The samples for the examples and comparative examples were weighed so that the total mass of each component was 300 g. At this time, the mixing ratios of the components constituting each sample for the examples and comparative examples are as shown in Figures 1 and 2. These mixing ratios shown in Figures 1 and 2 are based on mass, with ibuprofen set to 100.

[0014] Each weighed component was mixed in a mixer as part of the mixing process. However, magnesium stearate, one of the components, was not mixed during this process. The mixed mixture was then mixed with a granulation solvent and kneaded in a stirring mixer as part of the stirring process. A mixture of ethanol and water was used as the granulation solvent. However, this granulation solvent is not limited to a mixture of ethanol and water; any substance that does not impair the effectiveness of the pharmaceutical tablets in this embodiment can be arbitrarily selected.

[0015] The granules produced by adding a granulation solvent were dried in a dryer as a drying step. The dried granules were then compressed into tablets by adding magnesium stearate as a tablet powder production step. The resulting tablet powder was then compressed using a rotary tablet press. In this case, the punch shape of the tablet press had either a curved or flat surface. The mass of the pharmaceutical tablets compressed ranged from 140 mg to 420 mg. The diameter of the rotary tablet press punch was 7 mm to 10 mm. The rotation speed of the rotary tablet press was set to 30 rpm to 40 rpm.

[0016] The obtained examples and comparative examples were evaluated for changes in appearance and the presence or absence of unpleasant odors under pre-set test conditions. For the evaluation of changes in appearance, the samples were placed in glass bottles, which were left unsealed and exposed to the atmosphere. The test environment for storing the glass bottles was set to a temperature of 40°C and a relative humidity (RH) of 75%. The changes in appearance were visually inspected after 30 days under these test conditions. For the evaluation of unpleasant odors, the samples were placed in glass bottles, which were sealed with lids. The test environment for storing the glass bottles was set to a temperature of 50°C without humidity control. The unpleasant odors were evaluated by olfactorily detecting the smell immediately after opening the glass bottle lids after 30 days under these test conditions.

[0017] Changes in appearance were evaluated by assessing the presence or absence of spots on the sample as "spots," and the presence or absence of browning due to discoloration of the sample as "browning." In the evaluation of "spots," samples without visible spots were evaluated as "S." Samples with visible spots that did not impair the value as a product were evaluated as "A." On the other hand, samples with spots that impaired the value as a product were evaluated as "B." Samples with particularly severe spots were evaluated as "C."

[0018] In the evaluation of "browning", samples with no visible browning were evaluated as "S". Samples with browning that was visible but did not impair the value as a product were evaluated as "A". On the other hand, samples with browning that impaired the value as a product were evaluated as "B". In particular, samples with significant browning were evaluated as "C".

[0019] The unpleasant odor was sensorially evaluated as the odor immediately after opening the lid of the glass bottle as described above. In this evaluation of "unpleasant odor", samples with almost no unpleasant odor were evaluated as "S". Samples with an odor that was felt but did not impair the value as a product were evaluated as "A". On the other hand, samples with an unpleasant odor that impaired the value as a product were evaluated as "B". In particular, samples with a significant unpleasant odor were evaluated as "C". In the above evaluation, "S" or "A" is a pass, and "B" or "C" is a fail.

[0020] Examples 1 to 12 contain polyvinyl alcohols and cellulose derivatives as additives in addition to ibuprofen and amino acids. Specifically, Examples 1 to 12 contain glycine as amino acids, a partially saponified polyvinyl alcohol as polyvinyl alcohols, and low-substituted hydroxypropyl cellulose with an average particle size of 20 μm as cellulose derivatives. It can be seen that none of these Examples 1 to 12 have changes in appearance such as spots and browning. Also, in Examples 1 to 12, the evaluation of "unpleasant odor" is "S" or "A". In Example 7 where the blending ratio of the added polyvinyl alcohols is small, the evaluation of "unpleasant odor" is "A". From this, it can be seen that polyvinyl alcohols contribute to the reduction of unpleasant odor.

[0021] Example 13 contains aspartic acid as an amino acid, and Example 14 contains arginine as an amino acid. In both Examples 13 and 14, it can be seen that no changes in appearance such as spots or browning occurred due to the inclusion of polyvinyl alcohols. Furthermore, Example 13 received an "S" rating for "unpleasant odor," and Example 14 received an "A" rating for "unpleasant odor."

[0022] Example 15 contains fully saponified polyvinyl alcohol as the polyvinyl alcohol, and Example 16 contains a polyvinyl alcohol-acrylic acid-methyl methacrylate copolymer as the polyvinyl alcohol. In Examples 15 and 16, it can be seen that when fully saponified polyvinyl alcohol is used instead of partially saponified polyvinyl alcohol, and when copolymer is used, no changes in appearance such as spots and browning occur, or the changes in appearance are small. Furthermore, Example 15 received an "A" rating for "unpleasant odor," and Example 16 received an "S" rating for "unpleasant odor." From these results, it can be seen that the type of polyvinyl alcohol has little effect on unpleasant odor.

[0023] Example 17 does not contain a cellulose derivative. Example 17 received an "A" rating for "browning." That is, although Example 17 showed slight browning, it was not enough to affect its commercial value. This also indicates that polyvinyl alcohols in the pharmaceutical tablets of this embodiment contribute to suppressing changes in appearance, such as spotting and browning. Furthermore, Example 17 received an "S" rating for "unpleasant odor." These results indicate that the addition of a cellulose derivative is effective in improving appearance, particularly reducing browning.

[0024] Examples 18 to 20 differ in the type of cellulose derivative and the average particle size. In Examples 18 and 20, the average particle size of the cellulose derivative was relatively large at 55 μm, resulting in a "browning" rating of "A". In other words, although slight browning occurred in Examples 18 and 20, it did not affect the commercial value. On the other hand, Example 19, in which the average particle size of the cellulose derivative was relatively small at 20 μm, received a "browning" rating of "S". From these results, it can be seen that, when adding a cellulose derivative to the pharmaceutical tablets of this embodiment, it is preferable to have a smaller average particle size, regardless of the type of cellulose derivative. In addition, all of Examples 18 to 20 received an "unpleasant odor" rating of "S".

[0025] Comparative Examples 1 to 4 do not contain polyvinyl alcohols. In all of these Comparative Examples 1 to 4, at least one of the following changes in appearance, namely spotting or browning, occurred, along with an unpleasant odor. From these findings, it is clear that spotting, browning, and unpleasant odor can be improved by adding polyvinyl alcohols, as in this embodiment. In addition, Comparative Examples 3 and 4 have citric acid or xylitol added as a flavoring agent instead of amino acids. Comparative Examples 3 and 4, with these flavoring agents added, also exhibited browning and an unpleasant odor. Including these findings, it is clear that the polyvinyl alcohols, which are additives in this embodiment, contribute to reducing spotting, browning, and unpleasant odor in the mixture of ibuprofen and amino acids.

[0026] The pharmaceutical tablets of this embodiment, as described above, have polyvinyl alcohols added. As a result, the pharmaceutical tablets of this embodiment have reduced changes in appearance and the generation of unpleasant odors. Therefore, it is unnecessary to add various additives to suppress changes in appearance or the generation of unpleasant odors. In addition to the addition of additives, surface coating of the tablets is also unnecessary. As a result, the pharmaceutical tablets of this embodiment do not result in increased tablet size or an increase in the number of tablets to be taken due to an increase in additives, and additional processes such as coating are unnecessary. Therefore, it is possible to improve ease of administration and convenience while suppressing changes in appearance, bitterness and odor, and ensuring the effect of ibuprofen, without complicating the work process or decreasing productivity.

[0027] The present invention described above is not limited to the embodiments described above, and can be applied to various embodiments without departing from the spirit of the invention.

Claims

1. Ibuprofen and, amino acids selected from amino acids or their salts, A pharmaceutical tablet containing polyvinyl alcohols, When the ratio of ibuprofen is (A), the ratio of amino acids is (B), and the ratio of polyvinyl alcohols is (C), A:B:C = 100:30 to 231:2 to 93. Medicinal tablets.

2. The aforementioned amino acids are selected from glycine, aspartic acid, or arginine. A pharmaceutical tablet according to claim 1.

3. The polyvinyl alcohols are selected from either polyvinyl alcohol or polyvinyl alcohol-acrylic acid-methyl methacrylate copolymer. A pharmaceutical tablet according to claim 1.

4. It further contains a cellulose derivative, When the blending ratio of the cellulose derivative is (D), A:B:C:D = 100:30 to 231:2 to 93:5 to 74. A pharmaceutical tablet according to any one of claims 1 to 3.

5. The cellulose derivative has an average particle diameter of 20 μm or less. A pharmaceutical tablet according to claim 4.

6. The cellulose derivative is selected from either low-substituted hydroxypropyl cellulose or crystalline cellulose. A pharmaceutical tablet according to claim 4.

7. The cellulose derivative is selected from either low-substituted hydroxypropyl cellulose or crystalline cellulose. A pharmaceutical tablet according to claim 5.

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