JP2010270111A - Arginine-containing tablet - Google Patents

Abstract

A high-dose arginine-containing tablet with suppressed cracking and disintegration is provided.
A tablet having an arginine content of 16.9% by mass or more in the tablet, comprising 0.3 parts by mass or more of a hydrophobic substance with respect to 1 part by mass of arginine.
[Selection] Figure 1

Description

  The present invention relates to a tablet containing arginine and is used in the fields of food, pharmaceuticals and quasi drugs.

  Arginine is commercially available as a supplement and the like because it has the effect of increasing basal metabolism such as promoting growth hormone secretion and improving blood flow. The commercially available arginine preparations are mainly capsules and granules, but there are problems as described below in order to ingest an amount that can be expected to be effective with capsules and granules. That is, since the capsules have not undergone the compression process, a large amount of large capsules must be ingested, the granules are worried about the taste and smell of arginine, and the packaging is costly. . It is therefore desirable to provide tablets containing high doses of arginine.

  Until now, there have been reports on tablets containing arginine, but the content of arginine is almost 10% by mass or less (see Patent Documents 1 to 4), and higher dose arginine-containing tablets are available. It has been demanded.

JP 2007-1873 A JP 2007-197378 A WO 2004/078171 JP 2005-298373 A

  The present inventors have newly discovered that when an arginine-containing tablet contains a certain amount or more of arginine relative to the tablet, the tablet will crack or disintegrate under humidified conditions. The subject of this invention is providing the arginine containing tablet which suppressed the said crack and disintegration.

  As a result of various studies, the present inventors have found that arginine-containing tablets containing a hydrophobic substance of 0.3 parts by mass or more with respect to 1 part by mass of arginine are free from cracks and collapse and can solve the problem. The headline and the present invention were completed.

That is, the present invention
(1) A tablet having an arginine content of 16.9% by mass or more in the tablet, comprising 0.3 part by mass or more of a hydrophobic substance with respect to 1 part by mass of arginine.
(2) The tablet according to (1) above, wherein the hydrophobic substance is hydrogenated oil.
(3) The tablet according to (1) or (2) above, which is not coated.
(4) The arginine content in the tablet is 16.9, characterized by including a step of kneading and granulating a powder containing a hydrophobic substance of 0.3 part by mass or more with respect to 1 part by mass of arginine. The manufacturing method of the tablet which is the mass% or more.
(5) The method for producing a tablet according to the above (4), wherein the hydrophobic substance is hydrogenated oil.
(6) The method for producing a tablet according to the above (4) or (5), wherein no coating is applied.
It is.

  According to the present invention, a high-dose arginine-containing tablet without cracking and disintegration can be produced.

It is the photograph after preserve | saving for 5 hours on 25 degreeC60% RH conditions of the tablet manufactured in Example 1. FIG. It is a photograph immediately after manufacture of the tablet manufactured in Reference Example 4. It is the photograph after preserve | saving for 3 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 1. It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 2. It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 3. It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 4. It is a photograph immediately after manufacture of the tablet manufactured in Example 1. FIG. It is a photograph immediately after manufacture of the tablet manufactured in Comparative Example 1. It is the photograph after preserve | saving for 5 hours on 25 degreeC60% RH conditions of the tablet manufactured in the comparative example 1.

  In the present invention, arginine is preferably L-form arginine and may take the form of a salt. The arginine salt is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include hydrochloride, glutamate, and citrate. In the present invention, when an arginine salt is used, the content of arginine in the tablet is an amount converted to free arginine.

  Hydrophobic substances include, for example, hardened oils such as paraffin, hardened castor oil, hardened rapeseed oil, hardened cottonseed oil, higher fatty acids such as triglyceride, monoglyceride, stearic acid, higher fatty alcohols such as stearyl alcohol, carnauba wax, tetraglycerin penta Examples include stearate, polyglycerol fatty acid esters of tetraglycerol hexabehenate, and the like. Of these, hardened oil is preferable, and hardened castor oil is more preferable. As a commercially available product of the hardened oil, for example, a love wax (registered trademark, manufactured by Freund Sangyo Co., Ltd.) can be used.

  Kneading granulation is a method in which liquid or paste is added to powder to be mixed and granulated while kneading.

  Coating is to form and coat various substances on the surface of tablets and granules, preventing bad taste and odor, ensuring stability from external conditions such as water, light, oxygen, intestines, etc. It is applied for the purpose of imparting functions such as solubility and sustained release. In addition, although the tablet of this invention and the granulated product in the middle of the manufacture are not cracked and disintegrated even if it is not coated, the coating is not prevented. For example, it is effective to coat the tablet of the present invention when a component having bad taste or bad odor is blended or when a component unstable to water, light, oxygen or the like is blended.

  Tablet cracking and disintegration refers to a state in which the tablet surface or edge portion tears and collapses so as to peel off from the tablet surface. A photograph of an example of a tablet in which cracks and collapse occurred is shown in the drawing. The crack of a tablet is the state of FIG. 4 and FIG. 9, and the disintegration of a tablet is the state of FIG. 5 and FIG. It is considered that cracking and disintegration of the tablet occurs when arginine absorbs water and swells.

  An excipient can be blended in the arginine-containing tablet of the present invention. Examples of the excipient include lactose, starch, corn starch, crystalline cellulose, reduced maltose starch syrup, trehalose, sugar, glucose, calcium hydrogen phosphate, light anhydrous silicic acid and the like. These excipients can be used alone or in combination.

  Furthermore, the tablet of the present invention may contain a conventional additive. Examples of the additive include a binder, a disintegrant, a lubricant, and a flavoring agent. These additives can be used alone or as a mixture.

Examples of the binder include methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinyl pyrrolidone, and pullulan. Examples of the disintegrant include carboxymethyl cellulose calcium, croscarmellose sodium, low-substituted hydroxypropyl cellulose, crospovidone, carmellose calcium, carboxymethyl starch sodium, and partially pregelatinized starch.
Examples of the lubricant include stearic acid and its metal salt, talc, and sucrose fatty acid ester. Examples of the flavoring agent include sweeteners (eg, artificial sweeteners such as aspartame, acesulfame K, stevia, sucralose, sodium saccharin, dipotassium glycyrrhizin, etc.).

  Furthermore, generally used components such as various amino acids and salts thereof, various vitamins, other herbal medicines and herbal extracts can be blended in the present invention.

  Hereinafter, the present invention will be described in detail with reference examples, examples, comparative examples, and test examples.

Reference Examples 1-4
The following operations were performed to produce tablets of Reference Examples 1 to 4 so that the composition ratio shown in Table 1 was obtained.
L arginine, reduced maltose starch syrup, hydroxypropyl cellulose, light anhydrous silicic acid, and calcium stearate were weighed, mixed and pulverized, and then tableted with a tableting machine to produce tablets each having a mass of 370 mg. All the units in the table are mass%.

Example 1 and Comparative Example 1
The following operations were performed to produce tablets of Example 1 and Comparative Example 1 so that the composition ratio shown in Table 2 was obtained.

Larginine and hydrogenated oil were weighed, mixed and pulverized, hydroxypropylcellulose was dissolved in purified water, and a solution with a hydroxypropylcellulose concentration of 6.0% was used as a binding solution, kneading granulator Was granulated and dried to obtain a granulated product. Koujin extract powder, Hongjing heaven extract powder, black pepper extract, vitamin B ₆ , zinc-containing yeast, crystalline cellulose, carboxymethylcellulose calcium, light anhydrous silicic acid, calcium stearate, weighed, mixed and crushed, The mixture was mixed with the granulated product, and tableted with a tableting machine to produce tablets with a tablet mass of 360 mg. All the units in the table are mass%.

Test Example The tablets produced in Reference Examples 1, 2, 3, 4 and Example 1 and Comparative Example 1 were used as test samples.
The test sample was stored for an arbitrary time under conditions of 25 ° C. and 60% RH, and then the appearance change of the test sample was evaluated. The test results are shown in Tables 3 and 4. Moreover, the typical photograph about each tablet was shown in FIGS.

The evaluation results in the table are as follows.
0: No change 1: Crack in tablet 2: Disintegration of tablet

  From the reference example, the change in the appearance of the test sample under the condition of 25 ° C. and 60% RH depends on the content of L arginine. Therefore, the present invention is particularly effective when arginine is contained in an amount of 16.9% by mass or more based on the tablet. Note that the present invention can be applied to tablets having an arginine content of less than 16.9% by mass in order to suppress water absorption and swelling of arginine.

  When the appearance change of the test sample obtained in Example 1 under conditions of 25 ° C. and 60% RH was evaluated, it was confirmed that the tablet was stable without cracking or disintegrating. When the appearance change of the test sample obtained in Comparative Example 1 under the conditions of 25 ° C. and 60% RH was evaluated, it was confirmed that cracks occurred on the side surface of the tablet.

  From the above results, if the content of hydrogenated oil is 0.3 parts by mass with respect to 1 part by mass of L-arginine, it is stable under conditions of 25 ° C. and 60% RH even when the content of L-arginine is 55.6% by mass. Could provide a good tablet.

  The arginine-containing tablet of the present invention can be used as food, pharmaceuticals, quasi drugs and the like.

Claims (6)

A tablet having an arginine content of 16.9% by mass or more in the tablet, comprising 0.3 parts by mass or more of a hydrophobic substance with respect to 1 part by mass of arginine. The tablet according to claim 1, wherein the hydrophobic substance is hydrogenated oil. The tablet according to claim 1 or 2, wherein the tablet is not coated. The content of arginine in the tablet is 16.9% by mass or more, comprising a step of kneading and granulating a powder containing a hydrophobic substance of 0.3 part by mass or more with respect to 1 part by mass of arginine The manufacturing method of the tablet which is. The method for producing a tablet according to claim 4, wherein the hydrophobic substance is hydrogenated oil. The method for producing a tablet according to claim 4 or 5, wherein no coating is applied.

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