JP5476782B2 - Method for producing arginine-containing tablets - Google Patents

Method for producing arginine-containing tablets Download PDF

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JP5476782B2
JP5476782B2 JP2009102614A JP2009102614A JP5476782B2 JP 5476782 B2 JP5476782 B2 JP 5476782B2 JP 2009102614 A JP2009102614 A JP 2009102614A JP 2009102614 A JP2009102614 A JP 2009102614A JP 5476782 B2 JP5476782 B2 JP 5476782B2
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玄 奥平
義洋 佃
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Taisho Pharmaceutical Co Ltd
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Description

本発明は、アルギニンを含有した錠剤の製造方法に関し、食品、医薬品、医薬部外品の分野において利用される。   The present invention relates to a method for producing a tablet containing arginine and is used in the fields of foods, pharmaceuticals and quasi drugs.

アルギニンは、成長ホルモン分泌促進、血流改善等、基礎代謝を上昇させる効果を有していることから、サプリメント等として市販されている。市販されているアルギニン製剤は、カプセル剤や粒剤が主であるが、効果の期待できる量をカプセル剤や粒剤で摂取するには以下の通り、問題点を有している。すなわち、カプセル剤では圧縮工程を経ていないので、大きいカプセルを多量に摂取しなければならない点、粒剤ではアルギニンの味、臭いが気になる点、また包装にコストがかかる点等が問題となる。従ってアルギニンを含有する錠剤の提供が望まれている。   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. . Accordingly, it is desired to provide tablets containing arginine.

これまでにアルギニンを含有する錠剤については報告例があるが、コーティングを施している例がほとんどである(特許文献1〜4参照)。この理由の1つとして考えられるのが、アルギニンの吸水性である。アルギニンは吸水し膨潤する性質を有するので、吸水を避けるため、コーティング層を有する錠剤が多く報告されていると考えられる。しかしながら、コーティングには、悪味および悪臭の防止、水、光、酸素などの外的条件からの安定性確保等の利点がある一方で、長い製造時間に伴う製造コストの増加という問題点もあり、必要性に乏しければ錠剤に対してコーティングを施さない方が好ましい。   There have been reported examples of tablets containing arginine so far, but most of them have been coated (see Patent Documents 1 to 4). One possible reason is the water absorption of arginine. Since arginine absorbs water and swells, it is considered that many tablets having a coating layer have been reported to avoid water absorption. However, the coating has advantages such as prevention of bad taste and bad odor, ensuring stability from external conditions such as water, light, oxygen, etc., but also has the problem of increased production cost due to long production time. If there is little necessity, it is preferable not to coat the tablet.

特開2007−1873号公報JP 2007-1873 A 特開2007−197378号公報JP 2007-197378 A WO2004/078171号公報WO 2004/078171 特開2005−298373号公報JP 2005-298373 A

本発明者らは、アルギニン含有錠剤において、錠剤に対して一定量以上のアルギニンを含有させると、加湿条件下において錠剤に亀裂や崩壊が発生することを新たに発見した。本発明の課題は前記亀裂及び崩壊を抑制したアルギニン含有錠剤を提供することである。   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.

本発明者らは、種々検討した結果、水分を含んだアルギニンを含有する打錠用粉体を打錠してアルギニン含有錠剤を得ることで、コーティングを施さなくとも亀裂及び崩壊が発生せず、課題が解決できることを見出し、本発明を完成した。   As a result of various studies, the inventors obtained tablets for tableting containing tableted arginine containing moisture to obtain arginine-containing tablets, so that cracks and disintegration did not occur even without coating, The present invention has been completed by finding out that the problems can be solved.

すなわち、本発明は、
(1)水分を含んだアルギニンを含有する打錠用粉体を打錠することを特徴とする、アルギニンの膨潤に起因する錠剤の亀裂及び崩壊を抑制したアルギニン含有錠剤の製造方法。
(2)水分を含んだアルギニンを含有する打錠用粉体が、アルギニンを含有する粉体を湿式造粒して得られる造粒物を含有する粉体である上記(1)に記載のアルギニン含有錠剤の製造方法。
(3)アルギニンを含有する粉体を湿式造粒して得られる造粒物中の水分含有量が2.7質量%以上であることを特徴とする上記(2)に記載のアルギニン含有錠剤の製造方法。
(4)コーティングを施さないことを特徴とする上記(1)〜(3)のいずれか1項に記載のアルギニン含有錠剤の製造方法。
(5)アルギニンの含有量が、錠剤に対して16.9質量%以上であることを特徴とする上記(1)〜(4)のいずれか1項に記載のアルギニン含有錠剤の製造方法。
である。
That is, the present invention
(1) A method for producing an arginine-containing tablet that suppresses cracking and disintegration of the tablet due to swelling of arginine, wherein the tableting powder containing water-containing arginine is tableted.
(2) Arginine according to (1) above, wherein the tableting powder containing water-containing arginine is a powder containing a granulated product obtained by wet granulation of a powder containing arginine. Manufacturing method of containing tablet.
(3) The arginine-containing tablet according to (2) above, wherein the water content in the granulated product obtained by wet granulation of the powder containing arginine is 2.7% by mass or more. Production method.
(4) The method for producing an arginine-containing tablet according to any one of (1) to (3) above, wherein the coating is not applied.
(5) Content of arginine is 16.9 mass% or more with respect to a tablet, The manufacturing method of the arginine containing tablet of any one of said (1)-(4) characterized by the above-mentioned.
It is.

本発明により、コーティングを施さなくとも、亀裂及び崩壊の見られないアルギニン含有錠剤が製造できる。   According to the present invention, an arginine-containing tablet without cracking and disintegration can be produced without coating.

実施例1で製造した錠剤の、25℃60%RHの条件下にて3時間保存した後の写真である。It is the photograph after preserve | saving for 3 hours on 25 degreeC60% RH conditions of the tablet manufactured in Example 1. FIG. 参考例4で製造した錠剤の製造直後の写真である。It is a photograph immediately after manufacture of the tablet manufactured in Reference Example 4. 参考例1で製造した錠剤の、25℃60%RHの条件下にて3時間保存した後の写真である。It is the photograph after preserve | saving for 3 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 1. 参考例2で製造した錠剤の、25℃60%RHの条件下にて2時間保存した後の写真である。It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 2. 参考例3で製造した錠剤の、25℃60%RHの条件下にて2時間保存した後の写真である。It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 3. 参考例4で製造した錠剤の、25℃60%RHの条件下にて2時間保存した後の写真である。It is the photograph after preserve | saving for 2 hours on 25 degreeC60% RH conditions of the tablet manufactured in Reference Example 4. 実施例1で製造した錠剤の製造直後の写真である。It is a photograph immediately after manufacture of the tablet manufactured in Example 1. FIG. 比較例1で製造した錠剤の製造直後の写真である。It is a photograph immediately after manufacture of the tablet manufactured in Comparative Example 1. 比較例1で製造した錠剤の、25℃60%RHの条件下にて2時間保存した後の写真である。2 is a photograph of the tablet produced in Comparative Example 1 after being stored for 2 hours under conditions of 25 ° C. and 60% RH.

本発明において、アルギニンとは好ましくはL体のアルギニンであり、塩の形態をとっても良い。アルギニンの塩としては製剤学上許容される塩であれば特に限定されないが、例えば塩酸塩、グルタミン酸塩、クエン酸塩等を挙げることができる。本発明においてアルギニンの塩を使用した場合、錠剤におけるアルギニンの含有量とは、遊離体のアルギニンに換算した量である。   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.

錠剤の亀裂及び崩壊とは、錠剤表面やエッジ部分が裂け、錠剤表面から剥がれ落ちるように崩れていく状態を言う。亀裂及び崩壊が発生した錠剤例の写真を図面に示した。錠剤に亀裂が発生した状態が、図4及び図9に示される状態であり、錠剤の崩壊が発生した状態が、図5及び図6に示される状態である。錠剤の亀裂及び崩壊は、アルギニンが吸水し、膨潤することで発生すると考えられる。   The crack and disintegration of the tablet means a state in which the tablet surface or edge portion is torn and collapses so as to peel off from the tablet surface. A photograph of an example of a tablet in which cracks and collapse have occurred is shown in the drawing. The state in which the crack has occurred in the tablet is the state shown in FIGS. 4 and 9, and the state in which the tablet has collapsed is the state shown in FIGS. 5 and 6. It is considered that cracking and disintegration of the tablet occurs when arginine absorbs water and swells.

「水分を含んだアルギニンを含有する打錠用粉体(以下、打錠用粉体)」は、水分を含んだアルギニンを含有するほか、慣用の賦形剤、添加剤等によって構成され、生薬・ビタミン等の他の有効成分を含有しても良い。また、前記各成分を造粒し、必要に応じて該造粒物にさらに他の慣用成分を添加した粉体も、上記打錠用粉体の範疇に含まれる。さらに、上記打錠用粉体には、アルギニン及び、必要に応じて慣用の賦形剤、添加剤、有効成分等を混合した粉体に対して、水又は水とアルコールの混液(結合剤を溶解させた溶液でも良い)を用いて湿式造粒して得られる造粒物も含まれ、該造粒物にさらに他の慣用成分を添加した粉体も含まれる。すなわち、本発明における「打錠用粉体」中のアルギニンが、打錠する前に、何らかの方法で水分を含み、膨潤していることが重要である。こうすることで、打錠後にさらにアルギニンが吸水したとしても、錠剤の亀裂や崩壊を招くほどの、アルギニンの膨潤を避けることが出来る。   “Powder for tableting containing water-containing arginine (hereinafter referred to as tableting powder)” is composed of conventional excipients, additives, etc. in addition to containing water-containing arginine. -You may contain other active ingredients, such as a vitamin. In addition, powders obtained by granulating each of the above components and adding other conventional components to the granulated product as necessary are also included in the category of the above tableting powders. Further, the tableting powder is prepared by mixing water or a mixture of water and alcohol (with a binder) into a powder in which arginine and, if necessary, conventional excipients, additives, active ingredients and the like are mixed. A granulated product obtained by wet granulation using a dissolved solution may also be included, and a powder obtained by adding other conventional components to the granulated product may also be included. That is, it is important that the arginine in the “tablet powder” in the present invention contains water and swells in some way before tableting. By doing so, even if arginine absorbs more water after tableting, it is possible to avoid swelling of arginine so as to cause cracking or disintegration of the tablet.

本発明において、アルギニンを含有する粉体を湿式造粒して得られる造粒物を使用する場合、アルギニンの含有割合によっても異なってくるが、錠剤の亀裂及び崩壊の抑制の観点から、該造粒物に対して2.7質量%以上の水分を含んでいることが好ましい。水分含有量は造粒時に添加する水の量を制御するか、造粒後の乾燥条件を制御することで、適宜調整することができる。なお、水分量の上限については、打錠の容易性等を勘案して、当業者が適宜決定することができる。   In the present invention, when a granulated product obtained by wet granulation of a powder containing arginine is used, it varies depending on the content of arginine, but from the viewpoint of suppressing cracking and disintegration of tablets, the granulation is performed. It is preferable to contain 2.7% by mass or more of moisture with respect to the granules. The water content can be appropriately adjusted by controlling the amount of water added during granulation or by controlling the drying conditions after granulation. Note that the upper limit of the moisture content can be appropriately determined by those skilled in the art in consideration of ease of tableting and the like.

湿式造粒とは、粉体に溶媒又は、バインダーを含んだ溶液を噴霧し、溶媒を乾燥させることにより粒子同士を凝集させ、粒子を一定の大きさにまで成長させる方法であり、溶媒としては水、アルコールを使用することができる。湿式造粒法には攪拌造粒法、流動層造粒法、練合造粒法等の造粒法が知られており、本発明においては特に流動層造粒法が好ましい。   Wet granulation is a method in which particles or powders are sprayed with a solvent or a solution containing a binder, the particles are aggregated by drying the solvent, and the particles are grown to a certain size. Water and alcohol can be used. As the wet granulation method, granulation methods such as stirring granulation method, fluidized bed granulation method, kneading granulation method and the like are known, and in the present invention, fluidized bed granulation method is particularly preferable.

コーティングを施すとは、錠剤や顆粒の表面に、種々の物質被膜を形成し被覆することであり、悪味および悪臭の防止、水、光、酸素などの外的条件からの安定性確保、腸溶性や徐放性等の機能付与等を目的として施す。なお、本発明の錠剤及びその製造途中の造粒物にはコーティングを施さなくとも錠剤に亀裂及び崩壊が見られないが、コーティングすることを妨げるものではない。例えば、本発明の錠剤に悪味、悪臭を有する成分を配合した場合、又は水、光、酸素等に不安定な成分を配合した場合にコーティングを施すことは有効である。   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.

本発明において、錠剤及び湿式造粒して得られる造粒物の水分含有量は、乾燥減量法(70℃30分)により決定した値を用いる。すなわち、錠剤、造粒物を70℃30分の条件下に置いて、減少した重量から算出した値である。   In the present invention, the value determined by the loss on drying method (70 ° C. for 30 minutes) is used as the water content of the tablet and the granulated product obtained by wet granulation. That is, it is a value calculated from the weight reduced by placing the tablet and granulated product under conditions of 70 ° C. for 30 minutes.

本発明のアルギニン含有錠剤には賦形剤を配合することができる。該賦形剤としては、例えば、乳糖、デンプン、コーンスターチ、結晶セルロース、還元麦芽糖水飴、トレハロース、砂糖、ブドウ糖、リン酸水素カルシウム、軽質無水ケイ酸などが挙げられる。これらの賦形剤は一種又は二種以上使用できる。   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.

更に、本発明の錠剤は、慣用の添加剤を含んでいてもよい。添加剤としては、例えば、結合剤、崩壊剤、滑沢剤、嬌味剤などが挙げられる。該添加剤は単独でも混合物としても用いることができる。   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.

結合剤としては、例えば、メチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ポリビニルピロリドン、プルランなどが挙げられる。崩壊剤としては、例えば、カルボキシメチルセルロースカルシウム、クロスカルメロースナトリウム、低置換度ヒドロキシプロピルセルロース、クロスポビドン、カルメロースカルシウム、カルボキシメチルスターチナトリウム、部分α化デンプンなどが挙げられる。   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.

滑沢剤としては、例えば、ステアリン酸及びその金属塩、タルク、ショ糖脂肪酸エステルなどが挙げられる。嬌味剤としては、例えば、甘味剤(例えば、アスパルテーム、アセスルファムK、ステビア、スクラロース、サッカリンナトリウム、グリチルリチン二カリウムなどの人工甘味料など)などが挙げられる。   Examples of the lubricant include stearic acid and its metal salt, talc, and sucrose fatty acid ester. Examples of the flavoring agent include sweetening agents (eg, artificial sweeteners such as aspartame, acesulfame K, stevia, sucralose, sodium saccharin, dipotassium glycyrrhizin, etc.).

さらに、本発明には、各種アミノ酸及びその塩類、各種ビタミン類、その他の生薬及び生薬抽出物など一般に使用される有効成分を配合することができる。   Furthermore, in the present invention, various commonly used active ingredients such as various amino acids and salts thereof, various vitamins, other crude drugs and herbal extracts can be blended.

以下に参考例、実施例、比較例、及び試験例によって、本発明を詳細に説明する。   Hereinafter, the present invention will be described in detail with reference examples, examples, comparative examples, and test examples.

参考例1〜4
以下の操作を行い、表1に示す組成比になるように参考例1〜4を製造した。
Lアルギニン、還元麦芽糖水飴、ヒドロキシプロピルセルロース、軽質無水ケイ酸、ステアリン酸カルシウムをそれぞれ秤量し、混合、粉砕したものを、打錠機にて打錠し、1錠質量370mgの錠剤を製造した。表中の単位はいずれも質量%である。
Reference Examples 1-4
The following operations were performed to produce 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 units in the table are mass%.

Figure 0005476782
Figure 0005476782

以下の実施例1及び比較例1の配合成分の配合率(質量%)は、水以外の成分の総和を100質量%とした時の配合率である。   The blending ratio (mass%) of the blending components of Example 1 and Comparative Example 1 below is the blending ratio when the sum of components other than water is 100% by weight.

実施例1
Lアルギニン35.0質量%、コウジンエキス末1.6質量%、紅景天エキス末2.1質量%、黒胡椒抽出物0.2質量%、ビタミンB60.3質量%、亜鉛含有酵母8.3質量%、還元麦芽糖水飴11.7質量%、結晶セルロース35.0質量%、軽質無水ケイ酸1.9質量%の組成の粉体を粉砕し、該混合物に、ヒドロキシプロピルセルロース2.0質量%を精製水に溶解してヒドロキシプロピルセルロース濃度を6.0%とした溶液を結合液として、流動層造粒機を用い、造粒後の乾燥時間を制御して、造粒物を得た。該造粒物の水分含有量は、5gの造粒物を用いた乾燥減量法(70℃30分)により決定し、2.73質量%であった。該造粒物に、ステアリン酸カルシウム2.0質量%を混合し、打錠機にて打錠、1錠質量300mgの錠剤を製造した。該錠剤の水分含有量は、5gの錠剤を粉砕した粉末を用いた乾燥減量法(70℃30分)により決定し、2.97質量%であった。
Example 1
L arginine 35.0% by weight, Koujin extract powder 1.6% by weight, Hongjing extract powder 2.1% by weight, black pepper extract 0.2% by weight, vitamin B 6 0.3% by weight, zinc-containing yeast 8.3% by weight, reduced maltose starch syrup 11.7% by weight A solution having a composition of 35.0% by weight of crystalline cellulose and 1.9% by weight of light anhydrous silicic acid is pulverized, and 2.0% by weight of hydroxypropyl cellulose is dissolved in purified water to make a hydroxypropyl cellulose concentration of 6.0%. Using the fluidized bed granulator as a binder solution, the drying time after granulation was controlled to obtain a granulated product. The water content of the granulated product was determined by the loss on drying method (70 ° C., 30 minutes) using 5 g of the granulated product, and was 2.73 mass%. The granulated product was mixed with calcium stearate 2.0% by mass, and tableted with a tableting machine to produce a tablet with 1 tablet mass of 300 mg. The water content of the tablet was 2.97% by mass as determined by the loss on drying method (70 ° C., 30 minutes) using a powder obtained by pulverizing 5 g of the tablet.

比較例1
Lアルギニン35.0質量%、コウジンエキス末1.6質量%、紅景天エキス末2.1質量%、黒胡椒抽出物0.2質量%、ビタミンB60.3質量%、亜鉛含有酵母8.3質量%、還元麦芽糖水飴11.7質量%、結晶セルロース35.0質量%、軽質無水ケイ酸1.9質量%の組成の粉体を粉砕し、該混合物に、ヒドロキシプロピルセルロース2.0質量%を精製水に溶解してヒドロキシプロピルセルロース濃度を6.0%とした溶液を結合液として、流動層造粒機を用い、造粒後の乾燥時間を制御して、造粒物を得た。該造粒物の水分含有量は、5gの造粒物を用いた乾燥減量法(70℃30分)により決定し、2.44質量%であった。該造粒物に、ステアリン酸カルシウム2.0質量%を混合し、打錠機にて打錠、1錠質量300mgの錠剤を製造した。該錠剤の水分含有量は、5gの錠剤を粉砕した粉末を用いた乾燥減量法(70℃30分)により決定し、2.17質量%であった。
Comparative Example 1
L arginine 35.0% by weight, Koujin extract powder 1.6% by weight, Hongjing extract powder 2.1% by weight, black pepper extract 0.2% by weight, vitamin B 6 0.3% by weight, zinc-containing yeast 8.3% by weight, reduced maltose starch syrup 11.7% by weight A solution having a composition of 35.0% by weight of crystalline cellulose and 1.9% by weight of light anhydrous silicic acid is pulverized, and 2.0% by weight of hydroxypropyl cellulose is dissolved in purified water to make a hydroxypropyl cellulose concentration of 6.0%. Using the fluidized bed granulator as a binder solution, the drying time after granulation was controlled to obtain a granulated product. The water content of the granulated product was determined by the loss on drying method (70 ° C. for 30 minutes) using 5 g of the granulated product, and was 2.44% by mass. The granulated product was mixed with calcium stearate 2.0% by mass, and tableted with a tableting machine to produce a tablet with 1 tablet mass of 300 mg. The water content of the tablet was 2.17% by mass as determined by the loss on drying method (70 ° C., 30 minutes) using a powder obtained by grinding a 5 g tablet.

試験例
参考例1、2、3、4及び実施例1、比較例1で製造した錠剤を試験サンプルとした。試験サンプルを、25℃60%RHの条件下にて任意時間保存した後、試験サンプルの外観変化を評価した。試験結果を表2及び表3に示した。また、それぞれの錠剤について代表的な写真を図1〜図9に示した。
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 period of time at 25 ° C. and 60% RH, and then the appearance change of the test sample was evaluated. The test results are shown in Tables 2 and 3. Moreover, the typical photograph about each tablet was shown in FIGS.

Figure 0005476782
Figure 0005476782

Figure 0005476782
Figure 0005476782

表中の評価結果は以下の通りである。
0:変化無し
1:錠剤に亀裂
2:錠剤の崩壊
参考例より、25℃60%RHの条件下における試験サンプルの外観変化は、Lアルギニンの含有量に依存し、Lアルギニンの含有量が16.9質量%以上では錠剤に亀裂や崩壊を確認した。従って本発明はアルギニンを錠剤に対して16.9質量%以上含有させる場合に、特に効果を発揮する。なお、アルギニンの含有量が16.9質量%未満である錠剤に対しても、アルギニンの吸水、膨潤を抑制するために、本発明を適用することができる。
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, At mass% or more, cracks and disintegration were confirmed in the tablets. 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. The present invention can also 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.

実施例1で得られた試験サンプルの25℃60%RH条件下における外観変化を評価したところ、錠剤の亀裂や崩壊は確認されず、安定であることを確認した。しかし、比較例1で得られた試験サンプルの25℃60%RH条件下における外観変化を評価したところ、経時的な錠剤の亀裂が確認された。   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. However, when the appearance change of the test sample obtained in Comparative Example 1 under the condition of 25 ° C. and 60% RH was evaluated, cracks in the tablet over time were confirmed.

以上の結果より、湿式造粒して得られる造粒物の水分含有量が2.73質量%以上であれば、Lアルギニンの含有量が35.0質量%においても25℃60%RHの条件下にて安定な錠剤を提供することができた。   From the above results, if the moisture content of the granulated product obtained by wet granulation is 2.73 mass% or more, it is stable under the conditions of 25 ° C and 60% RH even when the L arginine content is 35.0 mass%. Could provide a good tablet.

本発明のアルギニン含有錠剤の製造方法は、食品、医薬品、医薬部外品等の分野において利用が可能である。   The manufacturing method of the arginine containing tablet of this invention can be utilized in field | areas, such as a foodstuff, a pharmaceutical, and a quasi-drug.

Claims (2)

アルギニンを含有する粉体を湿式造粒して得られる水分含有量が2.7質量%以上である造粒物を含有する打錠用粉体を打錠することを特徴とする、錠剤に対して16.9質量%以上の含有量のアルギニンの膨潤に起因する錠剤の亀裂及び崩壊を抑制したアルギニン含有錠剤の製造方法。 Water content obtained by powder containing arginine by wet granulation, characterized in that tabletting tabletting powder containing granulated product is at least 2.7 wt%, relative to the tablet The manufacturing method of the arginine containing tablet which suppressed the crack and disintegration of the tablet resulting from swelling of arginine of content more than 16.9 mass% . コーティングを施さないことを特徴とする請求項1に記載のアルギニン含有錠剤の製造方法。 The method for producing an arginine-containing tablet according to claim 1, wherein no coating is applied.
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