JP5499599B2 - Acetaminophen-containing tablets - Google Patents
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- JP5499599B2 JP5499599B2 JP2009223573A JP2009223573A JP5499599B2 JP 5499599 B2 JP5499599 B2 JP 5499599B2 JP 2009223573 A JP2009223573 A JP 2009223573A JP 2009223573 A JP2009223573 A JP 2009223573A JP 5499599 B2 JP5499599 B2 JP 5499599B2
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- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 title claims description 64
- 229960005489 paracetamol Drugs 0.000 title claims description 31
- 229920002678 cellulose Polymers 0.000 claims description 15
- 239000001913 cellulose Substances 0.000 claims description 15
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 14
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 14
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 14
- 239000003826 tablet Substances 0.000 description 74
- 239000008187 granular material Substances 0.000 description 14
- 230000000052 comparative effect Effects 0.000 description 10
- 239000000203 mixture Substances 0.000 description 10
- 238000007906 compression Methods 0.000 description 9
- 230000006835 compression Effects 0.000 description 9
- 238000009472 formulation Methods 0.000 description 7
- 238000000748 compression moulding Methods 0.000 description 4
- 238000005336 cracking Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000011230 binding agent Substances 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 240000007695 Nandina domestica Species 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000011812 mixed powder Substances 0.000 description 2
- 229940072651 tylenol Drugs 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 238000005550 wet granulation Methods 0.000 description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 239000007894 caplet Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 230000032798 delamination Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 238000007542 hardness measurement Methods 0.000 description 1
- 238000003475 lamination Methods 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000000452 restraining effect Effects 0.000 description 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 238000004513 sizing Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 210000003813 thumb Anatomy 0.000 description 1
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- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、アセトアミノフェンを高濃度に含有する錠剤に関し、固形製剤の分野に属する。 The present invention relates to a tablet containing acetaminophen at a high concentration, and belongs to the field of solid preparations.
解熱鎮痛成分であるアセトアミノフェンを高濃度に含有する商品としては、ジョンソン・エンド・ジョンソン社が提供するタイレノール（登録商標）が世界的にも著名である。ここで、代表的なタイレノール（登録商標）は、カプレットであり、円形の錠剤ではない。 As a product containing acetaminophen, which is an antipyretic analgesic component, at a high concentration, Tylenol (registered trademark) provided by Johnson & Johnson is famous worldwide. Here, a typical Tylenol (registered trademark) is a caplet, not a round tablet.
アセトアミノフェンは、圧縮・成形性が悪いという性質を有するため、アセトアミノフェンを高濃度に含有する錠剤を圧縮成形する際にはキャッピングと呼ばれる打錠障害が発生することがある。 Since acetaminophen has a property of poor compression and moldability, a tableting trouble called capping may occur when a tablet containing acetaminophen in a high concentration is compression molded.
これに対して、アセトアミノフェン含有顆粒の圧縮成形性を改善し、キャッピング等の打錠障害を改善する方法としては次のような手段が提供されている。 On the other hand, the following means are provided as methods for improving the compression moldability of acetaminophen-containing granules and improving tableting troubles such as capping.
例えば、特開２００５−４７８６１号公報には、アセトアミノフェン、ナンテンジツエキス及び結晶セルロースを含有する混合物を湿式造粒して得られる顆粒を打錠することにより、錠剤硬度を改善し、キャッピングを抑制する方法が開示されているが（特許文献１の請求項１２等を参照）、ナンテンジツエキスの配合が必須となる。 For example, Japanese Patent Application Laid-Open No. 2005-47861 discloses that tablet hardness is improved by capping granules obtained by wet granulation of a mixture containing acetaminophen, nantenjitsu extract and crystalline cellulose. Although the method of suppressing is disclosed (refer to claim 12 of patent document 1, etc.), the blending of the Nantenjitsu extract is essential.
また、服用性に鑑みると、錠剤はできるだけ小型である方が好ましいが、そのために錠剤面をＲ型の凸面とし、錠剤径を１０ｍｍ以下とすると、圧縮成形時の分散応力等に起因してよりキャッピング等の打錠障害が発生し易くなる。 In view of the ingestibility, it is preferable that the tablet is as small as possible. For this reason, if the tablet surface is an R-shaped convex surface and the tablet diameter is 10 mm or less, it is more due to dispersion stress during compression molding. Tableting troubles such as capping are likely to occur.
これを改善するために結合剤等の賦形剤を増量すると小型化の要請に反するし、一方、１錠中のアセトアミノフェンの含有量を減らせば、１回の服用錠剤数が増え、これまた服用性の悪化や包装容器の大型化等を招来し、好ましくない。 In order to improve this, increasing the amount of excipients such as binders is contrary to the demand for downsizing, while reducing the content of acetaminophen in one tablet increases the number of tablets taken at one time. In addition, it is not preferable because it leads to deterioration of ingestibility and enlargement of the packaging container.
本発明の目的は、圧縮成形性に優れたアセトアミノフェン高濃度含有顆粒を調製し、キャッピング等の打錠障害の発生を抑制して、Ｒ型の凸面を有する小型のアセトアミノフェン高濃度含有円形錠剤を提供することである。 The object of the present invention is to prepare acetaminophen high-concentration-containing granules excellent in compression moldability, suppress the occurrence of tableting troubles such as capping, and contain a small acetaminophen high-concentration having an R-shaped convex surface To provide a round tablet.
本発明者らは前記課題を解決するために鋭意検討を重ねた結果、アセトアミノフェンの含有量が多くても、繊維系の賦形剤である結晶セルロースと結合剤であるヒドロキシプロピルセルロースの配合量を調整すれば、ナンテンジツエキス等を配合しなくても、圧縮成形性に優れた顆粒が得られ、該顆粒を圧縮成形することにより、キャッピング等の打錠障害を抑制し、Ｒ型の凸面を有する小型の円形錠剤が得られることを見出した。 As a result of intensive studies in order to solve the above problems, the present inventors have found that even if the content of acetaminophen is large, a blend of crystalline cellulose as a fiber-based excipient and hydroxypropyl cellulose as a binder If the amount is adjusted, a granule excellent in compression moldability can be obtained without blending Nantenjitsu extract, etc., and by compressing the granule, tableting troubles such as capping are suppressed, It has been found that small round tablets with convex surfaces can be obtained.
かかる知見をもとに得られた本発明の態様は、アセトアミノフェンを７０〜８５質量％、結晶セルロースを５〜１５質量％、及びヒドロキシプロピルセルロースを５〜１０質量％含有し、ナンテンジツエキスを含有しないことを特徴とするＲ型の凸面を有する錠径７〜１０ｍｍの円形錠剤である。 The embodiment of the present invention obtained on the basis of such knowledge contains 70 to 85% by mass of acetaminophen, 5 to 15% by mass of crystalline cellulose, and 5 to 10% by mass of hydroxypropyl cellulose, It is a circular tablet with a tablet diameter of 7 to 10 mm having an R-shaped convex surface, characterized by not containing any.
本発明の他の態様は、アセトアミノフェンを７５〜８０質量％、結晶セルロースを７〜１２質量％、及びヒドロキシプロピルセルロースを５〜７質量％含有し、ナンテンジツエキスを含有しないことを特徴とするＲ型の凸面を有する錠径７〜１０ｍｍの円形錠剤である。 Another aspect of the present invention is characterized in that it contains 75 to 80% by mass of acetaminophen, 7 to 12% by mass of crystalline cellulose, and 5 to 7% by mass of hydroxypropyl cellulose, and does not contain a Nantenjitsu extract. It is a round tablet with a tablet diameter of 7 to 10 mm having an R-shaped convex surface.
本発明により、圧縮成形時のキャッピング等の打錠障害改善されたＲ型の凸面を有する小型のアセトアミノフェン高濃度含有円形錠剤を提供することが可能となった。 According to the present invention, it is possible to provide a small acetaminophen high-concentration circular tablet having an R-shaped convex surface with improved tableting troubles such as capping during compression molding.
「アセトアミノフェン」の含有（配合）量は、錠剤中７０〜８５質量％であり、錠剤中のアセトアミノフェンの含有量を高濃度にし、できるだけ錠剤を小型化させ、確実にキャッピングが生じないようにするという点からは、錠剤中７５〜８０質量％が好ましい。 The content (formulation) of “acetaminophen” is 70 to 85% by mass in the tablet, the content of acetaminophen in the tablet is made high, the tablet is miniaturized as much as possible, and capping does not occur reliably. From the point of doing, 75-80 mass% in a tablet is preferable.
「結晶セルロース」は、固形製剤の分野において汎用されている賦形剤で、種々のタイプ、グレードのものが提供されているが、できるだけ圧縮成形性の良いものが好ましい。 “Crystalline cellulose” is an excipient that is widely used in the field of solid preparations, and is provided in various types and grades, and those having good compression moldability are preferred.
結晶セルロースの含有（配合）量は、錠剤中５〜１５質量％であり、錠剤中のアセトアミノフェンの含有量との均衡、圧縮成形性を付与し、キャッピング等の打錠障害を抑制するという点からは、錠剤中７〜１２質量％が好ましい。 The content (formulation) of the crystalline cellulose is 5 to 15% by mass in the tablet, imparts a balance with the content of acetaminophen in the tablet, gives compression moldability, and suppresses tableting troubles such as capping. From the viewpoint, 7 to 12% by mass in the tablet is preferable.
「ヒドロキシプロピルセルロース」は、結合剤等として固形製剤の分野において汎用されている賦形剤である。 “Hydroxypropylcellulose” is an excipient widely used in the field of solid preparations as a binder and the like.
ヒドロキシプロピルセルロースの含有（配合）量は、錠剤中５〜１０質量％であり、錠剤中のアセトアミノフェンや結晶セルロースの含有量との均衡、圧縮成形性を付与し、キャッピング等の打錠障害を抑制するという点からは、錠剤中５〜７質量％が好ましい。 The content (formulation) of hydroxypropylcellulose is 5 to 10% by mass in the tablet, providing balance with the content of acetaminophen and crystalline cellulose in the tablet, compression molding properties, and clogging troubles such as capping. From the point of restraining, 5-7 mass% in a tablet is preferable.
「ナンテンジツエキス」とは、ナンテン属（めぎ科）Nandina domestica Thumb.の果実（南天実）等から抽出したエキスであり、鎮該作用等を有する。特許文献１として記載した特開２００５−４７８６１号公報によれば、顆粒の圧縮性を改善し、キャッピング等の打錠障害の抑制に寄与すると解されるが、本発明においては、顆粒の圧縮性を改善し、キャッピング等の打錠障害を抑制するに際し、ナンテンジツエキスの配合を要せず、その分だけアセトアミノフェン等の錠剤中の含有濃度を高めることができる。 The “nantenjitsu extract” is an extract extracted from the fruit of the genus Nanten (Nymidae) Nandina domestica Thumb. According to Japanese Patent Application Laid-Open No. 2005-47861 described as Patent Document 1, it is understood that the compressibility of the granules is improved, and it contributes to the suppression of tableting troubles such as capping. When the tableting troubles such as capping are suppressed and the blending of Nantenjitsu extract is not required, the concentration of acetaminophen or the like in the tablet can be increased accordingly.
本発明の錠剤には、他の公知の添加剤を配合しても良いが、アセトアミノフェンを高濃度に含有する錠剤を提供するという本発明の趣旨を損なわないように、その配合量は自ずと限定されるし、かかる趣旨からアセトアミノフェン以外の有効成分は原則として配合し得ない。 The tablet of the present invention may be blended with other known additives, but the blending amount is naturally not to impair the gist of the present invention to provide a tablet containing acetaminophen at a high concentration. For this purpose, active ingredients other than acetaminophen cannot be blended in principle.
本発明の錠剤は、円形で錠剤面がＲ型の凸面形状を有する故、圧縮成形時の分散応力等に起因する打錠障害、特に固形製剤の分野においてキャッピング（ラミネーションや層間剥離などと呼ばれることもある。）といわれる打錠障害が発生し易い。また、錠剤の服用性等に鑑みるに、その錠径は７〜１０ｍｍである。 Since the tablet of the present invention is round and the tablet surface has an R-shaped convex shape, it is called capping (lamination, delamination, etc.) in the field of tableting, particularly in the field of solid preparations due to dispersion stress during compression molding. There is also a tendency for tableting failure to occur. Further, in view of tablet dosing properties, the tablet diameter is 7 to 10 mm.
本発明の錠剤は、一例として次のような方法によって製造される。アセトアミノフェン、結晶セルロース及びヒドロキプロピルセルロースを含有し、他に必要があれば、軽質無水ケイ酸のような流動化剤を添加して、混合粉体を調製する。水やエタノールあるいはそれらの混合溶媒にヒドロキシプロピルセルロースを溶解させた造粒用溶液を調製し、前記混合粉体に噴霧して流動層造粒等の湿式造粒を行う。湿粒を乾燥させ、顆粒を得る。得られた顆粒にクロスカルメロースナトリウム、結晶セルロース、硬化油、ステリアン酸マグネシウムを添加・混合し、打錠用顆粒を調製する。該打錠用顆粒を、直径７〜１０ｍｍの２段Ｒ面等のＲ型の凸面を有する円形の打錠用杵を使って打錠機で圧縮成形することにより、Ｒ型の凸面を有する錠径７〜１０ｍｍのアセトアミノフェン含有円形錠剤が得られる。このとき打錠時の圧力は、錠剤の硬度や打錠用杵の耐圧許容度等を考慮して適宜に設定されるが、通常打錠用杵１本当り約３００〜５０００ｋｇ／ｃｍ2であり、好ましくは打錠用杵１本当り約１０００〜３０００ｋｇ／ｃｍ2である。 The tablet of this invention is manufactured by the following methods as an example. A mixed powder is prepared containing acetaminophen, crystalline cellulose and hydroxypropylcellulose, and if necessary, a fluidizing agent such as light anhydrous silicic acid is added. A granulation solution in which hydroxypropyl cellulose is dissolved in water, ethanol or a mixed solvent thereof is prepared and sprayed onto the mixed powder to perform wet granulation such as fluidized bed granulation. Dry the wet granules to obtain granules. To the obtained granules, croscarmellose sodium, crystalline cellulose, hydrogenated oil and magnesium stearate are added and mixed to prepare granules for tableting. Tablets having an R-shaped convex surface are formed by compressing the granules for tableting with a tableting machine using a circular tableting punch having an R-shaped convex surface such as a two-step R surface having a diameter of 7 to 10 mm. Acetaminophen-containing circular tablets having a diameter of 7 to 10 mm are obtained. At this time, the pressure at the time of tableting is appropriately set in consideration of the hardness of the tablet and the pressure tolerance of the tableting punch, and is usually about 300 to 5000 kg / cm 2 per tableting punch. The amount is preferably about 1000 to 3000 kg / cm 2 per tableting punch.
以下に、実施例、比較例及び試験例を挙げて、本発明をより詳しく説明する。 Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples, and Test Examples.
実施例１
表１記載の組成となるように原料を秤量後、粉体を混合・粉砕し、造粒用粉末を得た。該造粒用粉末を流動層造粒機（フローコーター；フロイント産業（株）、ＷＳＧ；（株）パウレック）に仕込み、造粒用溶液（精製水にヒドロキシプロピルセルロースを溶解させたもの）をスプレー添加しながら流動層造粒を行った。調粒後、得られた顆粒に添加剤を後末添加・混合した。得られた打錠用顆粒を打錠機（コレクト、ベラ；（株）菊水製作所）を使用し、９．５ｍｍφ２段Ｒ面の杵で打錠した。錠剤の１錠重量は、表１に記載の重量となるように調整し、錠径９．５ｍｍの錠剤を得た。打錠時の圧縮圧力は１０００ｋｇｆ、回転盤の回転数は５ｒｐｍに設定した。
Example 1
After the raw materials were weighed so as to have the composition shown in Table 1, the powder was mixed and pulverized to obtain a granulating powder. The granulating powder is charged into a fluidized bed granulator (flow coater; Freund Sangyo Co., Ltd., WSG; Paulek Co., Ltd.) and sprayed with a granulating solution (hydroxypropylcellulose dissolved in purified water). Fluidized bed granulation was performed while adding. After the sizing, an additive was added to the obtained granules and mixed. The obtained granules for tableting were tableted using a tableting machine (Collect, Vera; Kikusui Seisakusho Co., Ltd.) with a 9.5 mmφ 2-stage R-side punch. The weight of one tablet was adjusted to the weight shown in Table 1, and a tablet with a tablet diameter of 9.5 mm was obtained. The compression pressure at the time of tableting was set to 1000 kgf, and the rotation speed of the rotating disk was set to 5 rpm.
実施例２、３及び比較例１
表１に記載した処方で実施例１に準拠し、錠径９．５ｍｍの錠剤を得た。
Examples 2 and 3 and Comparative Example 1
Based on the formulation described in Table 1, in accordance with Example 1, tablets with a tablet diameter of 9.5 mm were obtained.
試験例１
実施例１〜３及び比較例１で得られた錠剤について水平方向の割れ（キャッピング）の有無を調べた。硬度計（シュロイニゲル社）を用いて各々１０錠ずつの錠剤硬度を測定した際に、水平方向の割れ（キャッピング）が発生した錠剤の個数を計測し、結果を表１に記載した。
なお、製品として提供することを考慮すると、硬度測定時に水平方向への割れが全く発生しないことが好ましい。
Test example 1
The tablets obtained in Examples 1 to 3 and Comparative Example 1 were examined for the presence of horizontal cracks (capping). When the tablet hardness of 10 tablets each was measured using a hardness meter (Schleunigel), the number of tablets in which horizontal cracking (capping) occurred was measured, and the results are shown in Table 1.
In consideration of providing as a product, it is preferable that no cracks in the horizontal direction occur at the time of hardness measurement.
錠剤中のアセトアミノフェン濃度が低い場合は、キャッピングは確認されなかった（比較例１）。錠剤中のアセトアミノフェン濃度が７５質量％から８０質量％において、錠剤中の結晶セルロース濃度が１１質量％以上、錠剤中のヒドロキシプロピルセルロース濃度が６質量％以上ではキャッピングの発生が観られなかった（実施例１〜３）。 When the acetaminophen concentration in the tablet was low, capping was not confirmed (Comparative Example 1). When the acetaminophen concentration in the tablet was 75% by mass to 80% by mass, the occurrence of capping was not observed when the crystalline cellulose concentration in the tablet was 11% by mass or more and the hydroxypropylcellulose concentration in the tablet was 6% by mass or more. (Examples 1-3).
実施例４及び比較例２
表２に記載した処方で実施例１に準拠し、錠径９．５ｍｍの錠剤を得た。
Example 4 and Comparative Example 2
Based on the formulation described in Table 2, the tablet having a tablet diameter of 9.5 mm was obtained according to Example 1.
試験例２
実施例４及び比較例２の錠剤に対し、試験例１と同様に水平方向の割れ（キャッピング）の有無を調べた。結果を表２に記載した。
Test example 2
The tablets of Example 4 and Comparative Example 2 were examined for the presence of horizontal cracking (capping) in the same manner as in Test Example 1. The results are shown in Table 2.
錠剤中のアセトアミノフェン濃度７８質量％、錠剤中のヒドロキシプロピルセルロース濃度７質量％、錠剤中の結晶セルロース濃度２質量％においてキャッピングが発生したが（比較例２）、錠剤中７質量％以上ではキャッピングは発生しなかった（実施例１及び４）。 Capping occurred when the concentration of acetaminophen in the tablet was 78% by mass, the concentration of hydroxypropylcellulose in the tablet was 7% by mass, and the concentration of crystalline cellulose in the tablet was 2% by mass (Comparative Example 2). Capping did not occur (Examples 1 and 4).
実施例５及び比較例３
表３に記載した処方で実施例１に準拠し、錠径９．５ｍｍの錠剤を得た。
Example 5 and Comparative Example 3
Based on the formulation described in Table 3, the tablet having a tablet diameter of 9.5 mm was obtained according to Example 1.
試験例３
実施例５及び比較例３の錠剤に対し、試験例１と同様に水平方向の割れ（キャッピング）の有無を調べた。結果を表３に記載した。
Test example 3
The tablets of Example 5 and Comparative Example 3 were examined for the presence of horizontal cracking (capping) in the same manner as in Test Example 1. The results are shown in Table 3.
錠剤中のアセトアミノフェン濃度７８質量％、錠剤中の結晶セルロース濃度１２質量％、錠剤中のヒドロキシプロピルセルロース濃度４質量％においてキャッピングが発生したが（比較例３）、錠剤中５質量％以上ではキャッピングは発生しなかった（実施例１及び５）。 Capping occurred when the acetaminophen concentration in the tablet was 78% by mass, the crystalline cellulose concentration in the tablet was 12% by mass, and the hydroxypropylcellulose concentration in the tablet was 4% by mass (Comparative Example 3). Capping did not occur (Examples 1 and 5).
表４に記載した処方で実施例１に準拠して打錠用顆粒を調製し、打錠機（コレクト；（株）菊水製作所）を使用し、７．０ｍｍφ１２Ｒ面の杵で打錠した。錠剤の１錠重量は、表４に記載の重量となるように調整し、錠径７．０ｍｍの錠剤を得た。打錠時の圧縮圧力は８００ｋｇｆ、回転盤の回転数は４０ｒｐｍに設定した。錠径７．０ｍｍの錠剤を得た。 Granules for tableting were prepared according to the formulation described in Table 4 according to Example 1, and tableted with a punch of 7.0 mmφ12R surface using a tableting machine (collect; Kikusui Seisakusho). The weight of one tablet was adjusted to the weight shown in Table 4 to obtain a tablet having a tablet diameter of 7.0 mm. The compression pressure at the time of tableting was set to 800 kgf, and the rotation speed of the rotating disk was set to 40 rpm. A tablet having a tablet diameter of 7.0 mm was obtained.
試験例４
実施例６の錠剤に対し、試験例１と同様に水平方向の割れ（キャッピング）の有無を調べた。結果を表４に記載した。
Test example 4
The tablet of Example 6 was examined for the presence of horizontal cracking (capping) in the same manner as in Test Example 1. The results are shown in Table 4.
錠剤中のアセトアミノフェン濃度７８質量％、錠剤中の結晶セルロース濃度１２質量％、錠剤中のヒドロキシプロピルセルロース濃度７質量％において、錠径７．０ｍｍの錠剤においてもキャッピングは発生しなかった（実施例６）。 No capping occurred even in tablets with a tablet diameter of 7.0 mm at an acetaminophen concentration of 78% by weight in tablets, a crystalline cellulose concentration of 12% by weight in tablets, and a hydroxypropylcellulose concentration of 7% by weight in tablets (implementation). Example 6).
本発明により、アセトアミノフェンを高濃度に含有し、服用しやすいＲ型の凸面形状を有する小型の円形錠剤の製品化が可能となった。 According to the present invention, it has become possible to commercialize a small round tablet having a high concentration of acetaminophen and having an R-shaped convex shape that is easy to take.
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