JP2004123731A - Tablet formulated with dioctyl sodium sulfosuccinate - Google Patents
Tablet formulated with dioctyl sodium sulfosuccinate Download PDFInfo
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- JP2004123731A JP2004123731A JP2003316233A JP2003316233A JP2004123731A JP 2004123731 A JP2004123731 A JP 2004123731A JP 2003316233 A JP2003316233 A JP 2003316233A JP 2003316233 A JP2003316233 A JP 2003316233A JP 2004123731 A JP2004123731 A JP 2004123731A
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- sodium sulfosuccinate
- dioctyl sodium
- tablet
- magnesium stearate
- mass
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- CDOUZKKFHVEKRI-UHFFFAOYSA-N 3-bromo-n-[(prop-2-enoylamino)methyl]propanamide Chemical compound BrCCC(=O)NCNC(=O)C=C CDOUZKKFHVEKRI-UHFFFAOYSA-N 0.000 title claims abstract description 44
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 title claims abstract description 44
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 49
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 24
- 239000000843 powder Substances 0.000 claims abstract description 17
- 238000004519 manufacturing process Methods 0.000 claims abstract description 10
- 238000004898 kneading Methods 0.000 claims abstract description 6
- 239000008187 granular material Substances 0.000 claims description 20
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims description 18
- 235000012239 silicon dioxide Nutrition 0.000 claims description 18
- KHOITXIGCFIULA-UHFFFAOYSA-N Alophen Chemical compound C1=CC(OC(=O)C)=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OC(C)=O)C=C1 KHOITXIGCFIULA-UHFFFAOYSA-N 0.000 claims description 8
- 229960000503 bisacodyl Drugs 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 8
- 238000002156 mixing Methods 0.000 claims description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 abstract description 10
- 239000000203 mixture Substances 0.000 abstract description 5
- 239000000463 material Substances 0.000 abstract 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 12
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 12
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 6
- 239000008101 lactose Substances 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 5
- 239000000314 lubricant Substances 0.000 description 5
- 230000000052 comparative effect Effects 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 238000004513 sizing Methods 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 229920003169 water-soluble polymer Polymers 0.000 description 4
- 230000000704 physical effect Effects 0.000 description 3
- 230000002000 scavenging effect Effects 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 238000013329 compounding Methods 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 238000009775 high-speed stirring Methods 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 238000010298 pulverizing process Methods 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000007916 tablet composition Substances 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000003463 adsorbent Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 238000010924 continuous production Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000008141 laxative Substances 0.000 description 1
- 230000002475 laxative effect Effects 0.000 description 1
- QXUAFCKBYYPTPQ-ZWKAXHIPSA-L magnesium (2R,3R,4S,5R,6S)-2-(hydroxymethyl)-6-[(2R,3S,4R,5R)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol octadecanoate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O QXUAFCKBYYPTPQ-ZWKAXHIPSA-L 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 239000004570 mortar (masonry) Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000012254 powdered material Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
本発明はジオクチルソジウムスルホサクシネート配合製剤における、錠剤製造時の打錠障害を防止し、大量生産が可能な製剤組成物に関する。 {Circle over (2)} The present invention relates to a pharmaceutical composition which is capable of mass-producing dioctyl sodium sulfosuccinate, which prevents tableting trouble during tablet production.
ジオクチルソジウムスルホサクシネートは瀉下薬として知られ、広く利用されている。しかしながらその性状は、ロウのような半固形物質であるので、固形製剤に配合する場合にはそのままでの配合は困難である。 Dioctyl sodium sulfosuccinate is known as a laxative and is widely used. However, since it is a semi-solid substance such as wax, it is difficult to mix it as it is when mixing it into a solid preparation.
従来、ジオクチルソジウムスルホサクシネートを固形製剤に配合する場合、軽質無水ケイ酸などの吸着剤に分散処理などを行うことにより粉状にして扱いやすくしていた。しかし、その様に粉状にしたものを錠剤の形に圧縮成形すると、打錠時に打錠機へ付着してしまい、連続して大量に生産する場合に打錠障害が発生することがあった。特に杵や臼への付着が発生すると、杵のきしみが起こり、錠剤質量にばらつきが生じたり、錠剤物性の変化が発生したりするなど扱いにくいものであった。 Conventionally, when dioctyl sodium sulfosuccinate is blended into a solid preparation, it has been made into a powder form by dispersing the adsorbent such as light anhydrous silicic acid to make it easier to handle. However, when such powdered material is compression-molded into a tablet form, it adheres to the tableting machine at the time of tableting, and tableting troubles may occur in continuous mass production. . In particular, when adhesion to a punch or a die occurs, the punch is squeezed, and the mass of the tablet is varied, or the physical properties of the tablet are changed.
通常打錠障害を防止するためにタルク、ステアリン酸などの滑沢剤を配合するのが一般的である。しかし、滑沢剤を多く配合すると得られた錠剤の強度が不十分で脆くなってしまうことから打錠障害を十分防止できる量を配合できない場合があったため、ジオクチルソジウムスルホサクシネートを配合した錠剤は限られた条件のものだけであった。 Generally, lubricants such as talc and stearic acid are generally blended to prevent tableting trouble. However, when a large amount of lubricant was added, the strength of the obtained tablet was insufficient and the tablet became brittle, so that it was not possible to mix an amount that could sufficiently prevent tableting failure, so that dioctyl sodium sulfosuccinate was added. The tablets were only in limited conditions.
従来ジオクチルソジウムスルホサクシネートを配合した製剤の打錠障害を改善する技術として、ジオクチルソジウムスルホサクシネートおよび微粉末を特殊な条件で粉末化する技術（特許文献１）などが知られている。 Conventionally, as a technique for improving the tableting trouble of a preparation containing dioctyl sodium sulfosuccinate, a technique of pulverizing dioctyl sodium sulfosuccinate and fine powder under special conditions is known (Patent Document 1). .
本発明は、ジオクチルソジウムスルホサクシネートを配合した処方で、錠剤を大量に製造しても製造障害が発生しない固形製剤を提供することを目的とする。 The object of the present invention is to provide a solid preparation which is formulated with dioctyl sodium sulfosuccinate and does not cause a production trouble even when a large number of tablets are produced.
本発明者らは上記課題を解決するために鋭意研究を重ねた結果、軽質無水ケイ酸およびステアリン酸マグネシウムからなる混合粉体に、ジオクチルソジウムスルホサクシネートを配合した溶液を用いて練合造粒を行うことにより、ジオクチルソジウムスルホサクシネート配合粉剤が得られ、得られた粉剤は大量に打錠しても打錠障害を発生せずに錠剤を大量に製造できることを見出し、本発明を完成した。 The present inventors have conducted intensive studies to solve the above problems, and as a result, kneaded using a solution in which dioctyl sodium sulfosuccinate is mixed with a mixed powder composed of light silicic anhydride and magnesium stearate. By performing the granulation, a dioctyl sodium sulfosuccinate-containing powder can be obtained, and it has been found that the obtained powder can be produced in a large number of tablets without causing a tableting trouble even if a large amount of the tablet is compressed. completed.
すなわち本発明は、(1)ジオクチルソジウムスルホサクシネート、軽質無水ケイ酸およびステアリン酸マグネシウムを配合したことを特徴とする錠剤、(2)ジオクチルソジウムスルホサクシネートを配合した溶液を用いて、軽質無水ケイ酸およびステアリン酸マグネシウムを配合した粉体を練合造粒し、これを打錠してなる錠剤、(3)ジオクチルソジウムスルホサクシネート１質量部に対する軽質無水ケイ酸の配合量が０.５〜１.５質量部である１または２に記載の錠剤、(4)ジオクチルソジウムスルホサクシネート１質量部に対するステアリン酸マグネシウムの配合量が０.０５〜０．５質量部である１または２に記載の錠剤、(5)ジオクチルソジウムスルホサクシネートを製剤全体の１０質量％以上配合したことを特徴とする１または２に記載の錠剤、(6)さらにビサコジルを配合したことを特徴とする１または２に記載の錠剤、(7)、ジオクチルソジウムスルホサクシネートを配合した溶液を用いて、軽質無水ケイ酸およびステアリン酸マグネシウムを配合した粉体を練合造粒してなる顆粒、(8)ジオクチルソジウムスルホサクシネートを配合した溶液を用いて、軽質無水ケイ酸およびステアリン酸マグネシウムを配合した粉体を練合造粒してなる粉体を用いることを特徴とする、ジオクチルソジウムスルホサクシネート配合錠剤の製造方法、である。 That is, the present invention, (1) dioctyl sodium sulfosuccinate, a tablet characterized by blending light anhydrous silicic acid and magnesium stearate, (2) using a solution blended dioctyl sodium sulfosuccinate, A tablet obtained by kneading and granulating a powder containing light anhydrous silicic acid and magnesium stearate and compressing the same, (3) the amount of light anhydrous silicic acid per 1 part by mass of dioctyl sodium sulfosuccinate is reduced. The tablet according to 1 or 2, which is 0.5 to 1.5 parts by mass, (4) the blending amount of magnesium stearate with respect to 1 part by mass of dioctyl sodium sulfosuccinate is 0.05 to 0.5 part by mass. The tablet according to 1 or 2, wherein the tablet according to 1 or 2, wherein (5) dioctyl sodium sulfosuccinate is incorporated in an amount of 10% by mass or more of the whole preparation. (6) Tablets according to 1 or 2, further comprising bisacodyl, (7), light anhydrous silicic acid and magnesium stearate are mixed using a solution containing dioctyl sodium sulfosuccinate. Using a solution containing (8) dioctyl sodium sulfosuccinate, the powder containing light anhydrous silicic acid and magnesium stearate was kneaded and granulated. A method for producing a tablet containing dioctyl sodium sulfosuccinate, characterized by using a powder comprising:
本発明は打錠した際にジオクチルソジウムスルホサクシネートの性状の影響を受けやすいことから、製剤中にジオクチルソジウムスルホサクシネートを製剤全体の１０質量％以上の高濃度で配合した場合に特に効果的である。 The present invention is easily affected by the properties of dioctyl sodium sulfosuccinate during tableting. Therefore, the present invention is particularly effective when the dioctyl sodium sulfosuccinate is incorporated in the preparation at a high concentration of 10% by mass or more of the whole preparation. It is effective.
一般的に錠剤を製造する際に滑沢剤であるステアリン酸マグネシウムを高濃度で配合すると、得られた錠剤は物性の低下を招くことが知られているが、本発明ではステアリン酸マグネシウムを粉体中に練り込むことにより、錠剤物性、特に崩壊性や錠剤硬度を低下させること無く配合することができる。 In general, it is known that when magnesium stearate, which is a lubricant, is blended at a high concentration when producing tablets, the resulting tablets are known to cause deterioration in physical properties.However, in the present invention, magnesium stearate is powdered. By kneading it into the body, it can be blended without lowering the physical properties of the tablet, especially the disintegration and tablet hardness.
本発明において、軽質無水ケイ酸はジオクチルソジウムスルホサクシネート１質量部に対して０．５〜１．５質量部の配合が好ましく、０.６〜１.３質量部の配合がさらに好ましい。１.５質量部を超えて配合すると、余剰の軽質無水ケイ酸などに起因する微粉末により、打錠時に障害が発生することがあるからである。 In the present invention, the light silicic anhydride is preferably added in an amount of 0.5 to 1.5 parts by mass, more preferably 0.6 to 1.3 parts by mass, per 1 part by mass of dioctyl sodium sulfosuccinate. If the amount is more than 1.5 parts by mass, an obstacle may be caused at the time of tableting due to a fine powder resulting from excess light anhydrous silicic acid or the like.
本発明においてステアリン酸マグネシウムはジオクチルソジウムスルホサクシネート１質量部に対して０.０５〜０.５質量部が好ましく、０.１〜０.３質量部の配合がより好ましい。 In the present invention, magnesium stearate is preferably used in an amount of 0.05 to 0.5 part by mass, more preferably 0.1 to 0.3 part by mass, per 1 part by mass of dioctyl sodium sulfosuccinate.
本発明の錠剤は以下のように製造される。 錠 剤 The tablet of the present invention is produced as follows.
ジオクチルソジウムスルホサクシネートおよび水溶性高分子を水、エタノールなどの溶媒に溶解して溶液とする。その溶液を噴霧しながらもしくは一括に添加し、軽質無水ケイ酸およびステアリン酸マグネシウムを混合した粉体を練合造粒して粉体を得る。 Dioctyl sodium sulfosuccinate and a water-soluble polymer are dissolved in a solvent such as water or ethanol to form a solution. The solution is sprayed or added all at once, and a powder obtained by mixing light anhydrous silicic acid and magnesium stearate is kneaded and granulated to obtain a powder.
得られた粉体に、必要があれば通常の医薬品製造に使用される他の薬効成分、添加剤などを加え、常法により、混合、粉砕、造粒等の工程を経て、錠剤やコーティング錠の剤形とすることができる。 To the obtained powder, if necessary, other medicinal ingredients and additives used in normal pharmaceutical production are added, and the mixture is subjected to mixing, pulverization, granulation, etc., in a conventional manner, to obtain tablets or coated tablets. Dosage form.
特にジオクチルソジウムスルホサクシネートと他の瀉下作用のある活性成分を同顆粒中、もしくは別顆粒とし、これを混合して打錠すると瀉下作用の向上が期待できるので好ましい。ここで他の瀉下作用のある活性成分としてはビサコジルが好ましく、その配合量は１日投与量で３〜１５mgが好ましい。 Particularly, dioctyl sodium sulfosuccinate and another active ingredient having a scavenging effect are preferably used in the same granules or as separate granules, and then mixed and tableted, which can be expected to improve the scavenging effect, which is preferable. Here, bisacodyl is preferable as the other active ingredient having a scavenging action, and its compounding amount is preferably 3 to 15 mg in a daily dose.
本発明では、ジオクチルソジウムスルホサクシネートを溶解させる溶媒に水溶性高分子を配合すると、得られる粉体の性状の点で好ましい。 In the present invention, it is preferable to mix a water-soluble polymer with a solvent in which dioctyl sodium sulfosuccinate is dissolved in view of the properties of the obtained powder.
配合する水溶性高分子は、結合剤として通常用いられるものを使用することができるが、好ましいものとしてヒドロキシプロピルセルロース、ポリビニルピロリドンおよびヒドロキシプロピルメチルセルロースをあげることができる。水溶性高分子の配合量は、ジオクチルソジウムスルホサクシネート１質量部に対し０．１〜０．３質量部が好ましい。 水溶 As the water-soluble polymer to be blended, those usually used as a binder can be used, and preferred examples thereof include hydroxypropylcellulose, polyvinylpyrrolidone and hydroxypropylmethylcellulose. The compounding amount of the water-soluble polymer is preferably 0.1 to 0.3 part by mass per 1 part by mass of dioctyl sodium sulfosuccinate.
上記のようにして得られた製剤組成物は、大量に連続的に打錠を行っても、杵や臼に付着が発生せず、打錠障害が発生しにくい。 (4) The tablet composition obtained as described above does not adhere to punches and dies even if tableting is continuously performed in a large amount, and tableting trouble hardly occurs.
本発明により、打錠時に起こるジオクチルソジウムスルホサクシネート由来の付着を防止し、連続生産可能な錠剤組成物を提供することが可能となった。 According to the present invention, it has become possible to provide a tablet composition capable of preventing continuous adhesion due to dioctyl sodium sulfosuccinate occurring at the time of tableting and capable of continuous production.
以下に実施例及び試験例をあげて本発明をさらに詳細に説明する。 Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples.
実施例１
（処方、製造方法）
Ａ顆粒
ビサコジル 120.0ｇ
乳糖 255.6ｇ
ヒドロキシプロピルセルロース 126.4ｇ
低置換度ヒドロキシプロピルセルロース 186.4ｇ
軽質無水ケイ酸 24.0ｇ
Ｂ顆粒
ジオクチルソジウムスルホサクシネート 192.0ｇ
ヒドロキシプロピルセルロース 40.0ｇ
軽質無水ケイ酸 192.0ｇ
ステアリン酸マグネシウム 57.6ｇ
瀉下活性成分のビサコジルに乳糖、ヒドロキシプロピルセルロース、低置換度ヒドロキシプロピルセルロース、軽質無水ケイ酸を混合し、精製水を溶媒とし、高速攪拌造粒を行い、乾燥、整粒後、顆粒Ａを得た。次に、ジオクチルソジウムスルホサクシネートとヒドロキシプロピルセルロースをエタノールに溶解し、溶解液を軽質無水ケイ酸とステアリン酸マグネシウムと共に練合造粒を行い、乾燥、整粒後、顆粒Ｂ得た。Ａ顆粒、Ｂ顆粒に、滑沢剤としてステアリン酸マグネシウム６．０ｇを添加し、５ｍｍ径、一錠質量５０ｍｇで打錠した。
Example 1
(Prescription, manufacturing method)
A granule Bisacodyl 120.0g
Lactose 255.6g
Hydroxypropyl cellulose 126.4g
Low substituted hydroxypropylcellulose 186.4g
Light silicic anhydride 24.0g
B granules dioctyl sodium sulfosuccinate 192.0g
Hydroxypropyl cellulose 40.0g
Light silicic anhydride 192.0g
Magnesium stearate 57.6g
Lactose, hydroxypropylcellulose, low-substituted hydroxypropylcellulose, and light anhydrous silicic acid are mixed with the distilling active ingredient bisacodyl, and high-speed stirring granulation is performed using purified water as a solvent, followed by drying and sizing to obtain granules A. Was. Next, dioctyl sodium sulfosuccinate and hydroxypropyl cellulose were dissolved in ethanol, and the resulting solution was kneaded and granulated with light anhydrous silicic acid and magnesium stearate. After drying and sizing, granules B were obtained. 6.0 g of magnesium stearate as a lubricant was added to the A granules and the B granules, and the mixture was tableted with a diameter of 5 mm and a tablet mass of 50 mg.
比較例１
（処方、製造方法）
Ａ顆粒
ビサコジル 120.0ｇ
乳糖 313.2ｇ
ヒドロキシプロピルセルロース 126.4ｇ
低置換度ヒドロキシプロピルセルロース 186.4ｇ
軽質無水ケイ酸 24.0ｇ
Ｂ顆粒
ジオクチルソジウムスルホサクシネート 192.0ｇ
ヒドロキシプロピルセルロース 40.0ｇ
軽質無水ケイ酸 192.0ｇ
活性成分であるジオクチルソジウムスルホサクシネートとヒドロキシプロピルセルロースをエタノールに溶解し、溶解液を軽質無水ケイ酸と共に練合造粒を行い、乾燥、整粒後、顆粒Ｂを得た。実施例1と同様にＡ顆粒を調製し、滑沢剤としてステアリン酸マグネシウム６．０ｇを添加し、５ｍｍ径、一錠質量５０ｍｇで打錠した。
Comparative Example 1
(Prescription, manufacturing method)
A granule Bisacodyl 120.0g
Lactose 313.2g
Hydroxypropyl cellulose 126.4g
Low substituted hydroxypropylcellulose 186.4g
Light silicic anhydride 24.0g
B granules dioctyl sodium sulfosuccinate 192.0g
Hydroxypropyl cellulose 40.0g
Light silicic anhydride 192.0g
The active ingredients, dioctyl sodium sulfosuccinate and hydroxypropyl cellulose, were dissolved in ethanol, and the solution was kneaded and granulated with light anhydrous silicic acid, and dried and sized to obtain granules B. A granule A was prepared in the same manner as in Example 1, and 6.0 g of magnesium stearate was added as a lubricant, and the mixture was tableted with a diameter of 5 mm and a tablet weight of 50 mg.
試験例１ 打錠時の付着状態の評価
試験方法
実施例１および比較例1で調製された顆粒を、ロータリー式打錠機を用い、連続で打錠した後に、杵（上杵、下杵）、臼への付着状態を目視により観察した。評価基準は以下の基準に従った。
（評価基準）
付着本数・１０本中の付着発生数
付着度・・・４段階評価
３；打錠障害に発展する著しい付着
２；付着あり
１；非常に軽微な付着
０；付着なし
Test Example 1 Evaluation of Adhesion at Tableting Test Method The granules prepared in Example 1 and Comparative Example 1 were continuously tableted using a rotary tableting machine, and then punched (upper punch, lower punch). The state of adhesion to the mortar was visually observed. Evaluation criteria were based on the following criteria.
(Evaluation criteria)
Number of adhesions / Number of adhesions out of 10 Adhesion degree: 4-grade evaluation 3: Significant adhesion that develops into tableting trouble 2: Adhesion 1: Very slight adhesion 0: No adhesion
試験結果
実施例1及び比較例1をそれぞれ同一条件下で７０００錠打錠し、打錠後の杵、臼への付着状態を目視評価した結果を表1に、実施例1の処方において３０万錠連続で打錠した結果を表２に示した。
Test Results Example 1 and Comparative Example 1 were each subjected to 7000 tablet compression under the same conditions, and the results of visual evaluation of the adhesion to punches and dies after compression were shown in Table 1. Table 2 shows the results of continuous tableting.
表から明らかなように実施例1で示される本発明の処方では比較例1に比較して、杵、臼への付着が大幅に軽減されることがわかった。また、３０万錠の連続打錠しても、打錠障害は発生しないことがわかった。 As is clear from the table, it was found that the formulation of the present invention shown in Example 1 significantly reduced the adhesion to punches and dies as compared with Comparative Example 1. It was also found that even if 300,000 tablets were continuously tableted, no tableting trouble occurred.
実施例２
（処方、製造方法）
Ａ顆粒
ビサコジル 120.0ｇ
乳糖 135.6ｇ
ヒドロキシプロピルセルロース 126.4ｇ
低置換度ヒドロキシプロピルセルロース 186.4ｇ
軽質無水ケイ酸 24.0ｇ
Ｂ顆粒
ジオクチルソジウムスルホサクシネート 192.0ｇ
ヒドロキシプロピルセルロース 40.0ｇ
軽質無水ケイ酸 192.0ｇ
ステアリン酸マグネシウム 57.6ｇ
後添加
造粒乳糖 120.0ｇ
ステアリン酸マグネシウム 6.0ｇ
瀉下活性成分のビサコジルに乳糖、ヒドロキシプロピルセルロース、低置換度ヒドロキシプロピルセルロース、軽質無水ケイ酸を混合し、精製水を溶媒とし、高速攪拌造粒を行い、乾燥、整粒後、顆粒Ａを得た。次に、ジオクチルソジウムスルホサクシネートとヒドロキシプロピルセルロースをエタノールに溶解し、溶解液を軽質無水ケイ酸とステアリン酸マグネシウムと共に練合造粒を行い、乾燥、整粒後、顆粒Ｂを得た。Ａ顆粒、Ｂ顆粒に、造粒乳糖、ステアリン酸マグネシウムを添加し、５ｍｍ径、一錠質量５０ｍｇで製錠した。
Example 2
(Prescription, manufacturing method)
A granule Bisacodyl 120.0g
Lactose 135.6g
Hydroxypropyl cellulose 126.4g
Low substituted hydroxypropylcellulose 186.4g
Light silicic anhydride 24.0g
B granules dioctyl sodium sulfosuccinate 192.0g
Hydroxypropyl cellulose 40.0g
Light silicic anhydride 192.0g
Magnesium stearate 57.6g
After addition <br/> Granulated lactose 120.0g
6.0g of magnesium stearate
Lactose, hydroxypropylcellulose, low-substituted hydroxypropylcellulose, and light anhydrous silicic acid are mixed with the distilling active ingredient bisacodyl, and high-speed stirring granulation is performed using purified water as a solvent, followed by drying and sizing to obtain granules A. Was. Next, dioctyl sodium sulfosuccinate and hydroxypropyl cellulose were dissolved in ethanol, and the resulting solution was kneaded and granulated with light anhydrous silicic acid and magnesium stearate. After drying and sizing, granules B were obtained. Granulated lactose and magnesium stearate were added to the A granules and the B granules, and tablets were prepared with a diameter of 5 mm and a mass of one tablet of 50 mg.
本発明によりＤＤＳを配合しても打錠障害が発生せずに錠剤を製造することが可能になったので医薬品などで有用である。
The present invention makes it possible to produce tablets without causing tableting trouble even when DDS is compounded, and thus is useful for pharmaceuticals and the like.
Claims (8)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2003316233A JP2004123731A (en) | 2002-09-10 | 2003-09-09 | Tablet formulated with dioctyl sodium sulfosuccinate |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2002264686 | 2002-09-10 | ||
| JP2003316233A JP2004123731A (en) | 2002-09-10 | 2003-09-09 | Tablet formulated with dioctyl sodium sulfosuccinate |
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| Publication Number | Publication Date |
|---|---|
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003316233A Pending JP2004123731A (en) | 2002-09-10 | 2003-09-09 | Tablet formulated with dioctyl sodium sulfosuccinate |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005255595A (en) * | 2004-03-10 | 2005-09-22 | Taisho Pharmaceut Co Ltd | Tablet formulated with dioctyl sodium sulfosuccinate |
| JP2007055969A (en) * | 2005-08-26 | 2007-03-08 | Taisho Pharmaceut Co Ltd | Bisacodyl dissolution-improving agent |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5799521A (en) * | 1980-12-11 | 1982-06-21 | Eisai Co Ltd | Solid composition containing bisacodyl |
| JPH02255613A (en) * | 1989-03-27 | 1990-10-16 | Lion Corp | Pharmaceutical containing dioctyl sodium sulfosuccinate blended therein |
| JPH11130662A (en) * | 1997-08-29 | 1999-05-18 | Toyama Chem Co Ltd | Quickly disintegrable solid preparation |
-
2003
- 2003-09-09 JP JP2003316233A patent/JP2004123731A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5799521A (en) * | 1980-12-11 | 1982-06-21 | Eisai Co Ltd | Solid composition containing bisacodyl |
| JPH02255613A (en) * | 1989-03-27 | 1990-10-16 | Lion Corp | Pharmaceutical containing dioctyl sodium sulfosuccinate blended therein |
| JPH11130662A (en) * | 1997-08-29 | 1999-05-18 | Toyama Chem Co Ltd | Quickly disintegrable solid preparation |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005255595A (en) * | 2004-03-10 | 2005-09-22 | Taisho Pharmaceut Co Ltd | Tablet formulated with dioctyl sodium sulfosuccinate |
| JP2007055969A (en) * | 2005-08-26 | 2007-03-08 | Taisho Pharmaceut Co Ltd | Bisacodyl dissolution-improving agent |
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