JP5433295B2 - Xanthan gum-coated water-soluble saccharide and compression-molded preparation - Google Patents
Xanthan gum-coated water-soluble saccharide and compression-molded preparation Download PDFInfo
- Publication number
- JP5433295B2 JP5433295B2 JP2009111749A JP2009111749A JP5433295B2 JP 5433295 B2 JP5433295 B2 JP 5433295B2 JP 2009111749 A JP2009111749 A JP 2009111749A JP 2009111749 A JP2009111749 A JP 2009111749A JP 5433295 B2 JP5433295 B2 JP 5433295B2
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- JP
- Japan
- Prior art keywords
- compression
- xanthan gum
- water
- hydrochloride
- mass
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001720 carbohydrates Chemical class 0.000 title claims description 68
- 239000000230 xanthan gum Substances 0.000 title claims description 56
- 229920001285 xanthan gum Polymers 0.000 title claims description 56
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- 229940082509 xanthan gum Drugs 0.000 title claims description 56
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 19
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- 229960002622 triacetin Drugs 0.000 description 1
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- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
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- LMJSLTNSBFUCMU-UHFFFAOYSA-N trichlormethiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC(C(Cl)Cl)NS2(=O)=O LMJSLTNSBFUCMU-UHFFFAOYSA-N 0.000 description 1
- WEAPVABOECTMGR-UHFFFAOYSA-N triethyl 2-acetyloxypropane-1,2,3-tricarboxylate Chemical compound CCOC(=O)CC(C(=O)OCC)(OC(C)=O)CC(=O)OCC WEAPVABOECTMGR-UHFFFAOYSA-N 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
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- 229960001082 trimethoprim Drugs 0.000 description 1
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- DUXYWXYOBMKGIN-UHFFFAOYSA-N trimyristin Chemical compound CCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCC DUXYWXYOBMKGIN-UHFFFAOYSA-N 0.000 description 1
- PVNIQBQSYATKKL-UHFFFAOYSA-N tripalmitin Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCC PVNIQBQSYATKKL-UHFFFAOYSA-N 0.000 description 1
- DCXXMTOCNZCJGO-UHFFFAOYSA-N tristearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
- 229960001530 trospium chloride Drugs 0.000 description 1
- 229960004747 ubidecarenone Drugs 0.000 description 1
- 229960001130 urapidil Drugs 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 229960001722 verapamil Drugs 0.000 description 1
- 229960000881 verapamil hydrochloride Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- NCYCYZXNIZJOKI-UHFFFAOYSA-N vitamin A aldehyde Natural products O=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-UHFFFAOYSA-N 0.000 description 1
- 235000010374 vitamin B1 Nutrition 0.000 description 1
- 239000011691 vitamin B1 Substances 0.000 description 1
- 235000019163 vitamin B12 Nutrition 0.000 description 1
- 239000011715 vitamin B12 Substances 0.000 description 1
- 235000019164 vitamin B2 Nutrition 0.000 description 1
- 239000011716 vitamin B2 Substances 0.000 description 1
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- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 229960000883 warfarin potassium Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
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Description
本発明は、キサンタンガムで被覆した水溶性糖類及びそれを使用した口腔内速崩壊性圧縮成形製剤に関するものである。 The present invention relates to a water-soluble saccharide coated with xanthan gum and an intraoral rapidly disintegrating compression-molded preparation using the same.
経口投与用の固形製剤としては、従来、細粒剤、顆粒剤、錠剤、カプセル剤などの形態の製剤が用いられている。しかしこれらの剤型の製剤には、乳児、高齢者、重症患者にとっては、嚥下が困難である等の問題があるため、これらの問題の少ない製剤、例えば口腔内速崩壊性圧縮成形製剤も各種開発されつつある。
一方、治療効果の改善、患者の服用性の向上などを目的として、製剤からの薬物放出速度の制御、製剤に含まれる薬物の味のマスキングなど種々の機能を付与された製剤が研究され、臨床の場においても使用されている。
口腔内速崩壊錠は服用したときに速やかに崩壊することが要求される一方、口腔内ですぐに崩壊するため、服用感も良好であることが望まれると共に、服用までの保存、運搬等においては破損したりしない適度な硬度を必要とする。
医薬製剤の賦形剤として多用されている乳糖やマンニトールなどの水溶性糖類は圧縮製剤製造時における流動性及び圧縮成形性等が悪く、口腔内速崩壊性圧縮成形製剤の賦形剤として通常の方法で使用すると、得られた製剤の硬度及び速崩壊性などの点で満足のできる口腔内速崩壊性圧縮成形製剤を得るのが難しい。そのため種々の工夫がなされている。
Conventionally, preparations in the form of fine granules, granules, tablets, capsules and the like are used as solid preparations for oral administration. However, these dosage forms have problems such as difficulty in swallowing for infants, the elderly, and severely ill patients. It is being developed.
On the other hand, for the purpose of improving the therapeutic effect and improving the patient's ingestion, the formulation with various functions such as the control of the drug release rate from the formulation and the masking of the taste of the drug contained in the formulation has been studied and clinically It is also used in the field.
Intraoral rapidly disintegrating tablets are required to disintegrate quickly when taken, but since they disintegrate quickly in the oral cavity, it is desirable that the feeling of taking is good, and in storage, transportation, etc. until taking Requires moderate hardness that does not break.
Water-soluble saccharides such as lactose and mannitol, which are frequently used as excipients for pharmaceutical preparations, have poor fluidity and compression moldability during production of compressed preparations, and are commonly used as excipients for intraorally rapidly disintegrating compression molded preparations. When used in the method, it is difficult to obtain an intraoral rapidly disintegrating compression-molded preparation that is satisfactory in terms of hardness and fast disintegration of the obtained preparation. Therefore, various ideas have been made.
例えば、特許文献1には、少なくとも1種の単糖類又は多糖類から誘導された結晶性糖アルコールの結晶マトリックス内に少なくとも一種の薬剤活性化合物の粒子を均一に分散させてなる薬剤組成物が記載されている。特許文献2には、結合性が低い、成形性の悪いマンニトール又は乳糖に嵩比重60g/100ml未満のソルビトール粉粒体を配合することにより、成形性の高い他の添加剤、例えばセルロース系化合物、アクリル酸系化合物、ゼラチン等の配合量低減が図れ、崩壊性に優れた固形製剤組成物として得られることが記載されている。特許文献3には、β−ラクトース含量の高い乳糖に糖アルコールを添加して、この水溶液をローラードライング法により乾燥させることにより乳糖の成形性を改善している。
また、特許文献4には汎用型の口腔内溶解型圧縮成型物が開示され、それによれば、乳糖又はマンニトール等の成形性の低い糖類に、マルトース等の成形性の高い糖類を結合剤として噴霧して被覆および/または造粒して得られた造粒物を、賦形剤として錠剤などの圧縮製剤に配合することにより口腔内速崩壊性の製剤が得られる旨開示されている。
For example, Patent Document 1 describes a pharmaceutical composition in which particles of at least one pharmaceutical active compound are uniformly dispersed in a crystalline sugar alcohol crystal matrix derived from at least one monosaccharide or polysaccharide. Has been. In Patent Document 2, by adding sorbitol powder having a bulk specific gravity of less than 60 g / 100 ml to mannitol or lactose having poor binding properties and poor moldability, other additives having high moldability, such as cellulose compounds, It is described that the blending amount of an acrylic acid compound, gelatin and the like can be reduced, and it can be obtained as a solid preparation composition excellent in disintegration. In Patent Document 3, sugar alcohol is added to lactose having a high β-lactose content, and this aqueous solution is dried by a roller drying method to improve lactose moldability.
Further, Patent Document 4 discloses a general-purpose intraoral dissolution type compression-molded product. According to this, a low-moldability saccharide such as lactose or mannitol is sprayed with a high-moldability saccharide such as maltose as a binder. It is disclosed that a rapidly disintegrating preparation in the oral cavity can be obtained by blending the granulated product obtained by coating and / or granulation with a compressed preparation such as a tablet as an excipient.
医薬用担体として多用されている水溶性糖類の中で、乳糖又はマンニトール等の糖類は成形性が悪いことが知られている。そのため、最近増加している口腔内速崩壊錠への使用には種々の工夫が必要とされている。本発明は医薬用担体として多用されている成形性の悪い糖類の流動性及び圧縮成形性を改善し、圧縮整形製剤、特に口腔内速崩壊錠等の賦形剤として適するようにすると共に、適度な硬度と速崩壊性を有し、服用もし易い口腔内速崩壊性圧縮成形製剤の開発を目的とするものである。 Among water-soluble saccharides frequently used as pharmaceutical carriers, saccharides such as lactose or mannitol are known to have poor moldability. For this reason, various devices are required for use in the rapidly increasing intraoral rapidly disintegrating tablets. The present invention improves the fluidity and compression moldability of poorly moldable saccharides that are frequently used as pharmaceutical carriers, makes them suitable as excipients for compression-molded preparations, especially intraoral quick disintegrating tablets, etc. The purpose is to develop an intraoral rapidly disintegrating compression-molded preparation that has high hardness and fast disintegration and is easy to take.
本発明者らは、上記目的を達成すべく鋭意検討をした結果、少量のキサンタンガムで被覆した水溶性糖類は成形性が改善され、目的とする口腔内速崩壊性圧縮成形製剤を容易に製造し得ることを見出し、本発明を完成した。 As a result of intensive studies to achieve the above-mentioned object, the present inventors have improved the moldability of the water-soluble saccharide coated with a small amount of xanthan gum, and easily produced the intended intraoral rapidly disintegrating compression-molded preparation. The present invention was completed.
即ち、本発明は
1.キサンタンガムで被覆された水溶性糖類であって、水溶性糖類100質量部に対して、キサンタンガムの量が0.05〜0.001質量部の割合である医薬製剤の賦形剤として用いる水溶性糖類、
2.水溶性糖類を撹拌しながらキサンタンガム水溶液を噴霧して得られた上記1に記載の水溶性糖類、
3.粒子径が30〜200μmである上記1又は2に記載の水溶性糖類、
4.水溶性糖類が乳糖又はマンニトールである上記1に記載の水溶性糖類、
5.キサンタンガムで被覆された水溶性糖類であって、水溶性糖類100質量部に対して、キサンタンガムの量が0.05〜0.001質量部の割合である水溶性糖類を製剤全量に対して、30〜99.8質量%含有する圧縮成形製剤、
6.口腔内速崩壊性圧縮成形製剤である上記5に記載の圧縮成形製剤、
7.口腔内速崩壊性圧縮成形製剤の引張強度が1MPa以上で、口腔内崩壊時間が60秒以内である上記6に記載の圧縮成形製剤、
8.医薬成分を製剤全量に対して、0.2〜5質量%含有する上記5〜7の何れか一項に記載の圧縮成形製剤、
9.製剤中に、キサンタンガムで被覆された水溶性糖類以外の他の賦形剤を含む上記5〜8の何れか一項に記載の圧縮成形製剤、
10.製剤中に崩壊剤を含む上記5〜9の何れか一項に記載の圧縮成形製剤、
に関するものである。
That is, the present invention is 1. A water-soluble saccharide coated with xanthan gum, which is used as an excipient of a pharmaceutical preparation in which the amount of xanthan gum is 0.05 to 0.001 part by mass with respect to 100 parts by mass of the water-soluble saccharide. ,
2. The water-soluble saccharide according to 1 above, obtained by spraying an aqueous xanthan gum solution while stirring the water-soluble saccharide,
3. The water-soluble saccharide according to 1 or 2, wherein the particle diameter is 30 to 200 µm,
4). The water-soluble saccharide according to 1 above, wherein the water-soluble saccharide is lactose or mannitol,
5. 30 water-soluble saccharides coated with xanthan gum, wherein the amount of xanthan gum is 0.05 to 0.001 parts by mass with respect to 100 parts by mass of water-soluble saccharides based on the total amount of the preparation. A compression-molded preparation containing ˜99.8% by mass,
6). The compression-molded preparation according to 5 above, which is an intraoral rapidly disintegrating compression-molded preparation,
7). The compression-molded preparation according to 6 above, wherein the intraoral rapidly disintegrating compression-molded preparation has a tensile strength of 1 MPa or more and an oral disintegration time of 60 seconds or less.
8). The compression-molded preparation according to any one of 5 to 7 above, containing 0.2 to 5% by mass of a pharmaceutical ingredient relative to the total amount of the preparation,
9. The compression-molded preparation according to any one of 5 to 8 above, which contains an excipient other than the water-soluble saccharide coated with xanthan gum in the preparation,
10. The compression-molded preparation according to any one of 5 to 9 above, which contains a disintegrant in the preparation,
It is about.
本発明のキサンタンガム被覆水溶性糖類は、被覆前の水溶性糖類に比して、流動性及び成形圧縮性が格段に良くなり、打錠機の臼に一定量の粉末を連続的に充填することが可能であり、更に打錠時における不具合の発生を抑制し、均一な金型充てんが可能であり、それにより質量の均一な製剤を得ることができる。また、該被覆水溶性糖類を圧縮製剤の賦形剤としたとき、該製剤は適当な硬度を有し、優れた口腔内速崩壊性圧縮製剤とすることができる。 The xanthan gum-coated water-soluble saccharide of the present invention has significantly improved flowability and molding compressibility as compared with the water-soluble saccharide before coating, and continuously fills a die of a tableting machine with a certain amount of powder. Furthermore, the occurrence of problems during tableting can be suppressed, and uniform mold filling is possible, whereby a preparation with uniform mass can be obtained. In addition, when the coated water-soluble saccharide is used as an excipient of a compression preparation, the preparation has an appropriate hardness and can be an excellent intraoral rapidly disintegrating compression preparation.
本発明で使用される水溶性糖類は、医薬品使用される水溶性糖類であれば特に限定されないが、一般的に成形性が悪いことが知られている水溶性糖類が好ましい。また、本発明において、特に断らない限り「糖類」は糖アルコールも含む意味で使用する。また、水溶性とは、常温(25℃)で、少なくとも5質量%以上の溶解度を示すものであれば支障は無い。主として単糖類又は二糖類が挙げられ、乳糖又はD−マンニトールが好ましい。これらの糖類の粒度は特に限定されないが、錠剤などの圧縮製剤に使用することを考慮すると、平均粒子径が30μm以上が好ましく、200μm以下が好ましい。より好ましくはこれらの糖類の平均粒子径は30〜100μm程度である。乳糖の場合、更に好ましくは50〜100μm程度である。
上記の好ましい糖類の乳糖及びD−マンニトールには、複数の結晶形のものが存在するが、何れも使用可能である。例えば乳糖ではα−含水乳糖、α−無水乳糖及びβ−無水乳糖等の結晶形の異なるものがあるが、いずれでも使用可能であり、またこれらの混合物でも差し支えない。本発明においては乳糖としては通常乳糖水和物が使用される。また、D−マンニトールではα−及びβ−結晶、及びアモルファスが存在するがいずれでも使用可能であり、またこれらの混合物でも差し支えない。これらの乳糖は何れも市販の医薬品用グレードのものであればいずれも使用可能であり、例えば、グラニュラック(GranuLac)100(メグレジャパン株式会社)又はファルマトーゼ(Pharmatose)200M(DMV ジャパン株式会社)等が挙げられる。
本発明で使用されるキサンタンガムは医薬品用のグレードとして、市場で一般的に入手できるものであれば特に支障はない。例えばケルトロールRTMCG(三晶株式会社製)等を挙げることができる。
なお、本発明における圧縮成形製剤は錠剤などの圧縮成形した製剤を意味する。また、以下の説明において、部又は%は特に断りの無い限り、質量部又は質量%を表す。また、上付のRTMは登録商標を示す。
The water-soluble saccharide used in the present invention is not particularly limited as long as it is a water-soluble saccharide used for pharmaceuticals, but a water-soluble saccharide generally known to have poor moldability is preferable. In the present invention, unless otherwise specified, “saccharide” is used in the meaning including sugar alcohol. Water solubility is not a problem as long as it exhibits a solubility of at least 5% by mass at room temperature (25 ° C.). Mainly monosaccharides or disaccharides can be mentioned, and lactose or D-mannitol is preferred. The particle size of these saccharides is not particularly limited, but considering that they are used for compressed preparations such as tablets, the average particle size is preferably 30 μm or more, more preferably 200 μm or less. More preferably, the average particle size of these saccharides is about 30 to 100 μm. In the case of lactose, it is more preferably about 50 to 100 μm.
There are a plurality of crystal forms of lactose and D-mannitol, which are preferable sugars, and any of them can be used. For example, lactose includes α-hydrated lactose, α-anhydrolactose and β-anhydrolactose having different crystal forms, and any of them can be used, and a mixture thereof may be used. In the present invention, lactose hydrate is usually used as lactose. D-mannitol includes α- and β-crystals and amorphous, but any of them can be used, and a mixture thereof may be used. Any of these lactose can be used as long as it is a commercially available pharmaceutical grade, such as Granulac 100 (Megure Japan Co., Ltd.) or Pharmatose 200M (DMV Japan Ltd.). Is mentioned.
The xanthan gum used in the present invention is not particularly limited as long as it is generally available on the market as a pharmaceutical grade. For example, Celtrol RTM CG (manufactured by Sanki Co., Ltd.) can be used.
In addition, the compression molding formulation in this invention means the formulation formed by compression molding, such as a tablet. Moreover, in the following description, unless otherwise indicated, a part or% represents a mass part or mass%. The superscript RTM indicates a registered trademark.
本発明におけるキサンタンガムで被覆された水溶性糖類(以下キサンタンガム被覆糖類或いは被覆糖類ともいう)はたとえば、キサンタンガムを、水、アルコール(エチルアルコール)または水・アルコ−ル(エチルアルコール)の混合液、好ましくは水、又は、水とエチルアルコールの混合液、最も好ましくは水などの溶媒に溶解して、噴霧用溶液とし、湿式造粒機などを用いて、糖類粉末を撹拌しながら、この溶液を噴霧して、糖類粉末を被覆することにより得ることができる。
噴霧用溶液におけるキサンタンガムの濃度は、噴霧に支障の無い濃度であればよく、通常0.004〜0.04%程度であり、好ましくは0.008〜0.03%であり、より好ましくは0.01〜0.03%である。
噴霧条件は特に限定されないが、通常排気温度を30℃以上に維持することが好ましく、乾燥空気を、温度35〜80℃で、給気しながら、上記噴霧用溶液を、被覆量が目的量となるように噴霧すればよい。
糖類へのキサンタンガムの被覆量は糖類に対して、0.1%未満でよく、下限は0.001%以上、好ましくは0.002%以上であればよい。通常糖類に対して、0.002%〜0.05%程度であり、好ましくは0.002〜0.03%程度、より好ましくは0.004〜0.02%、更に好ましくは0.004〜0.015%程度である。このような微量で、糖類の流動性及び圧縮成形性が顕著に改善されることは全く驚くべきことであった。
該被覆後の糖類の大きさは、原料に使用した糖類の大きさとほとんど変わらない。従って、その好ましい平均粒子径は30μm以上、200μm以下であり、より好ましくは30〜100μm程度である。乳糖の場合、更に好ましくは50〜100μm程度である。
なお、本発明においては便宜的に、糖類がキサンタンガムで「被覆された」又は「キサンタンガム被覆糖類」等と「被覆」と表現するが、実際に上記のような糖類の微粒子が、錠剤をコーティング剤でコーティングするときのように、完全にキサンタンガムで被覆されているか否かは明確では無く、粒子の一部に付着している場合もあり得るが、本発明においてはそれらの場合も含めて、便宜的に「被覆」と記載する。
The water-soluble saccharide coated with xanthan gum in the present invention (hereinafter also referred to as xanthan gum-coated saccharide or coated saccharide) is, for example, xanthan gum, water, alcohol (ethyl alcohol), or a mixed solution of water and alcohol (ethyl alcohol), preferably Is dissolved in water or a mixture of water and ethyl alcohol, most preferably in a solvent such as water to form a spray solution, and this solution is sprayed while stirring the saccharide powder using a wet granulator or the like. Then, it can be obtained by coating saccharide powder.
The concentration of xanthan gum in the spray solution may be any concentration that does not hinder spraying, and is usually about 0.004 to 0.04%, preferably 0.008 to 0.03%, and more preferably 0. 0.01-0.03%.
Although the spraying conditions are not particularly limited, it is usually preferable to maintain the exhaust temperature at 30 ° C. or higher. While supplying dry air at a temperature of 35 to 80 ° C., the above-mentioned spray solution is coated with the target amount. What is necessary is just to spray.
The amount of xanthan gum coated on the saccharide may be less than 0.1% with respect to the saccharide, and the lower limit may be 0.001% or more, preferably 0.002% or more. Usually, it is about 0.002% to 0.05% with respect to saccharides, preferably about 0.002 to 0.03%, more preferably 0.004 to 0.02%, and still more preferably 0.004 to 0.04%. It is about 0.015%. It was quite surprising that such a small amount significantly improved the fluidity and compression moldability of sugars.
The size of the saccharide after coating is almost the same as the size of the saccharide used for the raw material. Therefore, the preferable average particle diameter is 30 micrometers or more and 200 micrometers or less, More preferably, it is about 30-100 micrometers. In the case of lactose, it is more preferably about 50 to 100 μm.
In the present invention, for convenience, saccharides are expressed as “coated” with xanthan gum or “xanthan gum-coated saccharides”, etc., and “coated”. It is not clear whether it is completely covered with xanthan gum, as in the case of coating with, and may be attached to a part of the particles. The term “coating” is used.
上記のようにして得られたキサンタンガム被覆糖類は、その流動性及び圧縮成形性が改善されているので、医薬用の賦形剤、特に錠剤などの圧縮成形製剤用の賦形剤として好適に使用すること出来る。特に、口腔内速崩壊性錠剤などの口腔内速崩壊性圧縮成形製剤用の賦形剤として、最適である。
キサンタンガム被覆糖類を賦形剤として、圧縮成形製剤を製造するには、通常の圧縮成形製剤を製造する場合と同様に、キサンタンガム被覆糖類、必要に応じて添加するその他の添加剤、及び医薬成分を、混合若しくは必要に応じて造粒して、圧縮成形用混合物とした後、常法により、錠剤等に圧縮成形すればよい。
Since the fluidity and compression moldability of the xanthan gum-coated saccharide obtained as described above are improved, it is suitably used as a pharmaceutical excipient, particularly as an excipient for compression-molded preparations such as tablets. I can do it. In particular, it is optimal as an excipient for an intraoral rapidly disintegrating compression-molded preparation such as an intraoral rapidly disintegrating tablet.
In order to produce a compression-molded preparation using xanthan gum-coated saccharide as an excipient, as in the case of producing a normal compression-molded preparation, xanthan gum-coated saccharide, other additives to be added as necessary, and pharmaceutical ingredients are added. Then, after mixing or granulating as necessary to obtain a mixture for compression molding, the mixture may be compression molded into a tablet or the like by a conventional method.
本発明の圧縮成形製剤は、キサンタンガム被覆糖類を、製剤全量に対して、通常30〜99.8質量%、好ましくは30〜80%含有する。
該圧縮成形製剤としては錠剤、丸剤等の圧縮成形製剤であれば何れも使用出来るが、口腔内速崩壊錠などの口腔内速崩壊性圧縮成形製剤が好ましい。
本発明の該圧縮成形製剤は賦形剤として、上記キサンタンガム被覆糖類以外の他の賦形剤を含んでもよく、通常他の賦形剤と併用される。他の賦形剤の含量は、本発明の効果が達成させる限り、限定はないが、賦形剤全量に対して、0〜50%程度であり、好ましくは、10〜40%程度である。
The compression-molded preparation of the present invention usually contains 30 to 99.8% by mass, preferably 30 to 80%, of xanthan gum-coated saccharide with respect to the total amount of the preparation.
Any compression-molded preparation such as tablets and pills can be used as the compression-molded preparation, but intraoral quick-disintegrating compression-molded preparations such as intraoral quick-disintegrating tablets are preferred.
The compression-molded preparation of the present invention may contain an excipient other than the xanthan gum-coated saccharide as an excipient, and is usually used in combination with another excipient. The content of other excipients is not limited as long as the effect of the present invention is achieved, but is about 0 to 50%, preferably about 10 to 40%, based on the total amount of the excipient.
他の賦形剤としては、圧縮成形製剤に使用されるものは何れも使用することが出来る。例えば、乳糖、白糖、マンニトール、キシリトール、エリスリトール、ソルビトール、マルチトール、クエン酸カルシウム、リン酸カルシウム、結晶セルロース又はメタケイ酸アルミン酸マグネシウムなどを使用することができる。これらは一種であっても、二種以上であってもよい。本発明のキサンタンガム被覆糖類と併用する賦形剤としては、乳糖がより好ましい。 As other excipients, any of those used in compression-molded preparations can be used. For example, lactose, sucrose, mannitol, xylitol, erythritol, sorbitol, maltitol, calcium citrate, calcium phosphate, crystalline cellulose, magnesium aluminate metasilicate, or the like can be used. These may be one kind or two or more kinds. As an excipient used in combination with the xanthan gum-coated saccharide of the present invention, lactose is more preferable.
本発明の圧縮成形製剤が口腔内速崩壊錠などの口腔内速崩壊性圧縮成形製剤の場合、必ずしも崩壊剤を必要としないが、崩壊性を早める時には、崩壊剤を含む方が好ましい。崩壊剤の製剤全体に対する含量は、希望する崩壊性にもよるので一概にはいえないが、通常0〜5%程度で充分であり、0.5〜4%程度がより好ましく、0.5〜3%程度が更に好ましい。
通常口腔内速崩壊性圧縮成形製剤の場合、口腔内の唾液のみで90秒以内、好ましくは60秒以内に崩壊するものを言うが、本発明においては、60秒以内、好ましくは30秒以内で口腔内で崩壊する口腔内速崩壊性圧縮成形製剤とすることができる。
崩壊剤としては、トウモロコシデンプン、馬鈴薯デンプン、カルボキシメチルスターチナトリウム、部分アルファ化デンプン、カルボキシメチルセルロースカルシウム、カルボキシメチルセルロース、低置換度ヒドロキシプロピルセルロース、架橋カルボキシメチルセルロースナトリウム、架橋ポリビニルピロリドンなどを使用することができる。
When the compression-molded preparation of the present invention is an intraoral rapidly disintegrating compression-molded preparation such as an intraoral rapidly disintegrating tablet, a disintegrant is not necessarily required. However, when the disintegration is accelerated, it is preferable to include a disintegrant. The content of the disintegrant with respect to the whole preparation depends on the desired disintegration property, but it cannot be said unconditionally. However, about 0 to 5% is usually sufficient, about 0.5 to 4% is more preferable, 0.5 to About 3% is more preferable.
Usually, in the case of an intraoral rapidly disintegrating compression-molded preparation, it refers to those that disintegrate within 90 seconds, preferably within 60 seconds, only within the oral saliva, but in the present invention, within 60 seconds, preferably within 30 seconds. An intraoral rapidly disintegrating compression molding preparation that disintegrates in the oral cavity can be obtained.
As a disintegrating agent, corn starch, potato starch, carboxymethyl starch sodium, partially pregelatinized starch, carboxymethylcellulose calcium, carboxymethylcellulose, low-substituted hydroxypropylcellulose, crosslinked carboxymethylcellulose sodium, crosslinked polyvinylpyrrolidone, etc. can be used. .
本発明の圧縮成形製剤に使用される医薬成分は経口投与可能な薬物であれば任意の薬物を含有させることができ、その種類は特に限定されない。
以下に含有可能な薬物の例を挙げる。
解熱鎮痛消炎剤:例えば、インドメタシン、アセチルサリチル酸、ジクロフェナックナトリウム、ケトプロフェン、イブプロフェン、メフェナム酸、アズレン、フェナセチン、イソプロピルアンチピリン、アセトアミノフェノン、ベンザダック、フェニルブタゾン、フルフェナム酸、サリチル酸ナトリウム、サリチルアミド、サザピリン、エトドラクなど、
ステロイド系抗炎症剤:例えば、デキサメタゾン、ヒドロコルチゾン、プレドニゾロン、トリアムシノロンなど、
抗潰瘍剤:例えば、エカベトナトリウム、エンプロスチル、スルピリド、塩酸セトラキサート、ゲファルナート、マレイン酸イルソグラジン、シメチジン、塩酸ラニチジン、ファモチジン、ニザチジン、塩酸ロキサチジンアセテート、オメプラゾール、ランソプラゾールなど、
冠血管拡張剤:例えば、リスペリドン、硝酸イソソルビド、塩酸ジルチアゼム、トラピジル、ジピリダモール、塩酸ジラゼプ、ベラパミル、ニカルジピン、塩酸ニカルジピン、塩酸ベラパミルなど、
The pharmaceutical ingredient used in the compression-molded preparation of the present invention can contain any drug as long as it is a drug that can be administered orally, and the type thereof is not particularly limited.
Examples of drugs that can be contained are given below.
Antipyretic analgesics: for example, indomethacin, acetylsalicylic acid, diclofenac sodium, ketoprofen, ibuprofen, mefenamic acid, azulene, phenacetin, isopropylantipyrine, acetaminophenone, benzadac, phenylbutazone, flufenamic acid, sodium salicylate, salicylamide, sazapyrine, Etodolac etc.
Steroidal anti-inflammatory agents: for example, dexamethasone, hydrocortisone, prednisolone, triamcinolone,
Anti-ulcer agents: for example, ecabet sodium, enprostil, sulpiride, cetraxate hydrochloride, gefarnate, irsogladine maleate, cimetidine, ranitidine hydrochloride, famotidine, nizatidine, loxatidine acetate, omeprazole, lansoprazole, etc.
Coronary vasodilators: for example, risperidone, isosorbide nitrate, diltiazem hydrochloride, trapidil, dipyridamole, dilazep hydrochloride, verapamil, nicardipine, nicardipine hydrochloride, verapamil hydrochloride, etc.
末梢血管拡張剤:例えば、酒石酸イフェンプロジル、マレイン酸シネパジド、シクランデレート、シンナリジン、ペントキシフィリンなど、
抗生物質:例えば、アンピシリン、アモキシリン、セファレキシン、エチルコハク酸エリスロマイシン、塩酸バカンピシリン、塩酸ミノサイクリン、クロラルフェニコール、テトラサイクリン、エリスロマイシン、セフタジジム、セフロキシムナトリウム、アスポキシシリン、リチペネムアコキシル水和物など、
合成抗菌剤:例えば、ナリジクス酸、ピロミド酸、ピペミド酸三水和物、エノキサシン、シノキサシン、オフロキサシン、ノルフロキサシン、塩酸シプロフロキサシン、スルファメトキサゾール・トリメトプリムなど、
抗ウイルス剤:例えば、アシクロビル、ガンシクロビルなど、
鎮けい剤:例えば、臭化プロパンテリン、硫酸アトロピン、臭化オキサピウム、臭化チメピジウム、臭化ブチルスコポラミン、塩化トロスピウム、臭化ブトロピウム、N−メチルスコポラミンメチル硫酸、臭化メチルオクタトロピンなど、
鎮咳剤:例えば、ヒベンズ酸チペピジン、塩酸メチルエフェドリン、リン酸コデイン、トラニラスト、臭化水素酸デキストロメトルファン、リン酸ジメモルファン、塩酸クロブチノール、塩酸ホミノベン、リン酸ベンプロペリン、塩酸エプラジノン、塩酸クロフェダノール、塩酸エフェドリン、ノスカピン、クエン酸ペントキシベリン、クエン酸オキセラジン、クエン酸イソアミニルなど、
去たん剤:例えば、塩酸ブロムヘキシン、カルボシステイン、塩酸エチルシステイン、塩酸メチルシステインなど、
Peripheral vasodilators: for example, ifenprodil tartrate, cinepazide maleate, cyclandrate, cinnarizine, pentoxifylline, etc.
Antibiotics: for example, ampicillin, amoxiline, cephalexin, erythromycin ethyl succinate, bacampicillin hydrochloride, minocycline hydrochloride, chloralphenicol, tetracycline, erythromycin, ceftazidime, cefuroxime sodium, aspoxicillin, ritipenecoxil hydrate, etc.
Synthetic antibacterial agents: for example, nalidixic acid, pyromic acid, pipemidic acid trihydrate, enoxacin, sinoxacin, ofloxacin, norfloxacin, ciprofloxacin hydrochloride, sulfamethoxazole, trimethoprim, etc.
Antiviral agents: for example, acyclovir, ganciclovir, etc.
Antispasmodic: for example, propantheline bromide, atropine sulfate, oxapium bromide, timepidium bromide, butyl scopolamine bromide, trospium chloride, butropium bromide, N-methyl scopolamine methyl sulfate, methyl octatropine bromide, etc.
Antitussives: for example, tipepidine hibenzate, methylephedrine hydrochloride, codeine phosphate, tranilast, dextromethorphan hydrobromide, dimemorphan phosphate, clobutinol hydrochloride, hominoben hydrochloride, benproperin phosphate, eprazinone hydrochloride, clofedanol hydrochloride, hydrochloric acid Ephedrine, noscapine, pentoxyberine citrate, oxerazine citrate, isoaminyl citrate, etc.
Desiccant: For example, bromhexine hydrochloride, carbocysteine, ethylcysteine hydrochloride, methylcysteine hydrochloride, etc.
気管支拡張剤:例えば、テオフィリン、アミノフィリン、クロモグリク酸ナトリウム、塩酸プロカテロール、塩酸トリメトキノール、ジプロフィリン、硫酸サルブタモール、塩酸クロルプレナリン、フマル酸ホルモテロール、硫酸オルシプレナリン、塩酸ピルブテロール、硫酸ヘキソプレナリン、メシル酸ビトルテロール、塩酸クレンブテロール、硫酸テルブタリン、塩酸マブテロール、臭化水素酸フェノテロール、塩酸メトキシフェナミンなど、
強心剤:例えば、塩酸ドパミン、塩酸ドブタミン、ドカルパミン、デノパミン、カフェイン、ジゴキシン、ジギトキシン、ユビデカレノンなど;
利尿剤:例えば、フロセミド、アセタゾラミド、トリクロルメチアジド、メチクロチアジド、ヒドロクロロチアジド、ヒドロフルメチアジド、エチアジド、シクロペンチアジド、スピロノラクトン、トリアムテレン、フロロチアジド、ピレタニド、メフルシド、エタクリン酸、アゾセミド、クロフェナミドなど、
筋弛緩剤:例えば、カルバミン酸クロルフェネシン、塩酸トルペリゾン、塩酸エペリゾン、塩酸チザニジン、メフェネシン、クロルゾキサゾン、フェンプロバメート、メトカルバモール、クロルメザノン、メシル酸プリジノール、アフロクアロン、バクロフェン、ダントロレンナトリウムなど、
脳代謝改善剤:例えば、ニセルゴリン、塩酸メクロフェノキセート、タルチレリンなど、
マイナートランキライザー:例えば、オキサゾラム、ジアゼパム、クロチアゼパム、メダゼパム、テマゼパム、フルジアゼパム、メプロバメート、ニトラゼパム、クロルジアゼポキシドなど、
Bronchodilators: for example, theophylline, aminophylline, sodium cromoglycate, procaterol hydrochloride, trimethoquinol hydrochloride, diprofilin, salbutamol sulfate, chlorprenalin hydrochloride, formoterol fumarate, orciprenaline sulfate, pyrbuterol hydrochloride, hexoprenalin sulfate, vitorterol sulfate, hydrochloric acid Clenbuterol, terbutaline sulfate, mabuterol hydrochloride, fenoterol hydrobromide, methoxyphenamine hydrochloride, etc.
Cardiotonic agents: for example, dopamine hydrochloride, dobutamine hydrochloride, docarpamine, denopamine, caffeine, digoxin, digitoxin, ubidecarenone, etc .;
Diuretics: for example, furosemide, acetazolamide, trichloromethiazide, meticlothiazide, hydrochlorothiazide, hydroflumethiazide, ethiazide, cyclopenthiazide, spironolactone, triamterene, furothiazide, pyrethanide, mefluside, ethacrynic acid, azosemide, clofenamide, etc.
Muscle relaxants: for example, chlorphenesin carbamate, tolperisone hydrochloride, eperisone hydrochloride, tizanidine hydrochloride, mefenesin, chlorzoxazone, phenprobamate, metcarbamol, chlormezanone, pridinol mesylate, afroqualone, baclofen, dantrolene sodium, etc.
Brain metabolism improving agent: For example, nicergoline, meclofenoxate hydrochloride, tartilelin, etc.
Minor tranquilizers: For example, oxazolam, diazepam, clothiazepam, medazepam, temazepam, fludiazepam, meprobamate, nitrazepam, chlordiazepoxide, etc.
メジャートランキライザー:例えば、スルピリド、塩酸クロカプラミン、ゾテピン、クロルプロマジン、ハロペリドールなど、
β−ブロッカー:例えば、フマル酸ビソプロロール、ピンドロール、塩酸プロブラノロール、塩酸カルテオロール、酒石酸メトプロロール、塩酸ラベタノール、塩酸アセブトロール、塩酸ブフェトロール、塩酸アルプレノロール、塩酸アロチノロール、塩酸オクスプレノロール、ナドロール、塩酸ブクモロール、塩酸インデノロール、マレイン酸チモロール、塩酸ベフノロール、塩酸ブプラノロールなど、
抗不整脈剤:例えば、塩酸プロカインアミド、ジソピラミド、アジマリン、硫酸キニジン、塩酸アプリンジン、塩酸プロパフェノン、塩酸メキシレチン、塩酸アジミライドなど、 痛風治療剤:例えば、アロプリノール、プロベネシド、コルヒチン、スルフィンピラゾン、ベンズブロマロン、ブコロームなど、
Major tranquilizers: for example, sulpiride, clocapramine hydrochloride, zotepine, chlorpromazine, haloperidol, etc.
β-blocker: for example, bisoprolol fumarate, pindolol, probranolol hydrochloride, carteolol hydrochloride, metoprolol tartrate, rabetanol hydrochloride, acebutol hydrochloride, bubutolol hydrochloride, alprenolol hydrochloride, arotinolol hydrochloride, oxprenolol hydrochloride, nadolol, Bucmolol hydrochloride, indenolol hydrochloride, timolol maleate, befnolol hydrochloride, bupranolol hydrochloride, etc.
Antiarrhythmic agents: for example, procainamide hydrochloride, disopyramide, azimarin, quinidine sulfate, aprindine hydrochloride, propaphenone hydrochloride, mexiletine hydrochloride, azimiride hydrochloride, etc. Gout treatments: for example, allopurinol, probenecid, colchicine, sulfinpyrazone, benzbromarone , Bucolome, etc.
血液凝固阻止剤:例えば、塩酸チクロピジン、ジクマロール、ワルファリンカリウム、(2R、3R)−3−アセトキシ−5−〔2−(ジメチルアミノ)エチル〕−2、3−ジヒドロ−8−メチル−2−(4−メチルフェニル)−1、5−ベンゾチアゼピン−4(5H)−オン・マレイン酸塩など、
血栓溶解剤:例えば、メチル(2E、3Z)−3−ベンジリデン−4−(3、5−ジメトキシ−α−メチルベンジリデン)−N−(4−メチルピペラジン−1−イル)スクシナメート・塩酸塩など、
肝臓疾患用剤:例えば、(±)r−5−ヒドロキシメチル−t−7−(3、4−ジメトキシフェニル)−4−オキソ−4、5、6、7−テトラヒドロベンゾ〔b〕フラン−c−6−カルボン酸ラクトンなど、
抗てんかん剤:例えば、フェニトイン、バルプロ酸ナトリウム、メタルピタール、カルバマゼピンなど、
Anticoagulant: for example, ticlopidine hydrochloride, dicoumarol, warfarin potassium, (2R, 3R) -3-acetoxy-5- [2- (dimethylamino) ethyl] -2, 3-dihydro-8-methyl-2- ( 4-methylphenyl) -1,5-benzothiazepine-4 (5H) -one maleate,
Thrombolytic agent: For example, methyl (2E, 3Z) -3-benzylidene-4- (3,5-dimethoxy-α-methylbenzylidene) -N- (4-methylpiperazin-1-yl) succinamate hydrochloride
Liver disease agent: For example, (±) r-5-hydroxymethyl-t-7- (3,4-dimethoxyphenyl) -4-oxo-4,5,6,7-tetrahydrobenzo [b] furan-c -6-carboxylic acid lactone, etc.
Antiepileptic agents: for example, phenytoin, sodium valproate, metal pital, carbamazepine, etc.
抗ヒスタミン剤:例えば、マレイン酸クロルフェニラミン、フマル酸クレマスチン、メキタジン、酒石酸アリメマジン、塩酸サイクロヘブタジン、ベシル酸ベポタスチンなど、
鎮吐剤:例えば、塩酸ジフェニドール、メトクロプラミド、ドンペリドン、メシル酸ベタヒスチン、マレイン酸トリメブチンなど、
降圧剤:例えば、塩酸レセルピン酸ジメチルアミノエチル、レシナミン、メチルドパ、塩酸プラロゾシン、塩酸ブナゾシン、塩酸クロニジン、ブドララジン、ウラピジル、N−〔6−〔2−〔(5−ブロモ−2−ピリミジニル)オキシ〕エトキシ〕−5−(4−メチルフェニル)−4−ピリミジニル〕−4−(2−ヒドロキシ−1、1−ジメチルエチル)ベンゼンスルホンアミド・ナトリウム塩など、
高脂血症用剤:例えば、プラバスタチンナトリウム、フルバスタチンナトリウムなど、
交感神経興奮剤:例えば、メシル酸ジヒドロエルゴタミン、塩酸イソプロテレノール、塩酸エチレフリンなど、
経口糖尿病治療剤:例えば、グリベングラミド、トルブタミド、グリミジンナトリウムなど、
経口抗癌剤:例えば、マリマスタットなど、
アルカロイド系麻薬:例えば、モルヒネ、コデイン、コカインなど);
ビタミン剤:例えば、ビタミンB1、ビタミンB2、ビタミンB6、ビタミンB12、ビタミンC、葉酸など、
頻尿治療剤:例えば、塩酸フラボキサート、塩酸オキシブチニン、塩酸テロリジンなど、
アンジオテンシン変換酵素阻害剤:例えば、塩酸イミダプリル、マレイン酸エナラプリル、アラセプリル、塩酸デラプリルなど、
抗精神薬:例えば、アリピプラゾール、塩酸クロルプロマジン、塩酸アミトリプチリン、ネモナプリド、ハロペリドール、塩酸モペロン、ペルフェナジン、ジアゼパム、ロラゼパム、クロルジアゼポキシド、メチルフェニデート、ミルナシプラン、リスペリドン、バルプロ酸ナトリウムなどを挙げることができる。
Antihistamines: for example, chlorpheniramine maleate, clemastine fumarate, mequitazine, alimemazine tartrate, cyclohebutazine hydrochloride, bepotastine besylate,
Antiemetics: for example, diphenidol hydrochloride, metoclopramide, domperidone, betahistine mesylate, trimebutine maleate, etc.
Antihypertensive agents: for example, dimethylaminoethyl reserpine hydrochloride, resinamine, methyldopa, prarozocine hydrochloride, bunazosin hydrochloride, clonidine hydrochloride, budrarazine, urapidil, N- [6- [2-[(5-bromo-2-pyrimidinyl) oxy] ethoxy ] -5- (4-methylphenyl) -4-pyrimidinyl] -4- (2-hydroxy-1,1-dimethylethyl) benzenesulfonamide, sodium salt, etc.
Hyperlipidemia agent: For example, pravastatin sodium, fluvastatin sodium, etc.
Sympathomimetic agents: for example, dihydroergotamine mesylate, isoproterenol hydrochloride, ethylephrine hydrochloride,
Oral diabetes treatment agent: For example, glibengramide, tolbutamide, grimidine sodium, etc.
Oral anticancer agent: For example, marimastat
Alkaloid narcotics: for example, morphine, codeine, ***e, etc.);
Vitamin preparations: For example, vitamin B1, vitamin B2, vitamin B6, vitamin B12, vitamin C, folic acid, etc.
Frequent urine treatment agent: For example, flavoxate hydrochloride, oxybutynin hydrochloride, terroridine hydrochloride, etc.
Angiotensin converting enzyme inhibitor: For example, imidapril hydrochloride, enalapril maleate, alaspril, delapril hydrochloride, etc.
Antipsychotics: For example, aripiprazole, chlorpromazine hydrochloride, amitriptyline hydrochloride, nemonapride, haloperidol, moperone hydrochloride, perphenazine, diazepam, lorazepam, chlordiazepoxide, methylphenidate, milnacipran, risperidone, sodium valproate and the like.
上記の医薬成分は、圧縮成形用の混合物を得るまでの製造段階の何れの段階で添加してもよい。通常は、圧縮成形用の混合物を得る段階で、該医薬成分を添加して、本発明のキサンタンガム被覆糖類などと共に均一に混合するのが好ましい。また、該医薬成分は、上記の混合前の段階で、必要に応じて、予め、賦形剤等と造粒したもの(混合用造粒物)であっても、また、医薬成分の放出の制御、味のマスキング、遮光、プロテクト(他の賦形剤との接触防止)、防湿などの目的のために、医薬成分自体若しくは上記の混合用造粒物をコーティングしたものであってもよい。
本発明の圧縮成形製剤における医薬成分の含量は、医薬成分により異なるので、一概にはいえないが、製剤全量に対して、0.01〜10%程度であり、好ましくは、0.2〜5%程度である。
上記医薬成分は通常ある程度細かい方がよく、平均粒子径1μm〜200μm程度が好ましく、1〜100μm程度がより好ましい。
The above pharmaceutical ingredients may be added at any stage of the production stage until a mixture for compression molding is obtained. Usually, it is preferable to add the pharmaceutical ingredients and uniformly mix with the xanthan gum-coated saccharide of the present invention at the stage of obtaining a mixture for compression molding. In addition, the pharmaceutical component may be a product (granulated product for mixing) previously granulated with an excipient or the like, if necessary, at the stage before mixing, or may release the pharmaceutical component. For the purposes of control, taste masking, light shielding, protection (preventing contact with other excipients), moisture prevention, and the like, the pharmaceutical ingredients themselves or the above-mentioned granulated product for mixing may be coated.
Since the content of the pharmaceutical ingredient in the compression-molded preparation of the present invention varies depending on the pharmaceutical ingredient, it cannot be generally stated, but it is about 0.01 to 10%, preferably 0.2 to 5% with respect to the total amount of the preparation. %.
The medicinal component is usually finer to a certain degree, and the average particle size is preferably about 1 μm to 200 μm, more preferably about 1 to 100 μm.
上記のコーティングに用いるコーティング剤は、任意のものを使用することができる。具体的には、必要に応じて、水溶性高分子、水不溶性高分子、腸溶性高分子、胃溶性高分子、疎水性有機化合物などのコーティング剤を適宜選択して使用することができる。また上記のコーティング層は、1層のみならず、2層以上から構成されていてもよい。
水溶性高分子の例としては、(1)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などの水溶性セルロースエーテル;(2)ポリビニルピロリドン、ポリビニルアルコールなどの水溶性ポリビニル誘導体;及び(3)ポリエチレングリコール、ポリプロピレングリコールなどのアルキレンオキシド重合体を挙げることができる。
Arbitrary things can be used for the coating agent used for said coating. Specifically, a coating agent such as a water-soluble polymer, a water-insoluble polymer, an enteric polymer, a gastric polymer, and a hydrophobic organic compound can be appropriately selected and used as necessary. Moreover, said coating layer may be comprised not only from 1 layer but 2 layers or more.
Examples of water-soluble polymers include: (1) water-soluble cellulose ethers such as methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose; (2) water-soluble polyvinyl derivatives such as polyvinyl pyrrolidone and polyvinyl alcohol; and (3) polyethylene glycol, Mention may be made of alkylene oxide polymers such as polypropylene glycol.
水不溶性高分子の例としては、(1)エチルセルロースなどの水不溶性セルロースエーテル;及び(2)アクリル酸エチル・メタクリル酸メチル・メタクリル酸塩化トリメチルアンモニウムエチル共重合体(例えば、商品名:オイドラギットRS、レーム・ファーマ製)、メタクリル酸メチル・アクリル酸エチル共重合体(例えば、商品名:オイドラギットNE30D、レーム・ファーマ製)などの水不溶性アクリル酸系共重合体を挙げることができる。
腸溶性高分子の例としては、(1)ヒドロキシプロピルメチルセルロースアセテートサクシネート、ヒドロキシプロピルメチルセルロースフタレート、ヒドロキシメチルエチルセルロースフタレート、セルロースアセテートフタレート、セルロースアセテートサクシネート、セルロースアセテートマレエート、セルロースベンゾェートフタレート、セルロースプロピオネートフタレート、メチルセルロースフタレート、カルボキシメチルエチルセルロース、エチルヒドロキシエチルセルロースフタレートなど)などの腸溶性セルロース誘導体;(2)スチレン・アクリル酸共重合体、アクリル酸メチル・アクリル酸共重合体、アクリル酸メチル・メタクリル酸共重合体、アクリル酸ブチル・スチレン・アクリル酸共重合体、メタクリル酸・メタクリル酸メチル共重合体(例えば、商品名:オイドラギットL100、オイドラギットS、いずれもレーム・ファーマ社製)、メタクリル酸・アクリル酸エチル共重合体(例えば、商品名:オイドラギットL100−55、レーム・ファーマ社製)、アクリル酸メチル・メタクリル酸・アクリル酸オクチル共重合体などの腸溶性アクリル酸系共重合体;(3)酢酸ビニル・マレイン酸無水物共重合体、スチレン・マレイン酸無水物共重合体、スチレン・マレイン酸モノエステル共重合体、ビニルメチルエーテル・マレイン酸無水物共重合体、エチレン・マレイン酸無水物共重合体、ビニルブチルエーテル・マレイン酸無水物共重合体、アクリロニトリル・アクリル酸メチル・マレイン酸無水物共重合体、アクリル酸ブチル・スチレン・マレイン酸無水物共重合体などの腸溶性マレイン酸系共重合体;(4)ポリビニルアルコールフタレート、ポリビニルアセタールフタレート、ポリビニルブチレートフタレート、ポリビニルアセトアセタールフタレートなどの腸溶性ポリビニル誘導体を挙げることができる。
Examples of water-insoluble polymers include (1) water-insoluble cellulose ethers such as ethyl cellulose; and (2) ethyl acrylate / methyl methacrylate / methacrylated trimethylammonium ethyl copolymer (for example, trade name: Eudragit RS, And water-insoluble acrylic copolymers such as methyl methacrylate / ethyl acrylate copolymer (for example, trade name: Eudragit NE30D, manufactured by Rame Pharma).
Examples of enteric polymers include (1) hydroxypropyl methylcellulose acetate succinate, hydroxypropylmethylcellulose phthalate, hydroxymethylethylcellulose phthalate, cellulose acetate phthalate, cellulose acetate succinate, cellulose acetate maleate, cellulose benzoate phthalate, cellulose pro Enteric cellulose derivatives such as pionate phthalate, methylcellulose phthalate, carboxymethylethylcellulose, ethylhydroxyethylcellulose phthalate); (2) styrene / acrylic acid copolymer, methyl acrylate / acrylic acid copolymer, methyl acrylate / methacrylic acid Acid copolymer, butyl acrylate / styrene / acrylic acid copolymer, methacrylic acid / Methyl crylate copolymer (for example, trade name: Eudragit L100, Eudragit S, both manufactured by Laem Pharma), methacrylic acid / ethyl acrylate copolymer (for example, trade name: Eudragit L100-55, Laem Pharma) Enteric acrylic copolymer such as methyl acrylate / methacrylic acid / octyl acrylate copolymer; (3) vinyl acetate / maleic anhydride copolymer, styrene / maleic anhydride copolymer Styrene / maleic acid monoester copolymer, vinyl methyl ether / maleic anhydride copolymer, ethylene / maleic anhydride copolymer, vinyl butyl ether / maleic anhydride copolymer, acrylonitrile / methyl acrylate・ Maleic anhydride copolymer, butyl acrylate, styrene, male Enteric maleic acid copolymer, such as phosphate anhydride copolymer; (4) polyvinyl alcohol phthalate, polyvinyl acetal phthalate, polyvinyl butylate phthalate, may be mentioned enteric polyvinyl derivatives such as polyvinyl acetal phthalate.
胃溶性高分子の例としては、(1)ポリビニルアセタールジエチルアミノアセテートなどの胃溶性ポリビニル誘導体;及び(2)メタアクリル酸メチル・メタクリル酸ブチル・メタクリル酸ジメチルアミノエチル共重合体(例えば、商品名:オイドラギットE、レーム・ファーマ製)などの胃溶性アクリル酸系共重合体を挙げることができる。
疎水性有機化合物の例としては、(1)ステアリン酸、ラウリン酸、ミリスチン酸、パルミチン酸、ベヘン酸などの高級脂肪酸;(2)ラウリルアルコール、ミリスチルアルコール、セチルアルコール、ステアリルアルコール、ベヘニルアルコールなどの高級アルコール;(3)ステアリン酸トリグリセリド、ミリスチン酸トリグリセリド、パルミチン酸トリグリセリド、ラウリン酸トリグリセリドなどの高級脂肪酸のトリグリセリド;及び(4)硬化ひまし油、硬化ヤシ油、牛脂などの水素添加されていてもよい天然油脂を挙げることができる。
Examples of the gastric polymer include (1) gastrosoluble polyvinyl derivatives such as polyvinyl acetal diethylaminoacetate; and (2) methyl methacrylate / butyl methacrylate / dimethylaminoethyl methacrylate copolymer (for example, trade name: Gastric soluble acrylic acid copolymers such as Eudragit E, manufactured by Rohm Pharma).
Examples of hydrophobic organic compounds include (1) higher fatty acids such as stearic acid, lauric acid, myristic acid, palmitic acid, and behenic acid; (2) higher fatty acids such as lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, and behenyl alcohol. (3) higher fatty acid triglycerides such as stearic acid triglyceride, myristic acid triglyceride, palmitic acid triglyceride, lauric acid triglyceride; and (4) hydrogenated natural fats and oils such as hardened castor oil, hardened coconut oil, and beef tallow. Can be mentioned.
上記の医薬成分のコーティング層には、上記のようなコーティング剤成分のほか、必要に応じて着色剤、隠蔽剤、可塑剤、滑沢剤などの種々の添加剤を更に含有させることができる。このような着色剤としては、食用色素、レーキ色素、カラメル、カロチン、アナット、コチニール、三二酸化鉄などに加えて、レーキ色素とシロップを主体とした不透明着色剤オパラックス(OPALUX)などを挙げることができる。具体的には食用赤色2号、3号、黄色4号、5号、緑色3号、青色1号、2号、紫1号などの食用アルミニウムレーキ、アナット(ベニノキ由来の天然色素)、カルミン(カルミン酸アルミニウム塩)、パールエッセンス(グアニンを主成分とする)などを使用することができる。隠蔽剤としては、二酸化チタン、沈降炭酸カルシウム、リン酸水素カルシウム、硫酸カルシウムなどを使用することができる。可塑剤としては、ジエチルフタレート、ジブチルフタレート、ブチルフタリルブチルグリコレートなどのフタル酸誘導体のほか、シリコン油、クエン酸トリエチル、アセチルクエン酸トリエチル、トリアセチン、プロピレングリコール、ポリエチレングリコール、セタノール、モノステアリン酸グリセリンなどを使用することができる。また滑沢剤としては、ステアリン酸マグネシウム、タルク、合成ケイ酸マグネシウム、微粒子性酸化ケイ素、ショ糖脂肪酸エステルなどを使用することができる。 In addition to the coating agent component as described above, the pharmaceutical component coating layer may further contain various additives such as a colorant, a masking agent, a plasticizer, and a lubricant as necessary. Examples of such colorants include edible pigments, lake pigments, caramel, carotene, anat, cochineal, iron sesquioxide and the like, as well as opaque colorant Opalux (OPALUX) mainly composed of lake pigments and syrup. it can. Specifically, edible aluminum lakes such as edible red No. 2, No. 3, yellow No. 4, No. 5, green No. 3, blue No. 1, No. 2, purple No. 1, etc. Carminic acid aluminum salt), pearl essence (based on guanine) and the like can be used. As the masking agent, titanium dioxide, precipitated calcium carbonate, calcium hydrogen phosphate, calcium sulfate and the like can be used. Plasticizers include phthalic acid derivatives such as diethyl phthalate, dibutyl phthalate, and butyl phthalyl butyl glycolate, as well as silicone oil, triethyl citrate, triethyl acetyl citrate, triacetin, propylene glycol, polyethylene glycol, cetanol, and monostearic acid. Glycerin or the like can be used. As the lubricant, magnesium stearate, talc, synthetic magnesium silicate, particulate silicon oxide, sucrose fatty acid ester and the like can be used.
本発明の圧縮成形製剤には、上記賦形剤、崩壊剤及び医薬成分以外の添加剤として、必要に応じて、結合剤、滑沢剤又は流動化剤、界面活性剤、香料、着色剤、甘味剤、溶解補助剤などを含有させることができる。このような添加剤としては、製造される製剤の服用性、硬度、崩壊時間に悪影響を及ぼさない範囲で任意のものを使用することができる。
結合剤としては、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、ポリエチレングリコール、デキストリン、アルファー化デンプンなどを使用することができる。
滑沢剤又は流動化剤としては、ステアリン酸マグネシウム、ステアリン酸カルシウム、タルク、軽質無水ケイ酸、含水二酸化ケイ素などを使用することができる。
界面活性剤としては、リン脂質、グリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、ポリオキシエチレン脂肪酸エステル、ポリエチレングリコール脂肪酸エステル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンアルキルエーテル、庶糖脂肪酸エステルなどを使用することができる。
香料としては、マスカット、オレンジ油、ウイキョウ油、ケイヒ油、チョウジ油、テレピン油、ハッカ油、ユーカリ油、メントールを使用することができる。
着色剤としては、食用赤色2号、3号、食用黄色4号、5号、食用緑色3号、食用青色1号、2号、これらのアルミニウムレーキ、三二酸化鉄、黄色三二酸化鉄などを使用することができる。
甘味剤としては、サッカリン、アスパルテーム、アセスルファムカリウム、スクラロース、グリチルリチン酸モノアンモニウム、ソーマチン、などを使用することができる。
溶解補助剤としては、シクロデキストリン、アルギニン、リジン、トリスアミノメタンなどを使用することができる。
In the compression-molded preparation of the present invention, as additives other than the above excipients, disintegrants and pharmaceutical ingredients, a binder, a lubricant or a fluidizing agent, a surfactant, a fragrance, a colorant, Sweetening agents, solubilizing agents, and the like can be included. As such an additive, any additives can be used as long as they do not adversely affect the dosage, hardness, and disintegration time of the preparation to be produced.
As the binder, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, polyethylene glycol, dextrin, pregelatinized starch and the like can be used.
As the lubricant or fluidizing agent, magnesium stearate, calcium stearate, talc, light anhydrous silicic acid, hydrous silicon dioxide and the like can be used.
As the surfactant, phospholipid, glycerin fatty acid ester, sorbitan fatty acid ester, polyoxyethylene fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, sucrose fatty acid ester, etc. may be used. it can.
As the fragrance, muscat, orange oil, fennel oil, cinnamon oil, clove oil, turpentine oil, mint oil, eucalyptus oil and menthol can be used.
As the colorant, edible red No. 2, 3, edible yellow No. 4, 5, edible green No. 3, edible blue No. 1, No. 2, these aluminum lakes, ferric oxide, yellow ferric oxide, etc. are used. can do.
As the sweetening agent, saccharin, aspartame, acesulfame potassium, sucralose, monoammonium glycyrrhizinate, thaumatin, and the like can be used.
As the solubilizing agent, cyclodextrin, arginine, lysine, trisaminomethane and the like can be used.
本発明の圧縮成形製剤の製造において、キサンタンガム被覆糖類、必要に応じて添加するその他の添加剤、及び医薬成分を含む圧縮成形用混合物を得る際の混合は、一般に用いられる混合方法をそのまま使用することが出来る。
例えば、拡散式混合機(W型混合機、V型混合機など)を用いて、均一に混合すればよい。また、必要に応じてそれらの混合前に倍散混合、篩過倍散混合などの前処理をしても良い。他には、バーチカルグラニュレーターGV10(パウレック社製)、万能練合機(畑鉄工所製)、流動層造粒機FD−5S(パウレック社製)、ジヤイロシフター(徳寿製作所製)などを用いて混合することもできる。
In the production of the compression molding preparation of the present invention, generally used mixing methods are used as they are for mixing to obtain a compression molding mixture containing xanthan gum-coated saccharides, other additives to be added as necessary, and pharmaceutical ingredients. I can do it.
For example, it may be uniformly mixed using a diffusion mixer (W-type mixer, V-type mixer, etc.). Further, if necessary, pretreatment such as trituration mixing or sieving trituration mixing may be performed before mixing them. In addition, vertical granulator GV10 (manufactured by Paulek), universal kneader (manufactured by Hata Iron Works), fluidized bed granulator FD-5S (manufactured by Paulek), gyroscope (manufactured by Tokusu Seisakusho), etc. Can be mixed.
上記のようにして得られた圧縮成形用混合物は、常法によって圧縮成形することにより、本発明の圧縮成形製剤とすることができる。
例えば錠剤を得る場合、一般に錠剤の成型または造粒に用いられる装置が用いられる。例えば、単発錠剤機(菊水製作所製)、ロータリー式錠剤機(菊水製作所製)などが用いられる。打錠の際の成型圧力は、通常3〜160Kg/cm2(2.94×105〜1.57×107Pa)、好ましくは5〜130Kg/cm2(4.90×105〜1.27×107Pa)、より好ましくは8〜50Kg/cm2(7.84×105〜4.90×106Pa)程度である。
打錠時の温度は、糖類粒子が溶解又は溶融しない程度であり、通常室温(例えば20〜30℃程度)、好ましくは約25℃である。
The compression molding mixture obtained as described above can be made into the compression molding preparation of the present invention by compression molding by a conventional method.
For example, when a tablet is obtained, an apparatus generally used for molding or granulating a tablet is used. For example, a single tablet machine (manufactured by Kikusui Seisakusho), a rotary tablet machine (manufactured by Kikusui Seisakusho), etc. are used. The molding pressure at the time of tableting is usually 3 to 160 kg / cm 2 (2.94 × 105 to 1.57 × 107 Pa), preferably 5 to 130 kg / cm 2 (4.90 × 105 to 1.27 × 107 Pa). ), More preferably about 8 to 50 kg / cm 2 (7.84 × 10 5 to 4.90 × 10 6 Pa).
The temperature at the time of tableting is such that the saccharide particles do not dissolve or melt, and is usually room temperature (for example, about 20 to 30 ° C.), preferably about 25 ° C.
本発明の圧縮成形製剤の引張強度は、0.5MPa以上、好ましくは約0.8MPa以上、より好ましくは約1MPa以上である。また本製剤の第十五改正日本薬局方崩壊試験(試験液:水)による崩壊時間は、好ましくは5分以下、より好ましくは2分以下であり、口腔内速崩壊錠等における好ましい口腔内崩壊時間は約60秒以下、より好ましくは約30秒以下、最も好ましくは約20秒以下である。 The tensile strength of the compression-molded preparation of the present invention is 0.5 MPa or more, preferably about 0.8 MPa or more, more preferably about 1 MPa or more. In addition, the disintegration time according to the fifteenth revised Japanese Pharmacopoeia disintegration test (test solution: water) of this preparation is preferably 5 minutes or less, more preferably 2 minutes or less. The time is about 60 seconds or less, more preferably about 30 seconds or less, and most preferably about 20 seconds or less.
本発明の好ましい口腔内速崩壊錠の組成(製剤の総量に対する割合)の例を示すと下記の通りでる。
医薬成分 0.2〜5%
キサンタンガム被覆糖類 30〜80%
キサンタンガム被覆糖類以外の賦形剤 5〜50%
崩壊剤 0.5〜5%
その他の医薬添加剤 0.1〜10%
An example of the composition of the preferred intraorally rapidly disintegrating tablet of the present invention (ratio to the total amount of the preparation) is as follows.
Pharmaceutical ingredient 0.2-5%
Xanthan gum-coated saccharides 30-80%
Excipients other than xanthan gum-coated saccharides 5-50%
Disintegrant 0.5-5%
Other pharmaceutical additives 0.1-10%
上記において、キサンタンガム被覆糖類がキサンタンガムで被覆された乳糖又はマンニトールであるものが好ましく、キサンタンガム被覆乳糖が最も好ましい。キサンタンガム被覆糖類以外の賦形剤としては、乳糖又はマンニトールが好ましく、キサンタンガム被覆糖類と同じ糖類がより好ましい。また、結晶セルロースも賦形剤として好ましく、上記糖類と結晶セルロースの併用は好ましい態様の1つである。結晶セルロースを併用する場合、その含量は2〜30%程度である。崩壊剤は前記したものが何れも使用出来るが、トウモロコシデンプンは好ましいものの一つである。また、医薬成分としてリスペリドンなどが好ましい。 In the above, the xanthan gum-coated saccharide is preferably lactose or mannitol coated with xanthan gum, and xanthan gum-coated lactose is most preferred. As an excipient other than the xanthan gum-coated saccharide, lactose or mannitol is preferable, and the same saccharide as the xanthan gum-coated saccharide is more preferable. Crystalline cellulose is also preferred as an excipient, and the combined use of the saccharide and crystalline cellulose is one preferred embodiment. When crystalline cellulose is used in combination, the content is about 2 to 30%. Any of the aforementioned disintegrants can be used, but corn starch is one of the preferred ones. Moreover, risperidone etc. are preferable as a pharmaceutical ingredient.
本発明の圧縮成形製剤は、どの様な形状も採用することができ、例えば丸形、楕円形、球形、円柱状、棒状型、ドーナツ型の形状及び積層錠、有核錠等であってもよく、更にはコーティングによって被膜することもできる。また、識別性向上のためのマーク、文字などの刻印更には分割用の割線を付けても良い。通常は円柱状の錠剤が使用される。また、通常は錠剤のコーティングは不要である。
本発明の口腔内速崩壊性圧縮成形製剤は、唾液により、口腔内で速やかに崩壊し、ざらつきを残さずに滑らかに服用可能である。
なおこの製剤は、口腔内で崩壊させることなく服用することや、水と一緒に服用することもできる。
The compression-molded preparation of the present invention can adopt any shape, for example, a round shape, an oval shape, a spherical shape, a cylindrical shape, a rod shape, a donut shape, a laminated tablet, a dry-coated tablet, etc. It can also be coated by coating. In addition, markings for improving discrimination, characters, etc., and dividing lines for division may be provided. Usually, cylindrical tablets are used. Usually, no tablet coating is required.
The intraoral rapidly disintegrating compression-molded preparation of the present invention is rapidly disintegrated in the oral cavity by saliva and can be taken smoothly without leaving any roughness.
This preparation can be taken without being disintegrated in the oral cavity or taken with water.
以下、本発明を実施例及び試験例により具体的に説明するが、本発明はこれら実施例に限定されるものではない。 EXAMPLES Hereinafter, although an Example and a test example demonstrate this invention concretely, this invention is not limited to these Examples.
実施例1
(1)キサンタンガム0.024gを精製水(200ml)で攪拌溶解してコーティング用水溶液を得る。
(2)乳糖水和物(平均粒子径約98μm)600gを流動層造粒機に入れ、上記コーティング用水溶液を噴霧コーティングする。コーティング終了後そのまま流動層造粒機で乾燥し、キサンタンガム被覆乳糖(平均粒子径約102μm)を得た。
(3)上記キサンタンガム被覆乳糖99.8質量部に、ステアリン酸マグネシウム0.2質量部を混合して、打錠用末を得た。
(4)打錠用末をロータリー打錠機によって打錠圧約9KN(900Kg/cm2)で打錠し、錠剤径8mm、1錠の平均質量180mgの口腔内速崩壊錠を得た。
Example 1
(1) 0.024 g of xanthan gum is dissolved with stirring in purified water (200 ml) to obtain a coating aqueous solution.
(2) Lactose hydrate (average particle size: about 98 μm) (600 g) is placed in a fluidized bed granulator, and the above aqueous coating solution is spray-coated. After finishing the coating, it was dried as it was with a fluidized bed granulator to obtain xanthan gum-coated lactose (average particle size: about 102 μm).
(3) A tableting powder was obtained by mixing 99.8 parts by mass of the xanthan gum-coated lactose with 0.2 parts by mass of magnesium stearate.
(4) The tableting powder was tableted with a rotary tableting machine at a tableting pressure of about 9 KN (900 Kg / cm 2 ) to obtain an orally rapidly disintegrating tablet with a tablet diameter of 8 mm and an average mass of 180 mg.
比較例1
上記実施例1において、キサンタンガム被覆乳糖を、被覆前の乳糖水和物に変える以外は実施例1と同様にして、比較用の口腔内速崩壊錠を得た。
Comparative Example 1
A comparative intraorally rapidly disintegrating tablet was obtained in the same manner as in Example 1 except that xanthan gum-coated lactose in Example 1 was changed to lactose hydrate before coating.
試験例1
実施例1及び比較例1の錠剤硬度を錠剤硬度計PC−30(岡田精工社製)を用いて測定し、下記式(1)により引張強度(MPa)を算出し、その比較を行った。
また、口腔内崩壊測定器(富山化学産社製)を用いて口腔内崩壊時間の確認を行った。
その結果を表1に示す。
Test example 1
The tablet hardness of Example 1 and Comparative Example 1 was measured using a tablet hardness meter PC-30 (manufactured by Okada Seiko Co., Ltd.), the tensile strength (MPa) was calculated by the following formula (1), and the comparison was made.
In addition, the oral disintegration time was confirmed using an oral disintegration measuring instrument (manufactured by Toyama Chemical Co., Ltd.).
The results are shown in Table 1.
式(1) 引張強度(MPa)=2F/(πdh)÷9.8
F:錠剤硬度(kgf)
d:錠剤径(cm)
h:錠剤厚(cm)
Formula (1) Tensile strength (MPa) = 2F / (πdh) ÷ 9.8
F: Tablet hardness (kgf)
d: Tablet diameter (cm)
h: Tablet thickness (cm)
上表1から明らかなように通常の乳糖水和物を用いた比較例1は引張強度が0.62MPaにすぎないがキサンタンガム被覆乳糖を使用した実施例1は1.2Ma以上を示し、該被覆乳糖は圧縮成形性がほぼ2倍程度に向上し、且つ口腔内崩壊時間も短縮されていることが判る。 As apparent from Table 1 above, Comparative Example 1 using ordinary lactose hydrate has a tensile strength of only 0.62 MPa, but Example 1 using xanthan gum-coated lactose shows 1.2 Ma or more, and this coating It can be seen that lactose is improved in compression moldability by about twice, and the oral disintegration time is shortened.
実施例2
以下の(1)〜(4)の工程でリスペリドン口腔内速崩壊錠剤を製造した。
(1)キサンタンガム0.024gを精製水(200ml)で攪拌溶解してコーティング用水溶液を得た。
(2)乳糖水和物(平均粒子径約53μm)600gを流動層造粒機に入れ、上記コーティング用水溶液を用いて噴霧コーティングした。コーティング終了後そのまま流動層造粒機で乾燥し、キサンタンガム被覆乳糖(平均粒子径約57μm)を得た。
(3)上記キサンタンガム被覆乳糖60質量部に、リスペリドン1質量部、上記の乳糖水和物(平均粒子径約53μm)を18.5質量部、結晶セルロース(セオラスRTMPH301:旭化成ケミカルズ株式会社製)を14質量部、アスパルテームを3質量部、トウモロコシデンプンを2質量部、ステアリン酸マグネシウムを1.0質量部、軽質無水ケイ酸を0.5質量部及び香料(マスカット)を0.001質量部を混合して、打錠用末を得た。
(4)打錠用末をロータリー打錠機によって、打錠圧約7KNで打錠し、錠剤径6.5mm、1錠の平均質量100mgの口腔内速崩壊錠を得た。 得られた錠剤組成を後記表1に示す。
Example 2
Risperidone intraoral rapidly disintegrating tablets were produced by the following steps (1) to (4).
(1) 0.024 g of xanthan gum was dissolved with stirring in purified water (200 ml) to obtain a coating aqueous solution.
(2) Lactose hydrate (average particle size of about 53 μm) (600 g) was put in a fluidized bed granulator and spray-coated using the coating aqueous solution. After finishing the coating, it was dried as it was with a fluidized bed granulator to obtain xanthan gum-coated lactose (average particle size: about 57 μm).
(3) 60 parts by mass of the xanthan gum-coated lactose, 1 part by mass of risperidone, 18.5 parts by mass of the above lactose hydrate (average particle size of about 53 μm), crystalline cellulose (Ceolus RTM PH301: manufactured by Asahi Kasei Chemicals Corporation) 14 parts by weight, 3 parts by weight of aspartame, 2 parts by weight of corn starch, 1.0 part by weight of magnesium stearate, 0.5 parts by weight of light anhydrous silicic acid, and 0.001 part by weight of fragrance (muscat) By mixing, a powder for tableting was obtained.
(4) The tableting powder was tableted with a rotary tableting machine at a tableting pressure of about 7 KN to obtain an orally rapidly disintegrating tablet with a tablet diameter of 6.5 mm and an average mass of 100 mg. The obtained tablet composition is shown in Table 1 below.
実施例3
実施例2(3)におけるリスペリドン1質量部を1.54質量部に変え、乳糖水和物の添加量を、18.5質量部から17.96質量部に変え、実施例2(4)における錠剤径を6.5mmから7mmに変える以外は、実施例2と同様にして、1錠の平均質量130mgの口腔内速崩壊錠を得た。得られた錠剤組成を後記表2に示す。
Example 3
In Example 2 (4), 1 part by weight of risperidone in Example 2 (3) was changed to 1.54 parts by weight, and the addition amount of lactose hydrate was changed from 18.5 parts by weight to 17.96 parts by weight. An orally rapidly disintegrating tablet with an average mass of 130 mg was obtained in the same manner as in Example 2 except that the tablet diameter was changed from 6.5 mm to 7 mm. The obtained tablet composition is shown in Table 2 below.
比較例2
(1)リスペリドン1質量部、乳糖水和物(平均粒子径約53μm)を78.5質量部、結晶セルロース(セオラスRTMPH301:旭化成ケミカルズ株式会社製)を15質量部、アスパルテームを3質量部、トウモロコシデンプンを2質量部、ステアリン酸マグネシウムを1.0質量部、軽質無水ケイ酸を0.5質量部及び香料(マスカット)(三栄源エフ・エフ・アイ株式会社製)を0.001質量部を混合して、打錠用末を得た。
(2)打錠用末をロータリー打錠機によって、打錠圧約7KNで打錠し、錠剤径6.5mm、1錠の平均質量100mgの口腔内速崩壊錠を得た。 得られた錠剤組成を後記表3に示す。
Comparative Example 2
(1) 1 part by mass of risperidone, 78.5 parts by mass of lactose hydrate (average particle size of about 53 μm), 15 parts by mass of crystalline cellulose (Theorus RTM PH301: manufactured by Asahi Kasei Chemicals Corporation), 3 parts by mass of aspartame, 2 parts by weight of corn starch, 1.0 part by weight of magnesium stearate, 0.5 part by weight of light anhydrous silicic acid, and 0.001 part by weight of fragrance (Muscat) (manufactured by Saneigen FFI Co., Ltd.) Were mixed to obtain a tableting powder.
(2) The powder for tableting was tableted with a rotary tableting machine at a tableting pressure of about 7 KN to obtain an orally rapidly disintegrating tablet with a tablet diameter of 6.5 mm and an average mass of 100 mg. The obtained tablet composition is shown in Table 3 below.
比較例3
比較例2(1)におけるリスペリドン1質量部をリスペリドン1.54質量部へ、また、乳糖水和物(平均粒子径約53μm)の添加量を78.5質量部から、77.96質量部へ変更し、比較例2(1)における錠剤径7mm、1錠の平均質量130mgに変更する以外は比較例2と同様にして、口腔内速崩壊錠を得た。得られた錠剤組成を下記表3に示す。
Comparative Example 3
In Comparative Example 2 (1), 1 part by mass of risperidone was changed to 1.54 parts by mass of risperidone, and the addition amount of lactose hydrate (average particle size of about 53 μm) was changed from 78.5 parts by mass to 77.96 parts by mass. An orally rapidly disintegrating tablet was obtained in the same manner as in Comparative Example 2 except that the tablet diameter was changed to 7 mm in Comparative Example 2 (1) and the average mass of one tablet was changed to 130 mg. The obtained tablet composition is shown in Table 3 below.
試験例2
試験例1と同様にして、実施例2、3、比較例2及び3の錠剤硬度を測定し、引張強度(MPa)を算出し、その比較を行った。
また、口腔内崩壊測定器(富山化学産社製)を用いて口腔内崩壊時間の確認を行った。
その結果を表4に示す。
Test example 2
In the same manner as in Test Example 1, the tablet hardness in Example 2, 3, Comparative Examples 2 and 3 were measured, to calculate the tensile strength (MPa), it was carried out the comparison.
In addition, the oral disintegration time was confirmed using an oral disintegration measuring instrument (manufactured by Toyama Chemical Co., Ltd.).
The results are shown in Table 4.
実施例4
(1)キサンタンガム0.06gを精製水(200ml)で攪拌溶解してコーティング用水溶液を得る。
(2)乳糖水和物(平均粒子径約53μm)600gを流動層造粒機に入れ、上記コーティング用水溶液を用いて噴霧コーティングする。コーティング終了後そのまま流動層造粒機で乾燥し、キサンタンガム被覆乳糖(平均粒子径約57μm)を得た。
(3)上記キサンタンガム被覆乳糖99.8質量部に、ステアリン酸マグネシウム0.2質量部を混合して、打錠用末を得た。
(4)打錠用末をロータリー打錠機によって、打錠圧9KNで打錠し、錠剤径8.0mm、錠剤質量180mgの口腔内速崩壊錠を得た。
Example 4
(1) An aqueous solution for coating is obtained by stirring and dissolving 0.06 g of xanthan gum with purified water (200 ml).
(2) 600 g of lactose hydrate (average particle size of about 53 μm) is placed in a fluidized bed granulator and spray coated using the above aqueous coating solution. After finishing the coating, it was dried as it was with a fluidized bed granulator to obtain xanthan gum-coated lactose (average particle size: about 57 μm).
(3) A tableting powder was obtained by mixing 99.8 parts by mass of the xanthan gum-coated lactose with 0.2 parts by mass of magnesium stearate.
(4) The tableting powder was tableted with a tableting pressure of 9 KN using a rotary tableting machine to obtain an orally rapidly disintegrating tablet having a tablet diameter of 8.0 mm and a tablet mass of 180 mg.
実施例5
実施例4(1)におけるキサンタンガム0.06gを、0.12gに変える以外は、実施例4と同様にして、錠剤径8.0mm、錠剤質量180mgの口腔内速崩壊錠を得た。
試験例1と同様にして、実施例1、4及び5の錠剤硬度を測定し、引張強度(MPa)を算出した。また、口腔内崩壊測定器(富山化学産社製)を用いて口腔内崩壊時間の確認を行った。
その結果を表5に示す。
Example 5
An orally rapidly disintegrating tablet with a tablet diameter of 8.0 mm and a tablet mass of 180 mg was obtained in the same manner as in Example 4 except that 0.06 g of xanthan gum in Example 4 (1) was changed to 0.12 g.
In the same manner as in Test Example 1, the tablet hardness of Examples 1, 4 and 5 was measured, and the tensile strength (MPa) was calculated. In addition, the oral disintegration time was confirmed using an oral disintegration measuring instrument (manufactured by Toyama Chemical Co., Ltd.).
The results are shown in Table 5.
実施例6
(1)キサンタンガム0.024gを精製水(200ml)で攪拌溶解してコーティング用水溶液を得る。
(2)D-マンニトール(平均粒子径約37μm)600gを流動層造粒機に入れ、上記コーティング用水溶液を噴霧コーティングする。コーティング終了後そのまま流動層造粒機で乾燥し、キサンタンガム被覆マンニトール(平均粒子径約40μm)を得た。
(3)上記キサンタンガム被覆マンニトール99.8質量部に、ステアリン酸マグネシウム0.2質量部を混合して、打錠用末を得た。
(4)打錠用末をロータリー打錠機によって打錠圧約9KNで打錠し、錠剤径8mm、1錠の平均質量180mgの口腔内速崩壊錠を得た。
この口腔内速崩壊錠の引張強度(MPa)は1.2MPa以上であり、口腔内崩壊時間30秒以内であった。
Example 6
(1) 0.024 g of xanthan gum is dissolved with stirring in purified water (200 ml) to obtain a coating aqueous solution.
(2) 600 g of D-mannitol (average particle diameter of about 37 μm) is put into a fluidized bed granulator, and the above aqueous coating solution is spray-coated. After the coating was completed, it was dried as it was with a fluidized bed granulator to obtain xanthan gum-coated mannitol (average particle size of about 40 μm).
(3) A tableting powder was obtained by mixing 99.8 parts by mass of the xanthan gum-coated mannitol with 0.2 parts by mass of magnesium stearate.
(4) The powder for tableting was tableted with a tableting pressure of about 9 KN using a rotary tableting machine to obtain an orally rapidly disintegrating tablet with a tablet diameter of 8 mm and an average mass of 180 mg.
The intraoral rapidly disintegrating tablet had a tensile strength (MPa) of 1.2 MPa or more and an oral disintegration time of 30 seconds or less.
本発明のキサンタンガムで被覆された水溶性糖類は、流動性及び圧縮成形性が改善され、口腔内速崩壊性圧縮成形製剤に適する賦形剤として使用することが出来る。また、該被覆糖類を用いた錠剤末は錠剤などへの成形性がよく、流動性も向上していることから製造も容易であり、得られた口腔内速崩壊性圧縮成形製剤は硬度も高く、且つ口腔内での崩壊性が良く、口腔内で60秒以内、より好ましくは30秒以内での崩壊が可能である。従って本発明の口腔内速崩壊性圧縮成形製剤は種々の薬剤のための口腔内速崩壊性圧縮成形製剤として利用可能である。 The water-soluble saccharide coated with the xanthan gum of the present invention has improved fluidity and compression moldability, and can be used as an excipient suitable for an intraoral rapidly disintegrating compression molding preparation. In addition, tablet powders using the coated saccharide have good moldability to tablets and the like, and are easy to manufacture because of improved fluidity. The resulting intraorally rapidly disintegrating compression-molded preparation has high hardness. And disintegration in the oral cavity is good, and disintegration within the oral cavity is possible within 60 seconds, more preferably within 30 seconds. Therefore, the intraoral quick disintegrating compression molding preparation of the present invention can be used as an intraoral quick disintegrating compression molding preparation for various drugs.
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