JP2008037863A - 不快味を呈する薬物含有製剤粒子 - Google Patents
不快味を呈する薬物含有製剤粒子 Download PDFInfo
- Publication number
- JP2008037863A JP2008037863A JP2007179465A JP2007179465A JP2008037863A JP 2008037863 A JP2008037863 A JP 2008037863A JP 2007179465 A JP2007179465 A JP 2007179465A JP 2007179465 A JP2007179465 A JP 2007179465A JP 2008037863 A JP2008037863 A JP 2008037863A
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- JP
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- Prior art keywords
- water
- unpleasant taste
- drug
- soluble polymer
- preparation
- 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.)
- Granted
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Abstract
【解決手段】(1)不快味を呈する薬物を含有する核粒子、(2)水溶性高分子及び溶出促進剤を含有するアンダーコート層、並びに、(3)水溶性高分子、水不溶性高分子、及び、溶出促進剤を含有するオーバーコート層を有する製剤粒子。
【選択図】なし
Description
核粒子の製造法
イブプロフェン27000g、リボフラビン240g、軽質無水ケイ酸3000g、結晶セルロース12000g、アメ粉21000gを秤量、混合し、粉砕したものを、ヒドロキシプロピルセルロース(HPC−L)5400gを精製水54600gに溶解した溶液を結合液として、転動流動層造粒機(MP:パウレック社製)を用いて造粒し、核粒子を製造した。核粒子の平均粒子径は306μm、かさ密度は421.7kg/m3であった。(かさ密度の測定方法:体積既知の容器(例えば、直径30mm、100mLの円柱状容器)に粉体試料を加え、粉体の表面を擦り切って秤量し、このときの粉体試料の質量を容器の内容量で除した値である。この際、容器のタッピングは行わない。見掛け比重ともいう。本発明において「かさ密度」の測定には、筒井理化学社製のA.B.D粉体測定器を用いた。)
核粒子の製造法
イブプロフェン27000g、リボフラビン240g、軽質無水ケイ酸3000g、結晶セルロース12000g、アメ粉21000gを秤量、混合し、粉砕したものを、ヒドロキシプロピルセルロース(HPC−L)5400gを精製水48600gに溶解した溶液を結合液として、転動流動層造粒機(MP:パウレック社製)を用いて造粒し、核粒子を製造した。核粒子の平均粒子径は281μm、かさ密度は429.0kg/m3であった。
参考例1で得られた核粒子を、ヒドロキシプロピルメチルセルロース34.2g、タルク22.8g及びカルメロースカルシウム5.7gを精製水575gに溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施し、乾燥した後に、エチルセルロース46.2g、ヒドロキシプロピルメチルセルロース27.6g及びタルク49.2g及びカルメロースカルシウム12.3gを、エタノール1131g及び精製水283gの混合液に溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施して、顆粒を製造した。
参考例2で得られた核粒子を、ヒドロキシプロピルメチルセルロース34.2g、タルク22.8g及びマンニトール5.7gを精製水575gに溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施し、乾燥した後に、エチルセルロース46.2g、ヒドロキシプロピルメチルセルロース27.6g、タルク49.2g及びカルメロースカルシウム12.3gを、エタノール1131g及び精製水283gの混合液に溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施して、顆粒を製造した。
参考例1で得られた核粒子を、ヒドロキシプロピルメチルセルロース34.2g及びタルク22.8gを精製水575gに溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施し、乾燥した後に、エチルセルロース46.2g、ヒドロキシプロピルメチルセルロース27.6g及びタルク49.2gを、エタノール1131g及び精製水283gの混合液に溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施して、顆粒を製造した。
参考例2で得られた核粒子を、エチルセルロース46.2g、ヒドロキシプロピルメチルセルロース27.6g、タルク49.2g及びカルメロースカルシウム12.3gを、エタノール1131g及び精製水283gの混合液に溶解・分散し得られたコーティング剤で、ドラフトチューブ付き噴流層(GPCG:パウレック社製)を用いてコーティングを施して、顆粒を製造した。
実施例1及び2並びに比較例1及び2で調製したコーティング顆粒と、薬物及び賦形剤を秤量、混合、粉砕し、アルコール95%溶液を溶媒として高速撹拌造粒(バーチカルグラニュレーター:パウレック社製)を行うことにより得られた薬物を含有する顆粒を混合した処方を、試験サンプルとした。試験サンプルを、日本薬局方一般試験法溶出試験法パドル法にて試験液に水を用いて溶出試験を実施した。試験結果を図1に示した。
以上の結果より、イブプロフェン等の不快味を呈する薬物を含有し、薬物の不快味が十分にマスキングされ、且つ溶出性が改善された製剤粒子を提供することができた。
Claims (7)
- (1)不快味を呈する薬物を含有する核粒子、(2)水溶性高分子及び溶出促進剤を含有するアンダーコート層並びに(3)水溶性高分子、水不溶性高分子及び溶出促進剤を含有するオーバーコート層を有する製剤粒子。
- 水溶性高分子が、ヒドロキシプロピルメチルセルロース、ヒドロキシプロピルセルロース、ポリビニルピロリドン、ポリビニルアルコール、及び、メチルセルロースからなる群より選ばれる1種または2種以上である請求項1に記載の製剤粒子。
- 水不溶性高分子が、エチルセルロース、アミノアルキルメタアクリレート、及び、ポリビニルアセタールジエチルアミノアセテートからなる群より選ばれる1種または2種以上である請求項1に記載の製剤粒子。
- 溶出促進剤が、カルメロースカルシウム、マンニトール、クロスカルメロースナトリウム、低置換度ヒドロキシプロピルセルロース、カルメロース、カルメロースナトリウム、デンプン、部分アルファ化デンプン、カルボキシメチルスターチナトリウム、及び、プルランからなる群より選ばれる1種または2種以上である請求項1に記載の製剤粒子。
- 不快味を呈する薬物を含有する核粒子中の不快味を呈する薬物の含有量が30質量%以上である請求項1に記載の製剤粒子。
- 不快味を呈する薬物がイブプロフェンである請求項5に記載の製剤粒子。
- 不快味を呈する薬物を含有する核粒子に、水溶性高分子及び溶出促進剤を含有するコーティング液を用いてアンダーコートを施し、乾燥した後に、水溶性高分子、水不溶性高分子及び溶出促進剤を含有するフィルムコーティング液を用いてオーバーコートを施すことを特徴とする製剤粒子の製造方法。
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WO2010018614A1 (ja) * | 2008-08-11 | 2010-02-18 | 味の素株式会社 | 呈味性が改善された親水性アミノ酸含有製剤 |
JP2010037326A (ja) * | 2008-07-10 | 2010-02-18 | Taisho Pharmaceutical Co Ltd | 不快な呈味を有する薬物を含有する製剤粒子 |
JP2011125331A (ja) * | 2009-11-17 | 2011-06-30 | Taisho Pharmaceutical Co Ltd | 魚鱗粉末含有コーティング錠剤 |
JP2011136922A (ja) * | 2009-12-28 | 2011-07-14 | Lion Corp | イブプロフェン含有製剤 |
JP2012046493A (ja) * | 2010-07-30 | 2012-03-08 | Taisho Pharmaceutical Co Ltd | 内服液剤 |
JP2012240917A (ja) * | 2011-05-16 | 2012-12-10 | Zensei Yakuhin Kogyo Kk | 製剤化用微粒子とそれを含む製剤 |
JP2015221781A (ja) * | 2014-04-30 | 2015-12-10 | 大正製薬株式会社 | 固形製剤 |
JP2016060731A (ja) * | 2014-09-19 | 2016-04-25 | エスエス製薬株式会社 | 経口組成物 |
WO2017146052A1 (ja) * | 2016-02-23 | 2017-08-31 | ニプロ株式会社 | 医薬組成物粒子とそれを含む口腔内崩壊製剤、医薬組成物粒子の製造方法 |
KR20200001993A (ko) | 2018-06-28 | 2020-01-07 | 라이온 가부시키가이샤 | 내복 조성물 및 그 제조 방법 |
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JP2011125331A (ja) * | 2009-11-17 | 2011-06-30 | Taisho Pharmaceutical Co Ltd | 魚鱗粉末含有コーティング錠剤 |
JP2011136922A (ja) * | 2009-12-28 | 2011-07-14 | Lion Corp | イブプロフェン含有製剤 |
JP2012046493A (ja) * | 2010-07-30 | 2012-03-08 | Taisho Pharmaceutical Co Ltd | 内服液剤 |
JP2012240917A (ja) * | 2011-05-16 | 2012-12-10 | Zensei Yakuhin Kogyo Kk | 製剤化用微粒子とそれを含む製剤 |
JP2015221781A (ja) * | 2014-04-30 | 2015-12-10 | 大正製薬株式会社 | 固形製剤 |
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JP2019131615A (ja) * | 2014-04-30 | 2019-08-08 | 大正製薬株式会社 | 固形製剤 |
JP2016060731A (ja) * | 2014-09-19 | 2016-04-25 | エスエス製薬株式会社 | 経口組成物 |
WO2017146052A1 (ja) * | 2016-02-23 | 2017-08-31 | ニプロ株式会社 | 医薬組成物粒子とそれを含む口腔内崩壊製剤、医薬組成物粒子の製造方法 |
JPWO2017146052A1 (ja) * | 2016-02-23 | 2018-12-13 | ニプロ株式会社 | 医薬組成物粒子とそれを含む口腔内崩壊製剤、医薬組成物粒子の製造方法 |
US20190054029A1 (en) * | 2016-02-23 | 2019-02-21 | Nipro Corporation | Pharmaceutical composition particles, orally disintegrating preparation including same, and method for producing pharmaceutical composition particles |
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