JP6084776B2 - 結晶セルロースを利用した造粒物の製造方法 - Google Patents
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Description
を含む造粒物の製造方法が提供される。
上記の発明の好ましい態様によれば、吸湿結晶セルロースが吸湿前の結晶セルロース1質量部に対して1/8〜1/2質量部の水分を含む吸湿結晶セルロースである上記の方法;吸湿結晶セルロースに噴霧する結合剤溶液が薬物を含む上記の方法;吸湿結晶セルロースに噴霧する結合剤溶液が水及びエタノールを含む上記の方法:結合剤溶液におけるエタノールの含有量が0〜80%(w/w)である上記の方法;及び結合剤がヒドロキシプロピルセルロースである上記の方法が提供される。
例1
結晶セルロース(水で造粒された結晶セルロース粒、セルフィア(登録商標)CP-203、旭化成ケミカルズ株式会社)300 gを流動層造粒機(SFC-LABO)に投入し、風量を約0.4 m3/分として給気温度を30℃、回転数を300 rpmにて流動させた。はじめに水75 gを2 g/分の速度で噴霧した。次いでロキサチジン酢酸エステル塩酸塩(Roxa)120 g、ヒドロキシプロピルセルロース(HPC) 9 gを含む薬剤水溶液を同条件で流動させながら噴霧して造粒した。造粒物を給気温度(30℃)で乾燥した。上記操作にて得られた乾燥品を篩過器に投入し、JP30号篩(目開き:500μm)で整粒した。篩を通過した顆粒:413.7 g(100%)、篩上に残った顆粒は0.1 g(0.0%)であった。同様に例2〜5を行いそれぞれの製造例について収率及び団粒率を求めた。
収率(%)=(篩上に残存した粒子質量(B)+篩を通過した粒子質量(C))/原材料質量(A)×100
団粒率(%)=(B)/(B+C)×100
結晶セルロース(水で造粒された結晶セルロース粒、セルフィア(登録商標)CP-203、旭化成ケミカルズ株式会社)300 gを流動層造粒機(SFC-LABO)に投入し、風量を約0.4 m3/分として給気温度を30℃、回転数を300 rpmにて流動させた。次いでロキサチジン酢酸エステル塩酸塩120 g、HPC 9 gを含む薬剤水溶液を同条件で流動させながら噴霧して造粒を試みたところ、顆粒同士の凝集が多数発生して流動層造粒機の攪拌が困難な状態になった。得られた顆粒凝集塊は整粒操作を行うことができなかった。
結晶セルロース(セルフィア(登録商標)CP-203、旭化成ケミカルズ株式会社)32.7 kgを流動層造粒機(SFC-50)に投入し、給気風量を流動約12 m3/分、スリット約10 m3/分として給気温度を30℃、回転数をローター50 rpm、アジテーター150 rpmにて流動させた。はじめに精製水8.18 kgを300 g/分の速度で噴霧した。次いで、給気温度を約45℃に上げた後、Roxa16.8 kg、HPC 1.335 kgを含む薬剤水溶液を噴霧して造粒物を製造した。造粒物を給気温度(60℃)で乾燥した。上記操作にて得られた乾燥品を篩過器に投入し、JP30号篩(目開き:500μm)で整粒した。篩を通過した顆粒:49.85kg(100%)、篩上に残った顆粒は0.02 kg(0.0%)であった。
Claims (11)
- 吸湿結晶セルロース(該吸湿結晶セルロースは吸湿前の結晶セルロース1質量部に対して1/8〜1/4質量部の水分を含む)に結合剤溶液を噴霧して造粒を行う工程を含む造粒物の製造方法。
- 吸湿結晶セルロースに噴霧する結合剤溶液が水及び/又はエタノールを含む請求項1に記載の方法。
- 吸湿結晶セルロースに噴霧する結合剤溶液が水及びエタノールを含む請求項1又は2に記載の方法。
- 結合剤溶液におけるエタノールの含有量が80%(w/w)以下である請求項3に記載の方法。
- 吸湿前の結晶セルロースに水を噴霧して吸湿結晶セルロースを調製する工程を含む請求項1ないし4のいずれか1項に記載の方法。
- 造粒を流動層造粒機を用いて行う請求項1ないし5のいずれか1項に記載の方法。
- 結合剤溶液が1種又は2種以上の薬剤を含む請求項1ない6のいずれか1項に記載の方法。
- 薬剤がロキサチジン酢酸エステル塩酸塩である請求項7に記載の方法。
- ロキサチジン酢酸エステル塩酸塩及びエタノールを含むヒドロキシプロピルセルロース水溶液を吸湿結晶セルロースに噴霧する工程を含む請求項8に記載の方法。
- 吸湿前の結晶セルロースとして水で造粒された結晶セルロース粒を用いる請求項1ないし9のいずれか1項に記載の方法。
- 吸湿結晶セルロース(該吸湿結晶セルロースは吸湿前の結晶セルロース1質量部に対して1/8〜1/4質量部の水分を含む)に水及び/又はエタノールを含む結合剤溶液を噴霧して造粒を行って造粒物の製造する工程、及び上記工程により製造した造粒物を用いて固形製剤を製造する工程を含む、固形製剤の製造方法。
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R250 | Receipt of annual fees |
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R250 | Receipt of annual fees |
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R250 | Receipt of annual fees |
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