Formulation Approach for Nicorandil Pulsatile Release Tablet

• Maeda Hiroyuki

  Department of Pharmaceuticals, Faculty of Pharmaceutical Science, Toho University Formulation Technology Research Department, Chugai Pharmaceutical Co., Ltd.

• Ogawa Yutaka

  Formulation Technology Research Department, Chugai Pharmaceutical Co., Ltd.

• Ishiyama Masato

  CMC Coordination and Planning Department, Chugai Pharmaceutical Co., Ltd.

• Hirayama Tomoaki

  Formulation Technology Research Department, Chugai Pharmaceutical Co., Ltd.

• Terada Katsuhide

  Department of Pharmaceuticals, Faculty of Pharmaceutical Science, Toho University

抄録

The purpose of this study was to obtain a nicorandil pulsatile release tablet that has a well-regulated release lag time. When nicorandil is used as an antiangina drug, administration time control is important. A pulsatile release tablet is one of the effective approaches to modified release to reduce daily administration frequency. In this study, a pulsatile release tablet of nicorandil was formulated by fumaric acid dry coating around the core tablet including nicorandil. The model tablets, which had different content ratios of excipients in the dry-coating layer, were characterized by a dissolution test. The results showed that the release lag time was generated with fast release profiles. Various lag time controls of tablets were achieved, from 60 to 310 min on average, by variation of outer layer composition. From an analysis of the relation between lag times and outer layer composition, the key ingredient for prolongation of lag time was found to be fumaric acid. To analyze the lag time generation mechanism, water penetration for tablet was measured. The results indicated that the penetration depth was proportionate to the square root of time and the lag time formation mechanism was simple water penetration through the matrix of fumaric acid to the tablet core. The results also showed that the Washburn equation could be used to design the lag time of the pulsatile release tablet in this study. In conclusion, novel release control technology using fumaric acid was appropriate to obtain a nicorandil pulsatile release tablet that has well regulated lag time.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 56 (4), 464-467, 2008

  公益社団法人 日本薬学会

キーワード

• nicorandil
• pulsatile release
• tablet
• fumaric acid
• dry-coating

詳細情報

• CRID: 1390282679146594688
• NII論文ID: 110006649346
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.56.464
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 9432725
• Web Site: http://id.ndl.go.jp/bib/9432725
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I9432725
• Web Site: http://www.jstage.jst.go.jp/article/cpb/56/4/56_4_464/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2008231483
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • CiNii Articles
  • KAKEN
• 抄録ライセンスフラグ: 使用不可