Investigation and Evaluation of an in Situ Interpolymer Complex of Carbopol with Polyvinylpyrrolidone as a Matrix for Gastroretentive Tablets of Ranitidine Hydrochloride

• Yusif Rehab Mohammad

  Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University

• Abu Hashim Irhan Ibrahim

  Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University

• Mohamed Elham Abdelmonem

  Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University

• El Rakhawy Mohamed Magdy

  Department of Diagnostic Imaging and Intervention, Faculty of Medicine, Mansoura University

書誌事項

タイトル別名

• Investigation and Evaluation of an <i>in Situ</i> Interpolymer Complex of Carbopol with Polyvinylpyrrolidone as a Matrix for Gastroretentive Tablets of Ranitidine Hydrochloride

抄録

Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0.1 N HCl was investigated and characterized by Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Hence, directly compressed GR tablets of different combinations of PVP and CP with sodium bicarbonate (SB) as an effervescent agent were examined for prolonged gastroretention and sustained release of ranitidine hydrochloride (RHCl) as a model drug. Tablets were evaluated for in vitro buoyancy, bioadhesiveness, swelling, and drug release in 0.1 N HCl. All GR tablets containing PVP–CP combinations achieved more prolonged floating (>24 h) than CP tablets (5.2 h). Their bioadhesiveness, swelling, and drug release were dependent on the PVP molecular weight and its ratio to CP. Drug release profiles of all formulae followed non-Fickian diffusion. Formula containing the PVP K90–CP combination at a respective ratio of 1 : 3 (P₉₀C13) was a promising system, exhibiting good floating and bioadhesive properties as well as sustained drug release. Abdominal X-ray imaging of P₉₀C13 formula, loaded with barium sulfate, in six healthy volunteers showed a mean gastric retention period of 6.8±0.3 h.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 64 (1), 42-51, 2016

  公益社団法人 日本薬学会

キーワード

• polyvinylpyrrolidone
• carbopol
• interpolymer complex
• gastroretention
• ranitidine hydrochloride

詳細情報

• CRID: 1390001204177258624
• NII論文ID: 130005115800
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c15-00620
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 027012518
• PubMed: 26726743
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I027012518
• Web Site: https://www.jstage.jst.go.jp/article/cpb/64/1/64_c15-00620/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2016233211
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可