Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in‐vitro and in‐vivo study. (10th December 2014)

• Record Type: Journal Article
• Authors: Qi, Xiaole; Jiang, Yingchun; Zhang, Huiting; Wu, Zhenghong
• Is Part Of: Journal of pharmacy and pharmacology. Volume 67:Number 4(2015:Apr.)
• Page Start: 493
• Page End: 500
• Publication Date: 2014-12-10
• Subjects: bioavailability -- famotidine -- floating drug delivery system -- pellets -- tablets; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12339
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: The aim of this study was to prepare a disintegrating gastric floating tablet composed of floating pellets coated with acrylic resin to prolong the gastric residence time and increase the oral bioavailability of famotidine. Methods: The gastric floating pellets containing famotidine, stearyl alcohol and microcrystalline cellulose (1 : 10 : 1) were prepared by extrusion–spheronization process and coated with acrylic resin, then compressed into tablets with Avicel PH 301 pellets and cross‐linked polyvinylpyrrolidone. The coating weight, volume ratio of Eudragit RL30 D and RS30 D and solid content of coating fluid were optimized by Box–Behnken design. Key findings: In 0.1 M HCl, tablets can immediately disintegrate into pellets which can remain floating and sustained drug releasing over 12 h. The AUC0‐∞ of famotidine gastric floating pellets (7776.52 ± 1065.93 h ng/ml) administered into rats was significantly higher than that of marketed rapid release tablets Xingfading® (Xingyi, Shanghai, China) (4166.23 ± 312.43 h ng/ml), while the relative bioavailability was 187.01 ± 22.81%. Conclusions: The experimental results indicated that the optimized formulation did offer a new gastro retention and sustained release approach to enhance the oral absorption of famotidine.