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  • Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study.

Tablets compressed with gastric floating pellets coated with acrylic resin for gastro retention and sustained release of famotidine: in-vitro and in-vivo study.

The Journal of pharmacy and pharmacology (2014-12-17)
Xiaole Qi, Yingchun Jiang, Huiting Zhang, Zhenghong Wu
ABSTRACT

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. 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. 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%. 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.

MATERIALS
Product Number
Brand
Product Description

Supelco
Stearyl Alcohol, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Triethyl citrate, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
D-Lactose monohydrate, ACS reagent
Sigma-Aldrich
D-Lactose monohydrate, ≥99% (HPLC), BioUltra
Sigma-Aldrich
Triethyl citrate, ≥99%, FCC, FG
Sigma-Aldrich
Triethyl citrate, ≥98.0% (GC)
USP
Stearyl alcohol, United States Pharmacopeia (USP) Reference Standard
Stearyl alcohol, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
D-Lactose monohydrate, ≥98.0% (HPLC)
Sigma-Aldrich
D-Lactose monohydrate, tested according to Ph. Eur.
Supelco
Lactose (Monohydrate), Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Famotidine, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
1-Octadecanol, ReagentPlus®, 99%
Sigma-Aldrich
1-Octadecanol, 95%
Sigma-Aldrich
Famotidine
Supelco
1-Octadecanol, Selectophore, ≥99.0%
Famotidine for system suitability, European Pharmacopoeia (EP) Reference Standard
Famotidine, European Pharmacopoeia (EP) Reference Standard
USP
Lactose monohydrate, United States Pharmacopeia (USP) Reference Standard