A floating multiparticulate system for ofloxacin based on a multilayer structure: In vitro and in vivo evaluation

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• 作者：Chungang Zhang^a ; Ming Xu^a ; Xiaoguang Tao^a ; Jingya Tang^b ; Zitong Liu^a ; Yu Zhang^a ; Xia Lin^a ; Haibing He^a ; Xing Tang^a ; ^{tangpharm@yahoo.com.cn}
• 关键词：Ofloxacin ; Floating ; Sustained release pellets ; Abdominal X-ray imaging ; Bioavailability
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 出版时间：1 July, 2012
• 年：2012
• 卷：430
• 期：1-2
• 页码：141-150
• 全文大小：1697 K

文摘

The purpose of this research was to develop a novel gastroretentive multiparticulate system with floating ability. This system was designed to provide drug-loaded pellets coated with three successive coatings¡ªthe retarding film (ethyl cellulose), the effervescent layer (sodium bicarbonate) and the gas-entrapped polymeric membrane (Eudragit^? RL 30D). The floating pellets were evaluated for SEM, floating characteristic parameters, in vitro release and bioavailability in New Zealand rabbits. The zero-order release theory model is designed to interpret the release processes. Due to the swelling property, high flexibility and high water permeability, Eudragit^? RL 30D was used as a gas-entrapped polymeric membrane. The obtained pellets exhibit excellent floating ability and release characteristics. Analysis of the release mechanism showed a zero-order release for the first 8 h because of the osmotic pressure of the saturated solution inside of the membrane, which was in accordance with that predicted. Abdominal X-ray images showed that the gastroretention period of the floating barium sulfate-labeled pellets was no less than 6 h. The relative bioavailability of the floating pellets compared with reference tablets was 113.06 ¡À 23.83 % . All these results showed that the floating pellets are a feasible approach for the gastroretentive drug delivery system.