title: A floating multiparticulate system for ofloxacin based on a multilayer structure: In vitro and in vivo evaluation.
abstract: 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-the 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 8h 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 6h. The relative bioavailability of the floating pellets compared with reference tablets was 113.06 ± 23.83%. All these results showed that the floating pellets are a feasible approach for the gastroretentive drug delivery system.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China.
authors.forename: Chungang
authors.initials: C
authors.lastname: Zhang
authors.forename: Ming
authors.initials: M
authors.lastname: Xu
authors.forename: Xiaoguang
authors.initials: X
authors.lastname: Tao
authors.forename: Jingya
authors.initials: J
authors.lastname: Tang
authors.forename: Zitong
authors.initials: Z
authors.lastname: Liu
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xia
authors.initials: X
authors.lastname: Lin
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002853:Chromatography, Liquid; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D041981:Gastrointestinal Tract / Q000000981:diagnostic imaging / Q000378:metabolism; D008855:Microscopy, Electron, Scanning; D008956:Models, Chemical; D015242:Ofloxacin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010539:Permeability; D011817:Rabbits; D011859:Radiography; D017693:Sodium Bicarbonate / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties; D013608:Tablets, Enteric-Coated; D053719:Tandem Mass Spectrometry; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000180:Acrylic Resins; D000900:Anti-Bacterial Agents; D005079:Excipients; D013608:Tablets, Enteric-Coated; C050528:Eudragit RS; C013517:ethyl cellulose; D017693:Sodium Bicarbonate; D002482:Cellulose; D015242:Ofloxacin