title: Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.
abstract: To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo(®). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach.
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Xiaole
authors.initials: X
authors.lastname: Qi
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Chen
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Rui
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Fengjiao
authors.initials: F
authors.lastname: Yang
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Ning
authors.initials: N
authors.lastname: Ma
authors.affiliation: Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China; Yangtze River Pharmaceutical Group, State Key Laboratory for Advanced Formulation Technologies, Taizhou 225300, PR China. Electronic address: zhenghongwu66@cpu.edu.cn.
authors.forename: Zhenghong
authors.initials: Z
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding; D065546:Drug Liberation; D005750:Gastric Juice / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D015242:Ofloxacin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011817:Rabbits; D017693:Sodium Bicarbonate / Q000737:chemistry*; D013607:Tablets
chemical_list: D000464:Alginates; D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D013607:Tablets; D020723:Glucuronic Acid; D017693:Sodium Bicarbonate; D002482:Cellulose; C008079:hydroxypropylcellulose; D015242:Ofloxacin
keywords: Compression coating; Floating tablets; Hydroxypropyl cellulose; Ofloxacin; Sodium alginate; Zero-release