title: Clarithromycin highly-loaded gastro-floating fine granules prepared by high-shear melt granulation can enhance the efficacy of Helicobacter pylori eradication.
abstract: In an effort to develop a new gastro-retentive drug delivery system (GRDDS) without a large amount of additives, 75% clarithromycin (CAM) loaded fine granules were prepared with three different hydrophobic binders by high-shear melt granulation and their properties were evaluated. Granules containing the higher hydrophobic binder showed sustained drug release and were able to float over 24h. The synchrotron X-ray CT measurement indicated that both the high hydrophobicity of the binder and the void space inside the granules might be involved in their buoyancy. In an in vivo experiment, the floating granules more effectively eradicated Helicobacter pylori than a CAM suspension by remaining in the stomach for a longer period. In short, CAM highly-loaded gastro-floating fine granules can enhance the eradication efficiency of H. pylori compared with CAM alone.
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Hajime
authors.initials: H
authors.lastname: Aoki
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Iwao
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Midori
authors.initials: M
authors.lastname: Mizoguchi
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Shuji
authors.initials: S
authors.lastname: Noguchi
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan. Electronic address: s-itai@u-shizuoka-ken.ac.jp.
authors.forename: Shigeru
authors.initials: S
authors.lastname: Itai
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D017291:Clarithromycin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D003692:Delayed-Action Preparations; D004195:Disease Models, Animal; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D005753:Gastric Mucosa / Q000378:metabolism; D005849:Gerbillinae; D016481:Helicobacter Infections / Q000188:drug therapy* / Q000382:microbiology; D016480:Helicobacter pylori / Q000187:drug effects; D008297:Male; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D017291:Clarithromycin
keywords: Clarithromycin; Floating granules; Gastro-retentive drug delivery system; Helicobacter pylori eradication; High-shear melt granulation; Highly-drug loaded fine granules; Synchrotron X-ray computed tomography