Clarithromycin highly-loaded gastro-floating fine granules prepared by high-shear melt granulation can enhance the efficacy of Helicobacter pylori eradication

• 75% clarithromycin loaded granules were prepared by high-shear melt granulation.
• The granules prepared with highly-hydrophobic binder had large void spaces inside.
• The hydrophobic granules showed sustained-drug release and buoyancy over 24h.
• Strong water-repellency and low particle density were involved in their buoyancy.
• The floating granules improved recovery from H. pylori by remaining in the stomach.

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 24 h. 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.

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