PENGARUH KOKRISTALISASI DENGAN ASAM STEARAT TERHADAP KARAKTERISTIK FISIK DAN KOMPRESIBILITAS LEVOFLOXACIN HEMIHIDRAT

• Main Author: Ferica
• Format: Final Project
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/40186
• Institution: Institut Teknologi Bandung

Levofloxacin hemihydrate, a broadly used fluoroquinolone antibiotic in urinary and respiratory tract infection therapy, had poor powder flow properties (as indicated by compressibility index values > 38% and Haussner ratios < 1.6). The aim of the study was to investigate the physical and mechanical properties of levofloxacin hemihydrate-stearic acid cocrystal form which had shown an enhancement in active compound’s dissolution rate in simulated gastric fluid (pH 1,2), and low drug release in saliva (pH 6,6) that showed bitter taste masking ability. Cocrystal’s physical and mechanical properties characterization was carried out as preliminary study to investigate its potential as a new compressible form of levofloxacin hemihydrate. Cocrystal powder obtained from 1:1 stoichiometric ratio mixture of levofloxacin hemihydrate and stearic acid using solvent evaporation method had monoclinic crystal habit in the form of plate-like shape. Powder and tablet evaluation showed that levofloxacin hemihydrate-stearic acid cocrystal had relatively better powder flow properties, porosity, and compressibility than levofloxacin hemihydrate. The results agreed with the evaluation result of tablet made from powder with particle size 80-140 µm. The content uniformity of cocrystal tablet prepared was better than levofloxacin hemihydrate and stearic acid, because of better compressibility and less cohesive particles. Chipping and capping, that was observed in 90% of levofloxacin hemihydrate tablets, was not found in the cocrystal tablet. Therefore, it was possible to develop cocrystal form for solid drug production using direct compression method. After being compressed by 4.9-19.6 kN compression force, cocrystal showed worse compactibility, corresponded to the tablet hardness, compared to levofloxacin hemihydrate tablet which is caused by, either lower moisture content in cocrystal powder or absence of slip plane. Either of this causes should be investigated further.