• Journal of Pharmaceutical Investigation
• /
• v.28 no.2
• /
• pp.115-119
• /
• 1998

Five polymorphic modifications of Cephradin were prepared by recrystallization from organic solvents. The isolated crystal forms were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and X-ray crystallography powder diffractometry. Modificaition 1 was the most stable form and decomposed at $201.3^{\circ}C$. Modification 3 and 4 were metastable. The dissolution of modification 3 and 4 was faster than that of marketed form.

• YAKHAK HOEJI
• /
• v.43 no.6
• /
• pp.716-728
• /
• 1999

Whole oil and ketonic fraction (KF) of Leptospermum scoparium have been tested for their antimicrobial activity and combination effect with several antibiotics against various bacterial strains and fungi by using microbiological assay methods. Antibacterial activities of KF against a number of test strains were 2-3 fold stronger than those of whole oil. MICs of the KF were $65~125{\;}{\mu\textrm{g}}/ml$ against seven gram positive bacterial strains, $65~250{\;}{\mu\textrm{g}}/ml$ against 19 methicillin resistance Staphylococcus aureus strains, and $65~50{\;}{\mu\textrm{g}}/ml$ against 14 quinolone resistance strains. However, KF showed little or no activity against gram negative bacteria. MICs of the KF were $16~250{\;}{\mu\textrm{g}}/ml$ against more than 50% of the anaerobic bacterial strains tested. KF showed the higher antibacterial activity than bacitracin against 10 strains of Bacteroids thetaiotaomicron, or three strains of Bacteroides ovatus, and the more active than ciprofloxacin against one strain of Bacteroides thetaiotaomicron and three strains of Bacteroids ovatus. The MICs of KF was 63 and $250{\;}{\mu\textrm{g}}/ml$ against Aspergillus niger and Candida albicans, respectively. Antibacterial activities of KF in combination with 19 antibiotics against 14 strains and with four antifungal agents against one fungal strain were determined by paper strip diffusion method. While most of combination showed additivity, KF showed synergism with bacitracin, exfadroxil, cephradin, and meropenem for 29~57% of the strains tested. However, ofloxacin, enoxacin, sparfloxacin showed antagonism with KF for 43~71% of the strains. KF alone and in combination with bacitracin, gentamycin, neomycin, itraconazole, fluconazole, terfinafine and ketoconazole against five bacterial strains or one fungus strain synergistic effect was demonstrated against 33% of strains examined with FIC index value below 0.5 by checkerboard study. Synergistic effect of KF with gentamicin against Staphylococcus epidermidis 329 (QRS) was found by time-kill study.