• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.151-158
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• 2000

Gel and cream containing 5% and 10% ketonic fraction (KF) of Leptospermum scoparium, respectively were formulated. Antimicrobial activity, stability, anti-inflammatory effect, rheological properties, drug release and acute toxicity for these topical efficacy were evaluated. Gel and cream containing neomycin or gentamycin in combination with KF has potent antimicrobial activity. Gel and cream were physically stable and did not show any creaming for 6 months storage. Gel showed plastic flow with yield value and cream showed pseudoplastic flow with hysteresis loop. The gel and cream containing KF showed higher viscosity than control or commercial one. The viscosity increased as the concentration of KF increased. Both 10% gel and cream showed a significant decrease in swelling when applied to the carrageenan- injected paw, suggesting local antiinflammatory activity. Particularly, 10% gel preparation showed similar antiinflammatory activity when compared with commercially available drugs. Percent of drug released and diffusion coefficient were in the order of 5% gel, 10% gel, 5% cream, and 10% cream, respectively. There were no significant changes of body weight in rats percutaneously administered with 10% cream and gel when compared with control. There were no induced acute toxicity when 10% cream or gel was applied to rats. Leptospermum scoparium could be practicaly used in topical preparations.

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