• Journal of Pharmaceutical Investigation
• /
• 제30권3호
• /
• pp.151-158
• /
• 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.

• 약학회지
• /
• 제43권6호
• /
• 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.

• 약학회지
• /
• 제41권1호
• /
• pp.132-138
• /
• 1997

The antimicrobial activity of Manuka oil, a steam distillate from Leptospermum scoparium, was investigated, and it's MIC against ten kinds of microorganisms was determin ed. MICs against bacteria and fungi were measured by means of both two-fold dliution method and agar plate two-fold dilution method, respectively. MICs of Manuka oil against Staphylococcus aureus KCTC 1916 and Micrococcus luteus KCTC 1915, gram-positive microrganisms, were identical as 3.05 ${\mu}$g/ml, while it's antibacterial activity against gram-negative microrganisms such as Pseudomonas aeruginosa KCTC 2513, Escherichia coli KCFC 1682, Klebsiella pneunioniae KCTC 2001 or Proteus vulgaris KCTC 2433 was negligible(MIC: ${\geq}$ 1000 ${\mu}$g/ml), suggesting a high susceptibility of gram-positive bacteria to Manuka oil. In addition, MIC against Aspergillus niger KCTC 6077 was 24 ${\mu}$g/ml. and that against the other fungi, Tricophyton mentagrophytes KCTC 1374 and Candida albicans KCTC 1940 was ${\geq}$ 1000 ${\mu}$g/ml. When Manuka oil ointment was used in combination with other drugs. i.e.. gentamycin sulfate, chlotrimazol and hydrocortisone acetate, and diphenhydramine HCl and hydrocortisone acetate. it's antibacterial activity against Staphylococcus aureus KCTC 1916 was higher than Manuka oil ointment or other drugs alone. In conclusion, Manuka oil possesses a selective antibacterial activity against Staphylococcus aureus KCTC 1916, and can be used as a potent antibacterial agent against it.