| Objective: Present antifungal drugs are mainly chemically synthesized , their effects are affirmative, but they are expensive , have adverse reactions , and lead to drug resistance with a long-term usage. We hope to explore an potent traditional Chinese antifungal drug whose resource is abundant , technology of extraction is stabilized, quality is controllable , application is convenient and safe .Ginger oleoresin is a brownish-red-color oily liquid which is extracted from rhizome using the technique of supercritical fluid extraction, it is a concentration of all the active ingredients in rhizome. Our study wants to: (1) inspect the anti-dermatophyte activity of ginger oleoresin in vitro; (2) develop a stable prescription of ginger oleoresin praeparatum which is suitable for clinical application according to physical chemistry characteristics; (3) inspect the cutaneous stimulation and allergia of ginger oleoresin gel praeparatum , and its antidermatophyte activity in vivo; (4) institute the quality-control standard of ginger oleoresin gel praeparatum.Methods: (1)Use the antifungal susceptibility test scheme , M38-A micro-dilution method recommend by National Committee of Clinical Laboratory Standards (NCCLS) to dematiaceous fungi in 2003 ,to carry out and study the ginger oleoresin's bacteriostatic test to the common dermatopbytes and measure its MIC;(2) Use orthogonal experimental design to inspect the influence of carbomer-940's dosage , glycerol's concentration and tween-80's concentration to ginger oleoresin's appearance and stability; (3) Determine the skin irritating potency and sensitization rate of ginger oleoresin based on the relevant regulations of"Instructive principle for preclinic study of new Chinese drugs";Use abrasive-paper-establishing- model method to inoculate trichophyton mentagrophytes onto guinea pig's dorsal skin and observe the treatment of ginger oleoresin gel to guinea pig's skin lesions and the skin pathological changes; (4)Use HPLC to measure the content of 6-gingerol in ginger oleoresin gel(the reference substance was 6-gingerol , the chromatographic column was HYPERSIL BDS C18"4.6 mm×250 mm,5μm", the mobile phase was methanol and water"65:35", the detection wavelength was 280 nm,) ,institute the quality control standard of ginger oleoresin gel.Results: (1)The general MIC of ginger oleoresin to dermatophyte was 0.0002% - 0.0032%; and trichophyton rubrum: 0.0002% - 0.0008% ; trichophyton mentagrophytes: 0.0008% - 0.0032% ; microsporum canis: 0.0002% - 0.0016%; Epidermophyton floccosum: 0.0004% - 0.0008% respectively .(2)Optimum combination for the prescription of ginger oleoresin gel was: carbomer-940 (1g/100ml) , glycerol (5%) and tween-80 (3%); such preparation had uniform texture ,mezzo viscosity and good malleability ; under centrifugation (4000r/min,60min),it was stable and did not have stratification phenomenon ; its appearance and malleability did not change after 3 months at room temperature .(3) ginger oleoresin gel did not cause any stimulation such as erythema and edema and had no sensitization to guinea pig's skin ;to the animal model established by trichophyton mentagrophytes ,the cure rate of saline group was 0, matrix group 16.7% , miconazole nitrate group 75% , 10% ginger oleoresin gel 75% ,15% ginger oleoresin gel 100% , 20% ginger oleoresin gel 100% .(4)the linear range of 6-gingerol was 0.06mg/ml - 1.2mg/ml(r=0.9999) ; the relative standard deviation(RSD) of precision , repeatability and stability was no more than 2% ;the average recovery and its RSD was 98.30% and 0.95%.Conclusions: (1)The antidermatophyte effect of ginger oleoresin in vitro is good ;(2) the stability of ginger oleoresin gel is good ;(3) both the skin irritation and sensitization of ginger oleoresin gel accords with relative requirements; the treatment of 15% and 20% ginger oleoresin gel to the tinea corporis model established by trichophyton mentagrophytes is complete ;(4)the HPLC method in this study for determinating the content of 6- gingerol in ginger oleoresin gel has simple operation and reliable results ,could be used for ginger oleoresin gel's quality control.
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