Preparation Of Novel Ketoconazole Spraying Film And Effect On Both Eczema Model And Tinea Corporis Model

Army health and rear service systems (HRSS) of all nations in the world consider it as the key point to prevent and treat dermatophytosis, dermatisis and eczema that have high prevalence. During the Vietnam war, there were 73 percent of American soldiers who suffered from dermatophytosis, dermatisis or eczema during the first stage of four months while entering the Vietnam. A survey of dermatogic disease in the PLA in China showed that dermatophytosis, dermatisis and eczema were main diseases in the last two decades, that the rate of dermatophytes infection was up to 60%, and that dermatisis and eczema listed the second place. So far, main formations for these diseases include slurr, lotion, solutions and so on. However, these formations have two sides of one thing that are both virtues and flaws. To better serve the soldiers in the army, and further improve the ability of fighting, according to request of the Army "Fifteenth" Subjects(subject number: 01MA151),the present study aims to use novel substances and preparation techniques, to prepare a kind of more effective and slower released novel spraying film that equip with army to prevent these two kinds of skin diseases that showed a higher prevalent current in the army.In the present study, a series of preparing trials had been conducted to select 1% chitosan chlorhydrate as the membrane material, 1% ketoconazole, 0.05% desamethasone and 1% benadryl hydrochloride as the appreciate prescriptions and preparation techniques. The product is packed in a spurting bottle so that the drug liquid can be sprayed to eruption place quickly and forms a layer of thin drug film within 5-6minutes.In this study, the quality criterials of the novel ketoconazole spraying film had been worked out. The contents of ketoconazole and desamethasone in this spraying film were assayed with high performance liquid chromatograph (HPLC) according to China pharmacopeia 2000. The method has high recoveries(98.41% for ketoconazole and 97.84% for desamethasone respectively), exellent reproducibility (intra-day and infra-day relative standard deviations (RSD) for ketoconazole are 1.17% and 1.26% respectively; intra-day and infra-day RSD for desamethasone are 1.57% and 1.40% respectively), simpleoperations and accurate outcomes. The results showed that the contents of three ketoconazole and desamethasone samples are 96.52% -97.26% and 95.38%-96.50% labeled contents respectively. In addition, we made specify about the properties, identification, membrane characteristics and hygienical test, which are suitable for the quality control of this product.In the present study, the antifungal susceptibility of this spraying film was measured by the broth microdilution antifungal susceptibility test (Mi-AFST). The standard ketoconazole powder, ketoconazole sample and chitosan chlorhydrate were used to test their susceptibility to 24 dermatophyte isolates. According to MIC100, the results indicated that the standard ketoconazole and sample ketoconazole had the same antifungal activities(MIC4 - 0.0625ug/ml) and chitosan chlorhydrate had no effect on the dermatophyte isolates.A guinea pig eczema model was created by intradermal injection of ovalbumin (OVA) and banding a little patch containing 10% OVA, 5% SDS, 37% Vaseline, and 48% water. Then, a score standard for eczema model was clearly defined according to some related literatures. There were 100 eczema models which were on the average divided into five groups named A, B, C, D and E (n=20) respectively after stratification on the basis of their scores . Group A, B and C were treated with spraying film with high, moderate and low concentration desamethasone respectively, group D with desamethasone antipruritics cream, and group E acting as the negative control. After treatment for seven days and fourteen days, symptom scores and pathology scores of all these groups were performed respectively. The statistical difference of intragroups were tested by Kruskal-Wallis test, and intergroups with Dunett' s test. Compared with the control, there were sig...