The Development And Initial Pharmacological Experimental Research On Diadermic Preparation Of Chinese Medicine With Acaricidal Activity

In recent years the serious"3R"issue(residual,resistance and resurgance) that was caused by the use of the chemical insecticide had aroused the attention from the whole society.As the enhancement of awareness of health and enviroment of the public,studies of natural drug of safty,lowtoxicity, unresidual and unresistance are becoming the dominant direction of acaricide development. Therefore,this article is based on 23 plants used in the flavor of traditional Chinese medicine for acaricidal activity screening,and clove extract treatment,for the development of a green and efficient transdermal formulations.The content of this topic include five fractions:traditional Chinese medicine acaricidal activity of initial screening,screening of acaricidal active part of clove,clove extract developed transdermal formulations and evaluate permeate in vitro,stability test,acute toxieity test and experimentation of stimulate about clove extract TDS in vitro skin,and the effect of this preparation to kill mites of rabbit compared.The results obtainedwere as follows:1.Screening of acaricidal active plants:Acaricidal activity of industrial alcohol extract from 23 plants in 50%concentration on adult mites of P.communis cuniculi was investigated in vitro.The result showed that the crude extracts of clove had significant activities against mites and could kill all experimental mites in 14.3 min.The others hadn't significant activities against mites,among them 7 species of plants(immature orange fruit,hydnocapus,cortex and so on) couldn't kill the experimental mites in 7h.2.Screening of acaricidal active part of clove:The extracts of petroleum ether,chloroform,ethyl acetate,ethanol and distilled water were extracted by solvent extraction,and whose acaricidal activity were detected by killing P.communis cuniculi in vitro.Set up HPLC-UV method to determine the content of eugenol in clove,and experimented by orthogonal design,considerate the effect of three factors:extraction time,quanta of solvent and solvent concentration,take the content of eugenol as evaluation standard to choose better abstraction condition.The result of the acariaidal test showed that the extract of ethanol in 50%concentration could kill all experimental mites in 20 min.The time killing all experimental mites of the exacts of petroleum,ether chloroform and ethyl acetate were 115 min,82 min and 53 min respectively.But the acaricidal activity of the extracts of distilled water were not detected in this test.The exact of ethanol was the acaricidal active site of Eungenia caryophyllata.And the optimum extraction procedure was determined with 15 times of 85%alcohol extracting for 6 hours.The results also show that the effect of killing P.communis cuniculi in vitro is a positive correlation with the content of eugenol in extract clove.3.The developed transdermal formulations of clove extract and evaluate permeate in vitro:Set up HPLC-UV method to determine the content of eugenol in extract clove and its skin permeation in vitro.Made use of HPLC-UV method and permeation experimentation of classic in vitro to Sieve dissolvent and penetrate agent of the developed transdermal formulations of clove extract.Made use of orthogonal design.In vitro drug percutaneous permeation had been studied with Franz diffusion one cell apparatus.Temperature in cell apparatus was 37±0.5℃,speed of magetic force was 200r/min.Made use of white mouse skin.Result:2%borneo camphor,4%propylene glycol and 1% Azone had been mixed up as penetrant of the developed transdermal formulations of clove extract. The highest percutanous permeation rate was observed.Rate of speed permeation 19.874μg/h.cm~2,when dosage was 1.0mL on 10cm~2 skin area The developed transdermal formulations of clove extract,the osmolality was 807.694μg after 8 hours.The dose could be used in animal clinic.4.Rearch of stability in vitro skin,acute toxieity test and experimentation of stimulate about the developed transdermal formulations of clove extract:Made use of the developed transdermal formulations of clove extract initial equal-speed method to inspect stability of the developed transdermal formulations of clove extract and predict the period of validity.Acute skin toxieity and skin irritation tests were carried out on health rabbit.The result showed that the period of validity was 1.5years at room temperature.It was able to satisfy the demands from produetion,transportation, storage to usage.And there were some slender irritation of skin,it was disappeared afer 48hours.5.To compared effective to kill mites in rabbits of clove extract transdermal formulations:The application of clinical evaluation of the natural infection acariasis of rabbits in vitro tests and the effect of rabbits.The test investigated cloves of transdermal drug delivery solution system(high, medium and low dose) with the positive control group(10mg/ml Avermectin injection and Binapacryl Ling) comparison.The result showed that the solution of clove transdermal drug delivery systems(high,medium dose) in vitro and rabbit body to kill mites effect was significantly higher than Binapacryl Ling,and 10mg/ml avermectin injection with the same efficient,The effective rates were more than 92.6%in high and middle group.There was not adverse reactions during the clinical experiment.