Study On The Preparation And Quality Control Of Pingyangmycin Soluble Wax Sticks

Pingyangmycin was isolated from actinomycetes in soil of Pingyang, Zhejiang Province, whose composition is almost the same with that of bleomycin. Because pingyangmycin can inhibit the synthesis of epidermal DNA, it is also widely used in the treatment of psoriasis. But, because of the short half-life, a frequent long-term dosing in large amounts is required in clinic. The treatment effect is affected to some extent.To overcome the shortcomings of its short half-life, and increase patient compliance, an easily absorbed pingyangmycin wax stick, which was also very easy to use, was prepared. Also, the content determination and the effects on psoriasis were studied. A novel pingyangmycin formulation suits for psoriasis treatment became possible.Four parts were involved in this study:(1) Study on the matrix prescription of pingyangmycin soluble wax sticksMatrix prescription of pingyangmycin soluble wax sticks was screened, and the ultimate composition was:one gram of peregal and1gram of polyoxyl[40]stearate be added at the temperature of70℃with stirring for20min. The hardness, scalability, skin irritation, heat and cold stability of the wax stick prepared in this condition, all meat with the relevant standards.(2) Study on the determination of the pingyangmycin content in the wax stickThrough the study on the extraction solvent, time and methods, the optimum extraction conditions were settled down:water as the solvent, ultrasonic heating as the extraction conditions,30min as the extraction time. The study also showed that a stable and reliable results could be obtained if the determination was made within15h after the active substances were extracted.C8column, with the detection at wavelength of254nm, was used during the content determination by HPLC. Through the study on the mobile phase composition, mobile phase A was chosen as:1.88g of hexane sulfonate and1.96g of EDTA, dissolved in1000mL of0.08mol/L acetic acid solution, and pH was adjusted to4.3using ammonia; mobile phase B was methanol-acetonitrile with a mixing ratio of7:3. Compared with Chinese Pharmacopoeia method, an ideal result with better peak shape and shorter retention time was obtained.(3) Study on the transdermal properties of pingyangmycin soluble wax sticksTo determine whether pingyangmycin soluble wax stick could penetrate ratskin, effects of several different concentrations of the receiving fluid on penetrating ability were studied. The results showed that pingyangmycin could not penetrated through the skin, which indicated that possible less side toxic effect and only topical promising effects were both obtained.(4) Effects of pingyangmycin soluble wax sticks on psoriasis miceKungming mice were randomly divided into five groups, including blank control,0.05%dosing group,0.1%dosing group,0.2%dosing group and the positive control. Administration was cayyied out once a day lasting for14days. The results showed that the effect of pingyangmycin wax sticks on epidermal differentiation (granular layer generated) is not obvious, which indicated that a more high dosing amount or frequency may be needed for a better treating effects.