Evaluation And Optimization Of Oil-in-water Microemulsion Gel Analgesic Ointment

Objections:Microemulsion cataplasm is a mixed preparation which is consisted of microemulsion and microemulsion. In our former researches, the Zhi Tong microemulsion has been prepared, but this microemulsion cannot load enough essential oil in the Zhi Tong formulation. Hence, we decide to prepare a new kind of microemulsion whose microstructure is more exactive and can load more essential oil in Zhi Tong formulation. The former cataplasm base cannot load all the microemulsion in one dosage. Therefore it is very important to alert the base ingredients of the cataplasm by adding more polymer materials inorder to improve the compatitablity between the base and microemulsion. And then we investigate the initial adhesion, lasting adhesion and180degree adhesive strength force of cataplasm, the research of these physicochemical indexes is good for further research of Chinese medicine microemulsion cataplasm.Methods:1)Firstly, the surfactant phase has been screened by mixture surfactant method. Secondly the ratios of oil phase, water phase, surfactant phase and cosurfactant phase have all be changed by drawing the plot of water phase ratio vs conductivity of microemulsion. Thirdly, the formulation of microemulsion will be optimized by using D-optimal method. The particle size and the surface tension are chosen as indexs in the optimision experiment.2) the evaluation scroe table, initial adhesive, lasting adhesive and180degree force strength are indexs, which are used for screening the ingredients of the cataplsm base. And then the formulation of cataplasm will be optimized by centre response surface design. Lastly, the keeping moisture, the time for crosslinking and spreading are all researched.3) Ferulic acid and Imperatorin are selected as the indexs for In vitro transdermal experiments. The treated rats skin are used in this experiment. The accumulated absorption the percentage of ferulic acid and imperatorin in normal Zhi Tong cataplasm with enhancer, microemulsion Zhi Tong cataplasm with enhancer, normal Zhi Tong cataplasm and microemulsion Zhi Tong cataplasm are calculated. And the absorption dynamicalmodels of ferulic acid and imperatorin are simulated.4) Acetic acid in mice body torsion experiment and rabbit skin irritation experiments are used to evaluate the pharmacophore effect.Results:1) the formulation of microemulsionOil phase borneol and mixed essential oil:1.35gSurfactant Tween20and EL-35(1:4):2.02gCosurfactant Alcohol:1.35gWater phase Extract thick concrete of Chinese medicine in Zhi Tong formulation(1g·mL-1):11.82g The particle size of microemulsion is56.86nm, and surface tension is30.625N/cm, pH is3.892) the formulation of microemulsion cataplasm: glycerinum6.00g聚丙烯酸�'�7001.00gdihydroxyaluminum aminoacetate0.04g tartaric acid0.04g distill water12.50g Carbomer941O.lOg Carbomer9340.25g microemulsioon7.00gThe preparation method:Phase Ⅰ:put NP700, Carbomer934and Carbomer941in a container. Glycerinum are used to disperse these polymer materials. Water are added to make all the polymer materials swellingPhase Ⅱ Tartaric acid should be dissolved by small amount of waterPhase Ⅲ Zhi Tong microemulsionMix Phase Ⅱ and PhaseⅢ, and then add the mixture into Phase Ⅰ slowly until the mixed system become uniformity and transparency. Put the system into a dryer which moisture is43.16%for one hour then spread it on cloth. The prepared cataplasm is reserved in a sealed dyer for one days, and resverved in a sealed Aluminum Foil Bag.3) The results of in viro transdermal experiments show that the ferulic acid absorption in microemulsion cataplasm with enhancer is best correlation with zero dynamicalequation, the equation is Q=1-e-1×(t-0.787), and the Imperatorin in microemulsion cataplasm with enhancer is best correlation with first dynamical equation, the equation is Q=0.083x (t-4.072); the ferulic acid absorption in normal cataplasm with enhancer is best correlation with Higuchi dynamicalequation, the equation is Q=1×(t-0.922)1/2, the Imperatorin in normal cataplasm with enhancer is best correlation with first dynamical equation, the equation is Q=1×(t-0.900); the ferulic acid absorption in microemulsion cataplasm is best correlation with zero dynamica lequation, the equation is Q=1×(t-0.853)1/2, the Imperatorin in microemulsion cataplasm is best correlation with first dynamical equation, the equation is Q=1×(t-0.900); the ferulic acid absorption in normal cataplasm is best correlation with Higuchi dynamicalequation, the equation is Q=1×(t-0.765)1/2, the Imperatorin in normal cataplasm is best correlation with first dynamical equation, the equation is Q=1×(t-0.909)4) the physiochemical of new microemulsion cataplasm is very well, and the evualtion indexs can be quantization. The new microemulsion cataplasm can improve the transdermal absorption content of the effective compounds and reduce the skin irritation. So our study provide foundation for further Chinese medicine formulation microemulsion cataplasm research.