The Preparation Of Tan â…¡ Amicroemulsion/Gel-microemulsion And The Primary Pharmacodynamics Study

Objective:Tan ⅡA microemulsion/microemulsion gel was prepared. Primary pharma-codynamics study of Tan ⅡA microemulsion/microemulsion gel on treament of acne.Methods:During the Preformulation study, the analytical method of high performance liquid ehromatogram(HPLC) for Tan Ⅱ A microemulsion/microemulsion gel was established.The drug solubility and oil/water partition coefficient were determined. Based on the sotubility of Tan ⅡA, the oily phase, surfaetant and cosurfaetant composed of mieroemulsion were seleeted. The formulation of mieroemulsion was optimized through pseudo-ternary phase diagrams and characteristics of mieroemulsion. The optimal preparation of Tan ⅡA microemulsion was established by Orthogonal Test. The properties of prepared Tan ⅡA microemulsion,such as,appearance,diamrter, stability, morphology and pH were characterized and investigated. Gel-mieroemulsion of Tan ⅡA was prepared by adding the gel-matrix (carbomer 940) into the half amount of water of microemulsion, the best concentration of gel-matrix was selected according to the cumulative amount per unit area through of in vitro permeation experiments of gel-mieroemulsion. The preliminary stability, appearance, diamrter, morphology and pH were investigated Minimal inhibitory concentration of Tan ⅡA microemulsion and gel-mieroemulsion were measured by double dilution method, benzylpenicillin sodium and erythromycin lactobionate were selected as a positive control drug in this experiment.Results:1. The chromatographic condition of HPLC:methanol:water (85:15) solution as the mobile phase, at a flow rate of 1.0 mL/min, the column temperature was at 30 ℃, the detection wave-length was at 270 nm, the sample size was 10 μL.2. The optimum Tan ⅡA microemulsion formulation:mixture of Lavender Essential Oil: Rosemary Essential Oil:Grapefruit Essential Oil:TeaTree Essential Oil=2:2:1:1 as oily phase、mixture of Solutrol HS-15:Tween 80=7:3 as surfactant ethanol as cosur-factant、 the optimum formulation of microemulsion vehicle was determined as 7.4% oily phase、 27.8% surfactant 18.5% cosurfactant and 46.3% water.3. The optimal preparation of Tan ⅡA microemulsion were stirring time of 0.5 h、stirring speed of 250 r/min、and the blank microemulsion to dissolve drugs.4. The evaluation of Tan ⅡA microemulsion:the loaded drug、pH、particle size and mor-phology were 546.78μg/mL、 6.34、12.78 nm and the appearance of microemulsion droplets was uni-form、spherical shape in TEM image.5. The optimum Tan ⅡA gel-mieroemulsion formulation:mixture of Lavender Essential Oil:Rosemary Essential Oil:Grapefruit Essential Oil:TeaTree Essential Oil=2:2:1:1 as oily phase、mixture of Solutrol HS-15:Tween 80=7:3 as surfactant、ethanol as cosurfactant、 carbomer 940 as base、triethanolamine as pH adjusting agent,the optimum formulation of microemulsion vehicle was determined as 7.4% oily phase、27.8% surfactant 18.5% cosurfactant、46.3% water、0.5% carbomer 940 and 1% triethanolamine.6. The evaluation of Tan ⅡA gel-microemulsion:the pH、particle size、viscosity and morphology were 7.08、29.94 nm、104.2 Pa·s and the appearance of microemulsion droplets was uni-form,spherical shape in TEM image.7. Minimal inhibitory concentration:for staphylococcus aureus,the minimal inhibitory concentration of Tan ⅡA microemulsion and gel-mieroemulsion were 256 μg/mL;for propi-onibacterium acnes, the minimal inhibitory concentration of Tan ⅡA microem-ulsion and gel-mieroemulsion were 64 μg/mL.Conclusion:The preparation of Tan ⅡA microemulsion and gel-microemulsion had a certain effect on treating acne、improving the bioavailability and expanding the range of clinical applications of Tan ⅡA.