| Objective : Using MicroEmulsion technique, Shexiang zhuanggu paste will be prepared for a new formulations, which make Shexiang zhuanggu paste become more easier to use and more widely used, higher application value in clinical aspect.Methods:1. Study on extraction technology of volatile oil: Target the rate of volatile oil as index, screening factors affected the yield of volatile oil by the single factor experiment,then the optimum extraction process of volatile oil can be gain by using the orthogonal experiment design. 2. Study on preparation and quality evaluation of volatile oil Micro-Emulsion and Shexiang zhuanggu Micro-Emulsion: ○1 Volatile oil microemulsion preparation: Taking the volatile oil as oil phase, the pseudo ternary phase diagram screened surfactant, co-surfactant kinds and Km values. To optimize the volatile oil micro-emulsion formulation by taking the central composite design-response surface methodology.○2 Study on physical and chemical properties of volatile oil micro-emulsion. ○3 Shexiang zhuanggu Micro-Emulsion of preparation : On the basis of the micro-emulsion of volatile oil, further study of other ingredients joining methods to determine the optimal formulation of Micro-Emulsion Shexiang zhuanggu paste composition. And its quality evaluation.3.Study on anti-inflammatory and analgesic effects of the micro-emulsion of volatile oil and Shexiang zhuanggu :By the method of the establishment of the 4% formaldehyde induced pain model, compared with the Votalin emulgel which is the positive control drug, in targing early phase, later phase reaction occurred time, and the pain score, the PGE2 content in inflammatory foot organization, and serum the IL-6 and TNF- α,and morphological changes in the inflammatory foot skin as preparation, we are going to study Shexiang zhuanggu ME and volatile oil ME anti-inflammatory, and analgesic of preliminary efficacy. and to 5min for units, draws the group to pain big rat of limitation relationship curve, then integrated analysis, and evaluation the preliminary efficacy with each other.Results:1. Study on extraction technology of volatile oil:1.1 Establishment of volatile oil extraction process: soaking 0.5h, 8 times amount of water, extraction temperature for 180°C, under the condition, smash granularity(separategrinding) 40 mesh, the extraction time of 12 h, oil yield was 1.585%.2. Preparation and quality evaluation of Shexiang Zhuanggu microemulsion system:2.1 Preparation and physical and chemical properties of volatile oil microemulsion:2.1.1 The ratio of Micro-Emulsion formulation consists of Shexiang zhuanggu of the volatile oil: In the hole Micro-Emulsion, there has 24.8% of Tween80, 12.4% of ethanol,3.21% of volatile oils, 59.59% of the distilled water.2.1.2 Physical and chemical properties: The essential oil ME pH value and particle size were 5.40, 12.87 nm; electron microscopy showed a uniform and integrated sphere,for O / W micro-emulsion.2.2 Preparation and quality evaluation of Shexiang Zhuanggu microemulsion system:2.2.1 The finally optimum ratio of the Micro-Emulsion formulation of Shexiang zhuanggu : 24.35% of Tween 80, 12.17% of Ethanol, 0.20% of Musk, 3.15% volatile oil,0.49% of Borneol, 0.49% of camphor, 0.65% of menthol, 58.50% of liquid from water extracting and the precipitation of 90% ethanol.2.2.2 Quality evaluation of Shexiang zhuanggu Micro-Emulsion:Shexiang zhuanggu Micro-Emulsionof pH value of 5.47; size is 15.19 nm; under the electron microscope is a sphere of uniform, complete, good stability for o/w Micro-Emulsion.3. Studies on anti-inflammatory and analgesic effects of Micro-Emulsion:3.1 Pain behavioral observation:3.1.1 The two phases pain reaction occured time:The SX-ME 1 group, SX-ME 2(Shexiang Zhuanggu micro-emulsion of the frist and second group) were able to delay the two phases reaction time. Voltalin group,Volatilel oil ME only has delayed action in the earlier ten minutes, however, in the left process without significantly delayed effection.3.1.2First and second phase of pain behavior score:Volatile oil micro-emulsion group, to the SX-ME 1 group, SX-ME 2 group and positive-control group of rats of the first and second phase of pain reaction had some effection,which were approximate to each other.3.1.3Time-effection Curve:Compared to the normal control group, the remaining groups rats right foot were injected with 4% formaldehyde, whose the behavior score value changes over time.Thatshowed a certain trend, which called as two phaseand, similar laws in both of them. The behavioral performances were most serious for the model rats.3.1.4The inflammatory swelling of rats for comparison:The Voltalin group, the volatile oil ME group, the SX-ME 1 groups of drug administration, and the SX-ME 2 groups of foot swelling degree were significantly smaller than the model rats, which proved out that they had treatment effect for inflammatory.3.2 Detection of inflammatory mediators:The content of PGE2 is almostly same between the Voltalin group, the SX-ME 1group, the SX-ME 2 group, volatile oil ME and the model group,no far gap(P > 0.05). For IL-6 and TNF- alpha index, the result are that SX-ME 1 group, SX-ME 2 group<model group ≈Shexiang zhuanggu oil ME group, Votalin group.3.3 The morphological changes of the organizations:The results were that the Voltalin group, blank oil Micro-Emulsion group,The SX-ME1 Group and the SX-ME 2 Group, in some degree were against inflammation. By formalin-induced inflammatory pathology,which is mainly reflected in the skin’s epidermis and DermIS. However, with a lesser effect on the vessels and its surrounding the inflammatory of dorsum of the subcutaneous tissues, and striated muscle cells smaller,those parts were impacted hardly.Conclusion: It is feasible that Shexiang zhuanggu Plaster modified to be a new formulation, Shexiang zhuanggu Micro-Emulsion. Shexiang zhuanggu Micro-Emulsion and its volatile oil Micro-Emulsion, have treatment effects in formalin-induced painful model. Therefore, Shexiang Zhuanggu plaster can be prepared into new new type of micro-emulsion hopely, which is more convenient to use, and more wider in clinical range. |
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