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Objective: Tanshinone Ⅱ A (Tanshinone Ⅱ A) is from the root of Salvia Labiatae extract isolated diterpene quinones, as Salvia fat-soluble active ingredients, with a variety of biological activity, such as antibacterial, antioxidant, expansion of coronary artery , increased myocardial blood flow, anti-platelet, improve memory disorders. Particularly in anti-tumor, and its role causing widespread concern in academic circles. However, tanshinone Ⅱ A low solubility in water, the solid drug absorption is poor, difficult to be made suitable for intravenous dosage forms, affect their clinical application. A microemulsion as a drug targeting vector, the lymphatic system has a higher affinity, and has a sustained release effect, different from the other emulsion, microemulsion of small particle size, bioavailability, thermodynamically stable, suitable for an injection. However, at home and abroad injectable microemulsion listed yet. The research projects aimed at: 1. Conducted before Tanshinone Ⅱ A microemulsion research. 2 simplex grid method optimized formulation and investigate microemulsion preparation. 3 study in mice in vivo pharmacokinetics. Method: 1. Tanshinone Ⅱ A microemulsion preformulation studies: the establishment of tanshinone Ⅱ A measurement method for the determination of tanshinone Ⅱ A physicochemical properties, the use of composite emulsifier ternary phase diagram screening prescription, initially identified microemulsion composition ratio of each component range. (2) using simplex optimization microemulsion grid method, the average particle size and solubility of the indexes to determine the optimal ratio of tanshinone Ⅱ A, the process of investigation determined after preparation; HPLC Determination of Tanshinone Ⅱ A microemulsion drug loading; Electron microscopy microemulsion morphology; particle size measuring instrument measuring particle size and its distribution. 3 pharmacokinetic studies: Take healthy male Kunming mice 20, each two to 9.5mg · kg -1 intravenous bolus administration in before administration 5,10,20,30,45,60,120,240,360 min after blood and plasma concentration was measured by the DAS software processing pharmacokinetic parameters were calculated. Results: 1. Tanshinone Ⅱ A is fat-soluble substance, the results from the ternary phase diagram shows a greater availability of emulsifier O / W emulsion into the breast area. (2) The optimal formulation simplex grid method and obtained by the process of investigation and prescription preselected prescription Ⅰ Ⅱ, the average particle size was 107.4nm and 151.4nm, particle size distribution, good appearance, encapsulation rates were 92.28% and 90.13%. 3 Prescription Ⅱ samples were 20 healthy male Kunming mice after intravenous injection, the drug - time curve compartment model, AUC 0 - ∞ , AUC 0-t , T 1/2α , T 1/2β , respectively 65.433mg · l -1 · h, 81.721 mg · l -1 · h, 2.365h, 14.956h. Conclusions: 1. Tanshinone Ⅱ A fat-soluble substances, emulsifier application to expand its O / W microemulsion into milk ranges. (2) The grid method simplex optimization formulation and preparation process of study of tanshinone Ⅱ A microemulsion prescription and prescription Ⅰ Ⅱ of the indicators are in line with requirements. 3 Tanshinone Ⅱ A microemulsion in mice plasma schedule two compartment open model. The distribution and elimination half-life was prolonged, consistent microemulsion release characteristics. This experiment has the following innovations: 1. Tanshinone Ⅱ A microemulsion study abroad has not been reported, the first innovation developed entitled. 2 draws and ternary phase diagrams emulsifier composition ratio range for prescription primaries, using simplex optimized formulation component ratio grid method, the method advanced scientific and strong. 3 for the first time in mice injected with Tanshinone Ⅱ A microemulsion pharmacokinetic studies carried out, for the preparation of further research foundation.
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