Puerarin-phospholipid Complex And Self-emulsifying Formulation

Puerarin has a wide range of pharmacological activity, For the prevention and treatment of diseases such as hypertension, coronary heart disease has good curative effect. But it’s oral bioavailability is low, and injected compliance is poor. Phospholipid complex (Phytosome) is the relatively stable compound or complex. Which drugs and phospholipid molecules are formed by charge transfer effect.After formed phospholipid complex,the time of drug action can be extend,the adverse drug reactions are reduced, and the bioavailability of drug is improved, etc.Since the emulsion delivery systems (SEDDS) within the gastrointestinal tract or appropriate environmental temperature,via the gastrointestinal peristalsis or gentle stirring, It formed small particle size of emulsion,through automatic emulsion.It mainly aimed at the difficult soluble or fat soluble drugs, and can promote the drug absorption, improve bioavailability.Phytosome and SEDDS because of its unique mechanism of action, can be used as a good carrier in difficult solubility, poor oral absorption and low bioavailability of drugs,so it can be a new drug delivery system that Improving the difficult soluble drug bioavailability. This article will make puerarin into a new delivery systems by the technology of phospholipid complex and SEDDS,.In the first and the second part,preparing Puerarin-phospholipid complex and its characterization was studied.Before the preparation conditions for Phytosome were optimized by means of orthogonal design, single-factor study was performed. The characterization of new complex were analyzed by using the differential scanning calorimetry(DSC),polarimetric analysis, and fluorescence analysis.The results showed that the optimizing preparation conditions for puerarin phospholipid complex is anhydrous ethanol as reaction solvent, solvent amount to40ml, reaction temperature of30℃, reaction time2h, puerarin and soybean lecithin molar ratio of1:1;New material generated by heat and spectral analysis found that.Puerarin phospholipid complex is different from reactant monomer and puerarin and soybean phospholipids physical mixture.In the third part, preparation of Phytosome-SEDDS and their basic characteristics were studied,The formulation and preparation of Phytosome-SEDDS were obtained by solubility study in oils and(co-)surctants, the compatibility of oil phase, emulsifier.ternary phase diagram construction anddroplet size analysis, the prescription of Phytosome-SEDDS,determined,is phytosome100mg, ethylis oleas500mg, tween-80300mg,ethanol200mg,and the prescription was characterized.In the fourth part, preparation of Puerarin-SEDDS and the quality of the in vitro were studied. The formulation and preparation of Puerarin-SEDDS were obtained by solubility study in oils and (co-)surctants, the compatibility of oil phase, emulsifier,ternary phase diagram construction and droplet size analysis, the prescription of Puerarin-SEDDS determined,is Puerarin100mg, ethylis oleas100mg, tween-80200mg,glycerin700mg,and the quality in vitro is evaluated.