| We had developed a ethanol injection method, one of the most simple methods, to obtain small unilamellar vesicle liposomes of dehydroandrographolidi succinas. Through orthogonal experimental design, one optimum recipes of dehydroandrographolidi succinas liposomes was founded. A simple preparation method-ethanol injection method was modified to achieve preferable fideity and high percentage envelopment.A method was developed for the determination of envelopment and dehydroandrographol idi succinas concentration in liposomes and biological samples by HPLC, it was proved that this method was accurate, sensitive, specific and good enough to be used in pharmacokinetic study of dehydroandrographolidi succinas.The chemicophysical properties and stabilty of dehydroandrographolidi succinas liposomes were studied. The small unilamellar vesicle liposomes were seen though electron microscope. The mean diameter and zeta potential of Liposomal injection were 505.9nm and -27.61mv. In accelerated tests, which contained high temperature, low temperature and light exposing experiments, it was shown that liposmome injection was more stable than water solution. The liposmal injection had little change after it was stored at 6℃ for 6 months. Due to the oxidization and hydrolysis of phospholipids, it was advised that the production should be stored at 6℃ in oxygen-free atmosphere from lightoAfter intravenous injection of dehydroandrographolidi succinaswater solution and liposomes injection, the pharmacokinetics and tissue distribution of dehydroandrographolidi succinas liposomal injection were studied. The experimental results showed that the concentration-time curves of dehydroandrographolidi succinas fit in a two-compartement open model. To compair with water solution, biological half-life of liposomes injection prolonyed 1.7 hours. The retention time of dehydroandrographolidi succinas in each tissue of mice was prolonged. The concentration in tissues was determined by HPLC. The result showed that concentration of dehydroandrographolidi succinas was highest in liver, followed by lung, spleen, plasma, kidney, heart. These studies provided a basic foundation for further development and research liposomes . |