Study On JMS-Lipsome For Injection

Potentilla anserine L comes from rosaceous torment and its root is used as drug.according to the "New Drug Registration and Administration Law" of SFDA.We have finished the extracting, separating and the qualitative work of the compounds from the Potentilla anserine's total glycoside which has the activity of anti-HBV, finished the research of separating and configuration identification of the major compound for the active part of Potentilla anserine, finished the pre-clinic systematic research of the Potentilla anserine active part including the pharmacology, pharmacodynamics and toxicity study of anti-HBV, finished the preparation technology research of JMS troche (membrane packed tablet) and the quality standards of JMS and its preparations. Because of the poor water solubility of JMS ,the bioavailiability is little after oral administration. In this study, a liposome preparation method called thin-film dispersion was modified to contain effective component of JMS, which improves the solubility , eliminates the stimulus and increases the safety of JMS by vein injection.Total saponins were separated and purified by D101 macroreticular resin, which eliminating the interference from other impurities for the quantitative test, then measured by spectrophotometry with venina-perchlonic acid and the result is 91.2%; The liposomes were prepared with thin film evaporation and probe ultrasonic technique, then treated further by lyophilization. In order to ensure reproducibility and obtain higher entrapment efficiency, the basic formulation of JMS-Lipsome was determined using single factor investigation, the formulation and the preparation process were optimized by orthogonal design test. For further preparation, JMG, an important index components, were determined by HPLC. The content of JMG was 41.2%. Liposome physicochemical properties, stabilities, and primary pharmacodynamics were also investigated in this paper. The results in stability test showed that only minor changes in entrapment efficiency and content as a function of time. To study the mechanism of JMS, lipsome protective effects on experimental hepatic injury in mice have been done. JMS-Lipsome 50 mg·kg^-1 significantly inhibited the rising of serum GPT and GOT (p < 0. 01) .JMS-Lipsome 25 mg·kg^-1 inhibited the rising of serum GPT and GOT (P < 0. 05 ). JMS-Lipsome in high-dose and middle-dose groups could inhibit DHBV-DNA replication in vivo ( P < 0. 05 ). To some extent, JMS-Lipsome in 40 mg·kg^-1 and 80mg·kg^-1 could inhibit DHBV-DNA respectively.This paper indicated that JMS-Lipsome could provide a safe and effective dosage for JMS by vein injection. JMS-Lipsome had significant protective effects on experimental hepatic injury in mice, aslo, it could inhibit HBV and showed its potential clinical application in HBV treatment.