| Based on the theories and methods of physical chemistry and pharmacy, ginsenoside Rg3 microemulsion was prepared using micromulsion as drug delivery system and ginsenoside Rg3 as the material.We improved Shenyi capsule from the dosage form and route of administration,which can be used to intravenous inject diretly. This would ensure a marked rise in bioavailability and clinic.Based on the modern theory and method of quality control of medication , the quality of ginsenoside Rg3 microemulsion was assessed by transmission electron microscope , photon correlation spectrometer, HPLC and so on.This established the theoretical basis and supplied technical references for the exploiture of the new dosage form of ginsenoside Rg3. A new research field for the exploiture of the new dosage form of ginsenoside Rg3 was inaugurated.The literature indicated that the ginsenoside Rg3 has extensive pharmacological actions. It can restrain the proliferation of blood vessel endothelial cell induced by stomach cancer and the growth of galactophore wettability probe cancer transplanted tumor. The anti-cancer drug, Shenyi-capsule its essential component is ginsenoside Rg3, won the certificate of national new drug and has been applied to clinic. But,its bioavailability is so low that the Cmax is only (16±6)ng·mL-1 after oral taking 3.2mg-kg-l ginsenoside Rg3. Recently researches indicate that micromulsion as drug delivery system can improve the solubility of slightly solubility drugs,adsorption and bioavailability. So the ginsenoside Rg3 microemulsion could be prepared using micromulsion as its delivery system . Bioavailability of ginsenoside Rg3 can be improved by mainline.Ginsenoside Rg3 was isolated by low pressure Rp-18 column chromatography from protopanaxadiol saponins. Based on the physical and chemical data and their 1H-NMR,13C-NMR, it had been identified as ginsenoside Rg3. Ginsenoside Rg3 is pure, isolated by Rp-18 columnchromatography.We choose the Tween-80, Tween-20 and PC as surfactants, the Alcohol, iso-propyl alcohol and propylene glycol as cosurfactants, the soybean salad oil, earthnut oil and iso-proyl myristate as oil phase。 On the basis of the triangular phase diagrams, the effect of various elements and different additives on the formation of the microemulsion were investigated.Many factors that have had influence on proportion of microemulsion , surfactants, cosurfactants,oil phrase , Km ,and so on. Structure of microemulsion was invested by refractometry. HLB value of surfactant has had influence on structure of microemulsion. It is easy to form o/w microemulsion as the HLB value of surfactant is lager. It is easy to form w/o microemulsion as the HLB value of surfactant is lesser.To establish an accurate method for the determination of Rg3 in the solution of microemulsion. Ginsenoside Rg3 was determined by RP- HPLC with the condition of Shim-Pack CLS-ODS as the chromatographic column , acetonitrile- water(60 : 40) as the mobile phase ,and 203 nm as t he detection wavelength. The linear rang was 0.010mg/ml~0.10mg/ml(r=0.9998).Its average recovery rate was 99.96% and RSD % was 2.07%(n=5)。 The method was convenient, rapid, accurate and suitable for assay of ginsenoside Rg3 in the preparation.The effect of elements on the concentration of ginsenoside Rg3 in microemulsion was investigated the first time. Many factors that have had influence on proportion of microemulsion , surfactants, cosurfactants ,Km and AS/O and so on.We found that ginsenoside Rg3 exists in microemulsion almost in the form of sphaeroid and distributes uniformly by the figure and particle diameter of ginsenoside Rg3 in microemulsion with the method of transmission electron microscope. The distribution of particle diameter of ginsenoside Rg3 in ginsenoside Rg3 microemusion were determined by photon correlation spectrometer. The average particle diameter of ginsenosideRg3 was 18.3nm, and distributed in ortho state mostly.Acute toxicity test was carried out to judge the general toxicity of ginsenoside Rg3 microemulsion. The LD50 of gin... |
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