2.Study on totai flavonoids of Epimedium assisted with soybean polysaccharide spray-drying powder.
Hong-mei YAN ; Xiao-bin JIA ; Zhen-hai ZHANG ; E SUN ; Jia-hui DENG
China Journal of Chinese Materia Medica 2015;40(15):2994-2998
In order to evaluate the characteristics of the spray drying of total flavonoids of Epimedium extracts assisted with soybean polysaccharide, a certain percentage of soybean polysaccharide or polyvidone were added to the total flavonoids of Epimedium extract to conduct the spray drying. The effect of soybean polysaccharides against the wall sticking effect of the spray drying was detected, as well as the powder property of total flavonoids of Epimedium spray drying powder and the dissolution in vitro behavior of the effective component. Compared with the total flavonoids of Epimedium spray drying powder, soybean polysaccharide revealed a significant anti-wall sticking effect. The spray drying power which had no notable change in the grain size made a increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior. It was worth further studying the application of soybean polysaccharide in spray drying power of traditional Chinese medicine.
Epimedium
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chemistry
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Flavonoids
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analysis
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Particle Size
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Polysaccharides
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chemistry
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Powders
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Soybeans
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chemistry
3.Study on solid dispersion of precipitated calcium carbonate-based oleanolic acid.
Hong-mei YAN ; Zhen-hai ZHANG ; Xiao-bin JIA ; Yan-rong JIANG ; E SUN
China Journal of Chinese Materia Medica 2015;40(10):1935-1938
Oleanolic acid-precipitated calcium carbonate solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry and scanning electron microscopy (SEM). And its in vitro release also was investigated. The properties of the precipitated calcium carbonate was studied which was as a carrier of oleanolic acid solid dispersion. Differential scanning calorimetry analysis suggested that oleanolic acid may be present in solid dispersion as amorphous substance. The in vitro release determination results of oleanolic acid-precipitated calcium carbonate (1: 5) solid dispersion showed accumulated dissolution rate of.oleanolic acid was up to 90% at 45 min. Accelerating experiment showed that content and in vitro dissolution of oleanolic acid solid dispersion did not change after storing over 6 months. The results indicated that in vitro dissolution of oleanolic acid was improved greatly by the solid dispersion with precipitated calcium carbonate as a carrier. The solid dispersion is a stabilizing system which has actual applied value.
Calcium Carbonate
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chemistry
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Calorimetry, Differential Scanning
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Chemistry, Pharmaceutical
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Drug Carriers
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chemistry
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Drug Stability
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Microscopy, Electron, Scanning
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Oleanolic Acid
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chemistry
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Plant Extracts
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chemistry
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Solubility
4.Study on porous starch as solid dispersion carrier of total Epimedium flavonoids.
Hong-mei YAN ; Xiao-bin JIA ; Zhen-hai ZHANG ; E SUN ; Yi-hao XU
China Journal of Chinese Materia Medica 2015;40(9):1723-1726
In order to evaluate the characteristic of porous starch (PS) as the solid dispersions carrier of the total Epimedium flavonoids (TEF), the PS was used. The dissolution of icariin was selected as an indicator to analyze the differences of dissolution between TEF and its solid dispersion. TEF was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). Solid dispersion was irregular block and no powder characteristics of TEF and PS could be seen in SEM, DSC and XRD analysis suggested that TEF may be present in solid dispersion as amorphous substance. The dissolution rate of icariin has been improved significantly when the proportion of TEF and PS was 1:2. PS as a traditional solid dispersion carrier is worthy of further study.
Calorimetry, Differential Scanning
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Chemistry, Pharmaceutical
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Drugs, Chinese Herbal
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chemistry
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Epimedium
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chemistry
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Flavonoids
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chemistry
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Porosity
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Solubility
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Starch
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chemistry
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X-Ray Diffraction
5.Study on preparation of sagittatoside B with epimedin B converted from cellulase.
Feng-Juan XU ; E SUN ; Zhen-Hai ZHANG ; Li CUI ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(2):235-239
To prepare sagittatoside B with epimedin B Hydrolyzed from cellulase. With the conversion ratio as the index, the effects of pH value, temperature, reaction time, dosage of enzyme and concentration of substrates on the conversion ratio were detected. L9 (3(4)) orthogonal design was adopted to optimize the preparation process. Hydrolyzed products were identified by MS, 1H-NMR, and 13C-NMR. The results showed that the optimum reaction conditions for the enzymatic hydrolysis were that the temperature was 50 degrees C, the reaction medium was pH 5.6 acetic acid-sodium acetate buffer solution, the concentration of substrates was 20 g x L(-1), the mass ratio between enzyme and substrate was 3: 5, and the relative molecular mass of the reaction product was 646.23. NMR data proved that the product was sagittatoside B. The process is simple and reliable under mild reaction conditions, thus suitable for industrial production.
Cellulase
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metabolism
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Drug Compounding
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methods
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Flavonoids
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chemistry
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Hydrogen-Ion Concentration
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Hydrolysis
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Temperature
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Time Factors
6.Study on preparation of salvianolic acid phospholipid compound.
Xiao-Yun CHEN ; Zhen-Hai ZHANG ; Dan LIU ; Dan-Hong YU ; E SUN ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(2):216-221
To prepare salvianolic acid phospholipid compound. With the compound of salvianolic acids and soybean phospholipid as the index, mono-factor experiment and orthogonal design experiment were conducted to screen its technical parameters. According to the results, the optimal preparation conditions of salvianolic acid phospholipid compound were that THF were taken as the reaction solvent, the concentration time was 3 h, the reactant concentration was 5 g x L(-1), the mass ratio of salvianolic acids and phospholipid was 1: 1.5, and the reaction temperature was 40 degrees C. The oil/water partition coefficient of the prepared salvianolic acid phospholipid compound significant increased in water and buffers with different pH values. The results of phase analysis such as DSC, XRD and FTIR indicated that salvianolic acids existed in phospholipid in an amorphous state.
Alkenes
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chemistry
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metabolism
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Chemical Phenomena
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Chemistry, Pharmaceutical
;
methods
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Intestinal Absorption
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Phospholipids
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chemistry
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Polyphenols
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chemistry
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metabolism
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Soybeans
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chemistry
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Temperature
7.Study on oral absorption enhancers of astragalus polysaccharides.
Xiao-Yun CHEN ; Xiao-Bin TAN ; E SUN ; Dan LIU ; Xiao-Bin JIA ; Zhen-Hai ZHANG
China Journal of Chinese Materia Medica 2014;39(7):1243-1247
Astragalus polysaccharides was lounded to 4-(2-aminoethylphenol), followed by labeling the APS-Tyr with fluorescein-5-isothiocyanate (FITC) at the secondary amino group. The absorption enhancement effects of low molecular weight chitosan and protamine on astragalus polysaccharides were evaluated via Caco-2 cell culture model. The results show that the fluorecent labeling compound has good stability and high sensitivity. On the other hand low molecular weight chitosan and protamine also can promoted absorption of the astragalus polysaccharides without any cytotoxity, and the absorption increase was more significant with increasing the amount of low molecular weight chitosan and protamine. At the same time, the low molecular weight chitosan has slightly better effect. The transepithelial electric resistance (TEER) of Caco-2 cells show that absorption enhancers could improve its membrane transport permeability by opening tight junctions between cells and increasing the cell membrane fluidity.
Absorption
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Astragalus Plant
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chemistry
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Biological Transport
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Caco-2 Cells
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Fluorescein-5-isothiocyanate
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chemistry
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Fluorescent Dyes
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chemistry
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Humans
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Plant Extracts
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chemistry
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pharmacokinetics
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Polysaccharides
;
chemistry
;
pharmacokinetics
8.Studies on hydroxyapatite applicatied in coprecipitate of total salvianolic acids phospholipid complex.
Xiao-Yun CHEN ; Zhen-Hai ZHANG ; Dan LIU ; E SUN ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(6):992-996
The purpose of this research was to prepare total salvianolic acids-phytosome-HA coprecipitate to improve drug dissolution and its micromeritic properties. Firstly, the coprecipitate was prepared by solvent method and in vitro dissolution of tripterine was performed with the salvianolic acid B and danshensu as criteria. At the same time, the micromeritic properties was characterizated, the structure of samples was characterized by TEM, DSC, XRD and FTIR. Results showed that when the ratio of drug to HA was 1:2, it had a better dissolution, the accumulative drug-release percent in vitro at 60 min was over 90%. At the same time, it has good liquidity and low moisture absorption. Its micromeritic properties have improved. It is proved that the drug still existed amorphously by microstructure analysis. The preparation process is simple and feasible, it has practical value.
Alkenes
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chemistry
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Chemical Precipitation
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Chemistry, Pharmaceutical
;
methods
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Durapatite
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chemistry
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Phospholipids
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chemistry
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Polyphenols
;
chemistry
;
Time Factors
9.Effects of micronization on micromeritics properties of baicalin.
Hong-Mei YAN ; Dong-Mei DING ; E SUN ; Jing WANG ; Xiao-Bin JIA ; Zhen-Hai ZHANG
China Journal of Chinese Materia Medica 2014;39(4):653-656
Baicalin extremely fine powder was made by using ball-mill and the effect of micronization on the micromeritics properties of baicalin was studied and analyzed. The microstructures of baicalin ordinary and extremely fine powder were compared by scanning electron microscope, differential scanning calorimeter and X-ray diffraction and the powder characteristic of them was investigated. The hygroscopicity was studied. The effect of micronization on the dissolution of baicalin was investigated. The results showed that the chemical constituents of baicalin were not changed after micronization with better compressibility. It was confirmed that micronization technology had a certain application value in promoting the insoluble component of baicalin absorption with higher dissolution.
Calorimetry, Differential Scanning
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Drugs, Chinese Herbal
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chemistry
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Flavonoids
;
chemistry
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Particle Size
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Solubility
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Wettability
;
X-Ray Diffraction
10.Ideas and methods of two-dimensional zebrafish model combined with chromatographic techniques in high-throughput screening of active anti-osteoporosis components of traditional Chinese medicines.
Ying-Jie WEI ; Li-Jun JING ; Yang ZHAN ; E SUN ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2014;39(9):1739-1742
OBJECTIVETo break through the restrictions of the evaluation model and the quantity of compounds by using the two-dimensional zebrafish model combined with chromatographic techniques, and establish a new method for the high-throughput screening of active anti-osteoporosis components.
METHODAccording to the research group-related studies and relevant foreign literatures, on the basis of the fact that the zebrafish osteoporosis model could efficiently evaluate the activity, the zebrafish metabolism model could efficiently enrich metabolites and the chromatographic techniques could efficiently separate and analyze components of traditional Chinese medicines, we proposed that the inherent combination of the three methods is expected to efficiently decode in vivo and in vitro efficacious anti-osteoporosis materials of traditional Chinese medicines.
RESULT AND CONCLUSIONThe method makes it simple and efficient in the enrichment, separation and analysis on components of traditional Chinese medicines, particularly micro-components and metabolites and the screening anti-osteoporosis activity, fully reflects that efficacious materials of traditional Chinese medicines contain original components and metabolites, with characteristic of "multi-components, multi-targets and integral effect", which provides new ideas and methods for the early and rapid discovery of active anti-osteoporosis components of traditional Chinese medicines.
Animals ; Chromatography ; methods ; Disease Models, Animal ; Drug Evaluation, Preclinical ; methods ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Medicine, Chinese Traditional ; methods ; trends ; Osteoporosis ; drug therapy ; physiopathology ; Phytotherapy ; methods ; trends ; Reproducibility of Results ; Zebrafish ; physiology