1.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
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chemistry
;
pharmacokinetics
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.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
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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
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chemistry
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Time Factors
4.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
5.Study on absorbing volatile oil with mesoporous carbon.
Hong-mei YAN ; Xiao-bin JIA ; Zhen-hai ZHANG ; E SUN ; Yang NAN
China Journal of Chinese Materia Medica 2014;39(22):4340-4344
Clove oil and turmeric oil were absorbed by mesoporous carbon. The absorption ratio of mesoporous carbon to volatile oil was optimized with the eugenol yield and curcumol yield as criteria Curing powder was characterized by scanning electron microscopy (SEM) and differential scanning calorietry (DSC). The effects of mesoporous carbon on dissolution in vitro and thermal stability of active components were studied. They reached high adsorption rate when the absorption ratio of mesoporous carbon to volatile oil was 1:1. When volatile oil was absorbed, dissolution rate of active components had a little improvement and their thermal stability improved after volatile oil was absorbed by the loss rate decreasing more than 50%. Absorbing herbal volatile oil with mesoporous carbon deserves further studying.
Adsorption
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Carbon
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chemistry
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Drug Stability
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Microscopy, Electron, Scanning
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methods
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Oils, Volatile
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chemistry
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Sesquiterpenes
;
chemistry
6.Study on sustained release preparations of Epimedium component.
Hong-mei YAN ; Dong-mei DING ; Zhen-hai ZHANG ; E SUN ; Jie SONG ; Xiao-bin JIA
China Journal of Chinese Materia Medica 2015;40(8):1484-1488
The formulation for sustained release tablet of Epinedium component was selected and the evaluation equation of in vitro release was established. The liquidity of component was improved with the help of colloidal silica aided by spray drying, which would be the main drug in the sustained release tablets. Dissolution was selected as an evaluation index to investigate skeletal material type, fillers, impact porogen, lubricants and other materials on the quality of sustained release tablet. The sustained release tablets were prepared by dry compression. Formulation of sustained release preparations was main drug 35%, HPMC K(4M) 20% and HPMC K(15M) 10% as skeleton material, MCC 31% as filler, PEG6000 2% as porogen and magnesium stearate 2% as lubricant. The sustained release tablets released up to 80% in 8 h. The zero order equation, primary equation and Higuchi equation could simulate the release characteristics of sustained release tablets in vitro, the correlation coefficients r were larger than 0.96. The primary equation was most similar in vitro release characteristics and its correlation coefficient r was 0.9950. The preparation method is simple and the results of formulation selection are reliable. It can be used to guide the production of Epimedium component sustained release preparations.
Chemistry, Pharmaceutical
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methods
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Delayed-Action Preparations
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chemistry
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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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Kinetics
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Tablets
;
chemistry
7.Two-dimensional zebrafish model combined with hyphenated chromatographic techniques for evaluation anti-osteoporosis activity of epimendin A and its metabolite baohuoside I.
Yang ZHAN ; Ying-Jie WEI ; E SUN ; Feng-Juan XU ; Xiao-Bin JIA
Acta Pharmaceutica Sinica 2014;49(6):932-937
This article firstly established a new efficient method for screening anti-osteoporosis ingredients, which used two-dimensional zebrafish model combined with hyphenated chromatographic techniques to evaluate anti-osteoporosis activities of epimedin A and its metabolite baohuoside I. Adult zebrafish was used for metabolism of epimedin A in 0.5% DMSO, and LC-MS was used for analysis of the metabolite, which was captured by HPLC, and prednisolone-induced osteoporosis model of zebrafish was used to evaluate the anti-osteoporotic activities of trace amounts of epimedin A and baohuoside I. The results indicated that epimedin A and baohuoside I can prevent prednisolone-induced osteoporosis in zebrafish. The developed method in this paper enables the separation, enrichment and analysis of micro-amount metabolite of epimedin A, and anti-osteoporosis activities in vivo of epimedin A and baohuoside I was simple and efficient screening resorting to zebrafish osteoporosis mode. This paper would provide new ideas and methods for a rapid and early discovery of anti-osteoporosis activities of micro-ingredients and its metabolite of traditional Chinese medicine.
Animals
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Chromatography, High Pressure Liquid
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Chromatography, Liquid
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Drug Evaluation, Preclinical
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Drugs, Chinese Herbal
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pharmacology
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Flavonoids
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metabolism
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pharmacology
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Mass Spectrometry
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Osteoporosis
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drug therapy
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Zebrafish
8.Expression of both Albumin and Cytokeratin of Small Epithelial Cells in Human Hepatocellular Carcinoma
Jia-cheng, XIAO ; Shang-lin, ZHU ; Qin-yu, LI ; P, RUCK ; A, ADAM ; E, KAISERLING
Journal of Shanghai Jiaotong University(Medical Science) 2001;21(1):35-38
ObjectiveTo investigate whether small epithelial cells (SEC) exist in human hepa- tocellularcarcinoma (HCC) and if so, whether they exhibit immunolabelling for both albumin and cytokeratin 7 (CK7). MethodsThirty cases of human HCC from operative specimens were investi- gated by immunohistochemistry with antibody against albumin, a marker of hepatocyte differentiation and CK7, a marker of biliary differentiation. Ten cases were investigated by electron microscopy and by immuno- electron microscopy. ResultsThe SEC were found in 20 of 30 cases that located around the edges of the tumors and appeared as proliferative small biliary ductules. Under electron microscopy they were of small size, contained sparse cytoplasm, few free ribosomes, intracellular tonofilarnents, and intercellular junctions. Immunoelectron microscopically the SEC exhibited labelling for both albumin and CK7 in 5 out of 10 cases. ConclusionSEC in human HCC are found that represent the same mor- phology like those seen in hepatoblastoma and biliary atresia, co- expressed markers for hepatocytic and biliary differentiation.
9.Effect of suet oil on formation of self-assembled micelles of flavonoids in Epimedium.
Jie LI ; E SUN ; Zhen-hai ZHANG ; Jun JIANG ; Feng-juan XU ; Xiao-bin JIA
China Journal of Chinese Materia Medica 2014;39(17):3278-3282
In this paper, the action of suet oil in the preparation of self-assembled micelles of the active flavonoids in Epimedium in the simulated human environment was researched. Twelve suet oil samples were collected from different growing areas and different positions of sheep or goat to simulate the formation of micelles. Then the effects of the fatty acids in suet oil on the preparation of self-assembled micelles were studied furthermore. The results showed that the micelles had a dispersed state and spherical smooth surface. To compare the diameter, potential, encapsulation efficiency and drug loading of the 12 batches micelles, the micelles prepared by the suet oil from Qinghai were more stable and had a higher encapsulation efficiency. The fatty acids in suet oil could promote the formation of self-assembled micelles, but the whole suet oil had a better effect. Above all the study, we confirmed that the suet oil promoted the formation of self-assembled micelles of the flavonoids in Epimedium, it laid foundation for further research about increasing the efficacy of Epimedium and improved the absorption of the active flavonoids in Epimedium.
Animals
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Chemistry, Pharmaceutical
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methods
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China
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Drug Carriers
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chemistry
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Electric Conductivity
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Epimedium
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chemistry
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growth & development
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Fatty Acids
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chemistry
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Flavonoids
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chemistry
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Geography
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Goats
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Humans
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Micelles
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Oils
;
chemistry
;
Sheep
10.Solidification of volatile oil with graphene oxide.
Hong-Mei YAN ; Xiao-Bin JIA ; Zhen-Hai ZHANG ; E SUN ; Yi-Hao XU
Acta Pharmaceutica Sinica 2015;50(2):222-226
To evaluate the properties of solidifying volatile oil with graphene oxide, clove oil and zedoary turmeric oil were solidified by graphene oxide. The amount of graphene oxide was optimized with the eugenol yield and curcumol yield as criteria. Curing powder was characterized by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The effects of graphene oxide on dissolution in vitro and thermal stability of active components were studied. The optimum solidification ratio of graphene oxide to volatile oil was 1:1. Dissolution rate of active components had rare influence while their thermal stability improved after volatile oil was solidified. Solidifying herbal volatile oil with graphene oxide deserves further study.
Calorimetry, Differential Scanning
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Clove Oil
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chemistry
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Curcuma
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chemistry
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Eugenol
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Graphite
;
chemistry
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Microscopy, Electron, Scanning
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Oils, Volatile
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chemistry
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Oxides
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chemistry
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Plant Extracts
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chemistry
;
Powders
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Sesquiterpenes