2.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
3.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
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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
4.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
5.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
6.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
;
chemistry
;
Plant Extracts
;
chemistry
;
Solubility
7.Ethyl acetate-soluble chemical constituents from branch of Hypericum petiolulatum.
Qi ZHAO ; Hai-long ZHANG ; Xue ZHANG ; Xiao-meng LI ; Yu-zhen SUN ; Hang SU
China Journal of Chinese Materia Medica 2015;40(9):1755-1758
The stems and branches of Hypericum petiolulatum were extracted by alcohol and liquid-liquid extraction. Seven furofuran lignans were isolated from the ethyl acetate fraction of ethanol extract of H. petiolulatum by using silica gelchromatography, Sephadex LH-20 chromatography, medium-pressure liquid chromatography and preparative HPLC. Their structures were identified by the spectroscopic methods as pinoresinol (1), medioresinol (2), 8-acetoxypinoresinol (3), epipinoresinol (4), (+)-syringaresinol (5), (+)-1-hydroxysyringaresinol (6) and erythro-buddlenolE (7). All the isolates were firstly found in H. petiolulatum. In the bioassay, compound 7 showed remarkable antioxidative activity inhibiting Fe(+2)-cystine induced rat liver microsomal lipid peroxidation with inhibitory rate 38% at a concentration of 1 x 10(-6) mol · L(-1) (positive control Vit E with the inhibitory rate of 35% at the same concentration).
Animals
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Antioxidants
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chemistry
;
isolation & purification
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pharmacology
;
Drugs, Chinese Herbal
;
chemistry
;
isolation & purification
;
pharmacology
;
Hypericum
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chemistry
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Lipid Peroxidation
;
drug effects
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Microsomes, Liver
;
drug effects
;
metabolism
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Molecular Structure
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Oxidative Stress
;
drug effects
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Plant Stems
;
chemistry
;
Rats
8.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
;
chemistry
;
Epimedium
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chemistry
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Flavonoids
;
chemistry
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Porosity
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Solubility
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Starch
;
chemistry
;
X-Ray Diffraction
10.Gastrointestinal contrast agents for improving imaging quality of MRCP:comparison between Gd-DTPA and BaSO_4 suspension
qi, SUN ; xiao-long, DING ; wei-min, CHAI ; hai-xia, ZHANG
Journal of Shanghai Jiaotong University(Medical Science) 2006;0(01):-
Objective To assess and compare the effectiveness of gadolinium diethylenetriamine pentacetic acid(Gd-DTPA) solution and barium sulfate(BaSO4) suspension with different concentrations in improving the imaging quality of magnetic resonance cholangiopancreatography(MRCP). Methods The phantom study was carried out to determine the optimal concentration of Gd-DTPA and BaSO4 suspension used as an oral negative contrast agent in MRCP.The patients were grouped randomly and performed MRCP before and after using oral contrast agents in combination with intravenous injection of contrast agents.A comparison of the influence of BaSO4 suspension and Gd-DTPA with different concentrations on the signal intensity of the fluid in gastrointestinal tract on MRCP images was made.Results The phantom study showed that the dilution ratio 1∶10 of Gd-DTPA solution and 100%(W/V)BaSO4 suspension were the optimal concentrations in decreasing the signal intensity.In all patients the high signal intensity of the gastrointestinal fluid was completely suppressed after oral administration of Gd-DTPA diluted solution(P