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.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.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
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X-Ray Diffraction
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
;
chemistry
;
Lipid Peroxidation
;
drug effects
;
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
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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
;
Drugs, Chinese Herbal
;
chemistry
;
Epimedium
;
chemistry
;
Flavonoids
;
chemistry
;
Porosity
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Solubility
;
Starch
;
chemistry
;
X-Ray Diffraction
9.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
;
chemistry
;
Drug Stability
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Microscopy, Electron, Scanning
;
methods
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Oils, Volatile
;
chemistry
;
Sesquiterpenes
;
chemistry