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 ; Astragalus Plant ; chemistry ; Biological Transport ; Caco-2 Cells ; Fluorescein-5-isothiocyanate ; chemistry ; Fluorescent Dyes ; chemistry ; Humans ; Plant Extracts ; chemistry ; pharmacokinetics ; Polysaccharides ; chemistry ; pharmacokinetics

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 ; chemistry ; Flavonoids ; analysis ; Particle Size ; Polysaccharides ; chemistry ; Powders ; Soybeans ; chemistry

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 ; chemistry ; metabolism ; Chemical Phenomena ; Chemistry, Pharmaceutical ; methods ; Intestinal Absorption ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; metabolism ; Soybeans ; chemistry ; Temperature

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 ; chemistry ; Chemical Precipitation ; Chemistry, Pharmaceutical ; methods ; Durapatite ; chemistry ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; Time Factors

OBJECTIVETo compare the dissolution characteristics of colloidal silica and porous silica as the solid dispersion carrier, with baicalin as the model drug.

METHODThe baicalin solid dispersion was prepared by the solvent method, with colloidal silica and porous silica as the carriers. In the in vitro dissolution experiment, the solid dispersion was identified by scanning electron microscopy, differential scanning and X-ray diffraction.

RESULTThe solid dispersion carriers prepared with both colloidal silica and porous silica could achieve the purpose of rapid release. Along with the increase in the proportion of the carriers, the dissolution rate is accelerated to more than 80% within 60 min. Baicalin existed in the solid dispersion carriers in the non-crystalline form.

CONCLUSIONThe release behaviors of the baicalin solid dispersion prepared with two types of carrier were different. Among the two solid dispersion carriers, porous silica dissolved slowly than colloidal silica within 60 min, and they showed similar dissolutions after 60 min.

Calorimetry, Differential Scanning ; Colloids ; chemistry ; Drug Carriers ; chemistry ; Drug Delivery Systems ; instrumentation ; Flavonoids ; chemistry ; pharmacology ; Porosity ; Silicon Dioxide ; chemistry ; Solubility

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 ; metabolism ; Drug Compounding ; methods ; Flavonoids ; chemistry ; Hydrogen-Ion Concentration ; Hydrolysis ; Temperature ; Time Factors

Flavonoids are natural products that are ubiquitous in the natural world, with wide physiological activities and low toxic and side effects. In recent years, their anti-tumor effect has caused widespread concern and studies. According to the findings, flavonoids have prominent effects in preventing and treating lung cancer, breast cancer, colon cancer, prostate cancer, liver cancer, leukemia, ovarian cancer, gastric cancer and so on. Their anti-tumor mechanisms mainly include anti-oxidation, anti-free radical, induction of apoptosis of cancer cells, impact on cell cycle, immune regulation, inhibition of tumor angiogenesis, inhibition of COX-2, inhibition of telomerase activity and so on. This article focuses on the advance in domestic and foreign studies on anti-cancer activity and mechanism of flavonoids, in order to provide theoretical basis and research ideas for the further development and clinical application of flavonoids.
Animals ; Antineoplastic Agents ; pharmacology ; Antioxidants ; pharmacology ; Apoptosis ; drug effects ; Cell Cycle Checkpoints ; drug effects ; Cyclooxygenase 2 Inhibitors ; pharmacology ; Flavonoids ; pharmacology ; Humans

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 ; chemistry ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Drug Carriers ; chemistry ; Drug Stability ; Microscopy, Electron, Scanning ; Oleanolic Acid ; chemistry ; Plant Extracts ; chemistry ; Solubility

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 ; Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; Epimedium ; chemistry ; Flavonoids ; chemistry ; Porosity ; Solubility ; Starch ; chemistry ; X-Ray Diffraction

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 ; Carbon ; chemistry ; Drug Stability ; Microscopy, Electron, Scanning ; methods ; Oils, Volatile ; chemistry ; Sesquiterpenes ; chemistry