Evaluation on contribution rate of each component total salvianolic acids and characterization of apparent oil/water partition coefficient / 中国中药杂志

The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments: HUVECs oxidative damage experiment, 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B, rosmarinic acid and Danshensu were 28.85%, 30.11%, 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32, 1.06, 0.89, 0.98, 0.90, 0.13, 0.02, 0.20, 0.56 when in octanol-water/pH 1.2 dilute hydrochloric acid solution/ pH 2.0, 2.5, 5.0, 5.8, 6.8, 7.4, 7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.

Solidification of volatile oil with graphene oxide / 药学学报

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.

Advance in studies on anti-cancer activity and mechanism of flavonoids / 中国中药杂志

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.

Study on porous starch as solid dispersion carrier of total Epimedium flavonoids / 中国中药杂志

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.

Study on solid dispersion of precipitated calcium carbonate-based oleanolic acid / 中国中药杂志

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.

Effect of D-α-tocopherol polyethylene glycol 1000 succinate on inhibition of MCF-7 cell proliferation by baohuoside I / 中草药

Objective: To investigate the effect of D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) on the inhibition of proliferation of breast cancer cells MCF-7 by baohuoside I. Methods: The cytotoxicity of baohuoside I to MCF-7 cells was determined by MTT assay, the cellular uptake of baohuoside I was detected by fluorescence microscopy, and the intracellular baohuoside I was determined by HPLC. Results: The effect of baohuoside I on the inhibition of MCF-7 cell proliferation was enhanced in the presence of TPGS, especially on lower concentration. The uptake rates of MCF-7 within 2 h were 29.51%, 38.12%, and 40.37%, when the proportions of baohuosaide I and TPGS were 1:1, 1:2, and 1:4, respectively. The ratios were increased by 27.92%, 65.24%, and 74.99% compared with those using baohuoside I only. Conclusion: TPGS can increase the uptake rate of baohuoside I in MCF-7 cells and enhance the inhibition of MCF-7 cell proliferation.

Discussion about research ideas of Chinese materia medica based on Chinese materia medica components and "composition structure" theory / 中草药

Chinese materia medica (CMM) is the product of long-term practice of clinical traditional Chinese medicine (TCM), and it has the characteristics of overall effect of the multi-component and multilink multiple targets. Because of the complexity of CMM, it has not yet formed systematic and the scientific method for the TCM research, which seriously restricts the development of modernization of CMM. Under the guidance of TCM theory, we explore the study on the new mode of CMM whose components are divided into the functional units by the CMM research foundation of material basis, pharmacological mechanism, the structure optimization, and new idea on the CMM quality control based on composition structure theory and in vivo pharmacokinetic as well.

Preparation of scutellarin-piperine co-amorphous complex and its in vitro release / 中草药

Objective: To prepare scutellarin-piperine co-amorphous complex, in order to improve their dissolution and solubility. Methods: Scutellarin-piperine co-amorphous complex was prepared using solvent evaporation method. The microscopic structure and physicochemical properties of co-amorphous complex were analyzed using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD), and infrared vibrational spectra (IR). And its in vitro release also was investigated. The formation of the co-amorphous complex in scutellarin and piperine was studied. Results: DSC and XRD analysis suggested that scutellarin and piperine may be present as amorphous substance. IR results indicated molecular interactions between scutellarin and piperine. The in vitro release determination results of scutellarin-piperine co-amorphous complex showed accumulated dissolution rate of scutellarin and piperine could both be improved. Conclusion: The drug-drug co-amorphous system can provide certain reference for insoluble drugs to improve their dissolution and solubility.

Study on sustained release preparations of Epimedium component / 中国中药杂志

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.

Study on totai flavonoids of Epimedium assisted with soybean polysaccharide spray-drying powder / 中国中药杂志

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.

Effect of spray drying process on physical properties and dissolution of tanshinone / 中国中药杂志

In order to improve the dissolution in vitro of components by processing tanshinone with the pray drying method, the physical properties of tanshinone power was analyzed by BET, differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction, and its dissolution in vitro was also investigated. The results of characterization showed decreased power size and increased specific surface area of tanshinone powder, and its existence in an amorphous state. Within 4 h, the accumulated dissolutions of tanshinone I and tanshinone II(A) in components of tanshinone reached 78.3%, 81.9%, respectively. Therefore, the spray-drying method was conducive to enhance the dissolution of components of tanshinone.

Study on absorbing volatile oil with mesoporous carbon / 中国中药杂志

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.

Preparation of baicalin colon-specific solid dispersion and evaluation on its in vitro release / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release.</p><p><b>METHOD</b>Baicalin-eudragit S100 solid dispersion was prepared by using the solvent method. The microscopic structure and physicochemical properties were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared spectroscopy (IR). And its in vitro release was also investigated.</p><p><b>RESULT</b>The results of DSC and XRD analysis suggested that baicalin may be dispersed in solid dispersion in the amorphous state. IR results indicated a non-covalent bond effect may exist between baicalin and eudragit S100. The results of in vitro release determination showed that very few baicalins in pH 1.2 diluted hydrochloric acid solution for 2 h at the baicalin-eudragit S100 ratio of 1 : 6. The accumulated dissolution rate was less than 15% in pH 6.8 phosphate buffer solution for 4 h, but exceeding 90% in pH 7.6 phosphate buffer solution for 1 h.</p><p><b>CONCLUSION</b>The prepared baicalin-eudragit S100 solid dispersion could achieve the objective of colon-specific delivery and rapid drug release, and helps increase the concentration of baicalin in colons.</p>

Physicochemical properties of baohuoside I phytosomes and its anti-tumor activity / 中国药学杂志

OBJECTIVE: To prepare baohuoside I phytosomes and study its anti-tumor activities in vitro.

Study on co-processd excipient of microcrystalline cellulose and glycerol monostearate / 中草药

Objective: The co-processd excipient containing microcrystalline cellulose (MCC) and glycerol monostearate (GMS) was prepared. The humidity resistance of MCC used in Chinese materia medica (CMM) was improved and the possibility of this co-processd excipient used in the preparation of CMM tablet was explored. Methods: The co-processd excipient containing MCC and GMS was prepared by applying spray drying method. The moisture absorption, flow ability, compressibility, and disintegration were as the indexes to optimize the best preparation of co-processd excipient through uniform design methodology. The powder characteristic of co-processd excipient was investigated and the microstructures were studied by scanning electron microscope (SEM), differential scanning calorimeter (DSC), X-ray diffraction (XRD), and Flourier transform infra-red (FTIR) spectroscopy. The effect of co-processd excipient on the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts was investigated. The in vitro dissolution of hyperside and ferulic acid in Xinyueshu Tablet was studied. Results: The results showed that the optimal conditions of the preparation consisted of 1 portion of GMS, 12 portions of MCC, and 200 portions of water, emulsionzing temperature of 66°C, and mixing time of 1 h. It was confirmed that the chemical constituents in co-processd excipient were not changed after spray drying with smaller particle size and better fluidity. The co-processd excipient can improve the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts without affecting the disintegration of MCC. Conclusion: The co-processd excipient prepared has good humidity resistance and it is confirmed to have application prospect.

Preparation of baicalin-chitooligosaccharide compound and its characterization / 中国中药杂志

To apply chitooligosaccharide in the preparation of baicalin compound, in order to increase the drug dissolution in vitro, and investigate the basic property of the compound. Baicalin-chitooligosaccharide compound was prepared by using the solvent method. The structure and physicochemical properties of compound were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared vibrational spectrum (IR), and its dissolution behavior was also investigated. The results showed that the compound prepared at baicalin-chitooligosaccharide molar ratio of 1 : 1 could significantly improve the dissolution of baicalin. The results of DSC and XRD analysis suggested that baicalin may exist in an amorphous state. IR results indicated the interaction between baicalin and chitooligosaccharide. The baicalin-chitooligosaccharide compound could significantly improve dissolution in vitro of drug.

Effects of micronization on micromeritics properties of baicalin / 中国中药杂志

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.

Compared with colloidal silica and porous silica as baicalin solid dispersion carrier / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the dissolution characteristics of colloidal silica and porous silica as the solid dispersion carrier, with baicalin as the model drug.</p><p><b>METHOD</b>The 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.</p><p><b>RESULT</b>The 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.</p><p><b>CONCLUSION</b>The 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.</p>

Evaluation on preparation process of baicalin-Eudragit L100-55 enteric coated solid dispersion and its in vitro release / 中草药

Objective: To prepare the baicalin-Eudragit L100-55 (EL) enteric coated solid dispersion and to investigate the feasibility of this baicalin preparation. Methods: Baicalin-EL enteric coated solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD), and infrared vibrational spectra (IR). And its in vitro release was also investigated. Results: DSC and XRD analyses suggested that baicalin may be present in enteric coated solid dispersion as amorphous substance. IR results indicated the presence of interactions between baicalin and EL. The in vitro release showed the accumulated dissolution rate of baicalin was less than 3% in artificial pH 1.2 dilute hydrochloric acid solution for 2 h, but an accumulated dissolution rate exceeding 90% in pH 6.8 phosphate buffer solution for 2 h when baicalin-EL ratio reached 1:6. Conclusion: Baicalin-EL enteric coated solid dispersion prepared could release drug rapidly and increase local drug concentration and then improve the oral absorption of baicalin.

Study on Xinyueshu spray drying assisted with copovidone and its effect on powder property / 中国中药杂志

To study the application characteristics of copovidone (PVP-S630) in Xinyueshu extracts during the spray drying process, and its effect on such pharmaceutical properties as micromeritics and drug release behavior. PVP-S630 was added into Xinyueshu extracts to study on the spray drying, the effect of different dosages of PVP-S630 against the wall sticking effect of the spray drying, as well as the power property of Xinyueshu spray drying power and the dissolution in vitro behavior of the effective component of hyperoside. The results showed that PVP-S630 revealed a significant anti-wall sticking effect, with no notable change in the grain size of the spray drying power, increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior of hyperoside. It was worth further studying the application of PVP-S630 in spray drying power of traditional Chinese medicine.