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

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 ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Particle Size ; Solubility ; Wettability ; X-Ray Diffraction

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 ; methods ; Delayed-Action Preparations ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Epimedium ; chemistry ; Kinetics ; Tablets ; chemistry

OBJECTIVETo prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release.

METHODBaicalin-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.

RESULTThe 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.

CONCLUSIONThe 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.

Colon ; metabolism ; Flavonoids ; chemistry ; Hydrogen-Ion Concentration ; Polymethacrylic Acids ; chemistry ; Solubility ; Solvents ; chemistry ; X-Ray Diffraction ; methods

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.
Chemistry, Pharmaceutical ; methods ; Diterpenes, Abietane ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Particle Size ; Solubility

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

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 ; Clove Oil ; chemistry ; Curcuma ; chemistry ; Eugenol ; Graphite ; chemistry ; Microscopy, Electron, Scanning ; Oils, Volatile ; chemistry ; Oxides ; chemistry ; Plant Extracts ; chemistry ; Powders ; Sesquiterpenes

Objective: To observe the effect of acupuncture on Akt2 mRNA expression in skeletal muscle of insulin resistant rat models. Methods: Twenty-four SD rats were randomly divided into a control group, a model group and an acupuncture group. Fasting plasma glucose (FPG), fasting insulin (FINS), insulin sensitivity index (ISI), C peptide (C-P), as well as Akt2 mRNA expression in skeletal muscle of rats were detected by glucose oxidase method, ELISA and real-time PCR. Results: Compared with the control group, the level of FPG, FINS and C-P increased significantly (P<0.01) while ISI and Akt2 mRNA expression decreased markedly in the model group (P<0.01, P<0.05). In the acupuncture group, the levels of FPG, FINS and C-P were much lower than in the model group (P<0.01, P<0.01,P<0.05) and ISI and Akt2 mRNA expression increased markedly (P<0.01). Conclusion: The mechanism of acupuncture in treating insulin resistance may relate to the up-regulated of the Akt2 mRNA expression and to the improvement of the signal transduction of PI3K pathway.

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

Objective To investigate the learning curve of laparoscopy-assisted anorectoplasty in the treatment of high imperforate anus.Methods Sixty patients with high congenital anal atresia who were treated with laparoscopy-assisted anorectoplasty in the Capital Institute of Pediatrics from December 2008 to October 2015 by one experience surgeon were selected as observation group.Based on the criteria,the patients were divided into 4 groups(15 cases in each group) according to the sequence of the operation and every 15 cases served as a learning phase.The operating time,frequency of operation,complication rate,conversion rate to open surgery,blood loss,the rates of blood transfusion and hospital stay were compared among the 4 phases.Results The mean operation duration was (176.3 ±41.6) min,(128.8 ± 36.1) min,(127.3 ± 35.2) min,(124.0 ± 30.1) min in group A,B,C and D,respectively.The operation duration of 4 groups showed a declining trend.Group A has longer operation time than group B,C and D,the difference were statistically significant (P ＜ 0.05).In detail,the comparison of operation time between group A and group B was statistically significant (P ＜ 0.05).Furthermore,group A had significantly more median blood loss than group B,C and D,the differences were statistically significant [the 4 groups of data,respectively,group A:(17.5 ±6.5) mL,group B:(15.0±5.0) mL,group C:(14.5 ±5.5) mL,group D:(8.5 ±6.5) mL,P＜0.05].The mean capacity of blood loss was 12.7 mL.No significant difference was found in surgical complications,the rates of blood transfusion,total hospital stay,and postoperative hospital stay among the 4 groups(P ＞ 0.05).But the postoperative hospital stay decreased from 9.8 d (group A) to 7.4 d (group D).Conclusions For a well-trained surgeon in imperforate anus surgery.The learning curve of laparoscopy-assisted anorectoplasty in the treatment of high imperforate anus on about 15 cases helps to make a skillful surgeon.