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

Objective To analyse the sensitivity ,specificity and coincidence rate of genechip method in the detection of resistance to antibacterial agents in Mycobacterium tuberculosis(MTB) ,in order to provide a convenient ,accurate and rapid method for detec‐ting antibacterial resistance in MTB .Methods The DNA sequencing was taken as gold standard ,and antibacterial resistance of the strains of MTB isolated from sputum specimens of 250 cases of patients with tuberculosis from August to December 2014 were de‐tected by using the genechip method and proportion method for susceptibility testing at the same time .Efficacies of the two methods in detecting MTB resistance to rifarnpin and isoniazid were compared .Results The MTB resistance rate to rifarnpin detected by u‐sing the genechip method and proportion method for susceptibility testing was 3 .0% and 3 .5% respectively ;that to isoniazid was 6 .7% and 8 .2% respectively .For detecting M TB resistance to rifarnpin and isoniazid ,the DNA sequencing was taken as gold standard ,the sensitivity ,specificity and coincidence rate of genechip method was higher than those of proportion method for suscep‐tibility testing ,and the test time of genechip method was shorter than that of proportion method for susceptibility testing ,there were statistically significant differences(P<0 .05) .Conclusion Using the genechip method to detecting MTB resistance to rifampin and isoniazid has high sensitivity ,specificity and coincidence rate ,which could replace the proportion method for susceptibility tes‐ting and become an effective method .

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

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

OBJECTIVETo observe the effect of Baichanting Compound (BC) on dopamine (DA) in striatum of Parkinson's disease (PD) mice, and to screen the optimal component proportion.

METHODSThe PD model was established in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induced C57BL/6 mice. By using uniform design, they were intervened by three extracts of BC in different proportions [Acanthopanax senticosus extract (X1): white peony root extract (X2): Uncaria rhynchophylla extract (X3) = 30.00: 34.92: 82.50, 48.00: 19.98: 72.19, 18.00: 44.88: 61.88, 36.00: 29.94: 51.56, 54.00: 15.00: 41.25, 24.00: 39.90: 30.94, 42.00: 24.96: 20.63). Equal volume of 5% carboxymethylcellulose sodium was administered to mice in the model group and the normal group by gastrogavage. All medication was lasted for 20 successive days. The dopamine (DA) content was determined by ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS). Except 10 in the normal group, 20 PD model mice were screened and divided into the model group and the BC group (with the optimal proportion) according to random digit table. BC extract in optimal proportion was administered to mice in the BC group by gastrogavage, while equal volume of 5% carboxymethylcellulose sodium was administered to mice in the model group and the normal group by gastrogavage. All medication was lasted for 20 successive days. Praxiology was observed in each group. DA content in striatum was also detected. Results Compared with the normal group, the DA content in striatum decreased significantly in the model group (P < 0.01), suggesting a successful PD modeling. Compared with the model group, the DA content in striatum increased significantly in 1 and 2 groups (P<0.05). According to results of quadratic polynomial stepwise regression statistics, the regression equation obtained was: Y = 0.265 + 0.026 X 2 - 0.056 X 3 + 0.334 x 10(-3) x X1 x X3 + 0.691 x 10(-3) X X3(2). X3 extract was the main factor influencing the effectiveness (P < 0.01). The optimal proportion of BC was predicted by the regression equation: X1 = 54.00 mg/(kg x d), X2 = 44.88 mg/(kg x d), the X3 = 82.50 mg/(kg x d). The pole climbing time was shortened, times of autonomic activities increased, DA content was elevated, all with statistical difference in BC groups (P < 0.01, P < 0.05).

CONCLUSIONBC could increase DA content in PD model mice with the optimal proportion as 54.00: 44.88: 82.50.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine ; Animals ; Disease Models, Animal ; Dopamine ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Mass Spectrometry ; Mice ; Mice, Inbred C57BL ; Motor Activity ; Parkinson Disease ; drug therapy ; metabolism

Diagnosis, Differential ; Endothelium, Vascular ; metabolism ; pathology ; Female ; Humans ; Hyperplasia ; Jejunal Diseases ; metabolism ; pathology ; surgery ; Jejunum ; blood supply ; pathology ; surgery ; Middle Aged ; Platelet Endothelial Cell Adhesion Molecule-1 ; metabolism

OBJECTIVETo study the function of pancreatic islet beta cells, insulin resistance (IR) and features of TCM symptoms and syndromes in the non-diabetic first-grade relatives (ND1GR) of patients with type 2 diabetes mellitus (DM2).

METHODSA total of 68 ND1GR of DM2 patients were enrolled in the observed group and 45 healthy subjects with matched sex, age and body mass index (BMI) but without family history of DM were selected into the control group. Levels of fasting blood glucose (FBG), 2 hrs postprandial glucose (2hPG), fasting insulin (FINS) and 2 hrs postprandial insulin (2h INS) in all the subjects were measured to calculate and compare the IR and beta-cell function of the homeostatic model analog (HOMA-IR and HOMA-beta), and the insulin sensitive index (ISI). Moreover, the symptoms manifested in the ND1GR were also observed to analyze the features in them.

RESULTSFBG and FINS were obviously higher in the observed group than those in the control group (P < 0.01), while no significant difference was found in 2hPG or 2h INS (P > 0.05). HOMA-IR and HOMA-beta were significantly higher (P < 0.05) and ISI were significantly lower (P < 0.01) in the observed group than those in the control group. Compared with the control group, the main symptoms such as dark purplish tongue, listlessness, thready and thin pulse, lassitude in loin and legs in the observed group were seen more frequently. In the observed group syndrome of deficiency of Qi and Yin accounted for 51.47%, syndrome of deficiency of Yin for 30.88%, subjects with syndrome of blood stasis as the main accompanying syndrome accounts for 61.76%.

CONCLUSIONHigher beta cell secretion function and lower insulin sensitivity appear in ND1GR of DM2 patients, suggesting the existence of insulin resistance. The feature of TCM syndrome in them is characterized by deficiency of Qi and Yin with inner obstruction of blood stasis.

Adult ; Diabetes Mellitus, Type 2 ; genetics ; Diagnosis, Differential ; Female ; Glucose Tolerance Test ; Humans ; Insulin Resistance ; Insulin-Secreting Cells ; physiology ; Male ; Medicine, Chinese Traditional ; Middle Aged

BACKGROUND AND OBJECTIVEThe expression of transcription factor Elf-1 and inhibitor of apoptosis survivin in non-small cell lung cancer (NSCLC) is correlated with the angiogenic factor vascular endothelial growth factor (VEGF), and are both factors affecting the cell cycle. This study investigated the expression of Elf-1, survivin, and intratumoral microvessel density (iMVD) assessed by monoclonal antibody CD105 in NSCLC, and explored their correlations with clinicopathologic features and angiogenesis of NSCLC.

METHODSPowerVision(TM)-9000 immunohistochemistry was used to evaluate the expression of Elf-1, survivin, and CD105 in tissue microarrays containing 60 specimens of NSCLC and 9 specimens of normal tissue. Western blot analysis was used to evaluate the protein levels of Elf-1 and survivin in 17 specimens of NSCLC and 5 specimens of normal tissue.

RESULTSElf-1 and survivin were detected in 1 of the 9 normal tissues. The positive rates of Elf-1 and survivin in NSCLC were 70.0% and 65.0%, respectively. The expression levels of both Elf-1 and survivin were significantly related to tumor differentiation, lymphatic metastasis, clinical stage, and postoperative survival time (P < 0.05). Overexpression of both were related to poor prognosis: the survival rates were significantly lower in patients with positive expression than in those with negative expression (P < 0.01). Elf-1 expression was positively correlated with survivin expression (r = 0.769, P < 0.01). Elf-1 and survivin expressions were positively correlated with iMVD (r = 0.446, P < 0.01; r = 0.435, P < 0.01).

CONCLUSIONSThe expression of Elf-1 and survivin in NSCLC is related to differentiation, lymphatic metastasis, clinical stage, and prognosis, and both are positively correlated with iMVD. Detection their combined expression can help to predict the malignant behavior of NSCLC. Blocking the activity of Elf-1 and survivin may be a new way to inhibit angiogenesis in NSCLC.

Adult ; Aged ; Antigens, CD ; metabolism ; Carcinoma, Non-Small-Cell Lung ; metabolism ; pathology ; Carcinoma, Squamous Cell ; metabolism ; pathology ; Cell Differentiation ; Endoglin ; Female ; Humans ; Inhibitor of Apoptosis Proteins ; metabolism ; Lung Neoplasms ; metabolism ; pathology ; Lymphatic Metastasis ; Male ; Microvessels ; metabolism ; Middle Aged ; Neoplasm Staging ; Neovascularization, Pathologic ; metabolism ; pathology ; Nuclear Proteins ; metabolism ; Receptors, Cell Surface ; metabolism ; Survival Rate ; Transcription Factors ; metabolism