To design and synthesize novel vanillin derivatives and evaluate their anti-proliferation effect against HeLa cells.

Taking vanillin derivative SBE-13 as lead, 2-chloroquinoline fragment were introduced into the new compounds by the methods of electronic isosteric and skeleton transition. 2-Chloro-3-chloromethylquinoline and vanillin were used as raw materials to obtain the target compounds 4a~4k by etherification and reductive amination.

A total of 11 novel vanillin derivatives were designed and synthesized, and their structures were confirmed by ¹H NMR and ESI-MS. Most of the compounds exhibited good antiproliferative activities against HeLa cells. Notably, compound 4b potently inhibited HeLa cells with an IC₅₀=9.79 μmol·L^-1, a 10-fold improvement over SBE-13 (IC₅₀=78.30 μmol·L^-1).

Compound 4b displayed significant antiproliferative effect in vitro, which is worthy of further study.

To systematically study the polymorphism of compound CP0119.

Totally 100 conditions such as volatile crystallization, slurry crystallization, anti-solvent crystallization, cooling crystallization, diffusion crystallization and water vapor stress crystallization were used to select the crystal types. Different crystal types were characterized by X-ray powder diffraction analysis (XRPD), differential scanning thermal analysis (DSC), thermogravimetric analysis (TGA) and Fourier infrared spectroscopy (FT-IR). Dynamic water adsorption test (DVS) was used to determine the wettability of anhydrous crystal. The stability and translatability of the crystal samples were studied by stress testing. The most stable crystal in the corresponding solvent at room temperature was determined by crystal competition test and its stability was investigated.

In addition to the original crystal type (crystal type 1), 9 new crystal types were screened and prepared. Many kinds of methods could be used to identify the crystal samples in different material states. The competitive test showed that the crystal type 1 was the most stable crystal type, and the stability test showed that the crystal form and melting point crystal of type 1 were not changed when it was placed in long-term and accelerated conditions for 10 d.

By systematically studying the polycrystalline form of compound CP0119, the preparation method, material composition, crystal form stability and crystal form transformation rule of the 9 crystal forms were clarified, which provided scientific basis for the subsequent preparation process and preparation research.

To optimize the extraction conditions of Scutellaria baicalensis by ultrasound-assisted ionic liquid and evaluate the anti-inflammatory activity.

The extraction method of scutellarin, baicalin, baicalein, wogonoside, wogonin and oroxylin A by high performance liquid chromatography was established. The extraction process was optimized by Box-Behnken response surface method, with the index of comprehensive score such as weight coefficient and the anti-inflammatory activity was evaluated.

The optimal extraction conditions were as follows: the concentration of ionic liquid was 20%, the ratio of material to liquid was 1∶60 mL·g^-1, the extraction temperature was 35 ℃, the extraction time was 15 min. The contents of six chemicals were obtained as 0.73%, 10.05%, 2.61%, 1.30%, 0.45%, and 0.22% by the validation experiment. MTT assay showed that the cell viability significantly decreased as the concentration exceeded 50 μg·mL^-1. Compared with LPS group, the extraction at different concentrations significantly inhibited the release of NO (P<0.01), and the IC₅₀ value was 17.07 μg·mL^-1.

The extraction process is simple, feasible, green, high efficiency and highly reproducible and the total flavonoids of Scutellaria baicalensis have obvious anti-inflammatory activity.

To establish a determination method of polymer impurities in cefoxitin sodium injection.

Cefoxitin sodium was dissolved in water to prepare stock solution of cefoxitin sodium polymer. High performance size exclusion chromatography (HPSEC, TSK-gel G2000SWxl) and column switching-LC/MSn were applied to separate and deduce the poor retention impurities in the stock solution and to evaluate the specificity of HPSEC method. A new RP-HPLC method for polymer analysis was established with a Shimadzu Inertsil Ph-3 column, using a gradient elution by phosphate buffer solution (pH 3.2)-acetonitrile-methanol, and the method was validated.

Several cefoxitin sodium polymers were identified in stock solution of cefoxitin sodium polymer, 4 small molecular impurities were also detected. Polymer impurities were liable to co-elute with small molecular impurities by HPSEC method, making a poor quantification accuracy and specificity. Two indicative polymer impurities were detected by RP-HPLC method with an effective specificity.

HPSEC method was not suitable for the quality control of polymer impurities in cefoxitin sodium injection, while the new established RP-HPLC method was specific, which could effectively control the polymer impurities. Cefoxitin sodium polymer stock solution could be used to identify polymer peaks as the system suitability solution.

To evaluate the effectiveness, safety and economy of Binkgo biloba extract injection in ischemic stroke patients using rapid health technology assessment and to help efficiently and quickly provide evidence-based basis for clinical drug selection and decision makers.

Databases in Chinese and English, and HTA organization websites were searched. Studies were selected according to the inclusion and exclusion criteria, and the data were extracted and the quality of included literature was evaluated and analyzed.

At last, 7 systematic reviews and 4 pharmacoeconomic studies were included in this study. In patients with ischemic stroke, Ginkgo biloba extract injection improved clinical efficacy, neurological deficit scores and activity of daily living, ameliorated plasma viscosity and reduced fibrinogen, as well as improved the deterioration rate of the disease. There was no statistically significant difference in mortality compared with the control group. Few adverse reactions and no serious adverse reactions were observed. The quality of the included economics research literature was relatively low. Drug efficacy in experimental group and control group was equal. The cost-effectiveness analysis method was adopted in the economic evaluation, in which only the drug cost out of direct cost was included. The year of research is relatively early, which cannot match the current drug price, and results of the researches are difficult to be used as reference.

Ginkgo biloba extract injection is an efficacious and safe choice for ischemic stroke treatment. The evaluation of its economics still requires further high-quality pharmacoeconomic analysis.

To investigate the influence factors of blood concentration of tacrolimus, and to provide reference for clinical use of tacrolimus (FK506).

66 patients with nephrotic syndrome, who received hospitalized treatment in nephrology department of our hospital were enrolled in this study. The blood concentration of FK506, general data and laboratory testing values and so on, were recorded and analyzed using multiple linear regression method by SPSS 17.0 software.

Among the 66 patients, 40.91% patients' FK506 concentration fell in the effective range, 54.55% below the effective range, and 4.55% above the effective range. Correlations were found in unit dose of blood concentration for tacrolimus with total cholesterol (CHO) combination with drugs that increase the FK506 blood concentration, and serum creatinine (P<0.01).

The FK506 blood concentration in patients with nephrotic syndrome patients is greatly varied between individuals, and CHO, drugs that increase FK506 concentration and CK are main factors affecting FK506 blood concentration in nephrotic syndrome patients.