Objective To evaluate the effect of atorvastatin on human carotid plaque by high resolution nuclear magnetic resonance imaging(MRI 3. 0T). Methods Forty patients with carotid artery plaque were treated with atorvastatin at the dose of 20 mg daily for one year. Changes of the artery plaques were observed by MRI,and the levels of blood lipoproteins and C reactive protein( hs-CRP)were detected. Results After the treatment with atorvastatin for 6 months and 1 year,the number and average thickness of plaques were reduced. One year after the treatment,average thickness of stable plaques dropped from (2. 41±0. 54)mm to(2. 17±0. 49)mm,and the size of the unstable plaques decreased from(2. 38±0. 89)mm to(2. 01± 0. 32)mm,with significant differences(P﹤0. 05). The levels of TC,TG,LDL-C and Hs-CRP were significantly decreased(P﹤0. 05)and the level of HDL-C was increased. Conclusion High resolution nuclear magnetic resonance( MRI3. 0T)can clearly display the components of the atherosclerotic plaque and the degree of artery stenosis. Atorvastatin exerts a significant effect on carotid plaque by promoting the regression of the carotid atherosclerosis plaque.

Objective To investigate the association of ERCC1 and BRCA1 gene expression with clinical features and sensitivity to platinum-containing chemotherapy in patients with ovarian epithelial carcinoma. Methods Primary ovarian epithelial carcinoma tissues were harvested from 48 patients receiving staging surgery or cytoreductive surgery. Expression of ERCC1 and BRCA1 in the tumor samples was detected by immunohistochemistry. Results ERCC1 expression was correlated with clinical stage(P﹤0. 05)but not with age,pathological type or degree of differentiation(P﹥0. 05). BRCA1 expression was not correlated with any of the clinicopathological features(P﹥0. 05);ERCC1 expression was significantly higher in drug-resistant tissues than in drug-sensitive samples(P﹤0. 05);The expression of ERCC1 and BRCA1 was positive in 89. 58%and 25. 00%of the samples,respectively. Conclusion ERCC1 gene expression is correlated with clinical stage but not with age,pathological type or degree of differentiation. BRCA1 gene expression is not correlated with clinicopathological features. ERCC1 has high positive expression in epithelial ovarian cancer and is correlated with sensitivity of platinum-containing adjuvant chemotherapy.

Objective To evaluate the optimal dosage of misoprostol administered in the rectum for dilation of the cervix. Methods Two hundred and forty women at 40-60 day gestational age without vaginal delivery history were randomly divided into three groups,with 80 cases in each group. Patients received 200,400 or 600μg of misoprostol rectally one hour before electrical vacuum abortions in group A,B and C,respectively. Cervical dilation,blood loss,and drug side effects in the three groups were compared. Venous blood samples were taken before vein anesthesia,and misoprostol acid concentration in the serum was tested by liquid chromatography-mass spectrometry. Results The analgesic rate was 100. 00%in all three dose groups, and cervical dilation rate was 23. 75%,46. 25%and 70. 00%in groups A,B and C,respectively. The severity of drug side effects such as vaginal bleeding and abdominal pain is dose-dependent. Blood concentration of misoprostal acid was(117±65),(206± 98),and(303±149)pg·mL-1 ,in groups A,B and C,respectively. Conclusion The recommended dose of misoprostol is 400 μg administered in rectum. Rectal administration of misoprostol is cheap,safe,and convenient,and therefore could be widely applied.

Objective To study the antibiotic activities of leaf extract of Stellera chamaejasme L on the skin. Methods Activities of the leaf extract on Trichophyton gypseum and Staphylococcus aureus was examined by antibiotic susceptibility paper disk method and tube double dilution method. Results When extracted by 95%ethanol,the extract from Stellera chamaejasme L at 100 mg·mL-1 formed an inhibition zone with the diameter of 12. 8 mm for Staphylococcus aureus and 12. 0 mm for Trichophyton gypseum. When extracted by dichloromethane,the minimum inhibitory concentration( MIC)of the extract from Stellera chamaejasme L was 0. 25 mg·mL-1 for Staphylococcus aureus and 0. 50 mg·mL-1 for Trichophyton gypsem.
Conclusion Leaf extract of Stellera chamaejasme L has an antibacterial activity against Staphylococcus aureus and Trichophyton gypseum and the antibacterial activity against Staphylococcus aureus is stronger.

Objective To study the effects of pirfenidone on total enzyme and isoenzyme of liver microsomal cytochrome P450 in rats. Methods The activites of liver microsomal dimethyl nitrosamine N-demethylase( NDMA )and erythromycin demethylase( ERD ) were determined. Fifty-six SD rats were randomly divided into six groups,in which they received CMC,dexamethasone 100 mg·kg-1 ,ketoconazole 40 mg·kg-1 ,pirfenidone 25,50,100 mg·kg-1 ,respectively. After administration for 6 and 12 days,livers were prepared liver microsome,the concentration of proteinum in microsome and shade selection to plasma samples were determined by spectrophotometer. Results After administration of pirfenidone for 6 days, cytochrome P450 was significantly increased in 50 and 100 mg·kg-1 pirfenidone groups,as compared with solvent control group (1%sodium carboxymethylcellulose)(P﹤0. 01). After administration of pirfenidone for 6 and 12 days,NDMA of liver microsome was not changed significantly(P﹥0. 05). ERD of liver microsome was significantly increased in 100 mg·kg-1 pirfenidone group after administration for 12 days(P﹤0. 01). Conclusion Pirfenidone can induce P450 and ERD activities in a dose-and time-dependent manner.

Methods The maximum tolerated dose( MTD)of water and ethanol extracts of Radix millettiae speciosae were measured for the safety evaluation. Results Maximal tolerated dose( MTD)of water extract was higher than 1 000 g·kg-1 ,which equaled to 110 times the dose for human adults(60 kg). MTD of ethanol extract was higher than 1 700 g·kg-1 ,which equaled to 186 times the dose for human adults(60 kg). Conclusion Radix millettiae speciosae does not have obvious toxicity,thus its routine clinical dose is safe and feasible.

Objective To investigate the protection mechanism of ulinastatin on bacterial endotoxin-induced acute lung injury. Methods Acute lung injury was induced by Escherichia colilipo-polysaccharide(LPS)5 mg·kg-1·d-1,intratracheally. Twenty SD rats were randomly divided into control group(n=10)and ulinastatin group(n=10). Ulinastatid group received ulinastatin 50 kU·kg-1 ,the control groups received the same amount of 0. 9% sodium chloride solution. Then the expression changes of rat AQP-1 and AQP-5,alveolar wall thickness change and the degree of pulmonary edema were detected. Results After the injection of LPS into the rat,the expression of AQP-1 and AQP-5 in control group were continuously decreased,but those in ulinastatin group decreased were not obvious. The lung wet/dry weight ratio in the control group increased significantly,the not obvious changes in the ulinastain group. The thickness of the alveolar in 24,48,72 h of the control group were(3. 84±0. 68),(6. 32±1. 08),(11. 03±2. 47)μm, respectively,and those in the ulinastian groups were(2. 31±0. 44)(,3. 76±0. 82)(,2. 94±0. 67)μm,respectively. Conclusion The AQP-1 and AQP-5 induced the occurrence of pulmonary edema by changing the cell permeability. Ulinastatin can slow down the process so as to reduce the degree of endotoxin-induced lung injury.

Objective To prepare nifedipine( NF)sustained-release pellet tablets,and study of its release behavior in vitro. Methods Soluplus was selected as a carrier to prepare solid dispersion of NF by hot melt extrusion technique( HME), and the ratio of the drug to carrier was 1:1. The samples were validated as the solid dispersion by differential scanning calorimetry(DSC). Extrusion-spheronization technique was introduced to prepare NF pellets and EudragitRS 30D was used as the coating material. The NF sustained-release tablets were prepared by direct compression of the coated pellets and suitable excipients. Results The release data in vitro proved that the drug release from the tablets was steady and complete over 24 hours. Conclusion The release of NF from sustained-release tablets is slow and steady. The method is easy to operate. The in vitro drug release pattern follows first-order kinetics.

Objective To establish a new quality control standard for danshen capsules. Methods The qualitative identification of danshen capsules was characterized by ultraviolet fluorescence and thin-layer chromatography( TLC ). The contents of tanshinoneⅡA,cryptotanshinone,salvianolic acid B,danshensu and protocatechuic aldehyde in danshen capsules were determined by high performance liquid chromatography(HPLC)on a C18 column. The flow rate was 1 mL·min-1,and the column temperature was 35 ℃. Results The HPLC linear ranges of tanshinone ⅡA,cryptotanshinone,salvianolic acid B, danshensu and protocatechuic aldehyde were 2. 046-40. 92 μg · mL-1 ,1. 482 25 -59. 29 μg · mL-1 ,1. 502 55 -60. 102 μg·mL-1 ,11. 49-459. 582 μg·mL-1 ,and 0. 617 4-24. 696 μg·mL-1 ,respectively,and r values were 0. 999 9. The average recoveries were 99. 66%(RSD of 0. 91%)for tanshinoneⅡA,99. 26%(RSD of 0. 88%)for cryptotanshinone,99. 09%(RSD of 0. 76%)for salvianolic acid B,100. 51%(RSD of 0. 62%)for danshensu,and 100. 62%(RSD of 0. 82%)for protocatechuic aldehyde,respectively. The contents of the tanshinoneⅡA,cryptotanshinone,salvianolic acid B,danshensu showed a certain high level in the 3 batches of danshen capsule samples,but protocatechuic aldehyde was low by comparison. Conclusion The HPLC method is proven to be sensitive,accurate,repeatable,and can be used for quality control of the danshen capsules.

Objective To develop the ribavirin purity certified reference material( CRM ) which has measurement traceability and high accuracy,and establish an effective method of evaluation. Methods The homogeneity and the stability were checked by differential scanning calorimetry(DSC). High performance liquid chromatography(HPLC)and DSC methods were used for purity determination of ribavirin. Results Ribavirin showed satisfactory homogeneity and stability. The certified value of ribavirin was 99. 5%with an uncertainty of 0. 4%(k=2,P=0. 95). Conclusion Ribavirin purity CRM obtained in this paper has been proven to be a national primary CRM with high accuracy and traceability,which can be used to validate analytical methods,improve the accuracy of measurement data,establish meteorological traceability of analytical results as well as control the quality of ribavirin in the pharmaceutical industry.