(0.05)) during dobutamine 5 ?g?kg~(-1)?min~(-1) stage. Blood pressure had significant increase both in dobutamine 10 ?g?kg~(-1)?min~(-1) stage and post-coronary revascularization. The sensitivity,specificity,accuracy of dobutamine 5 and 10 ?g?kg~(-1)?min~(-1) were (73.0)% and (89.6)%, (81.7)% and (82.8)%,(76.9)% and (86.5)%, respectively. Conclusions LDDSE is a simple,safe and no injury means to identify survival myocardium in myocardial infarction.

In this article, the projects in drug metabolism and pharmacokinetics funded by NSFC during "10th Five Year Plan" (2001~2005) in China were reviewed. The major research fields of these projects in drug metabolism and pharmacokinetics funded by NSFC during the financial years were overviewed and analyzed. Finally, current problems in these research fields in China were also briefly analyzed.

Objective To study the life quality and influencing factors for empty nester elderly in rural area in Hunan,and to provide the scientific basis for the effective interventions.Methods The two villages of Yiyang and Huaihua were randomly selected by cluster sampling from June 2011 to December 2011 in Hunan.Data of the world health organizations quality of life instrument-short version (WHOQOL-BREF) was collected by face to face interview with the empty nesters.The risk factors for the quality of life in empty nester elderly in rural area were analyzed by the multiple linear regression analysis.Results A total of 785 valid questionnaires were acquired,among which 472 cases were from empty nester elderly (60.1％,472/785),the average age of them was (69.3±7.3) years,and the male:female ratio was 1.1:1 (250:222).The literacy of 81.8％ of empty nester elderly were under junior middle school,69.7％ of them married with consorts who were still living,74.4％ of them were farmer,75.2％ of them had monthly income under 500 Yuan,56.4％ of them got the income from their own labor,69.9％ of them considered that their relationship with children were harmony.64.2 ％ of empty nester elderly in village suffered from chronic diseases and 16.7 ％ of them suffered from accidental injury within the last one year.The scores in physiological health,psychological health and quality of life were lower in empty nester elderly than in the non-empty nester elderly [(60.8±15.7) vs.(63.1±13.5),(59.0±12.1) w (64.6±17.4),(59.5±9.8) vs.(63.0 ± 10.1),t=3.18,4.43,4.91,all P＜0.05].The multiple linear regression analysis showed that the influencing factors for quality of life in empty nester elderly were education background,marital status,source of finance,relationship with children,chronic disease and accidental injury within the last one year (β=1.693,2.426,0.779,1.060,-7.007,-3.784,all P＜0.05).Conclusions The empty-nest elderly accounts for more than half of the elderly in rural area,who have the lower levels in physio-psychological health and quality of life.We should improve their awareness and knowledge of health,build their harmonious relationship with spouse and children,improve the social security and medical insurance system,actively promote the knowledge of chronic disease and accidental injury,in order to improve the quality of life in empty nester elderly and achieve the healthy aging.

Objective To determine the solubility and apparent oil/ water partition coefficient of sitafloxacin in different solvents. Methods High performance liquid chromatography (HPLC) was used. The column was Dikma Diamonsil C18 (2) (4. 6 mmí250 mm,5 μm). The mobile phase was 0. 05 mol·L-1 KH2 PO4 solution (pH was adjusted with H3 PO4 to 2. 4)-acetonitrile (7030). The column temperature was set at room temperature. The flow rate was 1. 0 mL·min-1 . The detection wavelength was 295 nm and the injection volume was 10 μL. The solubility of sitafloxacin and the apparent oil/ water partition coefficient at pH 2. 0,4. 3,5. 8,6. 6,7. 4,8. 0,10. 0 and 11. 2 were determined. Results The equilibrium solubility of sitafloxacin in water was 0. 44 mg·mL-1 and the apparent oil/ water partition coefficient was 0. 23 (lgP= -0. 64) at (37±2) ℃ . Sitafloxacin has the lowest equilibrium solubility (0. 13 mg·mL-1 ) and the highest apparent oil/ water partition coefficient in pH7. 4 buffer solution system. At pH>10 and pH<5. 8,the solubility of sitafloxacin increased obviously and apparent oil/ water partition coefficient decreased. Conclusion Sitafloxacin is insoluble in water and also poorly soluble in oil,but its solubility could be improved significantly in acidic or alkaline solution.

Identification and validation of a new target is one of the most important steps for new antituberculosis (TB) drug discovery. Researches have shown that Mycobacterium tuberculosis (Mtb) encodes 20 CYP450 enzymes which play important roles in the synthesis and metabolism of lipid, cholesterol utilization, and the electron transport of respiratory chain in Mtb. With the critical roles within the organism as well as the protein structures of six Mtb CYP450 enzymes being clarified, some of them have been highlighted as potential anti-tuberculosis targets. In this paper, the phylogenetic analysis, the structural features, and the enzymatic functions of Mtb CYPs, as well as the mechanism of interactions with selective inhibitors such as azole antifungal agents for the CYPs have been reviewed and summarized. The druggability of the CYPs has also been analyzed for their further utility as targets in high throughput screening and rational design of more selective inhibitors.

Objective To study the tortuosity coefficient (TC) values of basilar arteries in the adult,and its change in cerebral basilar artery infarction.Methods TC values of basilar arteries was prospectively analyzed using the magnetic resonance angiography images of 135 controls(19-80 years of age,male 90,female 45)and 42 patients with cerebral infarction(5l-70 years of age,male 28,female 14).The relationship between TC values and posterior circulation infarction was statistically evaluated.Results Differences of TC between age groups were statistically significant except group B (31-50 years)and C(51-70 years)(F=10.31,P<0.01).The infarction group had greater TC value(2.497±1.200)than the control group(1.939±0.850,t=2.39,P=0.0195).Conclusions (1)Basilar artery tortuosity is positively related to age,reflecting the degree of arteriosclerosis;(2)Basilar artery tortuosity increases in patients with posterior circulation infarction.

Objective For bioequivalence test of the consistency evaluation of generic drug products,providing a reference of varieties of biowaiver.Methods Based on Human bioequivalence test waiver guidelines (draft),on condition that first drug of the consistency evaluation,to introduce and conclude briefly the standards of biowaiver and varieties of biowaiver in FDA,WHO and EMA.Results Contrast to FDA,there are 59 varieties applied for the waiver and 19 varieties not applied for the waiver in the 289 varietie;compared to WHO,10 drugs are exempted and 1 grug is exempted in EMA.Conclusion At present,the specific list of drugs are not published of biowaiver in our country,the pharmaceutical companies should compare and consult revelant standards and specific drugs in China and abroad,to speed up the progress of the consistency evaluation.

Objective To build a RNA interference vector for PQ-loop repeat protein (LRP) gene,and to evaluate the effect of the vector on the expression of PQ-LRP gene in Microsporum canis.Methods The PUC-PLULT and PCB309-PLULT vectors were constructed sequentially by using Agrobacterium tumefaciens-mediated T-DNA insertional mutagenesis,adding multiple cloning sites,and introducing the hygromycin-resistance gene.Microsporum canis was transformed with the PCB309-PLULT vector followed by a series of passages and hygromycin selection.Real-time quantitative PCR was performed to measure the expression of PQ-LRP gene in Microsporum canis before and after transformation.Results The intermediate vectors PUC-PLUT and PUC-PLULT were constructed and identified by PCR and gene sequencing.The 8 825-bp interference vector PCB309-PLULT was successfully built and confirmed by enzyme digestion.The optimum concentration of hygromycin for screening for Microsporum canis transformants was determined as 300 mg/L.The mRNA expression level of PQ-LRP was decreased by 61％ in the transformants as compared with untransformed Microsporum canis (0.39 vs.1.00).Conclusion The constructed PCB309-PLULT interference vector can effectively inhibit the expression of PQ-LRP gene in Microsporum canis.

Objective To study the effect of surfactants on the dissolution profiles of poorly water-soluble acidic drug nimesulide from sustained-release tablets.Methods The anionic surfactant sodium dodecyl sulfate (SDS), cationic sur-factant cetyltrimethyl ammonium bromide (CTAB) and nonionic surfactant polysorbate 80 (Tween 80) were used to prepare nimesulide micelles .The effect of the buffer , surfactant and ionic strength on the equilibrium solubility of the drug and the in vitro release of sustained-release tablets was studied .Results and Conclusion In pH 1.2 HCl solution, water and pH 6.8 phosphate buffer, the solubilization capacity of CTAB was the highest.However, in pH 9.0 Tris buffer, when CTAB concen-tration was at about 1%, the equilibrium solubility of nimesulide was at the trough value .The in vitro release results were similar to those of equilibrium solubility and the kinetic pattern conformed to the first order equation according to the coefficient R .

Objective To optimize the formulation of metoprolol succinate ( MS) controlled release pellets by central composite design-response surface methodology .Methods MS sustained-release pellets were prepared using sugar pellet cores as starter beads , ethyl cellulose as coating materials and MS itself as a pore former .The formulation of MS sustained-release pellets was optimized by a central composite design with two factors at five levels .These two factors ( two independ-ent variables) were the pore former level and coating level , and the evaluated indexes ( namely dependent variables ) included the in vitro cumulative release percentages of MS at 1, 4, 8, 12 and 16 h, respectively.Results and Conclusion The results of mathematical equation fitting suggested that the second-order quadratic model was the optimal fitting equa-tion.According to the response surfaces , the optimum values at the pore former level and coating level weve ranged from 16%to 18%and 20% to 25%, respectively .The in vitro cumulative release percentage of MS from the pellets at 1 h reached 9.15%,which consequently eliminated the lag phase in the initial release period and exhibited a good sustained-release effect.Central composite design-response surface methodology can be applied to optimizing the coating formulation for MS sustained release pellets .