pazopanib血药浓度个体差异与细胞色素P450 3A4基因多态性的关系初探

目的：分析健康受试者口服pazopanib片后体内药代动力学（PK）规律，初步探讨pazopanib片PK个体差异的遗传学机制。方法：14例健康男性受试者分别在给药当天单次口服pazopanib片（200 mg）后，采集基线至96 h血液样本，用LC-MS/MS法测定服药后各时间点血药浓度，用WinNonlin 6.3软件计算药代动力学相关参数，采用SNapShot法测定细胞色素P450 3A4（CYP3A4）基因多态性。结果：Cmax变化范围（7 361.65-26 081.00） ng/mL，平均值±标准差（15 410.72±6 366.21） ng/mL ；tmax变化范围（1.50-4.00） h、平均值±标准差（2.50±0.83） h；AUC0-t变化范围（228 013.55-775 231.63）ng·mL-1·h，平均值±标准差（516 279.90±175 688.41）ng·mL-1·h。个体间Cmax、AUC相差达3倍以上，tmax可相差2倍以上；14例受试者CYP3A4（RS35599367）位点皆为野生型。结论：pazopanib片在中国健康男性志愿者中个体差异较大，未观察到CYP3A4（rs35599367）位点单核苷酸多态性，pazopanib个体间PK差异可能与其他药物代谢相关基因多态性有关。     

Autolysis and the endogenous proteinases characterised in beardless barb (Anematichthys apogon) muscle

Beardless barb is a common fish species used in fermentation of fish paste Ka-pi-plaa. Autolytic profile of beardless barb muscle showed the maximum autolysis was at 50 °C, at both acidic and alkaline pH values. With augmentation concentration of NaCl, autolytic activity slightly decreased. Endogenous proteinases isolated from fish muscle in crude extract forms were also characterised. The acidic proteinases had optimum activity at pH 3.0 and 50°C, and they showed higher proteolytic activity than the alkaline proteinases which were optimally active at pH 9.0 and 50 °C. Proteinases in peak at pH 3.0 were inhibited by pepstatin A, but those in peak at pH 9.0 were highly inhibited by PMSF, TLCK and soybean trypsin inhibitor, suggesting that both aspartic and serine proteinases were existed in beardless barb muscle. The proteinases were stable in pH range of 2.0-5.0 but unstable at the temperatures higher than 40 °C. NaCl suppressed the proteolytic activity, ATP activated the proteinase activity, while CaCl₂, MgCl₂ and CoCl₂ exhibited no influence on the activity. The results implied that cathepsin D is the predominant proteinase responsible for autolysis in beardless barb. The findings were useful to improve the processing and qualities of Ka-pi-plaa product using beardless barb as raw material.     

A first-principles investigation on mechanical and metallic properties of titanium carbides under pressure

The titanium carbides are potential candidates to achieve both high hardness and refractory property. We carried out a structural search for titanium carbides at three pressures of 0 GPa, 30 GPa and 50 GPa. A phase diagram of the Ti-C system at 0 K was obtained by elucidating formation enthalpies as a function of compositions, and their mechanical and metallic properties of titanium carbides were investigated systematically. We also discussed the relation of titanium concentration to the both mechanical and metallic properties of titanium carbides. It has been found that the average valence electron density and tractility improved at higher concentrations of titanium, while the degree of covalent bonding directionality decreased. To this effect, the hardness of titanium carbide decreases as the content of titanium increases. Our results indicated that the titanium content significantly affected the metallic properties of the Ti-C system.     

ZSM-5沸石膜用于生物油的脱水分离及其再生过程研究

在水热条件下通过无模板剂法合成了连续的ZSM-5沸石膜，并将其用于生物油的渗透汽化以进行高效脱水分离。ZSM-5沸石膜在强酸性、多组分的生物油体系中保持了很好的化学稳定性和优异的分离选择性，但在分离过程中面临着较强的膜污染问题，导致了膜通量的大幅下降。ZSM-5沸石膜的再生研究表明，膜的渗透通量随着再生温度的升高而逐渐提高。当再生温度为220℃时，ZSM-5沸石膜的渗透通量可以恢复至初始的88%。再生的机理研究表明，ZSM-5沸石膜中大量的晶内孔在生物油体系中极易被污染，从而导致渗透通量迅速下降；而相对较大的晶间孔却难以被完全堵塞，水分子在被污染的ZSM-5沸石膜中主要通过晶间孔进行渗透。上述结果表明，通过合理调控ZSM-5沸石膜的晶间孔的数量和尺寸大小可有效提升ZSM-5沸石膜在生物油中的渗透汽化脱水分离性能。     

简体接管边缘应力区局部减薄处应力特征

参考《压力容器定期检验规则》第40条,采用有限元方法计算了筒体接管边缘应力区局部减薄处的应力分布,得到了局部减薄处凹坑的尺寸与位置对应力的影响趋势,讨论了应力集中系数随尺寸变化的规律,为筒体接管边缘应力区局部减薄处的强度评定提供了一定的计算依据。     

铌和钨对γ-TiAl基合金热稳定性的影响

采用光学显微镜(OM)，扫描电镜(SEM)，X射线衍射研究了TiAl—5Nb，TiAl—14．3Nb，TiAl—8Nb—1W，TiAl—12．3Nb-2W四种合金片层组织在1000℃的热稳定性。结果表明，TiAl—12．3Nb-2W合金热稳定性最好，但合金元素对TiAl基合金热稳定性的影响机理还有待进一步的研究。     

乌江索风营水电站地下厂房岩锚梁镜面混凝土施工技术

镜面混凝土是水电工程建设中新兴的一门施工技术,在乌江索风营水电站地下厂房岩锚梁混凝土施工中采用了镜面混凝土,这在技术上是一次大胆的尝试和创新,既满足了功能上的要求,同时也达到了美观和装饰地下厂房的效果,为今后水电工程施工中广泛采用镜面混凝土技术提供了样本和宝贵经验。     

RI/VI联用测定聚乙烯相对分子质量及其分布

150℃测试温度下，以1，2，4-三氯苯为溶剂，采用示差折光指数器，毛细管黏度计双检测器联用凝胶渗透色谱技术测定了聚乙烯的相对分子质量及其分布。与常规凝胶渗透色谱法对比，该方法不仅能直接得到聚乙烯较精确的相对分子质量和分布形态，同时可以得到聚乙烯的特性黏数分布。     

溶剂脱沥青组合工艺生产重交通道路沥青

中国石化荆门分公司以江汉-阿曼混合原油和江汉-鲁宁混合原油为原料,分别采用减压蒸馏—丙烷脱沥青和减压蒸馏—添加催化裂化油浆—丙烷脱沥青工艺,生产出符合SH 0522—2000的100号道路沥青。结果表明,江汉-阿曼混合原油减压渣油中掺兑质量分数为30%的催化裂化油浆后,脱油沥青的各项性能均满足AH-70或AH-90重交通道路沥青的要求,而且薄膜烘箱试验表明,试样延度超过标准要求。