直肠癌患者头发微量元素分析

应用装存EPM-810Q电子探针的扫描分析电镜，对53例直肠癌患者作单根头发中镁、铝、镉，钙，铬、铁、铜、锌、铅、锰、硒11种微量元素分析。并与健康对照组进行比较，结果表明：直肠癌患者头发中镁、铝，钙含量明显低于正常。     

Development and validation of an LC‐MS/MS method for the determination of mesalazine in beagle dog plasma and its application to a pharmacokinetic study

A simple, specific and sensitive LC‐MS/MS method was developed and validated for the determination of mesalazine in beagle dog plasma. The plasma samples were prepared by protein precipitation, then the separation of the analyte was achieved on a Waters Spherisorb C₆ column (150 × 4.6 mm, 5 µm) with a mobile phase consisting of 0.2% formic acid in water–methanol (20:80, v/v). The flow rate was set at 1.0 mL/min with a split ratio of 3:2. Mass spectrometric detection was achieved by a triple‐quadrupole mass spectrometer equipped with an electrospray source interface in positive ionization mode. Quantitation was performed using selected reaction monitoring of precursor–product ion transitions at m/z 154 → m/z 108 for mesalazine and m/z 285 → m/z 193 for diazepam (internal standard). The linear calibration curve of mesalazine was obtained over the concentration range 50–30,000 ng/mL. The matrix effect of mesalazine was within ±9.8%. The intra‐ and inter‐day precisions were <7.9% and the accuracy (relative error) was within ±3.5%. The validated method was successfully applied to investigate the pharmacokinetics of mesalazine in healthy beagle dogs after rectal administration of mesalazine suppository. Copyright © 2014 John Wiley & Sons, Ltd.     

Thermostability and polymorphism of theobroma oil and palm kernel oil as suppository bases

Thermal stability of pharmaceutical ingredients is an important aspect. In this study, we adopted differential scanning calorimetry (DSC) to investigate thermal stability of suppository bases, theobroma oil (cocoa butter) and a palm kernel oil (PKO) blend. The study shows theobroma oil possesses six polymorphic forms whilst the palm kernel oil blend has three. Upon rescanning, the PKO blend does not show changes in the enthalpy of fusion and the melting point with time, whilst the theobroma oil shows significant reduction, and only regained its thermal stable state after 10 days. This indicates that PKO blend possesses better thermal stability.     

氯化钠强化硫酸吗啡缓释液体栓制备及其性能

根据温敏原位凝胶的特性制备了以泊洛沙姆407/188为主要基质,卡波姆、氯化钠、氮酮和2,6-二叔丁基-4-甲基苯酚为添加剂的硫酸吗啡缓释液体栓,测定了其凝胶温度、凝胶强度和生物黏附力,研究了其体外溶出和在Beagle犬体内的药物吸收.用3p97程序计算药物代谢动力学参数,进行体外释放和体内吸收的相关性研究.结果表明,一定量的氯化钠与卡波姆产生协同作用,使凝胶温度下降,凝胶强度增加.该缓释液体栓在体外释药符合零级模式,在Beagle犬体内释药过程符合一室模型.其中,经氯化钠强化的处方（卡波姆为0.8%,氯化钠为1.0%）相关药物代谢动力学参数为：峰浓度为409.7 ng.mL-1,血药浓度-时间曲线下面积（AUC）为5 708 ng.h.mL-1,体内平均滞留时间（MRT）为10.92 h,体外释药时间为7~10 h,体内缓释时限达9~18 h,显示出良好的缓控释特征.     

直肠癌组织与直肠正常组织的荧光光谱研究

用荧光光谱仪对12例离体直肠癌组织和对应的直肠正常组织的荧光光谱(激发光的波长为320 nm)进行了研究。并与相应的红外光谱结果进行了对比。结果表明直肠正常组织的荧光强度明显高于直肠癌组织的荧光强度。直肠组织在波长为492和544 nm的荧光强度的差别可用于区分直肠正常和直肠癌组织。     

Investigation of Ethacrynic Acid and Random-methyl-β-cyclodextrin Binary Complexes

Cyclodextrin complexation was applied to achieve better aqueous solubility of the drug and to formulate suppositories. Binary products were prepared in several mole ratios by two different methods. The dissolution profiles and in vitro membrane diffusion behaviour of the compositions were investigated. Thermoanalytical studies were performed in order to confirm inclusion complex formation. Compositions were selected for further detailed investigations and for incorporation into suppository dosage form.     

II、III期直肠癌术前与术后放化疗疗效比较的Meta分析

目的通过Meta分析比较术前与术后放化疗对II、III期直肠癌的疗效。方法检索2014年12月前发表的有关II、III期直肠癌术前与术后放化疗疗效比较的文献,纳入本研究的文献为随机对照试验（RCT）,提取其短期及长期临床疗效指标进行分析。结果共包括1642例直肠癌患者的5项RCT纳入本研究。术前放化疗组患者较术后放化疗组5年局部复发率低（OR＝0.60,95%CI:0.41~0.88,P=0.008）,两组5年远处转移率（OR=0.87,95%CI:0.67~1.11,P=0.26）、5年无病生存率（HR=0.84,95%CI:0.70~1.00,P=0.05）及总生存率（HR=0.90,95%CI:0.75~1.08,P=0.27）比较均无统计学差异,术前放化疗组毒性反应发生率较术后放化疗组低（OR=0.64,95%CI:0.50~0.82,P＜0.01）。结论采用术前放化疗的患者较术后放化疗的患者对直肠癌复发及毒性反应发生风险小,但远处转移及远期预后无明显差别。     

Improvement in biopharmaceutics of prednisolone by β- and γ-cyclodextrins

Inclusion complexes of prednisolone with - and -cyclodextrins in the molar ratio of 1:2 and 2:3, respectively, were prepared, and their dissolutions, permeations through a cellophane membrane, releases from a suppository base, andin vivo absorption behaviors were examined. The apparent rates of dissolution and permeation of prednisolone were significantly increased by the formations of inclusion complexes with - and -cyclodextrins. The release of the drug from Witepsol H₁₅ suppositories was also increased by complexation. The serum levels of prednisolone following oral and rectal administrations of the cyclodextrin complexes to rabbits were higher than those of the drug alone. The enhanced initial absorption of prednisolone by cyclodextrin complexation suggested the possibility of smaller doses in prednisolone therapy.     

鉴别直肠组织癌变的环丙沙星铽络合物荧光染色新方法

用具有较强荧光性能的环丙沙星铽配合物对多例直肠正常和直肠癌组织切片进行了染色研究,并与传统的HE染色结果进行了对比。结果表明用环丙沙星铽配合物染色后的效果与HE染色具有相同的图像和光学反差。并同时通过测定直肠正常和直肠癌组织的荧光光谱和红外光谱得到的组织病变判据,其结论与染色结果相一致。     

O-GIcNAc 转移酶在直肠癌中的分布及其对预后的影响

目的了解O-GIcNAc转移酶(O-GlcNAc transferase,OGT)在直肠癌中的表达情况及对预后的影响。方法利用免疫组化技术,在直肠癌组织芯片上染色OGT,确定表达情况,并与患者临床资料结合,了解OGT的表达与直肠癌患者的生存是否有差异。结果OGT 在直肠癌组织中的表达情况：“- ”12.22%、“+”27.78%、“++”44.44%、“+++”15.56%,癌旁组织中的表达情况：“-”18.89%、“+”42.22%、“++”37.78%、“+++”1.11% ;癌组织中OGT 高表达（++ 和+++）为60.00%,高于癌旁组织中OGT高标的量38.89%;OGT 高表达直肠癌患者的3年生存率分别是82.90%和60.00%,两者比较有统计学差异（字2=7.452,P=0.006）。结论 OGT在直肠癌中的表达高于周围正常组织,直肠癌中高表达的3年生存率较低,OGT可能参加了肿瘤的发生、发展过程。