Pharmacokinetics of articaine hydrochloride and its metabolite articainic acid after subcutaneous administration in red deer (Cervus elaphus)

AIM: To develop and validate a simple and sensitive method using liquid chromatography-mass spectrometry (LC-MS) for quantification of articaine, and its major metabolite articainic acid, in plasma of red deer (Cervus elaphus), and to investigate the pharmacokinetics of articaine hydrochloride and articainic acid in red deer following S/C administration of articaine hydrochloride as a complete ring block around the antler pedicle.

METHODS: The LC-MS method was validated by determining linearity, sensitivity, recovery, carry-over and repeatability. Articaine hydrochloride (40?mg/mL) was administered S/C to six healthy male red deer, at a dose of 1?mL/cm of pedicle circumference, as a complete ring block around the base of each antler. Blood samples were collected at various times over the following 12 hours. Concentrations in plasma of articaine and articainic acid were quantified using the validated LC-MS method. Pharmacokinetic parameters of articaine and articainic acid were estimated using non-compartmental analysis.

RESULTS: Calibration curves were linear for both articaine and articainic acid. The limits of quantifications for articaine and articainic acid were 5 and 10?ng/mL, respectively. Extraction recoveries were >72% for articaine and >68% for articainic acid. After S/C administration as a ring block around the base of each antler, mean maximum concentrations in plasma (C_max) of articaine were 1,013.9 (SD 510.1) ng/mL, detected at 0.17 (SD 0.00) hours, and the C_max for articainic acid was 762.6 (SD 95.4) ng/mL at 0.50 (SD 0.00) hours. The elimination half-lives of articaine hydrochloride and articainic acid were 1.12 (SD 0.17) and 0.90 (SD 0.07) hours, respectively.

CONCLUSIONS AND CLINICAL RELEVANCE: The LC-MS method used for the quantification of articaine and its metabolite articainic acid in the plasma of red deer was simple, accurate and sensitive. Articaine hydrochloride was rapidly absorbed, hydrolysed to its inactive metabolite articainic acid, and eliminated following S/C administration as a ring block in red deer. These favourable pharmacokinetic properties suggest that articaine hydrochloride should be tested for efficacy as a local anaesthetic in red deer for removal of velvet antlers. Further studies to evaluate the safety and residues of articaine hydrochloride and articainic acid are required before articaine can be recommended for use as a local anaesthetic for this purpose.     

逆固相基质分散净化和气质联机检测土壤中的六氯苯残留

建立了逆固相基质分散净化和气质联机法(GC-MS)快速、简便测定土壤中六氯苯(HCB)残留量的方法。以丙酮-正己烷(1∶ 1,体积比)为提取剂,采用超声波萃取,经固相基质PSA(primary secondary amine)吸附净化后采用GC-MS选择离子模式检测。结果表明,六氯苯在0.05~5 mg/L浓度范围内呈现出较好的线性关系,相关系数R2=0.999 5; 方法检测限为0.3 μg/kg,定量限为0.9 μg/kg,在0.89、1.78、8.90 mg/kg 3个添加水平上的平均回收率分别为106.6％、108.2％和108.1％。用该方法测定了天津某生产厂厂区地下1~10 m深的土壤样本,发现六氯苯的残留量在2.3~25 912 mg/kg 之间,表现出显著的空间变异趋势。该方法快速、简便、经济、高效、实用并且安全,适合大批量样本中六氯苯的快速检测。     

气相色谱-负化学源质谱法测定辣椒中咪鲜胺及2,4,6-三氯苯酚

建立了气相色谱-负化学源质谱法同时测定辣椒中咪鲜胺及其代谢物2,4,6-三氯苯酚的方法。结果表明：在负化学源下对目标物检测具有良好的响应,并对比了净化吸附剂PSA、C₁₈和GCB的净化效果,最终选择C₁₈为前处理净化吸附剂;辣椒中咪鲜胺和2,4,6-三氯苯酚的定量限为0.05 mg/kg;咪鲜胺在辣椒中的回收率为85.0%～92.3%,相对标准偏差(RSD)为0.3%～2.3%;2,4,6-三氯苯酚在辣椒中的回收率为82.3%～96.4%,RSD为0.8%～1.7%。该方法简单、快速、高效,可用于同时对咪鲜胺和2,4,6-三氯苯酚农药残留进行测定。     

水浴湿法消化Zeeman石墨炉原子吸收法测定肉鸡肝组织中硒含量

采用水浴湿法消化 ,以 Pd( NO3) 2 - Triton X- 10 0作为基体改进剂 ,应用 Zeem an石墨炉原子吸收法测定了肝组织硒含量。试验结果表明 ,肝组织经水浴湿法消化测得的硒含量与消化炉湿法消化测定结果基本一致 ( P >0 .0 5) ,相对标准偏差为 1.11%,回收率为 95.80 %～ 10 0 .4 0 %。石墨炉原子吸收法测定硒的检测限为 5.0 μg/ L     

儿茶素的药理作用研究综述

目的研究表儿茶素(EC)对小鼠急性肺损伤(ALI)炎症反应的调节作用。方法采用吸入式气管滴注法在BALB/c小鼠中建立ALI模型,H8LE染色观察肺组织病理学变化,并结合基于超高效液相色谱与四极杆—飞行时间质谱联用技术(HILIC UHPLC-Q-TOF MS)的非靶向代谢组学方法对小鼠肺组织进行研究。结果对比空白对照组,LPS处理后的小鼠肺组织发生严重的炎症变化,而EC预处理组炎症现象比LPS组轻。经肺组织代谢轮廓分析发现：二十羟基花生四烯酸、色氨酸、苯丙氨酸、酪氨酸、ATP、磷酸胆碱、二十碳四烯酸、磷酸、烯醇和二磷酸葡萄糖等差异物与小鼠急性肺损伤内源性代谢密切相关,且涉及甘油酯代谢、糖酵解、甘油磷脂代谢、苯丙氨酸、酪氨酸和色氨酸生物合成、抗坏血酸代谢和胆碱代谢等6条代谢路径。结论运用代谢组学方法探讨了EC干预小鼠ALI的差异代谢物变化情况,为表儿茶素抗炎特性的研究提供了理论依据。     

初乳真空冷冻干燥传热传质系数测定与分析

应用准稳态传热传质理论，在考虑水蒸气扩散对传热作用情况下，分别建立了奶牛初乳在真空冷冻干燥中多孔干燥层有效导热系数，冻结层导热系数和水蒸气扩散系数的测试模型，利用在冻干机上测取的试验数据，回归得到初乳的传热系数与水蒸气扩散系数，分析了压力与系数间的关系，结果表明，在１０Ｐａ～１２０Ｐａ范围内，干燥层有效导热系数随压力增大而增加，尤其在１０Ｐａ～６０Ｐａ范围内更为明显，而水蒸气扩散系数随压力的改变变     

顶空固相微萃取气相色谱质谱嗅觉测量联用初探鲢肉的挥发性风味物质

为探明鲢肉挥发性气味特征物质,通过顶空固相微萃取法提取和浓缩了鲢肉中的挥发性物质,并利用气相色谱质谱联用以及气相色谱〖CD*7/9〗嗅觉测量法对气味物质进行了定性分析及气味特征的评价。由8人组成的评价小组通过检测频率法进行嗅觉测量。结果表明,经GCMS分析鉴定得到了29种挥发性气味物质,主要是一些羰基类和醇类化合物,占了总挥发性物质的88%。通过检测频率分析法鉴定出12种化合物具有气味特征,表现为鱼腥、金属、青草、油脂氧化、蘑菇等特征。另外有4种未知物也显示了较强的风味特性,它们协同作用构成了鲢的特殊气味。     

PASSAT领驭2.0自动变速箱偶尔出现紧急运行状况检修分析

结合PASSAT领驭2.0轿车偶尔出现自动变速箱Ⅲ挡运行的紧急运行状况故障,分析了故障码、有关传感器电路,以及故障产生的原因,据此找出了故障点,并排除了故障。     

甲砜霉素在鲤鱼及鲫鱼体内的残留研究

本研究旨在分析甲砜霉素在鲤鱼和鲫鱼体内的残留消除规律并为制定休药期提供依据。按照30 mg/kg的给药量对鲤鱼和鲫鱼连续口灌给药甲砜霉素3天,定时取样,外标法定量,采用高效液相色谱-串联质谱法(HPLC-MS/MS)检测采样组织中甲砜霉素的残留量。结果显示：甲砜霉素在0.1~200 ng/mL范围内有良好的线性关系,相关系数为0.9987。回收率在81.33%~109.72%之间。甲砜霉素在停止给药后鱼体各检测组织中残留量呈下降趋势,在停药25天后,甲砜霉素残留量低于中国与欧盟规定的最高残留限量(MRLs)。根据结果,建议休药期为25天。