Pharmacokinetics of intravenously administered sodium dichloroacetate in rabbits

ＰｈａｒｍａｃｏｋｉｎｅｔｉｃｓｏｆｉｎｔｒａｖｅｎｏｕｓｌｙａｄｍｉｎｉｓｔｅｒｅｄｓｏｄｉｕｍｄｉｃｈｌｏｒｏａｃｅｔａｔｅｉｎｒａｂｂｉｔｓＧｕＢｉｎ（顾斌）；ＳｏｎｇＬｉｎｇ（宋岭）；ＪｉａｎｇＹｏｎｇｐｅｉ（蒋永培）；ＷｅｎＡｉｄｏｎｇ（文...     

人体中氧氟沙星的立体选择性代谢

５名健康志愿者日服单剂３００ｍｇ氧氟沙星［（±）－Ｏｆ１］后，采用立体选择性的ＲＰ－ＨＰＬＣ手性流动相添加剂法测定尿中Ｓ－（－）－Ｏｆ１和Ｒ－（＋）－Ｏｆ１浓度结果显示Ｏｆ１在人体内呈现立体选择性代谢。尿中排泄的Ｓ－（－）－Ｏｆ１／Ｒ－（＋）－Ｏｆ１之比随时间变化。服药后２ｈＳ／Ｒ是０．８７５，２４ｈ增加到１．１５０．Ｓ－（－）－Ｏｆ１的消除半衰期（ｔ１／２）是４．５７ｈ；消除速率常数（ｋ）是０．１５４ｈ；药时曲线下的面积（ＡＵＣ）为１．１７ｍｇ·ｈ－１．ｍＬ－１；Ｒ－（＋）－Ｏｆ１的ｔ１／２为４．１８ｈ，ｋ为０．１６８ｈ－１，ＡＵＣ是１．７８ｍｇ·ｈ－１·ｍＬ－１；经配对ｔ检验这三对参数间有显著性差异，Ｐ值分别小于０．０１，０．００１和０．００５．因此两对映体在人体内呈现立体选择性处置     

Radium-228 determination of natural waters via concentration on manganese dioxide and separation using Diphonix ion exchange resin

The objective of this work was to establish a new procedure for ²²⁸Ra determination of natural waters via preconcentration of radium on MnO₂ and separation of its daughter, ²²⁸Ac, using Diphonix ion exchange resin. Following removal of potential interferences via passage through an initial Diphonix Resin column, the first daughter of ²²⁸Ra, ²²⁸Ac, is isolated by chromatographic separation via a second Diphonix column. A holding time of >30 h for ²²⁸Ac ingrowth in between the two column separations ensures secular equilibrium. Barium-133 is used as a yield tracer. Actinium-228 is eluted from the second Diphonix Resin with 5 ml 1 M 1-Hydroxyethane-1,1-diphosphonic acid (HEDPA) and quantified by addition of scintillation cocktail and LSC counting. Radium (and ¹³³Ba) from the load and rinse solutions from the 2nd Diphonix column may be prepared for alpha spectrometry (for determination of ²²³Ra, ²²⁴Ra, and ²²⁶Ra) by BaSO₄ microprecipitation and filtration. Decontamination tests indicate that U, Th, and Ra series nuclides do not interfere with these measurements, although high contents of ⁹⁰Sr (⁹⁰Y) require additional treatment for accurate measurement of ²²⁸Ra. Addition of stable Sr as a “hold back” carrier during the initial MnO₂ preconcentration step was shown to remove most ⁹⁰Sr interference.     

次氯酸对人血清白蛋白的氧化修饰影响及与高级氧化蛋白产物的关系

目的 研究次氯酸对人血清白蛋白(HSA)的氧化修饰影响及与高级氧化蛋白产物(AOPPs)之间的关系。 方法 有氧条件下在恒定浓度的HSA(60 mg/ml)内加入不同浓度次氯酸(0、1、5、10、20、30、40、50、60 mmol/L，最终浓度)，观察氧化剂对HSA的修饰作用。凝胶排阻色谱法检验HSA氧化修饰结果，在线光谱扫描(190 nm~400 nm)分析修饰产物的光谱特性。结果 次氯酸可氧化修饰人血清白蛋白，其修饰产物主要为二聚体HSA和六聚体HSA。发现次氯酸对HSA单体和HSA二聚体的氧化修饰为一级反应；对诱导生成的AOPPs为准一级反应；而对诱导生成的HSA六聚体则为二级修饰反应。同时发现白蛋白对AOPPs的主要贡献者是六聚体形式的HSA，光谱分析表明HSA聚集体的最大吸收峰发生红移，提示HSA聚集体是由于蛋白中的酪氨酸残基通过氧化交联方式而聚集形成的。 结论 HSA经次氯酸处理后主要发生了蛋白聚集。而对AOPPs的主要贡献者是六聚体形式的HSA。     

Biological characterization of glutaraldehyde-modified Parietaria judaica pollen extracts

BACKGROUND: Allergoids are widely used in specific immunotherapy (SIT) for the treatment of IgE-mediated allergic diseases, but all techniques for standardization of conventional allergic extracts may not be appropriate for standardization of a glutaraldehyde (GA)-modified extract because of the unique characteristics of these extracts. OBJECTIVE: To assess an accurate methodology for standardization of chemically modified extracts. METHODS: GA-modified extracts from Parietaria judaica pollen were purified by diafiltration. Biochemical properties were investigated by determination of amino groups, chromatography, and SDS-PAGE. The IgE-binding activity was determined by skin prick test, enzyme allergosorbent test inhibition, basophil activation, and histamine release tests. Peripheral blood mononuclear cells (PBMCs) from P. judaica pollen-allergic subjects were stimulated with either native or allergoid extracts, and proliferation was measured. RESULTS: Biochemical data indicated a high degree of allergen polymerization resulting in extract components higher than 100 kDa. IgE-binding activity, both in vivo and in vitro, was reduced by more than 99.8%. Both allergen and allergoid induced PBMC proliferation and synthesis of blocking IgG antibodies at similar rates. Moreover, no evidence of introduction of new determinants by chemical modification was found. CONCLUSIONS: The preparation of GA-modified extracts by diafiltration is faster and more reliable than previous chromatographic methods. These modified extracts have drastically reduced their allergenicity while maintaining their immunogenicity, and therefore they can be used in safer and shortened schedules of SIT.     

急性脑出血患者血清谷氨酸动态变化分析

目的通过观察脑出血（intracerebral hemorrhage，ICH）患者血清中谷氨酸的动态变化来进一步评价谷氨酸对脑出血的作用。方法选择符合条件的30例急性高血压脑实质出血患者，给予神经内科脑出血常规治疗，采用高效液相色谱法检测起病后2d内、5．6d、8-9d和15．16d的血清谷氨酸浓度，同步进行神经功能评定，同时于发病后1．3d、d5-6d及d15．16行头部CT检查了解血肿体积大小。结果脑出血患者血中谷氨酸浓度与血肿体积及神经功能缺损评分之间呈正的直线相关。经治疗后，所有病例谷氨酸水平迅速下降，在5-6d和8—9d下降速度更加明显。结论谷氨酸可能参与了自发性脑出血患者的急性期脑损伤作用。     

高压液相色谱纯化肾综合征出血热病毒血凝素及其性状分析

用吐温８０－乙醚（ＴＥ）法、蔗糖－丙酮（ＳＡ）法、丙酮－乙醚（ＡＥ）法分别从肾综合征出血热病毒（ＨＦＲＳＶ）感染的Ｖｅｒｏ－Ｅ６细胞培养和乳小白鼠脑组织中制备病毒血凝素（ＨＡＮ），定量对比证明其制备效果，结果无明显差异。粗制ＨＡＮ经高压液相色谱（ＥＰＬＣ）纯化，有４个洗脱峰，血凝活性物质存在于峰１。纯化ＨＡＮ在ＳＤＳ－ＰＡＧＥ中呈单一区带，分子量５６．６ＫＤ，ＨＡＮ相对含量７９．６％。纯化ＨＡＮ在蔗糖密度梯度液中有一条１．１５～１．１６ｇ／ｃｍ３的沉淀，粗制ＨＡＮ有３条沉淀。电镜观察纯化ＨＡＮ中为大小相等的球状颗粒。粗制ＨＡＮ的高密度沉淀中可见到病样颗粒。对几种常用消毒剂、氧化剂、去垢剂对ＨＡＮ的灭活作用做了实验对比观察。     

PHA RMA COKINETICS OF CUPRIC－BIS（SALICYLALDEHYDE－2－FURA NTHIOCA RBOXY－HYDRAZONATE） DICHLORIDE（CSFTCH） IN RABBITS

ＰＨＡＲＭＡＣＯＫＩＮＥＴＩＣＳＯＦＣＵＰＲＩＣ－ＢＩＳ（ＳＡＬＩＣＹＬＡＬＤＥＨＹＤＥ－２－ＦＵＲＡＮＴＨＩＯＣＡＲＢＯＸＹ－ＨＹＤＲＡＺＯＮＡＴＥ）ＤＩＣＨＬＯＲＩＤＥ（ＣＳＦＴＣＨ）ＩＮＲＡＢＢＩＴＳ￥ＧａｏＹｕｎｓｈｅｎｇ；ＺｈｕＹｕｙｕｎ（...     

辐射反应性A1蛋白质的分离纯化

本文撮道了用制备电泳和柱层析二种方法结合分离纯化放射病反应性增多的A₁蛋白质。方法简便,操作流程短,重复性娥经鉴定A₁蛋白质是一种未见文献报道的蛋白质。以此制备抗血清可用于放射病临床治疗的监测和放射病病理机制的研究。     

高效液相色谱法检测血中表阿霉素的研究

用ＺｏｒｂａｘＣ－８柱成功地分离了阿霉素、表阿霉素及其代谢产物。在此基础上建立了用阿霉素作内标物定量测定表阿霉素的分析方法，其最低检测限为２ｎｇ／ｍｌ，线性范围１０－３００ｎｇ／ｍｌ。