Pharmacokinetics of C-1027 in mice as determined by TCA-RA method

AIM: To validate a radioactivity assay, the TCA-RA method, for the measurement of C-1027 in serum and to evaluate its application in determination of pharmacokinetics of C-1027 in mice. METHODS: 125I-C-1027 was prepared by the lodogen method and separated by HPLC. The radioactivity assay was established and used to determine 125I-C-1027 in mice at doses of 10, 50 and 100 μg/kg after precipitation with 20% trichloroacetic acid (TCA-RA method). Several pharmacokinetic parameters were determined after intravenous injection of 125I-C-1027 to mice. RESULTS: After intravenous injection of 125I-C-1027 to mice, at doses of 10, 50 and 100μg/kg; the apparent distribution volumes (Vd) were 0.26, 0.31 and 0.33 L/kg; the biological half-lives (T1/2) were 3.10, 3.40 and 3.90 h; the areas under curve (AUC) were 18.41, 103.69 and 202.74 ng/h/mL; the elimination rate constants (A) were 1.04, 1.26 and 0.58/h; and the total body clearance (Cl) were 0.54, 0.48 and 0.49 L/kg/h, respectively. CONCLUSION: TCA-RA is a sensitive, reliable and suitable method for the determination of 125I-C-1027 in mouse serum.

Tissue distribution and excretion of ^(125)I-lidamycin in mice and rats

AIM: To investigate the tissue distribution, urinary and fecal excretions of 125I-lidamycin (125I-C-1027) in mice and its biliary excretion in rats. METHODS:The total radioactivity assay (RA method) and the radioactivity assay after precipitation with 200 mL/L trichloroacetic add (TCA-RA method) were used to dete-rmine the tissue distribution,and the urinary and fecal excretions of 125I-C-1027 in mice and its biliary excretion in rats. RESULTS:Tissue concentrations reached the peak at the fifth minute after administration of 125I-C-1027 to mice. The highest concentration was in kidney, and the lowest in brain at all test-time points. The organs of the concentrations of 125I-C-1027 from high to low were kidney, lung, liver, stomach, spleen, uterus, ovary, intestine, muscle, heart, testis, fat, and brain in mice. The accumulative excretion amounts of 0-24 h, and 0-96 h after administration of 125I-C-1027 were 68.36 and 71.64% in urine, and 2.60 and 3.21% in feces of mice, respectively, and the accumulative excretion amount of 0-24 h was 3.57% in bile in rats. CONCLUSION: Our results reflect the characteristics of the tissue distribution, urinary and fecal excretions of 125I-C-1027 in mice and the biliary excretion of 125I-C-1027 and its metabolites in rats, and indicate that 125I-C-1027 and its metabolites are mainly distributed in kidney, and excreted in urine.

三氯醋酸-放射性同位素法研究重组人集成干扰素α的豚鼠药动学

目的测定豚鼠皮下注射重组人集成干扰素α（recombinant human consersus interferon-a,以下简称rhCIFN）后的吸收、分布、排泄以及药动学参数.方法采用三氯醋酸沉淀蛋白后,测定沉淀物中放射性的方法（简称三氯醋酸-放射性同位素法,TCA-RA法）,计算豚鼠皮下注射125^Ⅰ标记rhCIFN后血液、组织或排泄物中的总放射性以及药动学参数.结果豚鼠皮下注射125^Ⅰ标记rhCIFN 3μg·kg^-1后的药物消除符合二房室消除模型,消除相半衰期（t1/2β）为13.2 h;tmax为2 h;ρmax为4.76μg·L^-1;AUC0～48为50.9μg·h·L^-1.豚鼠静脉注射125Ⅰ标记rhCIFN 3μg·kg^-1后AUC0-48为71.2μg·h·L^-1,豚鼠皮下注射rhCIFN的相对生物利用度为71.5%.豚鼠皮下注射125Ⅰ标记rhCIFN 3μg·kg^-1后测定不同组织的药物含量,发现药物在组织中的浓度除肾脏和脾脏外其他组织均低于同时间的血药浓度,所有组织含药量均于给药后2 h达到最高,以后逐渐降低.在各时间点以肾脏含药量最高,脾、肺和肝组织含量次之,脑、肌肉和脂肪组织的药物含量最少;96h内有89.7%放射性从尿中回收,5.7%从粪中回收,尿粪总排泄量达给药剂量的95.4%,表明该药主要经肾由尿排泄.结论用TCA-RA测定了豚鼠皮下注射rhCIFN后的吸收、分布、排泄以及药动学参数,灵敏度高、特异性强、准确性好,可用于动物和以后临床的药动学研究.

TCAS系统多目标机冲突决策处理的研究

本文主要介绍空中交通多目标机冲突的Pairwise决策方式。以空中交通警戒和防撞系统（TCAS）对多目标冲突处理为例，介绍了Pairwise处理方式在实际案例中的应用。详细分析了TCAS系统对多目标机冲突处理的原理、处理流程以及主要处理功能模块。介绍了TCAS对多目标机冲突的分类以及分类后的具体Pairwise处理方式。最后对比了Pairwise与Global两种多目标机冲突的处理方式，分析了两种处理方式的优缺点。

基于Qt的TCAS显示输出验证装置设计与实现

在机载航电设备综合集成的趋势下,综合显示器取代了原来各分系统的独立显示器。各航电产品在设计开发过程中,为了对产品处理生成的图形信息进行输出显示,根据显示输出内容开展产品的功能和性能验证,就需要根据航电设备的功能和接口,设计开发专用的显示输出验证装置。本文介绍了一种空中交通预警和防撞系统(TCAS)显示输出验证装置的实现方法,该装置可以接收TCAS的输出、显示空中入侵机标识和状态、显示防撞指令等,实现了对TCAS产品的显示输出和功能性能验证测试。