二氟沙星在鸡体内的药物代谢动力学及生物利用度研究

将 30只艾维茵肉鸡随机分为 3组 ,进行了静脉注射、肌肉注射及内服二氟沙星的药物代谢动力学研究。血浆样品经甲醇沉淀血浆蛋白 ,高速离心 ,用反相高效液相色谱法测定鸡血浆中二氟沙星的浓度 ,MCPKP计算机程序处理血浆药物浓度 时间数据。结果 ,健康鸡静脉注射给药的药时数据适合二室开放模型 ,主要药物代谢动力学参数为 :t1/ 2α=0 .6 9h± 0 .4 3h ;t1/ 2 β=6 .11h± 1.5 0h ;V1=1.70L/kg±0 .33L/kg ;Vd(area) =3.10L/kg± 0 .6 7L/kg ;ClB=0 .37L/ (kg·h)±0 .10L/ (kg·h) ;AUC =2 9.16 μg/ (mL·h)± 8.0 4 μg/ (mL·h)。健康鸡肌肉注射及内服给药的药时数据适合一级吸收一室模型 ,前者的主要药物代谢动力学参数为 :t1/ 2Ka=0 .17h± 0 .12h ,t1/ 2Ke=5 .6 4h± 0 .74h ,tmax =0 .86h± 0 .4 0h ,Cmax =2 .5 1μg/mL± 0 .36 μg/mL ,AUC =2 2 .6 2μg/ (mL·h) ± 3.2 8μg/ (mL·h) ,F =77.0 %± 11.8% ;后者的药物代谢动力学参数为 :t1/ 2Ka=1.4 6h± 1.0 0h ,t1/ 2Ke=8.2 0h± 3.12h ,tmax=4 .34h± 2 .4 0h ,Cmax=1.0 0 μg/mL± 0 .2 1μg/mL ,AUC =15 .82 μg/ (mL·h) ± 3.6 7μg/ (mL·h) ,F =5 4.2 %± 12 .6 %。二氟沙星在健康鸡体内的主要药物代谢动力学特征为 :表观分布容积大     

乙酰甲喹在家兔体内药物代谢动力学和首过效应的研究

为探讨家兔单次静脉注射和灌胃乙酰甲喹(30mg/kg)后的血浆药物代谢动力学特征,15只家兔被随机均分为A、B、C三组,A、B两组均通过消化道给药,但A组自心脏采血,B组自肝门静脉采血,C组则经耳缘静脉给药,自心脏采血。利用高效液相色谱法(定量限为0.1μg/mL)检测每个血浆样品中乙酰甲喹的质量浓度,之后以非房室分析法计算乙酰甲喹的药物代谢动力学参数。经消化道给药之后,A、B两组中乙酰甲喹的大多数药物代谢动力学参数均具有显著差异:消除速率常数(λz)分别为0.43h-1±0.11h-1和0.19h-1±0.02h-1;消除半衰期(t1/2λz)分别为1.76h±0.65h和3.69h±0.44h;药时曲线下面积(AUC0-∞)则分别为29.28(h·μg)/mL±4.4(h·μg)/mL和78.39(h·μg)/mL±7.28(h·μg)/mL。而静脉注射(C组)后,这些参数的数值分别为0.35h-1±0.03h-1、2.02h±0.18h和40.86(h·μg)/mL±6.76(h·μg)/mL,而体清除率(Cl)为747.93mL/(h·kg)±103.76mL/(h·kg),表观分布容积(Vz)为2 170.19mL/kg±308.96mL/kg。乙酰甲喹在A组和B组中的口服生物利用度分别为71.65%和192.85%。结果表明,静脉注射后,乙酰甲喹在家兔体内分布广泛、消除迅速;而灌胃给药后,乙酰甲喹吸收迅速,但存在明显的首过效应。     

氟苯尼考混悬注射液与普通注射液在猪体内的药代动力学比较

按20 mg/kg剂量分别给猪注射氟苯尼考混悬注射液与普通注射液后,用HPLC-UV法测定了血浆中氟苯尼考的浓度,所得药-时数据用3P97药代动力学软件进行了处理.静脉注射氟笨尼考普通注射液后的药-时数据符合无吸收二室开放模型,动力学参数为:t1/2a=(8.74±1.92)h,V/F(c)=(0.88±0.11)L/kg,AUC=(85.39±5.70)ìg/(mL·h),Cl(s)=(0.24±0.02)L/(kg·h).肌肉注射氟苯尼考混悬注射液及普通注射液后的药-时数据分别符合一室、二室开放模型,动力学参数分别为:t1/2ka=(0.60±0.11)h和(0.19±0.05)h,t1/2ke=(23.13±4.06)h和(22.77±2.58)h,Tamax=(9.00±1.00)h和(1.42±1.00)h,Camax=(2.10±0.27)ìg/mL和(2.99±0.12)ìg/mL,F=76.20%±5.54 %和6和72.50%±7.89%.表明,氟苯尼考混悬注射液具有吸收慢、消除慢、生物利用度高、有效血药浓度时间长及缓释的特点.     

泰拉霉素在猪体内的药动学特征及其血浆蛋白结合率的研究

本研究旨在比较自制泰拉霉素注射液和瑞可新注射液在猪体内的药代动力学特征,并测定泰拉霉素在猪体内的血浆蛋白结合率。18头健康猪被随机分为3组,分别进行单剂量(2.5 mg/kg)静脉注射、肌内注射泰拉霉素注射液和肌内注射瑞可新注射液,超高效液相色谱-串联质谱(UPLC-MS/MS)法测定猪血浆中泰拉霉素的浓度,采用药动学软件Winnonlin 5.2.1处理血浆药物浓度-时间数据,并计算出有关药动学参数。采用超滤法考察泰拉霉素在猪体内的血浆蛋白结合率。结果,静脉注射自制泰拉霉素注射液后,其主要药动学参数为t_(1/2β)=72.20 h±20.35 h,AUC_(last)=11.31 g·h/mL±4.20 g·h/mL,MRT=72.01 h±14.81 h。肌内注射泰拉霉素注射液和瑞可新注射液后的主要药动学参数如下,t_(max)分别为0.50 h±0.22 h,0.22 h±0.07h;C_(max)分别为1.18 g/mL±0.55 g/mL,1.81 g/mL±0.68 g/mL;AUC_(last)分别为10.85 g·h/mL±4.76g·h/mL,12.06 g·h/mL±3.08 g·h/mL;t1/2β分别为68.59 h±14.29 h,68.01 h±15.10 h。与瑞可新相比,自制泰拉霉素注射液相对生物利用度为92.95%±16.89%,绝对生物利用度为93.90%±19.11%。上述结果表明,猪肌内注射泰拉霉素后吸收迅速,体内分布广泛,消除缓慢,生物利用度高;自制泰拉霉素注射液与瑞可新的药动学特征相似,生物利用度相当;泰拉霉素的血浆蛋白结合率高达95.17%,属于高蛋白结合率化合物且无浓度依赖性。     

喹烯酮在鲤和斑点叉尾鮰体内的药代动力学及组织分布

为了研究喹烯酮在鱼体内的药物代谢动力学及组织分布情况,在(15±1)℃的水温条件下,按50mg/kg单剂量口服给药后,采用高效液相色谱法测定喹烯酮在鲤、斑点叉尾鮰血浆与组织中的药物浓度.结果,喹烯酮在鲤和斑点叉尾鮰体内的药代动力学模型均符合两室开放模型.喹烯酮在鲤血液中2 h时达到最高血药浓度(Cmax)为0.452 μg/mL,在肝、肾、肌肉组织中达峰时间分别为8、16和16 h,主要药代动力学参数t1/2(ka)、t1/2β、AUC分别为1.263 h、35.866 h、24.585(μg/mL)·h;喹烯酮在癍点叉尾鮰血液中8 h达到最高血药浓度(Cmax)为0.029μg/mL,在肝、肾、肌肉组织中达峰时间分别为16、48和72 h,主要药代动力学参数t1/2(ka)、t1/kβ、AUC分别为4.669 h、31.164 h、1.388(μg/mL)·h.结果表明,喹烯酮在鲤与斑点叉尾鮰体内吸收较快,分布较广,主要经肝、肾代谢.     

高效液相色谱仪检测猪组织器官喹烯酮残留方法的建立

建立一种用高效液相色谱仪检测猪组织器官中喹烯酮含量的方法 ,用于监测猪食用组织中喹烯酮的残留。肝、肾、肌肉、脂肪组织样品经乙酸乙酯、乙腈、正己烷、氯仿等试剂提取、纯化后 ,采用Waters 5 10高效液相色谱仪在 312nm波长处检测 ,流速为 1.0mL/min。检测结果 ,脂肪、肝、肾、肌肉的标准曲线及线性范围分别为Y =4× 10 - 5X - 0 .0 2 4 3、0 .0 0 5～ 0 .0 80 μg/g ;Y =7× 10 - 5X - 0 .0 2 32、0 .0 0 5～ 0 .80 0 μg/g ;Y =2× 10 - 4X - 0 .14 2 4、0 .0 0 8～ 0 .0 80 μg/g ;Y =8×10 - 5X - 0 .0 5 2 4、0 .0 0 8～ 0 .0 80 μg/g。在本试验条件下 ,脂肪、肝的最低检出浓度为 0 .0 0 4 μg/g ;肾、肌肉为 0 .0 75 μg/g。平均回收率 :肌肉 99.85 %± 4 .95 % ,脂肪 10 3.15 %± 8.2 5 % ,肝 96 .5 5 %± 9.16 % ,肾 10 2 .10 %± 6 .87%。精密度测试喹烯酮的日内各组织不同浓度的RSD(相对标准差 )均小于 12 .0 % ,日间均小于 18.5 %。本方法灵敏度高 ,重复性好 ,符合兽药残留试验技术规范的要求     

阿散酸在猪体内的药动学与生物利用度研究

选用体重25 kg左右的长×大二元杂健康猪8头,按双周期双交叉试验设计,进行静脉注射与内服阿散酸(10 mg/kg)的药动学研究。采用高效液相色谱法测定猪血浆中阿散酸的浓度,用统计矩原理处理血浆药物浓度-时间数据。结果显示:健康猪静脉注射阿散酸后的主要药动学参数为β=0.55 h-1±0.01h-1,t1/2β=1.26h±0.03 h,Vz=0.30L/kg±0.01 L/kg,Vdss=0.29 L/kg±0.01 L/kg,CL=0.17 L/(kg.h)±0.01 L/(kg.h),MRT=1.75 h±0.07 h,AUC=60.44μg/mL.h±0.01μg/mL.h;内服给药的主要药动学参数为β=0.39 h-1±0.02 h-1,t1/2β=1.79 h±0.09 h,tmax=1.81 h±0.09 h,Cmax=3.43μg/mL±0.53μg/mL,MRT=3.95 h±0.13 h,AUC=15.12μg/mL.h±0.01μg/mL.h,F=24.5%±3.4%。研究结果表明,阿散酸在健康猪体内的药动学特征为内服吸收迅速,血药浓度达峰时间短,但药物峰浓度低,绝对生物利用度低,消除快...     

吉他霉素在猪体内的药代动力学特征及残留检测方法的研究

对7头健康猪按随机交叉设计经单剂量(2.5×104U/kg)内服吉他霉素原药及其微囊制剂进行了药代动力学试验。血浆样品经磷酸氢二钾溶液碱化、无水乙醚提取后,采用HPLC法测定血药浓度。结果表明,药时数据均符合一级吸收二室开放模型,主要药代动力学参数为:原药t1/2ka=0.23h±0.05h,t1/2β=6.43h±2.38h,tmax=0.65h±0.17h,Cmax=6.97μg/mL±1.40μg/mL,AUC=19.98mg/(L.h)±8.16mg/(L.h);微囊制剂t1/2ka=0.55h±0.16h,t1/2β=10.63h±3.73h,tmax=1.25h±0.23h,Cmax=7.97μg/mL±1.63μg/mL,AUC=36.24mg/(L.h)±6.15mg/(L.h)。吉他霉素原药在猪体内吸收较快,但其微囊制剂分布更广泛并消除较缓慢。对猪肌肉、肝和肾等添加吉他霉素标样后均采用0.2%偏磷酸-甲醇萃取后过SCX小柱用甲醇抽提吹干,脂肪加标样采用正己烷除脂后用甲醇反萃取减压蒸干。采用HPLC法测定组织浓度。结果,各组织在0.05～6.4μg/g范围内线性关系良好(r0.999),吉他霉素在各组织中回收率均大于65.38%,批内及批间变异系数分别小于5.56%和4.60%,检测限为0.05μg/g。结果表明,此方法重复性好、灵敏度高,可用于猪组织中吉他霉素残留的检测。     

咪唑苯脲缓释剂在黄牛体内的药代动力学及组织残留量测定

用紫外分光光度计测定了咪唑苯脲缓释剂在黄牛体内不同时间的血浆药物浓度及组织药物残留量.结果为该药药代动力学符合一室吸收模型、动力学方程为C=2.7885(e-0.0032t-e-0.4229t).药代动力学参数为达峰时间Tmax为11.320 h±0.2955 h,峰浓度为2.804μg/mL±0.0029 μg/mL,吸收相半衰期t(1/2)α为1.643 h±0.9960 h,消除相半衰期t(1/2)β为215.061 h±22.2836 h,与肌肉注射咪唑苯脲注射液相比,半衰期延长了210.383 h.组织含量检测结果为注射后3月时脑、肝、脾、肾、心肌、肌肉中药物残留量分别为0.134 μg/g±0.0302μg/g、0.976 μg/g±1.2432μg/g、0.743μg/g±0.1864 μg/g、0.527 μg/g±0.2243μg/g、0.313μg/g±0.1723 μg/g和0.373 μg/g±0.0420 μg/g;4月时肝、脾、肾分别为0.276 μg/g±0.0437μg/g、0.113μg/g±0.0252 μg/g和0.182 μg/g±0.0337 μg/g.结果表明,咪唑苯脲缓释剂优于其他咪唑苯脲剂型.     

麻保沙星在番鸭体内的药代动力学研究

将30只健康番鸭随机分为3组,静脉注射、肌肉注射及内服麻保沙星(2.5mg/kg)后,采用反相高效液相色谱法测定血浆中麻保沙星的浓度,用Kinetica4.4.1药代动力学软件处理所得到的血药浓度-时间数据。结果显示,健康番鸭静脉注射给药的药时数据适合二室开放模型,主要药代动力学参数分别为:t1/2α=(0.45±0.17)h,t1/2β=(3.28±0.33)h,Vc=(0.8±0.1)L/kg,Vd(area)=(1.39±0.28)L/kg,Vd(ss)=(1.25±0.22)L/kg,Cl=(0.23±0.05)L/(h.kg),AUC=(9.24±1.35)mg/(h.L)。健康番鸭肌肉注射给药的药时数据适合一级吸收一室开放模型,主要药代动力学参数分别为:t1/2ka=(0.16±0.06)h,t1/2kel=(2.82±0.36)h,tmax=(0.59±0.11)h,Cmax=(1.8±0.29)μg/mL,AUC=(7.92±1.09)mg/(h.L),F=(90.4±1.73)%。健康番鸭内服给药的药时数据适合一级吸收一室开放模型,主要药代动力学参数分别为:t1/2ka=(0.34±0.09)h,t1/2kel=(4.61±0.57)h,tmax=(1.41±0.3)h,Cmax=(1.13±0.21)μg/mL,AUC=(8.8±1.15)mg/(h.L),F=(96.98±5.16)%。结果表明,麻保沙星在健康番鸭体内的药代动力学特征是:吸收迅速且完全,分布广泛,消除缓慢,组织渗透力强,生物利用度高。     

China＇s Rise vs. International Order Evolution

A heated debate over the rise of China has been going on unabated in the international community for nearly two decades. However, with the elapse of time, the initial divergence of views in the mainstream opinion has gradually diminished and the gap in China policy among nations has likewise narrowed down. Instead, reason and a realistic approach have eventually taken center stare.     

The U. S. Policy toward DPRK: Opportunities and Constraints

布什政府上台以来,始终未能阻止朝鲜拥核步伐.朝核试后,美对朝政策有了新的调整,六方会谈得以复会.但美朝双方受各自国家利益和政策目标的限制,在朝鲜半岛无核化问题上的尖锐分歧难以解决,朝核危机仍存在再度升级的可能.     

Marxist Philosophy vs. International Relations Research in China

This article argues for the confirmation of Marxist philosophy as the ideology that guides international relations （IR） studies in China. Justification comes through the following points. According to Marxism, correct theoretical guidance serves as the prerequisite for correct practice. Marxist philosophy embodies, by nature, righteousness, in opposition to political hegemony. Accordingly, practice under its guidance represents fruitful revolutionary realism. Finally, advanced studies of international relations in this country cannot be separated from philosophical thinking. Using these arguments as background, this article specifically advocates materialism, patriotism, and service to the people as the corner-stone of China＇s IR theory building.     

The Development of EU-Russian Relations

The EU＇s strategy for Russia since the end of the cold war has to a large extent failed, and the direct consequences are the currently deadlocked EU-Russia relationship. There are three reasons for this： the EU and Russia＇s respective strength and status relative to each other have been changing since the beginning of this century; the EU＇s strategy towards Russia has been more fragmenting in recently years; and the American factor. The EU-Russia relations could continue to be in poor shape in the years to come, and it is very likely sometimes even further worsening. But the two sides would refrain from extreme measures and prevent their relations from sliding into real cold war.     

Excavating Concealed Tradeoffs: How Russians Watch the News

Citizens in democracies are expected to make better decisions if they understand policy tradeoffs. However, politicians rarely have incentives to communicate them; citizens are uncomfortable choosing among valued outcomes; and devising a common metric is difficult. It is not surprising that in the United States the environment provides relatively little cuing or priming of tradeoffs in television news. Russian citizens, on the other hand, face a media environment in which tradeoff cuing is intentionally suppressed by owners' agendas, yet viewers detect concealed tradeoffs even in the absence of tradeoff priming and viewpoint diversity. Analysis of discourse among ordinary Russians in 16 focus groups convened in four cities, differentiated by political reform and media market environments, showed that when watching news in which tradeoffs are thoroughly concealed, viewers challenge stories by offering a broad spectrum of uncued tradeoffs. Tradeoffs come from diverse policy domains and represent a range of cognitive strategies, some of which are considerably more abstract than others and link elements of their observations and assumptions (together with what they can extract from the stories) into complex reasoning outcomes.     

The U.S. Global Strategy as Seen from the Debate in the Primary Election

There may be more than one year to go before the 2008 U.S. presidential election, but the primary election of the two parties has already begun ahead of time. Both the Democratic and Republican candidates for the     

Young American China Watchers＇ Views on China

In this paper, the author has made a thorough study over the new generation of American China Watchers. Most of the pages are devoted to a detailed comparison between the old generation and the young generation of American China Watchers regarding to their background, education, and views over China. At the end of the paper, the author also gives some policy suggestions for both the Chinese and U.S. government based on the findings in this study.     

The Balance Between Coercion and Accommodation

1. Introduction
On the morning of April 1st, 2001, a U.S. EP-3 surveillance aircraft was conducting an intelligence flight along the Chinese territorial border in the airspace south-east of China＇s Hainan Island. Two Chinese fighter jets intercepted the spy plane and followed its flight, as is considered ordinary international practice. For reasons unknown, the EP-3 airplane made a sudden maneuver and crashed into one of the Chinese planes. The Chinese plane dropped into the sea, the pilot missing. The U.S. spy plane was also severely damaged. It intruded into Chinese territorial space and landed on Hainan Island without official permission from the Chinese side. After landing, the spy plane and 24 crew on board were detained by the Chinese authorities. This air collision episode was the first of its kind in the China-U.S. relations and an urgent diplomatic crisis ensued.     

Constitution of the Chinese Associa tion for Interna tiona l Understa nding(Approved by the Plenary Session of the Eleventh Executive Council on April 2, 2014)

正Chapter I General Rules Article 1 The Chinese Association for International Understanding is a national non-governmental organization(NGO)in the People’s Republic of China.Article 2 The official name of the Association is"Zhong Guo Guo Ji Jiao Liu Xie Hui"in Chinese,or"Jiao Liu Xie Hui"for short.Its English translation is"Chinese Association for International Understanding",and abbreviated as"CAFIU".     

Guide to Authors

正Published by China Institute of International Studies,China International Studies is China’s first English-language journal on diplomacy and international politics for formal circulation.The magazine mainly publishes the latest research achievements of Chinese scholars and specialists on China’s diplomacy,international politics and international relations under such columns as China’s Diplomacy,International Relations,International Politics,International Security,Regional Issues and World Economy.