不同给药方式下恩诺沙星在鲤体内的药动学研究

对两组鲤分别进行腹腔注射、口灌恩诺沙星后,应用高效液相色谱法测定了其组织中的药物浓度,研究了恩诺沙星在鲤(Cyprinus carpio)体内的吸收、分布与消除等药代动力学参数.结果表明:两种给药方式下,鲤血浆、肝脏、肾脏和肌肉组织的药时曲线符合一级消除二室模型.腹腔注射给药血浆动力学参数:AUC为59.185 6 μg·h·mL-1、Ka为75.762 7 h-1、t1/2β为96.545 6 h、T(peak)为0.073 0 h、C(max)为3.297 0 μg·mL-1;灌服给药血浆动力学参数:AUC为600.296 1 μg·h·mL-1、Ka为0.169 3 h-1、t1/2β为168.287 1 h、T(peak)为3.665 5 h、C(max)为3.266 1 μg·mL-1.这说明腹腔注射给药比口灌给药吸收快,血药达峰时间短,达峰浓度高.     

诺氟沙星在淡水青虾体内药物代谢动力学研究

在(26±1)℃的水温条件下,青虾一次性肌肉注射25mg/kg诺氟沙星后,用反相高效液相色谱法测定青虾血淋巴和肌肉组织中诺氟沙星含量。青虾血淋巴药一时曲线和肌肉药一时曲线均可以用二室开放模型来描述,诺氟沙星在青虾血淋巴液中的主要药动学参数为:分布相半衰期t1/2α为1.66h,消除相半衰期t1/2β为1.69h,达峰时间T(Peak)为1.82h,峰浓度C(max)为6.0081μg/mL,曲下面积AUC为30.75μg·mL-1·h-1,吸收相半衰期t1/2ka为1.66h。肌肉中的主要药动学参数为:分布相半衰期t1/2α为0.08h,消除相半衰期t1/2β为4.42h,达峰时间T(Peak)为0.03h,峰浓度C(max)为16.72μg/mL,曲下面积AUC为12.34μg·mL-1·h-1,吸收相半衰期t1/2ka为0.08h。结果表明青虾肌注诺氟沙星后,能比较迅速的被吸收,并且在组织中维持较高的药物浓度。     

水温对培氟沙星在鲤体内的药动学及残留的影响研究

为研究不同水温对培氟沙星在鲤体内药代动力学特征和残留消除规律的影响,以期对培氟沙星药物残留进行有效监控,选取18和25℃水温条件下,按体质量10mg/kg的剂量对鲤单次混饲口灌给药后,于不同时间点采集组织样品经超高效液相色谱法测定培氟沙星含量.结果显示:高温组的达峰时间(2h)早于低温组(4h),达峰浓度(2.360mg/L)高于低温组(2.092mg/L);高温组和低温组的表观分布容积Vd、总体清除率CL与温度呈正相关,分别为5.73L/kg、0.191L·h-1·kg-1和5.464L/kg、0.17L·h-1·kg-1;药时曲线下总面积AUC与消除半衰期t1/2 z与水温呈负相关,分别为66.278mg·L-1·h-1、20.317h和88.346mg·L-1·h-1、22.301h;肌肉、肝胰脏、肾脏组织中培氟沙星的药物含量于给药后2h时高温组较低温组分别提高了8.9%、15.6%和17.4%.研究结果表明,水温变化对鲤体内药物的吸收、分布、代谢和消除均有显著影响.     

畜禽用复方微量元素注射液中铜元素在猪体内的药物动力学研究

目的:明确畜禽用复方微量元素注射液中铜元素在猪体内的药物动力学参数.方法:猪单剂量肌注畜禽用复方微量元素注射液0.3 mL/kg(铜210 μg/kg),24 h不同时间10次前腔静脉采血,火焰原子吸收法(AAS)测定猪血清中铜元素的浓度,采用3P97软件对数据进行分析.结果:铜在猪体内的药动学过程均符合开放型一室模型,最佳药时曲线方程为C=1.213 0 e-0.145 5t-1.213 0 e-0.885 9t.其主要药动学参数为:吸收半衰期(T1/2Ka)=0.744 1±0.213 4 h,消除半衰期(T1/2Kel) =5.097 1±1.385 9 h,达峰时间(Tm)=2.352 0±0.439 h,达峰浓度(Cm)=0.706 9±0.068 8 μg/mL,曲线下面积(AUC) =7.108 0±1.114 7μg·h/mL.结论:肌肉注射畜禽用复方微量元素注射液后,元素铜在猪体内吸收较快,消除也相对较快.     

益脑康片人参皂苷Rb1药动学及生物利用度研究

考察复方片剂中人参皂苷Rb1体内药动学特征及相对生物利用度,以获得药动学参数为临床疗效提供参考依据.方法:两组大鼠分别灌服益脑康片剂混悬液及三七西洋参提取物(灌胃剂量均相当给予人参皂苷Rb190 mg/kg)后,于不同时间采集血样,用高效液相色谱仪测定血药质量浓度,通过3p97药动学软件自动拟合数据获得药动学参数.大鼠灌胃给予益脑康片剂粉末(试验制剂)及三七和西洋参提取物(参比制剂)后,人参皂苷Rb1药动学行为均符合一室模型,试验制剂药动学参数为Ka=22.217 4 h-1、t1/2Ka=0.031 1 h、Ke=0.144 5 h-1、t1/2Ke=4.7979 h、AUC=666.1752(μg/mL).h;参比制剂药动学参数为Ka=5.428 9 h-1、t1/2Ka=0.1276 h、Ke=0.134 8 h-1、t1/2Ke=5.1413 h、AUC=622.526 0(μg/mL).h.由药动学参数求得益脑康片人参皂苷Rb1的相对生物利用度为107%.实验结果表明益脑康片剂中人参皂苷Rb1在体内的分布较快而代谢排除的速度较慢.人参皂苷Rb1相对生物利用度很高,预示可有较好的疗效.     

抗风湿涂膜剂的体内药物动力学研究

考察抗风湿涂膜剂中辣椒素和乌头类总生物碱在生物体内药动学特征,以获得药动学参数为临床应用提供参考依据.方法为给家兔背部按一定面积涂抹抗风湿涂膜剂后,于不同时间采取血样.分别用高效液相色谱仪和紫外可见分光光度计测定血药质量浓度,通过3P97药动学软件对所得的数据自动拟合获得药动学参数,得辣椒素药动学行为符合一室模型,主要药动学参数为Ka=1.160 013h-1t、1/2(Ka)=0.597 534 h、Ke=0.219 206 2 h-1t、1/2(Ke)=3.162 079 h、AUC=22.084 286(μg/mL)h;乌头类总生物碱药动学行为符合一室模型,主要药动学参数为Ka=0.300 004 9 h-1t、1/2(Ka)=2.310 453 h、Ke=0.185 421t、1/2(Ke)=3.738 234 h、AUC=22.389984(μg/mL).h.药代动力学实验表明,本制剂中辣椒素在动物体内吸收分布速率较快,而代谢消除速率较慢;而乌头类总生物碱吸收与代谢均较慢.二者吸收程度均较好.     

复方氨酚右敏溶液在健康人体的药代动力学研究

研究复方氨酚右敏溶液在健康人体的药代动力学.12名健康受试者以自身为对照采用随机交叉给药方式,单次空腹口服3个剂量复方氨酚右敏溶液(低、中、高3个剂量分别为7.5、15、30 mL,每mL含对乙酰氨基酚32 mg、马来酸右氯苯那敏0.1 mg).用液相色谱-串联质谱法(LC-MS/MS)测定血浆中对乙酰氨基酚和马来酸右氯苯那敏的浓度,计算2种药物的药代动力学参数,评价其药代动力学特征.对乙酰氨基酚在人体内的动力学过程符合二室模型,低、中、高3个剂量主要药代动力学参数消除半衰期t1/2分别为(2.93±0.47)、(3.08±0.43)、(3.01±0.49) h,血药质量浓度时间曲线下面积AUC0～t分别为(12.29±3.91)、(27.80±7.64)、(60.41±17.24) μg·h·mL-1;右氯苯那敏在人体内的动力学过程符合一室模型,低、中、高3个剂量主要药代动力学t1/2分别为(20.49±7.86)、(19.66±5.05)、(19.96±6.48) h;AUC0～t分别为(32.61±13.65)、(67.58±23.31)、(158.12±56.44) ng·h·mL-1.对乙酰氨基酚和右氯苯那敏药动学参数ρmax、AUC0～t、AUC0～∞均与给药剂量呈线性相关(P<0.001),复方氨酚右敏溶液在7.5～30 mL剂量范围内呈线性人体药代动力学特征.     

药饵投喂下诺氟沙星在凡纳滨对虾主要组织中的分布及消除规律研究

将诺氟沙星原药(98%)按质量比为1:1 000制成颗粒饵料投喂凡纳滨对虾,研究在养殖模式下诺氟沙星在凡纳滨对虾各组织中的分布及消除规律。采用高效液相色谱法结合药代动力学分析软件3P97分析诺氟沙星在凡纳滨对虾体内的药物回收率、动力学参数、药时曲线等参数。结果表明,诺氟沙星血药浓度时间曲线符合吸收二室模型,动力学方程分别为:C血淋巴=9.236 e-0.662 t+56.938 e-0.01 t-66.174 e-0.985 t,C肌肉=21.491 e-0.576 t+0.328 e-0.047 t-21.819 e-0.726 t,C肝胰腺=30 115.96 e-0.355 t+39.314 e-0.01 t-30 155.274 e-0.378 t。血淋巴、肌肉、肝胰腺中诺氟沙星达峰时间Tmax分别为1 h、4 h和4 h,峰浓度值Cmax分别为13.527 5 mg/L、1.904 4 mg/L和698.916 7 mg/L,表观分布容积V1/F分别为0.017 L/kg、0.210 L/kg和0.001 L/kg,吸收半衰期T1/2Ka分别为0.704 h、0.954 h和1.832 h,分布半衰期T1/2α分别为1.047 h、1.204 h和1.951 h,消除半衰期T1/2β分别为69.315 h、14.812 h和69.315 h,中央室向周边室转运的一级速率常数K12分别为4.347 h-1、0.098 h-1和0.098 h-1,周边室向中央室转运的一级速率常数K21分别为0.629 h-1、0.081 h-1和0.017 h-1,药时曲线下面积AUC分别为6.764 mg·h-1·L-1、9.538 mg·h-1·L-1和7013.467 mg·h-1·L-1。血淋巴、肌肉、肝胰腺组织中诺氟沙星浓度水平的结果表明,诺氟沙星在凡纳滨对虾3种组织中浓度最高的为肝胰腺;肌肉和血淋巴中诺氟沙星代谢较快,在投喂8 h后药物残留接近于零,但肝胰腺组织易蓄积诺氟沙星,其残留时间至16 d才未被检测到。实验实施期间为9月份,平均水温为28℃,因此,使用质量比为1:1 000制成颗粒饵料投喂凡纳滨对虾至少应经过448℃.d后才能消除。     

IDO抑制剂PCC0208009在结肠癌CT26荷瘤小鼠的PK/PD研究

通过研究吲哚胺2,3-双加氧酶(IDO)抑制剂PCC0208009在结肠癌CT26荷瘤小鼠中的药代动力学(PK)和药效动力学(PD)特点,为后续IDO抑制剂的开发和临床治疗效果的预测提供参考依据.研究采用结肠癌CT26荷瘤小鼠,以Kyn/Trp为药效评价指标,考察IDO抑制剂PCC0208009在小鼠体内的药代动力学(PK)与药效动力学(PD)特点及相关性.单次灌胃给予200 mg/kg PCC0208009,药物在血浆中的T_(max)、T_(1/2)、平均C_(max)和AUC_(0-last)分别为0.25 h、6.22 h、13.3μg/mL和22.9 h·μg/mL,在肿瘤中分别为0.5h、7.08 h、13.3μg/mL和17.5 h·μg/g;PCC0208009在给药后2～8 h内可有效抑制血浆和肿瘤中Kyn/Trp.单次或多次灌胃给予25-400 mg/kg PCC0208009 4 h时,PCC0208009在血浆和肿瘤中的药物浓度以及对Kyn/Trp的抑制作用均呈剂量依赖性.结果表明,PCC0208009在给药后2～8 h内能有效抑制荷瘤小鼠血浆和肿瘤的IDO活性,在血浆和肿瘤中的药物浓度及对IDO的抑制作用均呈剂量依赖性,PK和PD间具有较好的相关性.     

山茱萸总甙滴眼液眼内药代动力学及药效学的实验研究

目的 :研制出山茱萸总甙 (COG)滴眼液 ,对该滴眼液的药代动力学进行研究 ,并观察其局部应用对角膜移植免疫排斥反应的影响。方法 :用高效液相色谱法对该滴眼液的药代动力学参数进行研究。建立封闭群大鼠角膜移植模型 ,随机分为 4组 :A组为空白对照组 ,B、C、D组分别为使用质量分数 0 5 %、1%和 2 %COG滴眼液组。用裂隙灯显微镜记录及比较各组角膜排斥反应发生时间。结果 :COG滴眼液在新西兰白兔眼内为一室模型 ,主要药代动力学参数为 :A =4 316 μg/mL ,Ke=2 0 5 6h- 1,Ka=2 5 79h- 1,LagTime =0 198h ,t1/ 2 ,Ka=0 0 2 3h ,t1/ 2 ,Ke=0 2 5 7h ,Tmax=0 986h ,ρmax=1 2 94 μg/mL ,AUC =1 6 0 1μg·h/mL ,其拟合的动力学方程为 ρ(t) =10 6 0 5×Dose×(e- 2 0 56× (t- 0 198) -e- 2 579× (t- 0 198) )。术后各组发生角膜移植排斥时间 ,A组与B、C、D组、B组与C、D组、C组与D组间两两比较均有显著性差异 (P <0 0 1)。其中作用最强的为C组。结论 :COG滴眼液能有效地防治角膜移植免疫排斥反应。COG滴眼液眼内有效峰浓度出现在点药后 0 986h ,4h基本被代谢清除     

Markedness and its Interpretation in Language Use

Language markedness is a common phenomenon in languages, and is reflected from hearing, vision and sense, i.e. the variation in the three aspects such as phonology, morphology and semantics. This paper focuses on the interpretation of markedness in language use following the three perspectives, i.e. pragmatic interpretation, psychological interpretation and cognitive interpretation, with an aim to define the function of markedness.     

Characterization of Ordovician carbonate reservoirs, southeastern Saskatchewan, Canada

The discovery of the prolific Ordovician Red River reservoirs in 1995 in southeastern Saskatchewan was the catalyst for extensive exploration activity which resulted in the discovery of more than 15 new Red River pools. The best yields of Red River production to date have been from dolomite reservoirs. Understanding the processes of dolomitization is, therefore, crucial for the prediction of the connectivity, spatial distribution and heterogeneity of dolomite reservoirs.The Red River reservoirs in the Midale area consist of 3～4 thin dolomitized zones, with a total thickness of about 20 m, which occur at the top of the Yeoman Formation. Two types of replacement dolomite were recognized in the Red River reservoir: dolomitized burrow infills and dolomitized host matrix. The spatial distribution of dolomite suggests that burrowing organisms played an important role in facilitating the fluid flow in the backfilled sediments. This resulted in penecontemporaneous dolomitization of burrow infills by normal seawater. The dolomite in the host matrix is interpreted as having occurred at shallow burial by evaporitic seawater during precipitation of Lake Almar anhydrite that immediately overlies the Yeoman Formation. However, the low δ18O values of dolomited burrow infills (-5.9‰～ -7.8‰, PDB) and matrix dolomites (-6.6‰～ -8.1‰, avg. -7.4‰ PDB) compared to the estimated values for the late Ordovician marine dolomite could be attributed to modification and alteration of dolomite at higher temperatures during deeper burial, which could also be responsible for its 87Sr/86Sr ratios (0.7084～0.7088) that are higher than suggested for the late Ordovician seawaters (0.7078～0.7080). The trace amounts of saddle dolomite cement in the Red River carbonates are probably related to "cannibalization" of earlier replacement dolomite during the chemical compaction.     

Features of Women's language

Language is a means of verbal communication. People use language to communicate with each other. In the society, no two speakers are exactly alike in the way of speaking. Some differences are due to age, gender, statue and personality. Above all, gender is one of the obvious reasons. The writer of this paper tries to describe the features of women＇s language from these perspectives： pronunciation, intonation, diction, subjects, grammar and discourse. From the discussion of the features of women＇s language, more attention should be paid to language use in social context. What＇s more, the linguistic phenomena in a speaking community can be understood more thoroughly.     

A computer generator for randomly layered structures

AcomputergeneratorforrandomlylayeredstructuresYUJia shun1,2,HEZhen hua2(1.TheInstituteofGeologicalandNuclearSciences,NewZealand;2.StateKeyLaboratoryofOilandGasReservoirGeologyandExploitation,ChengduUniversityofTechnology,China)Abstract:Analgorithmisintrod…     

低渗透非均质砂岩油藏启动压力梯度研究

理论推导与室内实验相结合,建立了低渗透非均质砂岩油藏启动压力梯度确定方法。首先借助油藏流场与电场相似的原理,推导了非均质砂岩油藏启动压力梯度计算公式。其次基于稳定流实验方法,建立了非均质砂岩油藏启动压力梯度测试方法。结果表明:低渗透非均质砂岩油藏的启动压力梯度确定遵循两个等效原则。平面非均质油藏的启动压力梯度等于各级渗透率段的启动压力梯度关于长度的加权平均;纵向非均质油藏的启动压力梯度等于各渗透率层的启动压力梯度关于渗透率与渗流面积乘积的加权平均。研究成果可用于有效指导低渗透非均质砂岩油藏的合理井距确定,促进该类油藏的高效开发。     

On Tragic Consciousness In The Works By Ernest Hemingway

As an American modern novelist who were famous in the literary world, Hemingway was not a person who always followed the trend but a sharp observer. At the same time, he was a tragedy maestro, he paid great attention on existence, fate and end-result. The dramatis personae's tragedy of his works was an extreme limit by all means tragedy on the meaning of fearless challenge that failed. The beauty of tragedy was not produced on the destruction of life, but now this kind of value was in the impact activity. They performed for the reader about the tragedy on challenging for the limit and the death.     

An Index mechanism for multi-scale view in spatial databases

There are numerous geometric objects stored in the spatial databases. An importance function in a spatial database is that users can browse the geometric objects as a map efficiently. Thus the spatial database should display the geometric objects users concern about swiftly onto the display window. This process includes two operations:retrieve data from database and then draw them onto screen. Accordingly, to improve the efficiency, we should try to reduce time of both retrieving object and displaying them. The former can be achieved with the aid of spatial index such as R-tree, the latter require to simplify the objects. Simplification means that objects are shown with sufficient but not with unnecessary detail which depend on the scale of browse. So the major problem is how to retrieve data at different detail level efficiently. This paper introduces the implementation of a multi-scale index in the spatial database SISP (Spatial Information Shared Platform) which is generalized from R-tree. The difference between the generalization and the R-tree lies on two facets: One is that every node and geometric object in the generalization is assigned with a importance value which denote the importance of them, and every vertex in the objects are assigned with a importance value,too. The importance value can be use to decide which data should be retrieve from disk in a query. The other difference is that geometric objects in the generalization are divided into one or more sub-blocks, and vertexes are total ordered by their importance value. With the help of the generalized R-tree, one can easily retrieve data at different detail levels.Some experiments are performed on real-life data to evaluate the performance of solutions that separately use normal spatial index and multi-scale spatial index. The results show that the solution using multi-scale index in SISP is satisfying.     

海南岛地体及其毗邻陆缘晚中生代—新生代古地磁研究和构造演化

本文叙述了对海南岛及其毗邻大陆边缘白垩纪到第四纪地层岩石进行古地磁研究的全部工作过程。通过分析岩石中剩余磁矢量的磁偏角及磁倾角的变化,提出海南岛白垩纪以来经历的构造演化模式如下:早期伴随顺时针旋转而向南迁移,后期伴随逆时针转动并向北运移。联系该地区及邻区的地质、地球物理资料,对海南岛上述的构造地体运动提出以下认识:北部湾内早期有一拉张作用,主要是该作用使湾内地壳显著伸长减薄,形成北部湾盆地。从而导致了海南岛的早期构造运动,而海南岛后期的构造运动则主要是受南海海底扩张的影响。海南地体运动规律的阐明对于了解北部湾油气盆地的形成演化有重要的理论和实际意义。     

Jane Eyre——A Feminist In The 19th Century

In the 19th century the society was controlled by men, and women were just appendants of them, they had not any rights and freedom. But Jane was an exception, she showed some characteristics of early feminist. Jane showed her characteristics of feminism in three aspects: rebellion, equality, and independence. These characteristics were helpful to her success, and feminism is the only way out for women of that time.     

《Chinese Science Bulletin》SUBJECT INDEX TO VOLUME 59(2014)

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