国产卡莫氟在犬体内的药代动力学及片剂绝对生物利用度研究

按随机交叉实验设计法,对5尺犬口服和静脉注射卡莫氟(10mg/kg)的药代动力学及绝对生物利用度进行了研究,应用反相高效波相色谱法测定血清药物浓度。结果表明静注给药的药时曲线符合二室开放规型,T1/2α=1.67min,T1/2β=34.55min,Vc=0.2525L/kg,C1=0.3205L/kg/h,AuCiv=498.44μg·min/m;口服卡莫氟片的药时曲线符合一室开放模型,T1/2a=12.min,T1/2e=38.51minTmax=28.46min,Cmax=2.09μg/m1,AuCpo=407.90μg.min/m1;由AuCiv和AuCpo算得绝对生物利用度F=82.14％。     

右美托咪啶对老年手术患者血清S-100β蛋白、NSE浓度的影响

［摘要］目的　评价右美托咪啶对老年手术患者血清S-100β蛋白、NSE浓度的影响．方法 选择髋关节置换术老年患者100例,ASA分级Ⅱ或Ⅲ级,性别不限,年龄65~75岁,体重指数＜25 kg/m2．采用随机数字表法,将患者分为2组（n＝50）:生理盐水对照组（C组）和右美托咪啶组（D组）．D组麻醉诱导前经15 min静脉注射右美托咪啶0.5 μg/kg,随后以0.4 μg/（kg·h）的速率静脉输注至术毕前30 min,C组给予等容量生理盐水．5 min后静脉注射舒芬太尼0.4 μg/kg、丙泊酚1～2 mg/kg、罗库溴铵0.6 mg/kg麻醉诱导,气管插管后行机械通气．靶控吸入七氟醚呼气末靶浓度1 %~3 %、静脉输注舒芬太尼0.2 μg/（kg·h）维持麻醉,术中维持BIS值40～60．于麻醉诱导前（T0）、术毕（T1）、术后12 h（T2）时采集颈内静脉血样,采用ELISA法测定血清S-100β蛋白和NSE浓度．术毕待拔除气管导管后送术后监护病房．采用ICU谵妄评估法对患者进行谵妄评测,记录术后24 h内谵妄的发生情况．结果　与T0时比较,2组T1~2时血清S-100β蛋白、NSE浓度升高;与C组比较,D组丙泊酚和七氟醚用量减少、T1~2时血清S-100β蛋白和NSE浓度降低、术后24 h内谵妄的发生率降低（P＜0.05）．结论　右美托咪啶可降低血清S-100β蛋白、NSE的浓度,降低老年患者术后谵妄的发生,提示其有脑保护效应．     

重度创伤后急性期体内锌含量及其抗氧化功能的实验研究

目的:研究重度创伤时机体锌含量及其相关抗氧化功能的影响,及其引发的急性锌缺乏与多器官功能衰竭和死亡 率的关系。方法:建立兔轻伤(ISS=13)和重伤(ISS=22)模型,检测伤前及伤后12h,60h,6d,9d,14d,28d血清及肝Zn 含量、Cu／Zn-SOD活性及肝MT含量。结果:轻伤后1d-6d血Zn值17.23 umol/L±1.48 umol／L,与伤前23.8 umol／L±15.08umol/L 比较下降显著,P<0.05。重伤后1d-28d血Zn含量下降明显。其中1d-14d为7.87 umol／L±2.92 umol／L,P<0.01,28d为12.14 umol／L ±9.46umol／L,P<0.05。重伤组中死亡率为35％,死亡动物血Zn水平比未死动物伤后1d下降显著,P<0.05。重伤组肝Zn含量 伤后上升,血清Cu／Zn-SOD活性持续两周高于伤前,P<0.05,肝Cu／Zn-SOD及MT水平均呈先升后降趋势。结论:重伤后体内 存在急性TE缺乏及其引发的一系列失代偿性功能代谢变化,可能为重度创伤合并院内感染或多器官衰竭,甚至死亡的重要因素 之一。     

高效液相色普法测定兔灌胃后血清中百草枯浓度及其变化特征

目的 探索建立高效液相色谱法（HPLC）在测定兔血清中百草枯浓度的可行性,并观察不同剂量 百草枯灌胃后兔血清浓度的经时变化情况。方法 12 只家兔按照随机数字表法分为两组,每组6 只,分别灌胃 给予100 mg/kg（高剂量组）和20 mg/kg（低剂量组）百草枯,于给药后1、2、5、12、24、48 及72 h 采集血 清,血清用乙腈直接沉淀蛋白处理后进行高效液相测定。色谱柱条件：流动相为0.1 mol/L 磷酸缓冲液（含 12.5 mmol/L 庚烷磺酸钠）- 乙腈（90 ︰ 10,TFA 调pH=2.8）,流速为1.0 ml/min,检测波长为258 nm,柱温为 30℃。结果 所建立的方法在0.2 ～ 100.0 mg/L 浓度范围内线性关系良好（r =0.999）。相对回收率在97.82% ～ 101.20% 之间,绝对回收率在84.37% ～ 88.80% 之间,日内和日间精密度（RSD）<5%。百草枯血药浓度时间 曲线为单峰,无论是高剂量组还是低剂量组,给药2 h 后其血清浓度达到峰值,之后逐渐下降,其中,高剂量组于 给药后72 h 后检测不出百草枯,低剂量组于药后24 h 检测不出百草枯。重复测量设计的方差分析结果显示, 不同时间点间、不同剂量组间的百草枯浓度及高、低剂量组随时间变化趋势差异有统计学意义。结论 所建 立的HPLC 方法可用于测定兔血清百草枯浓度,不同剂量百草枯兔灌胃后其血清浓度和蓄积的时间与剂量有 关,给药2 h 后血药浓度达峰值。     

帕瑞昔布钠镇痛对老年急诊股骨头置换术患者神经系统的影响

目的 探讨帕瑞昔布钠围手术期镇痛对老年急症股骨头置换术患者血清神经元特异性烯醇化酶(NSE)、S-100β蛋白浓度与术后谵妄(POD)、术后认知功能障碍(POCD)发生率的影响.方法 经医院伦理学委员会同意并与患者家属签订知情同意书,选择2011年1月至2012年5月在青岛市市立医院与海慈医疗集团骨科腰麻-硬膜外联合麻醉下急诊股骨头置换术患者80例,年龄＞70岁,随机数字法分为2组(n=40):吗啡组(C组)及帕瑞昔布钠组(P组).P组采用帕瑞昔布钠20 mg或40 mg(体质量50 kg为依据)静脉注射镇痛,每12h1次,连续6次;C组首次静脉注射吗啡2 mg或4 mg作为对照.2组均额外每次追加吗啡2 mg使患者疼痛视觉模拟评分达3分以下.主要观察指标:(1)2组术后住院时间,吗啡追加量;(2)2组POD的发生率与术后3 d(T1)、1周(T2)、3个月(T3)及6个月(T4)患者POCD的发生率;(3)2组各随机抽取20例于采取镇痛措施前(t0)、麻醉前(t1)、术毕(t2)、术后6 h(t3)、24 h(t4)及48 h(t5)检测血清神经元特异性烯醇化酶(NSE)、S-100β蛋白浓度;(4)其他严重并发症.结果 与C组相比较,P组吗啡追加量及术后住院时间降低[(7.9±2.6) mg比(31.3±3.9)mg,(11.4±1.5)d比(12.3±1.6)d,均P＜0.05];P组POD及T1～T4 POCD发生率降低(22.5％比45％,17.5％、12.5％、7.5％、2.5％比37.5％、32.5％、25％、17.5％,均P ＜0.05);P组血清NSE浓度在t2 ～t5时降低[(7.1±2.7) μg/L、(9.5±3.6)μg/L、(8.4±3.6) μg/L、(7.2±2.8)μg/L比(9.4±4.1)μg/L、(13.6±5.0) μg/L、(11.1±3.7) μg/L、(9.4±3.3) μg/L,均P＜0.05],血清S-100β蛋白浓度在t1～t5时降低[(0.61 ±0.27) μg/L、(0.99±0.38) μg/L、(0.73±0.25) μg/L、(0.65±0.28) μg/L、(0.87±0.32) μg/L比(0.83±0.36) μg/L、(1.48±0.57) μg/L、(0.98 ±0.37)μg/L、(0.88±0.29) μg/L、(1.12 ±0.45) μg/L,均P＜0.05],其他时间点2组比较差异无统计学意义(P＞0.05);2组均无严重并发症发生.结论 帕瑞昔布钠围手术期镇痛减轻中枢神经系统损伤,改善老年患者术后认知功能,利于患者康复.     

导数光谱法对兔体内安眠酮药物的药动学研究

利用一阶导数紫外分光光度法测定兔体内安眠酮血药浓度,在0.1～0.5μg/ml浓度范围内,239nm附近的峰-谷间半振幅与浓度呈线性关系,H=0.003621+0.07990C,r=0.9997。回收率为83.4％±1.9～97.0％±1.5(加入量为5.00～0.50μg/ml)。4只家兔一次口服安眠酮30mg/kg,测定安眠酮血药浓度,得到血药浓度——时间曲线呈二室模型。药动学参数为a=1.01h-1,β=0.22h-1;Ka=2.16h-1;K12=0.201h-1;K21=0.721h-1;Kel=0.301h-1;t1/g(a)=0.686h;t1/2(β)=3.13h;tp=1.07h;Cmax=16.44μg/ml;AUC=81.25h·mg/L。     

~(125)碘放射免疫分析法对人体内苯妥英钠(DPH)药代动力学的研究

本文用~(125)碘-苯妥英钠放免(PEG)分析法,研究6位志愿者服DPH(片)300mg的药代动学显示,5位志愿者DPH血浓度经时变化较规律,“AKAIKE”判别值显示两种药动学模型,主要参数值分别为,开放一室T_1/2kd=30.7053±31.9156(h),Vd=0.2471±0.02569(L/kg)。Cl=0.1112 0.009549(L/kg·h),AUC·~∞=791.7059±631.253(μg·h/ml);开放二室T_1/2β=27.9154±0.9312(h),Vd=0.2967±0.0084(L/kg),Cl=0.007373±0.O005(L/kg·h,AUC·~∞ =695.5453±213.773(μg·h/ml)。DPH唾药浓度经时变化不规律,与DPH血浓度相关不显著(P>0.05),用于药动学研究意义不大。     

硫酸依替米星的药代动力学及临床疗效观察

目的:了解硫酸依替米星的药代动力学及临床疗效。方法:采用微生物法测定10例肺部感染患者静脉滴注200mg硫酸依替米星血中药物浓度,并进行药代动力学研究。结果:该药在肺部感染患者体内最高血药浓度为14.74μg/ml,12h仍维持在0.29μg/ml。经PKBP-N_1药代动力学程序拟合符合二室开放动力学模型,其参数为T_(1/2)α=0.257h,T_(1/2)β=2.22h,Ve=34.32L,K_(21)=2.14h~(-1),K_(12)=0.48h~(-1),K_(10)=0.39h~(-1)。10例患者经一个疗程治疗后,临床有效率100.0％,细菌阴转率94.2％,清除率89.8％。不良反应发生率10.0％。结论:硫酸依替米星在不同年龄、不同疾病患者体内的吸收分布、代谢、排泄存在明显差异,治疗中应进行血药浓度的监测以防不良反应的发生。该药对呼吸道感染疗效较佳。     

搏动灌注和非搏动灌注对肾功能的影响

目的研究体外循环（CPB）时应用搏动灌注（PP）和非搏动灌注（NPP）对患者术后肾功能的影响。方法拟行CPB的患者60例,采用随机、双盲的方法分为搏动灌注组（PP组）和非搏动灌注组（NPP组）,每组30例。PP组在人工心肺机泵后串联双搏动式心肺辅助装置,在主动脉阻断期间采用搏动灌注。NPP组全程均采用非搏动灌注。两组灌流量控制在2.3～2.8 L/（min .m2）。分别于术前（T1）、CPB后4 h（T2）、12 h（T3）、24 h（T4）、48 h（T5）抽取外周静脉血及留取新鲜尿液,测定血清肌酐（Scr）、血清尿素氮（BUN）、血清β2-微球蛋白（β2-MG）和尿β2-MG浓度。结果两组患者一般资料差异无统计学意义。与T1比较,两组血清Scr、BUN浓度在T4～T5明显升高（P〈0.01）;血清β2-MG、尿β2-MG浓度在T2～T5明显升高（P〈0.05）。与NPP组比较,PP组血清Scr、BUN浓度在T4～T5明显降低（P〈0.05）;血清β2-MG、尿β2-MG浓度在T2～T5明显降低（P〈0.05）。结论 PP能有效地减轻CPB后肾脏损伤,降低肾功能损害的程度。     

右美托咪定和丙泊酚对先天性心脏病患儿体外循环后脑保护作用的对比

目的 比较右美托咪定和丙泊酚对先天性心脏病患儿体外循环(CPB)后血清中星形胶质细胞S100β蛋白(S1 00 β)及神经元特异性烯醇化酶(NSE)的浓度的影响.方法 选择择期体外循环下行先天性心脏病患儿45例,年龄1～～2岁之间,采用随机数字表法,分成3组:丙泊酚组(B1)、右美托咪定组(B2)和对照组(C),麻醉诱导后B1组给予丙泊酚8 mg/(kg·h)静脉持续泵入至术毕;B2组给予右美托咪定0.4μg/(kg·h)(1 5min内),随后以0.1μg/(kg·h)匀速泵入至术毕;C组采用与B1组相同给药方式静脉持续泵入等体积生理盐水.3组术中均持续泵入维库溴胺60.0～100.0μg/(kg·h)、舒芬太尼2.0μg/(kg·h),持续吸入七氟烷1％～3％,分别于手术开始前(T1)、CPB结束(T2)、CPB结束后6 h(T3)、12 h(T4)、24 h(T5)检测血液中S-100 β蛋白和NSE的浓度.结果 T1时,3组患儿血清中的S100β蛋白及神经元特异性烯醇化酶(NSE)的浓度差异无统计学意义.T2、T3、T4点时,B1、B2组血清中S100 β和NSE的浓度均低于C组,差异具有统计学意义(P＜0.05);B2与B1组相比,B2组血清中S100 β和NSE浓度上升幅度较低,差异具有统计学意义(P＜0.05).各组患儿围术期血压、心率等血流动力学指标差异无统计学意义.结论 右美托咪定和丙泊酚均可降低CPB下先天性心脏病患儿血清中IL-1 β及S100蛋白的浓度,具有一定的脑保护作用,且右美托咪定的脑保护作用较丙泊酚强.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Dr.Zhang Ren''''s Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

Luo Lingjie''''s Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.     

Survey and practice of reporting quality of randomized controlled clinical trials on traditional Chinese medicine

Evidence obtained from randomized controlled trials （RCTs） has been generally accepted as the gold standard in the evaluation of clinical effectiveness. Readers need to understand the trial design, implementation, results, analysis and interpretation, so as to fully Jnderstand the results of RCTs. Thus, the investigators of RCTs have to report these items in a complete, accurate and clear manner. Since 1998, we have conducted several evaluations on the reporting quality of RCTs published in Chinese journals on traditional Chinese medicine （TCM） and results have shown that there is an urgent need for higher quality RCTs on TCM.     

TCM Treatment of Ankylosing Spondylitis by Tonifying the Kidney and Strengthening the Governor Vessel

Ankylosing spondylitis is a chronic and progressive disorder with inflammation mainly involving the central axis joints. It mainly affects the cervical spine and the lumbosacral area, with the pathogenesis closely related to the kidney and the Governor Vessel (GV). TCM holds that the syndrome is deficiency in origin and excess in superficiality, which is due to insufficiency of the kidney, deficiency of GV, and blocking of the channels with the invasion of exogenous evil, leading to poor circulation of qi and blood and malnutrition of the bones, muscles and joints. The TCM method of tonifying the kidney and strengthening GV to regulate circulation of qi and blood and check the arthralgia pain should be adopted, with the Kidney-Tonifying and GV Strengthening Decoction (益肾强督汤) prescribed.     

IMPROVING P-gp EXPRESSION IN HUMAN MONONUCLEAR CELLS IN VITRO TRANSFECTED BY MULTIDRUG RESISTANCE-1 mRNA

CHEMOTHERAPY playsa greatrolein the treat- ment of malignanttumors,especiallyingynecolo- gicalones.But inanticancerchemotherapy,leuko-cytopeniaisfrequentlytheprimarydose-limitingsideeffect factor.Moreover,cancersarefrequentlychemoresistantbe-causeof overexpressionof P-glycoprotein(P-gp), which isencodedby multidrugresistancegene (MDR1 ) and detectableinup to50% ofhuman cancersand renderscellsresistancetoanticancerdrugs.The safetyand potentialtherapeuticbenefitof mdr1 gene transferredto h…