板蓝根总生物碱中表告依春在发热大鼠体内的药动学-药效学结合模型研究

目的应用药动学与药效学结合模型,研究板蓝根总生物碱中主要成分表告依春在酵母致热大鼠体内的药动学和药效学之间的关系。方法给大鼠ig板蓝根总生物碱,不同时间取血并对体温进行观察,采用高效液相法测定血浆中表告依春的浓度,用一房室模型计算药动学参数,采用3种药动学与药效学拟合模型,分别对药效学参数进行拟合。结果表告依春在正常大鼠和发热大鼠体内的主要药动学参数t1/2、Cmax、AUC分别为:(4.94±0.84)h、(4.01±0.21)μg/mL、(28.37±2.42)μg.h/mL和(5.71±0.91)h、(4.15±0.25)μg/mL、(30.35±2.58)μg.h/mL。药理效应与效应室浓度之间的关系用间接反应中的药效产生抑制模型拟合较好,相应的药效学参数分别为Kin为(0.70±0.10)h-1,Kout为(0.54±0.12)h-1,R0为1.33±0.16,IC50为(0.94±0.66)mg/L。结论板蓝根总生物碱中表告依春在正常大鼠和发热大鼠体内的药动学行为无明显差异,表告依春在发热大鼠体内药动学与药效学间符合间接反应中的药效产生抑制模型。     

非参数药效模型法分析硫酸镁血药浓度与降血压效应的关系

硫酸镁治疗妊娠诱发高血压孕妇的药动学与药效学的关系，一般用参数法描述，需用假设药效学模型。本文在不假设药效学模型的前提下，分析硫酸镁浓度与降血压效应的关系。由非参数法分析和得出的Ｋｅｏ＝０．３５±０．３３ｈ－１与参数法拟合而得的Ｋｅｏ相接近。另外，非参数法拟合结果对选择药效模型和Ｋｅｏ初值具有独特的作用     

中药复方及单味药材中淫羊藿苷的大鼠体内药动学分析

目的：利用反相高效液相色谱法,分别比较复方与单味药材提取物中淫羊藿苷在大鼠体内的药代动力学（药动学）参数差别,探讨配伍对药效成分体内过程的影响。方法：实验大鼠分别灌胃复方及单味药材提取物后。测定不同时间点血浆中淫羊藿苷的浓度,采用药动学程序3P97对数据进行统计学处理,进行药动学模型拟合并计算相关药代动办学参数。结果：复方及单味药材中淫羊藿苷在大鼠体内分别呈二室和一室模型,主要药代动力学参数为：复方组Cmax=（3．133±0．290）μg／ml,t1/2（Ka）=（0．753±0．809）h,Tmax=（2．089±0．144）h,AUC0-24=（30．839±3．680）μg·h／ml。单味药材组Cmax=（2.318±0．218）μg／ml,Tmax=（1．497±0．521）h,AUC0-24=（19．947±2．555）μg·h／ml。结论：与单味药材相比,复方中淫羊藿苷在大鼠体内吸收增加、消除及达峰时间延长、血浆清除率减少。因此复方配伍对淫羊藿苷体内过程有显著影响。     

UPLC／MS／MS法研究拉西地平片的人体药动学

目的：建立血浆中拉西地平浓度的测定方法并应用于人体药动学研究。方法：采用ACQUITY UPLC^TM超高效液相色谱仪测定血药浓度,色谱条件：Acquity UPLC^TM BEH C18（50mm×2．1mm,1．7μm）色谱柱;流动相为乙腈-30mmol／L醋酸铵（82：18,v／v）;流速为0．28mL／min,质谱条件：Quattro Premier串联质谱检测器,离子源：EsI;极性（检出模式）,计算拉西地平药动学参数。结果：拉西地平在血药浓度范围为0．025～10．000μg／L内线性关系良好（r=0．9978）;定量下限为0．025μg／L,日内、日间误差〈10％。用此方法测定了12例志愿者口服拉西地平4mg后的血药浓度,主要药动学参数为：AUC0-24为（9．449±5．864）ng／h·mL^-1,AUC0-∞为（10．618±6．485）ng／h·mL^-1,Cax为（2．358±2．024）ng／mL,tmax为（1．59±0．40）h,t1／2为（8．49±2．29）h。药动学参数个体间差异大。结论：所建立的方法灵敏可靠,适合拉西地平体内药动学研究;拉西地平体内药动学参数个体差异大,应个体化给药。     

家兔多剂量口服溴吡斯的明缓释片的药动学和生物利用度评价

目的 以溴吡斯的明普通片为对照,通过多剂量口服给药后,评价溴吡斯的明缓释片的药动学和生物利用。方法 6只新西兰兔随机分成2组,采用自身交叉对照实验,多剂量口服溴吡斯的明缓释制片或普通片后,采用高效液相色谱法测定血浆中溴吡斯的明浓度,计算药动学参数和相对生物利用度。 结果 溴吡斯的明普通片与缓释片给药后,药动学参数如下：tmax分别为（2.00 ± 0）h和（4.00 ± 0）h; Cmax 分别为（25.477 ± 0.177）mg•L-1和（19.236 ± 0.446）mg•L-1;AUC0-∞分别为（321.424 ± 4.955）mg•h•L-1和（370.083 ± 12.229）mg•h•L-1;与普通片相比,缓释片的相对生物利用度为119.15%。结论 溴吡斯的明缓释片具有缓释动力学特征,与普通片生物等效。     

不同剂量泮托拉唑对CYP2C19PMs消化性溃疡个体药动学和药效的影响

目的：研究不同剂量泮托拉唑治疗细胞色素氧化酶P4502C19（CYP2C19）弱代谢型（poormetabolisersPMs）消化性溃疡（pepticulcerPU）个体药动学和药效的影响。方法：聚合酶链限制性片断长度多态性（PCR—RFLP）分析确定CYP2C19PMs个体,高效液相色谱法测定药动学参数,电子胃镜复查观察疗效。结果：弱代谢型占受试者20％。CYP2C19PMsPU个体20mg组与40mg组主要药动学参数如下：AUC（5900．43±1046．92）和（5316．40士1437．00）9tg·h·L^-1;CL（3．67±1．79）和（8．09±1．93）mL·h^-1;Cmax（1133．01±248．12）和（1242．08±160．71）ug·L^-1;TI,2（2．74±0．48）和（2．82±0．81）／h,组间无显著性差异（P〉0．05）。胃镜复查治疗效果20mg组与40mg组治愈率、愈合率、有效率分别为37．5％、37．5％、25％和50％、50％、25％,组问无显著性差异（P〉0．05）。结论：CYP2C19PMs个体口服PAN20mg／d即可获得预期治疗效果;CYP2C19基因分型可为泮托拉唑治疗消化性溃疡的个体化方案提供依据。     

肾移植患者应用更昔洛韦后环孢菌素A的药动学及临床生化？…

对１０例肾移植患者应用与未用更昔洛韦后环孢菌素Ａ的药协学参数及临床生化指标进行研究。采用荧光偏振免疫法测定血药浓度,３Ｐ８７程序拟合药劝学参数。结果显示：应用更昔洛韦后,环孢菌素Ａ药动学参数Ｋｅ、ｔ１／２（Ｋａ）分别由未用组的（０．１６±０．０４）ｈ＾－１和（１．３９±０．７６）ｈ降至（０．０９±０．０５）ｈ＾－１和（０．５０±０．３２）ｈ,Ｔｍａｘ由（３．６７±０．７７）ｈ减至（２．００±０．７     

大鼠静脉注射康莱特注射液的药动学研究

目的：研究康莱特注射液在正常大鼠体内的药动学。方法：采用甘油三酯试剂盒检测康莱特注射液经尾iv后大鼠血清中外源性甘油三酯的浓度变化,外源性甘油三酯浓度为测定血样中甘油三酯扣除本底后的浓度,采用3P97药代软件计算药动学参数。C_max为实测值,AUC计算采用梯形法。结果：康莱特注射液10、5 mL/kg剂量的主要药动学参数：C_max分别为（8.532±1.031）、（5.418±0.764）mmol/L,AUC_0-t分别为（13.248±3.692）、（5.339±1.219）mmol/L?h,V_c分别为（1.030±0.131）、（0.756±0.150）L²/（kg·mol）,CL_s分别为（0.838±0.319）、（0.975±0.330）L²/（kg·mol·h）,t _1/2α 分别为（0.481±0.168）、（0.322±0.109）h,t _1/2β分别为（1.452±0.776）、（1.384±0.404）h。结论：康莱特注射液经尾iv给药后在大鼠体内的药动学过程经拟合为二室模型。     

头孢氨苄缓释片在健康人体内的生物利用度和药物动力学

目的:比较头孢氨苄缓释片和普通胶囊的生物利用度和药物动力学。方法：10例健康志愿者分别单剂量口服500mg头孢氨苄缓释片和普通胶囊，血药浓度测定方法为HPLC法。结果：两种剂型体内过程均符合一室开放模型，缓释片的达峰时间（Tmax）为（2．58±0．59）h，峰浓度（Cmax）为（10．08±1．68）μg／ml．吸收速率常数（Ka）为（0．90±0．53）／h，消除速率常数（Ke）为（0.26±0.02）／g，半衰期（T1／2）为（2.67±0.23）h，清除率（Cl）为（6.93±1.71）L／h，分布容积（Vd）为（26.66±6.72）L，药一时曲线下面积（AUC）为（48.31±9.32）μg·h／ml。两种剂型T一C一Ka、Ke、T1／2和Cl均存在显著性差异（P＜0．01），Vd、AUC无显著性差异（P＞0．05）；缓释片的相对生物利用度为（104．90±8．35）％。结论：缓释片的吸收减慢，Tmax推迟，T1／2延长，可减少服药次数，提高药物治疗的顺应性。     

头孢克罗在健康人体内的药动学研究

建立了高效液相色谱法并测定10名男性健康志愿者血浆中的头孢克罗浓度。结果表明：该方法简便、快速、精密度高、灵敏度好，血浆平均回收率为（102．18±4．01）％，平均日间及日内差均＜6％，最低检测限为0．05μg／ml。数据经3P87程序处理，血药浓度-时间曲线符合-室模型，其药动学参数为Ka＝2．76h-1，Ke＝1．22h-1，T1／2＝0．66h，Tmax＝0．52h及Cmax＝14．63μg／ml。     

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…