盐酸氟桂利嗪胶囊人体相对生物利用度研究

目的:研究盐酸氟桂利嗪胶囊在正常人体内的药代动力学与相对生物利用度.方法:采用HPLC法测定18名健康男性志愿者随机自身交叉单剂量po20mg金花盐酸氟桂利嗪胶囊和杨森盐酸氟桂利嗪胶囊后的血药浓度,计算两者的药代动力学参数及相对生物利用度,并以AUC(0～24),Tmax,Cmax为指标,用方差分析、单双侧t检验及(1-2a)置信区间法分析金花胶囊与杨森胶囊的生物等效性.结果:金花与杨森盐酸氟桂利嗪胶囊的药-时曲线符合po吸收一房室模型.AUC(0～24)分别为(391.28±170.77)ng@h/L与(407.18±174.25)ng@h/L;Tmax分别为(2.89±0.44)h与(2.97±0.47)h;Cmax分别为(62.70±21.67)ng/ml与(56.15±15.71)ng/ml;统计学检验结果表明AUC(0～24),Tmax,Cmax均无显著性差异(P＞0.05).结论:金花盐酸氟桂利嗪胶囊对杨森盐酸氟桂利嗪胶囊的相对生物利用度为(96.10±14.07)%,金花与杨森两种盐酸氟桂利嗪胶囊具有生物等效性.     

HPLC法测定中国健康人血浆中依帕司他浓度及药动学研究

目的 建立血浆中依帕司他的HPLC测定方法，研究依帕司他胶囊在中国健康男性的药动学特性。方法 HPLC测定以地西泮作内标，测定20名健康志愿受试者口服50mg依帕司他胶囊后血药浓度-时间过程。用非房室模型参数估算法计算药动学参数。结果 方法回收率大于90％，日内、日间变异系数均低于5％，线性范围20．2～8080ng／ml(r=0．9996，n=5)，最低检测浓度2ng／ml，符合生物样品的分析要求。结论 本研究建立的HPLC测定方法专属性较好，血浆中杂质不干扰样品的测定，适合于依帕司他的临床药动学研究。     

盐酸氟桂利嗪治疗偏头痛32例疗效分析

目的：观察盐酸氟桂利嗪治疗偏头痛的疗效。方法：将64例偏头痛患者随机分为2组．对照组先口服罗通定60—90mg，30次/日，疼痛缓解后口服心得安10mg,3次／日；治疗组给盐酸氟桂利嗪5-10mg，1次／日，睡前口服．疗程12周。结果：治疗组与对照组的总有效率分别为81．25％和46．88％（P〈0．05）。结论：盐酸氟桂利嗪治疗偏头痛疗效佳。     

氟桂利嗪口服液的人体相对生物利用度研究

用高效液相色谱(HPLC)法测定氟桂利嗪血药浓度.Spherisorb-C18为固定相,流动相为甲醇∶醋酸缓冲液(8∶2,pH5.5),UV210nm检测,线性浓度范围5～10mg/ml,方法回收率80.4%～83.2%.应用该法研究了氟桂利嗪口服液的人体相对生物利用度为(109.4±6.8)%,结果表明,两种制剂的AUC、Tmax、Cmax之间无显著性差异.     

HPLC法测定大鼠组织中的桂利嗪

目的:建立大鼠组织中桂利嗪的HPLC测定法,用于小剂量尾静脉注射给药后测定桂利嗪在大鼠组织中分布.方法:组织样品加NaOH碱化,以甲基叔丁基醚提取,采用Hypersil C18 柱,甲醇-水- 冰醋酸-三乙胺(70:30:0.6:0.4)为流动相,254 nm波长处检测,测定了尾静脉给药2 mg/kg桂利嗪注射液后在SD大鼠心、肝、脾、肺、肾、胃、小肠、脑、脂肪、睾丸等10个组织脏器中的分布情况.结果:肝组织样品最低检测限0.02 μg/ml,线性范围0.05～2 μg/ml,小肠组织样品最低检测限0.02 μg /ml,线性范围0.05～1 μg/ml,符合生物样品分析要求.桂利嗪广泛地分布于大鼠的多个组织脏器中,其中肺部浓度最高.结论:本法简便、准确、灵敏,适合桂利嗪临床前药代动力学组织分布研究.     

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。     

盐酸氟桂利嗪在10名健康志愿者的药物动力学及相对生物利用度

目的：比较两种国产盐酸氟桂利嗪胶囊在人体内的药物动力学及相对生物利用度。方法：１０名男性健康志愿者随机交叉口单剂量１２ｍｇ盐酸氟桂利嗪胶囊后,用高效液相－紫外法测定血浆药物浓度。结果：血药浓度－时间曲线拟合表明该药体内过程符合有滞后时间的一级吸收,一清除动力学模型,胶囊Ａ和Ｂ的主要药代学参数：：Ｃｍａｘ（４３．７±６．２）ｍｇ．Ｌ＾－１和（４７．４±１３．８）ｍｇ．Ｌ＾－１,Ｔｍａｘ（３．０４±０     

盐酸氟桂利嗪经眼部给药后在大鼠脑内的递送

目的： 眼部给药是临床上常用的一种给药途径,但大多只用于治疗眼局部性疾病。基于眼部结构的特 殊性,本文主要探索盐酸氟桂利嗪经眼部给药治疗缺血性脑血管疾病的可行性。方法： 150 只健康雄性SD大鼠随机 分为滴眼组、灌胃组和注射组。滴眼组和灌胃组均以14 mg/kg 的剂量给药,注射组剂量为5 mg/kg。采用高效液相色 谱法(high performance liquid chromatography,HPLC)测定大鼠血浆和脑组织中的盐酸氟桂利嗪的含量,评价主要药代 动力学参数和生物利用度,并通过药物脑靶向指数(drug targeting index of brain,DTIbrain)研究盐酸氟桂利嗪眼部给药 的脑靶向性。结果： 盐酸氟桂利嗪经眼部给药后血浆Cmax和AUC0-t,脑组织Cmax和AUC0-t均高于经灌胃给药,差异有 统计学意义(均P<0.05)。经眼部给药血浆和脑组织的生物利用度分别为18.67%和34.67%,均高于经灌胃给药的 14.32%和21.56%。滴眼和灌胃两种给药途径的DTIbrain分别为1.84 和1.48。结论： 盐酸氟桂利嗪经眼部给药后能吸收 进入血液和脑组织,眼部给药的生物利用度和DTIbrain高于灌胃给药。     

血塞通联合氟桂利嗪治疗偏头痛的临床疗效观察

目的：观察血塞通联合氟桂利嗪治疗偏头痛的临床疗效。方法：将本院2011年4月-2013年2月收治的90例偏头痛患者随机分为观察组（n=45）和对照组（n=45）,观察组患者采用血塞通联合氟桂利嗪治疗,对照组患者采用氟桂利嗪治疗,分析两组患者的疗效。结果：观察组治疗总有效率为93．33％（42／45）、VAS评分（3．13±1．12）分、发作持续时间（3．37±0．49）h、发作频率（8．02±0．96）次,月;对照组则分别为75．56％（34／45）、（5．24±1．53）分、（6．34±0．58）h、（14．24±0．88）次,月。观察组上述指标均优于对照组,差异具有统计学意义（P〈0．05）。结论：血塞通联合氟桂利嗪治疗偏头痛疗效确切,具有协同加强作用,值得临床推广应用。     

盐酸氟桂利嗪添加治疗月经期癫痫的临床观察

目的研究盐酸氟桂利嗪小剂量添加治疗女性月经期癫痫的疗效。方法对18例月经期癫痫在原有抗癫痫药物基础上,添加盐酸氟桂利嗪5-10mg／d。观察添加治疗前后癫痫发作次数,及不良反应,判定疗效。结果添加盐酸氟桂利嗪6个月后,显效13例,有效5例;对各种发作类型都有效。结论盐酸氟桂利嗪小剂量添加治疗女性月经期癫痫,是一个可供选择的方法。     

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…