胆石症并胆道感染者胆汁与血细菌培养比较

目的探讨胆石症并胆道感染者胆汁与血细菌培养阳性率比较以及致病菌的耐药性分析。方法对该院收治的胆石症并胆道感染者在高热寒战时取静脉血以及ERCP术(或胆管探查术)时取胆汁进行致病菌的筛查以及耐药性分析。结果胆汁培养阳性率为55.3%(73/132),明显高于血培养的24.2%(32/132)(P0.05);肺炎克雷伯菌、大肠埃希菌、阴沟肠杆菌、铜绿假单胞菌、粪肠球菌、凝固酶阴性葡萄球菌为主要致病菌;革兰阴性杆菌对头孢哌酮/舒巴坦、亚胺培南、头孢他啶等具有较好敏感性,而对磺胺甲唑/甲氧苄啶、头孢唑林、氨苄西林等具有较高的耐药性;革兰阳性菌对氨苄新林/舒巴坦、青霉素G、红霉素、庆大霉素具有较高的耐药性,对万古霉素、呋喃妥因具有良好敏感性。结论胆石症并胆道感染者行胆汁培养其致病菌检出率较高,临床用药中应当针对相关致病菌的药敏结果进行指导用药。     

102例胆总管结石ERCP术中胆汁细菌培养结果分析

目的了解胆总管结石并胆道感染患者胆汁中主要致病菌的分布及其耐药情况。方法对本院2005年6月至2007年12月间收治的胆总管结石逆行内镜胰胆管造影术（ERCP）中抽取的胆汁标本进行细菌培养和药敏试验分布情况及耐药情况作回顾性分析。结果培养出109株细菌,革兰阴性杆菌86株（78．9％）,大肠埃希菌37株（33．94％）,肺炎克雷伯菌16株（14．68％）;革兰阳性球菌22株（20．18％）,其中肠球菌14株（14．84％）;真菌属1株0．92％）。结论胆道感染主要病原菌是大肠埃希氏菌、肠球菌和肺炎克雷伯菌;对胆道细菌敏感的药物有亚胺培南、万古霉素、左旋氧氟沙星、头孢哌酮／舒巴坦、头孢他啶、阿米卡星。     

头孢哌酮／舒巴坦治疗胆道感染的临床研究

目的：探讨头孢哌酮/舒巴坦治疗胆道感染的临床疗效。方法对160例确诊为胆道感染的住院患者采用头孢哌酮/舒巴坦进行治疗,并评定其细菌学疗效、临床疗效及不良反应。结果头孢哌酮/舒巴坦治疗胆道感染,平均退热时间为（3．08±1．82） d;有效率为86．76％（138/160）;细菌学上的清除率为85.72％（18/21）;患者均无不良反应发生。结论头孢哌酮/舒巴坦可有效治疗胆道感染,是首选药物之一。     

国产头孢哌酮舒巴坦钠与进口头孢哌酮舒巴坦钠治疗胆道感染的成本－效果分析

目的：评价国产头孢哌酮舒巴坦钠与进口头孢哌酮舒巴坦钠治疗胆道系统急性细菌性感染的有效性和安全性。方法选择急性胆道感染患者,随机分为国产头孢哌酮舒巴坦钠与进口头孢哌酮舒巴坦钠治疗组,比较两组成本、有效率及不良反应率。结果国产头孢哌酮舒巴坦钠与进口头孢哌酮舒巴坦钠相比,有效率的差异有统计学意义,但费用更低。结论两种头孢哌酮舒巴坦钠治疗胆道感染均可获得较佳的临床疗效,国产头孢哌酮舒巴坦钠比进口头孢哌酮舒巴坦钠有更好的成本－效果比,因此治疗胆道系统急性细菌性感染可根据患者病情、经济状况选择药物。     

237例急性细菌性结膜炎患者结膜囊分泌物标本的细菌培养结果及耐药性研究

目的:探究急性细菌性结膜炎患者结膜囊分泌物中致病菌群分布及其对不同抗菌药物的耐药性。方法:选取医院2017年10月-2019年4月间收治的急性细菌性结膜炎患者237例资料,统计其患者结膜囊分泌物细菌培养及药敏试验结果,分析其致病菌群的分布及主要致病菌对不同抗菌药物的耐药性。结果:237例患者结膜囊分泌物中分离出致病菌248株,其中革兰阳性菌203株(81.85%)、革兰阴性菌45株(18.15%);革兰阳性菌对头孢哌酮的耐药性较低,革兰阴性菌对氧氟沙星、庆大霉素的耐药性较低。结论:基于结膜囊分泌物细菌培养及药敏试验结果,明确急性细菌性结膜炎患者致病菌结构及耐药性,有助于为临床科学、合理用药;在充分考虑患者耐受程度、不良反应等前提下,可选择头孢哌酮作为临床经验用药。     

HPLC法测定头孢哌酮在胆汁中的药物浓度-时间的分布

目的 本文研究头孢哌酮在家犬胆汁中药物浓度-时间分布规律,为预防和治疗胆道感染用药提供参考和依据.方法 家犬麻醉后行胆囊造瘘术,留取空白胆汁,静脉推注头孢哌酮后在不同时间点采集胆汁标本.取空白胆汁加头孢哌酮对照品和流动相配成100～2 500 μg/ml不同浓度的系列胆汁样品.采用外标法行药物色谱峰面积定量,以胆汁样品药物浓度对色谱峰面积进行线性回归分析.注射头孢哌酮后的家犬胆汁样品经预处理后用高效液相色谱仪测定峰面积,按标准曲线回归方程计算得出胆汁药物浓度,从而了解头孢哌酮的胆汁药物浓度-时间分布情况.结果 采用流动相色谱条件下测定药物,胆汁杂质峰、头孢哌酮药物色谱峰分离效果良好(r=0.998 5).家犬静脉注射头孢哌酮在胆汁中浓度远远超过其对革兰氏阴性杆菌的最小抑菌浓度(MIC90),之后头孢哌酮的胆汁药物浓度随时间而缓慢降低.用药后3 h仍能检测到胆汁中的药物浓度,并且达药物治疗浓度.结论 头孢哌酮在胆汁中能达到较高的有效杀菌浓度,可作为预防和治疗胆道感染的较佳的药物.由于消除速度缓慢,临床用药应延长间隔时间.     

头孢美唑和头孢哌酮他唑巴坦预防胆道手术后感染的疗效评价

目的:比较头孢美唑与头孢哌酮他唑巴坦预防胆道手术后感染的疗效分析,并进行药物经济学分析,为临床合理用药提供依据。方法:回顾性分析比较头孢美唑与头孢哌酮他唑巴坦预防胆道手术后感染的疗效,运用药物经济学方法进行成本-效果分析。结果:头孢美唑与头孢哌酮他唑巴坦预防胆道手术后感染的总有效率分别为96.00%和95.70%,二者差异无统计学意义(P>0.05);治疗成本分别为483.2元和797.6元,差异有统计学意义(P<0.05)。结论:应用头孢美唑预防胆道手术后感染的疗效确切,可作为胆道手术预防用药;头孢美唑的成本-效果比优于头孢哌酮他唑巴坦,为较优的治疗方案。     

2009～2010年我院呼吸内科感染致病菌分布与抗菌药物使用情况分析

目的:了解我院呼吸内科患者住院期间感染致病菌的分布特点及耐药情况,为临床合理选择抗菌药物提供依据。方法:通过医院信息系统回顾性调取2009～2010年呼吸内科送检各类标本,分析其感染致病菌的分布特点及耐药情况,并结合呼吸内科抗菌药物的使用情况进行讨论。结果:两年内呼吸内科共检出感染致病菌651株,其中革兰阴性菌576株,占总菌数的88.48%,革兰阳性菌75株,占总菌数的11.52%。革兰阴性菌对头孢吡肟和头孢哌酮/舒巴坦的耐药率较低,为30%左右;其次是阿米卡星、亚胺培南和哌拉西林/他唑巴坦,为40%～50%;革兰阳性菌对万古霉素和替考拉宁高度敏感。两年间呼吸内科抗菌药物的使用主要以喹诺酮(左氧氟沙星和莫西沙星)、四代头孢(头孢吡肟)及内酰胺酶抑制剂类(头孢哌酮/舒巴坦)为主。结论:2009～2010年我院呼吸内科抗菌药物的使用基本符合感染致病菌的药敏结果,但抗菌药物的用量有明显的上升,需进一步规范用药。     

72例复发性尿路感染患者致病菌的分布及其对抗菌药物的耐药性分析

目的:分析复发性尿路感染患者致病菌的分布及其对抗菌药物的耐药性,为临床合理使用抗菌药物提供参考。方法:抽取2016年4月—2017年4月间诊治的复发性尿路感染患者72例资料,采用回顾性分析法,分析其致病菌的分布及其对抗菌药物的耐药性。结果:72例复发性尿路感染患者中,经尿液细菌培养结果示阳性者35例,其阳性率为48.61%;感染致病菌主要为大肠埃希菌,而大肠埃希菌对青霉烯类、头孢哌酮-舒巴坦、头孢呋辛、阿莫西林、哌拉西坦-他唑巴坦较为敏感。结论:根据尿液细菌培养和药敏试验结果,合理选用抗菌药物降低复发率。     

128株口腔感染致病菌的分布及其耐药性分析

目的:分析口腔感染患者致病菌的分布及其耐药性。方法:选取2014年4月—2016年8月间诊治的口腔感染患者86例,采用药敏分析仪和全自动细菌鉴定仪分析和检测所得的致病菌。结果:86例口腔感染患者中,有60.16%为革兰阳性球菌感染,有31.25%为革兰阴性菌染,有8.59%为真菌感染;比较发现真菌与革兰阴性菌的构成比显著低于革兰阳性球菌(P<0.05);头孢哌酮和氨苄西林对铜绿假单胞菌、大肠埃希菌和肺炎克雷伯菌具有一定的耐药性。结论:革兰阳性球菌是口腔感染患者的主要致病菌,其耐药性的特点也是各不相同的,根据药敏结果合理选用抗菌药物治疗。     

洛美沙星对大鼠血胰屏障通透性的研究

目的 :研究洛美沙星对大鼠血胰屏障的通透性。方法 :经尾静脉推注洛美沙星 (20mg/kg) ,在规定的时间点取样 ,用高效液相色谱法 (HPLC)测定胰腺、肝脏组织和血清中药物的含量。结果 :洛美沙星在大鼠体内过程符合二室模型 ;血清、胰腺、肝脏组织药物浓度在5min时最高 ,分别为65 551μg/ml、48 801μg/g、84 121μg/g ,然后持续下降 ;10min时胰组织的药物浓度已高于血清 ,480min胰组织中仍维持较高浓度 ;药物对血胰屏障的通透率 (PR)在5min时最低 (0 744) ,然后上升 ,480min时达到3 817。结论 :静脉推注洛美沙星后 ,药物对血胰屏障具有良好的通透性 ,值得向临床推荐用于预防和治疗胰腺感染     

Prophylactic administration of an antibiotic in neurosurgical operations--penetration of cefotiam into the cerebrospinal fluid

Various antibiotics are widely used for the purpose of protection against postoperative infections. Neurosurgeon must select the effective antibiotics to bacterium, that which penetrated enough to the intracranial organ through the blood-brain barrier. Eighteen cases with ventriculo-peritoneal shunt received intravenous drip infusion of cefotiam (CTM) and the concentration of CTM in blood and cerebrospinal fluid (CSF) was measured. The conclusion drawn from this study on penetration of CTM is summarized as follows: The concentration of CTM in CSF and its ratio to that of serum (CSF/serum %) showed the values of 0.543 microgram/ml (3.66%) in the group of 1 g CTM injection and 0.900 microgram/ml (4.02%) in the group of 2 g CTM injection, 2 hours after an intravenous administration. The concentration of CTM in CSF were gradually decreased in comparison with antibiotic levels in the blood. The most cases of 1 g or 2 g intravenous administration were able to get the sufficient concentration in the CSF, which exceeds MIC (minimal inhibitory concentration) against Gram-positive cocci and Gram-negative bacilli. As a result of penetration of CTM into cerebrospinal fluid, we recommend the intermittent intravenous injection of 2 g CTM for prophylaxis of postoperative infections.     

Penetration of cefotiam dihydrochloride into cerebrospinal fluid (author's transl)

It is well recognized that only very low concentration of antibiotics is obtained from cerebrospinal fluid (CSF) despite its high blood concentration. It has been attributed to the blood-brain and blood-CSF barriers. Penetration of CTM into CSF was studied in 7 patients. Two of them were complicated with septic meningitis, and others were not infected. CTM was administered intravenously and samples were obtained from both serum and CSF from 15 minutes to 4 hours for determination of concentration of the antibiotics. In 2 patients with meningitis, the peak level of CTM in CSF after intravenous injection of 2 g and 1 g of CTM was 197 mcg/ml (46% of peak serum concentration), and 17.3 mcg/ml (38% of peak serum level), respectively. In noninfected patients the peak level of CTM in CSF after intravenous injection of 1g of CTM was from 0.3 mcg/ml to 1.9 mcg/ml (0.84% approximately 3.64% of peak serum concentration). We conclude that the percent penetration of CTM into CSF increases in the presence of the inflamed meninges and that prophylactic dosage of CTM for postoperative meningitis will be intravenous administration of 2 g of CTM in adults.     

A study of cefoperazone levels in the cerebrospinal fluid of patients with hydrocephalus

Eleven neurosurgical patients without intracranial infection were given 4 g cefoperazone (CPZ) intravenously for 30 minutes. Ventricular drainage was performed in 10 cases, and 1 case with cisternal drainage. Eight of 11 cases showed moderate to severe ventricular dilatation. Serum and ventricular cerebrospinal fluid (CSF) concentrations of CPZ were measured for 8 hours after injection. Average peak serum concentration of CPZ was 476 micrograms/ml and the half-life was 150 minutes. Patients with obstructive hydrocephalus showed relative good penetration of CPZ in CSF (2.74 approximately 5.29 micrograms/ml). Especially, those who had severe dilatation of ventricles demonstrated sequential increased concentration (5.48 approximately 6.25 micrograms/ml at 8 hours). In poor risk patient and intracerebral hemorrhage with ventricular hemorrhage cases, who had normal range of CSF cell counts and protein, CPZ level was low, less than 2 micrograms/ml. In cases with severe subarachnoid hemorrhage, sufficient concentration (11 micrograms/ml) of CPZ was observed in cisternal CSF. The CPZ concentrations in CSF after 4 g administration did not seem to exceed comparing to 2 g dosing.     

阿洛西林在狗的药物动力学参数的反相高效液相色谱法测定

本文用反相高效液相法测定犬静注和肌注阿洛西林20mg/kg后的血中药物浓度,并据此计算有关药物动力学参数。ODS-C_(18)为固定相,甲醇/67mmol/L磷酸缓冲液(1:1,vol/vo1)为流动相,紫外(uv)检测。以对硝基丙酰苯胺为内标物对血清中阿洛西林进行定量测定。根据F值,r 2/1值和AIC(Akaike's Information Criterion)值判断静注和肌注药物后在体内的转运过程分别符合开放型二室和一室模型。静注后即刻血药浓度为218±13μg/mL,T_(1/2α)为0.13h。肌注后T_(max)和T_(1/2ka)分别为0.75和0.24h,C_(max)为16±6μg/mL,但im后AUC仅为iv相同剂量后的38％。该药iv和im后的T_(1/2)分别为1.5和1.7h,V_d分别为0.35和0.43L/kg。本实验结果与微生物法测定结果间无显著差异。     

Transportation of cefotiam from serum to cerebrospinal fluid (author's transl)

Cefotiam (1 g) was administered by one-shot intravenous injection to the patients proceeding a brain surgery. The cerebrospinal fluid (CSF) and serum were taken as a specimen, and the concentration CTM was assayed by agar-well method using Proteus mirabilis ATCC 21100. The most high concentration of CTM was 2,273 micrograms/ml in serum, and 2.3 micrograms/ml in CSF, respectively. The concentration of CTM in serum, CSF, and CSF/serum ration were determined at the indicated time. It appears likely that CTM can pass into CSF more easily than other cephalosporins.     

Concentration of ethambutol in cerebrospinal fluid in man as a function of the non-protein-bound drug fraction in serum

Summary Using a chemical assay method, which had been confirmed by chromatography, the concentration of ethambutol in CSF and serum was determined in 13 patients. Ethambutol entered the CSF, even at low serum concentrations. For serum levels greater than 1 µg/ml, a linear correlation was found between the serum and CSF concentrations. In order to reach therapeutic levels in CSF (more than 1 µg/ml) the serum concentration should be at least 2 µg/ml, corresponding to a daily dose of about 20–30 mg/kg. The serum protein binding of ethambutol varied from 39.3% at a serum level of 0.61 µg/ml, to 8.3% at a serum level of 4.82 µg/ml.     

Comparative kinetics of oxiracetam in serum and CSF of patients with dementia of Alzheimer type

The purpose of the study was to determine whether oxiracetam crosses the human blood-brain barrier and to evaluate its comparative kinetics in serum and in cerebro-spinal fluid (CSF). Six DAT patients, undergoing CSF collection for diagnostic purposes, received 2 g oxiracetam daily, by a 60 min i.v. infusion, for 7 days. On the last day, in four patients blood samples were collected at time 0, 30, 60 and 120 min, and lumbar drainage was performed at the end of infusion: at this time mean CSF concentration was 3.5 micrograms/ml, i.e. 4.0% of the serum one, demonstrating that oxiracetam crosses the blood-brain barrier. In two patients, blood samples were collected at time 0, 60, 120 and 240 min, and lumbar drainage was performed 60 min after the end of infusion: at this time mean CSF concentration was 2.8 micrograms/ml, i.e. 5.3% of the serum one, indicating a persistence of oxiracetam within this deep compartment. These results provide the first evidence in humans that oxiracetam penetrates the central nervous system and contribute to the understanding of its long-lasting pharmacodynamic effect in man.     

Investigation of the high partition of YM992, a novel antidepressant,in rat brain - in vitro and in vivo evidence for the high binding in brain and the high permeability at the BBB

Brain extracellular fluid (ECF) concentration of YM992, a novel antidepressant, was determined using brain microdialysis to investigate the high partition of this drug to the brain after systemic administration to rats. Plasma, cerebrospinal fluid (CSF), ECF and brain concentrations were determined at the steady-state after intravenous infusion to rats. The concentration ratio of brain to plasma at the total concentration base was 71.3, while those of ECF to plasma and CSF to plasma at the free concentration base were comparable. The distribution volume in brain was 375 ml/g brain and in vitro binding of YM992 to rat brain was 98.1-98.5%, suggesting a high binding in the brain. The carotid artery injection study showed that the brain uptake index of YM992 was 141%, furthermore, the uptake clearance into brain after i.v. dosing to rats was 0.6 ml/min/g brain, indicating a high permeability at the blood-brain barrier (BBB). These findings suggest that the high partition of YM992 to rat brain is attributed to its high level of binding in the brain as well as its high permeability at the BBB.     

黄芩透过人胎盘屏障体外模型药物成分研究

目的研究黄芩透过人胎盘屏障药物成分。方法用尤斯灌流室技术建立人胎盘屏障体外模型,预平衡30 min后,于母体池加入10 mg·mL-1黄芩溶液,分别于5~240 min内在胎儿池取样,用高效液相色谱技术分析样品中所含药物成分。色谱柱:Agilent Zorbax-C18(4.6 mm×250 mm,5μm),流动相为乙腈-0.1%甲酸水(梯度洗脱),内标为葛根素,流速为1.0 mL·min^-1,检测波长为278 nm,柱温20℃,进样量为5μL。结果从5 min开始,黄芩苷、汉黄芩苷、汉黄芩素即可透过人胎盘屏障;黄芩素和千层纸素A从20 min开始才透过胎盘屏障;30 min后检测到的11种药物成分均可透过胎盘屏障,且在后续取样时间点未见新的物质生成。结论黄芩中的5种黄酮类成分(黄芩苷、汉黄芩苷、黄芩素、汉黄芩素和千层纸素A)均可透过人胎盘屏障体外模型。