氢氯噻嗪对替米沙坦蛋白结合率影响的研究

目的 测定氢氯噻嗪对替米沙坦的蛋白结合串的影响。方法 采用超滤法结合高效液相法测出游离药物浓度，比较未加及加入氢氯噻嗪后的替米沙坦的蛋白结合率。结果 未加及加入氯噻嗪后的替米沙坦的蛋白结合率分别为93．8％和94．1％。结论氢氯噻嗪对替米沙坦的蛋白结合率基本无影响。     

氢氯噻嗪对替米沙坦蛋白结合率影响的研究

目的　测定氢氯噻嗪对替米沙坦的蛋白结合率的影响。方法　采用超滤法结合高效液相法测出游离药物浓度 ,比较未加及加入氢氯噻嗪后的替米沙坦的蛋白结合率。结果　未加及加入氢氯噻嗪后的替米沙坦的蛋白结合率分别为93 8%和 94 1%。结论　氢氯噻嗪对替米沙坦的蛋白结合率基本无影响。     

阿莫西林对格列美脲血浆蛋白结合率的影响

目的 研究阿莫西林对格列美脲蛋白结合率的影响。方法 采用平衡透析法结合高效液相色谱法，比较未加和加入阿莫西林后格列美脲的血浆蛋白结合率。结果 4种浓度下，单用格列美脲时的血浆蛋白结合率分别为94.2％、92.8％、91．4％、91．0％；与阿莫西林合用时，格列美脲的血浆蛋白结合率依次变为90．9％、89．0％、89．6％、90．0％。结论 与阿莫西林合用后，格列美脲的血浆蛋白结合率下降。     

格列齐特对氯沙坦钾血浆蛋白结合率的影响

目的 研究格列齐特对氯沙坦钾血浆蛋白结合率的影响。方法 采用平衡透析法并结合HPLC,测定未加和加入格列齐特后氯沙坦钾的人血浆蛋白结合率。结果 3种浓度下,未加格列齐特时氯沙坦钾的血浆蛋白结合率分别为97.4%,97.8%,98.2%,与格列齐特合用时,氯沙坦钾的血浆蛋白结合率依次为94.1%,94.8%,94.9%。结论 氯沙坦钾与格列齐特合用后,血浆蛋白结合率显著下降(P<0.01)。     

头孢噻肟钠与甲硝唑注射液配伍的稳定性研究

目的：研究在常温条件下头孢噻肟钠与甲硝唑注射液配伍的稳定性。方法：取头孢噻肟钠加适量注射用水溶解，加入甲硝唑注射液中，在常温条件下观察配伍液的外观变化，用双波长分光光度法测定配伍后不同时间两组分的浓度，同时测定配伍液的pH值及不溶性微粒变化。结果：二配伍液常温放置6h内，溶液澄明度、pH值、含量没有明显变化，微粒符合规定。结论：头孢噻肟钠与甲硝唑注射液配伍6h内是稳定的。     

超滤法结合液质联用法测定姜黄素大鼠血浆蛋白结合率

目的建立液相色谱串联质谱（LC-MS）测定方法并检测姜黄素的大鼠血浆蛋白结合率。方法建立LC-MS检测方法,结合超滤法测定姜黄素的血浆蛋白结合率。结果3种浓度（100、300和1000ng·mL^-1）姜黄素与大鼠血浆蛋白结合率分别为（80．3±5．28）％、（75．3±4．45）％和（62．64—1．98）％。结论姜黄素血浆蛋白结合率较高,LC—MS可用于姜黄素血浆蛋白结合率的测定。     

头孢噻肟钠和甲硝唑静滴混合液的稳定性

本文研究了头孢噻肟钠和甲硝唑的静滴混合液在8℃时的稳定性。取市售注射用头孢噻肟钠1g用生理盐水溶解稀释至5ml,加入甲硝唑注射(500mg/100ml)中,从中取2ml用水稀释至100ml,取1ml稀释液至试管中,共取30份,于8℃冷藏保存。在混合液制备后的1、2、4、8、12、24、26、48和72h,取出试管置冷冻的自动取样器中,用HPLC法分析其中头孢噻肟钠和甲硝唑含量的稳定性。     

超滤法测定药物血浆蛋白结合率的影响因素

目的:考察超滤法测定药物血浆蛋白结合率的影响因素.方法:采用紫外分光光度法测定在不同条件下用超滤法分离的游离药物浓度.结果:随超滤时间延长结合率略增;而超滤时所受压力增加结合率降低;不同型号的超滤膜对测定结果影响不同.结论:采用超滤法测定血浆蛋白结合率时,选择25＃-82膜,1200r/min,离心60min.作为超滤实验条件为宜.     

硫酸依替米星治疗急性细菌性感染63例

目的：观察硫酸依替米星与头孢噻肟钠在治疗急性细菌性感染的临床疗效及安全性。方法：将122例急性细菌性感染患,分A、B两组、A组用硫酸依替米星注射液治疗,B缄用头孢噻肟钠注液治疗,记录患症状,体征、辅助检查的变化。结果：A组有效率为76．2％,治率为92．1％,B组有效率为79．65,治愈率为91．5％,不良反应分别为A组6．3％,B组5．1％,结论：硫酸依替米星注射液和头孢噻肟钠注液对各部位的感染均有较好的临床疗效,安全性高。     

两种三联疗法治疗幽门螺旋杆菌感染临床分析

目的：探讨根除小儿幽门螺旋杆菌（HP）感染的最佳疗法,观察盐酸克拉霉素三联疗法与甲硝唑三联疗法的效果。方法：选择我院HP阳性的消化性溃疡患儿90例,随机分成盐酸克拉霉素三联组45例,甲硝唑三联组45例,三联治疗2周,疗程结束后4周复查胃镜。观察HP根除率、溃疡愈合率。结果：消化性溃疡患儿盐酸克拉霉素组与甲硝唑组HP根除率分别N95．56％（43／45）和91．11％（41／45）．两组比较差异无显著性,溃疡愈合率盐酸克拉霉素组与甲硝唑组分别为97．78％（44／45）和82．22％（37／45）,两组比较差异有显著性。结论：治疗小儿消化性溃疡,根除HP感染两种方案效果类似,但盐酸克拉霉素组对溃疡愈合优于甲硝唑组。     

Stability of cefotaxime sodium and metronidazole in an i.v. admixture at 8 degrees C

The stability of cefotaxime and metronidazole in i.v. admixture at 8 degrees C was studied. The commercially available injectable formulation of cefotaxime sodium 1 g was diluted to 5 mL with 0.9% sodium chloride injection and added to metronidazole injection 500 mg/100 mL. A 2-mL sample was removed and diluted to 100 mL with water. Thirty 1-mL portions were transferred to glass vials and refrigerated at 8 degrees C. At 0, 1, 2, 4, 8, 12, 24, 36, 48, and 72 hours after the admixture was prepared, the vials were removed, placed in a refrigerated autosampler, and assayed for cefotaxime and metronidazole concentrations by stability-indicating high-performance liquid chromatography. Over the 72-hour study period, the concentration of cefotaxime remaining at all assay times was 95.91-101.13% of the initial concentration. The concentration of metronidazole remaining at each assay time was 93.08-102.19% of the initial concentration. Cefotaxime sodium 10 mg/mL and metronidazole 5 mg/mL were stable for 72 hours at 8 degrees C in an i.v. admixture prepared from commercially available injectable formulations.     

剖宫产围手术期预防性应用抗生素的临床分析

目的　探讨择期剖宫产围手术期预防性应用抗生素用药时间、剂量与术后感染的关系。方法　回顾性分析 6 5例择期剖宫产手术病人 ,根据预防性用药方法不同分为 3组 :A组 (围手术期用药组 ) 2 1例 ,选用甲硝唑与头孢噻肟钠 ,于手术前 30min内单次静脉冲击给药 ,术中冲洗宫腔、子宫切口及腹腔留置 ;B组 (手术期及术后用药组 ) 2 4例 ,术中甲硝唑冲洗宫腔、子宫切口及腹腔留置 ,术后头孢噻肟钠用药 3d ;C组 (传统术后用药组 )2 0例 ,术后头孢噻肟钠 +甲硝唑全身用药 5d。结果　术后最高体温、退热时间 3组间差异有统计学意义 (P <0 0 5 ) ;术后病率、腹部伤口感染、子宫内膜炎 3组间差异无统计学意义 (P >0 .0 5 ) ;术后副反应中白细胞计数、胃肠道反应及药物性皮疹 3组间差异无统计学意义 (P >0 .0 5 )。结论　择期剖宫产围手术期预防性使用抗生素安全、有效 ,且剂量小、疗程短 ,优于术后用药。     

Disposition of ceftriaxone in rat: application of a pharmacokinetic-protein binding model and comparison with cefotaxime

1. The pharmacokinetic profile and protein binding parameters of ceftriaxone were determined in rat, and compared with those of cefotaxime. 2. Plasma concentration-time curves of ceftriaxone and cefotaxime (single i.v. bolus; 100 mg/kg each) were described by a two-compartment, protein-binding model. 3. The corrected VTss (ml/kg) of ceftriaxone was lower than that of cefotaxime. The AUCs of both drugs were similar. The t1/2 beta of the two drugs differed significantly, being 29 min for ceftriaxone and 17 min for cefotaxime. 4. In vivo protein binding constants of both drugs were similar, but the concentrations of protein binding sites differed significantly. The average free fractions in plasma (Fp) of ceftriaxone and cefotaxime were 0.22 and 0.48 respectively. 5. Saturation of the binding site for cefotaxime was estimated to occur at about 30 micrograms/ml in plasma, whereas saturation for ceftriaxone was seen at lower concentrations.     

防治小儿急性阑尾炎术后感染的3种治疗方案的药物经济学评价

目的 :运用药物经济学评价防治小儿急性阑尾炎术后感染的3种治疗方案。方法 :选择119例患急性阑尾炎并行阑尾切除术的患儿 ,根据阑尾病理切片结果将其分为Ⅰ组和Ⅱ组 ,分别给予A、B、C3种不同的治疗方案。A方案 :头孢唑啉钠 +青霉素G +甲硝唑 ;B方案 :头孢噻肟钠 +青霉素G +甲硝唑 ;C方案 :头孢唑啉钠 +青霉素G +甲硝唑 +凯福隆。对3种方案进行回顾性分析评价。结果 :对于Ⅰ组患儿 ,A、B方案为优选治疗方案 ;对于Ⅱ组患儿 ,A方案为较佳治疗方案。结论 :应用药物经济学可优化治疗方案 ,指导合理用药     

防治小儿急性阑尾炎术后感染的3种治疗方案的药物经济学评价

目的运用药物经济学评价防治小儿急性阑尾炎术后感染的3种治疗方案.方法选择119例患急性阑尾炎并行阑尾切除术的患儿,根据阑尾病理切片结果将其分为Ⅰ组和Ⅱ组,分别给予A、B、C3种不同的治疗方案.A方案头孢唑啉钠+青霉素G+甲硝唑B方案头孢噻肟钠+青霉素G+甲硝唑;C方案头孢唑啉钠+青霉素G+甲硝唑+凯福隆.对3种方案进行回顾性分析评价结果对于Ⅰ组惠儿,A、B方案为优选治疗方案;对于Ⅱ组患儿,A方案为较佳治疗方案.结论应用药物经济学可优化治疗方案,指导合理用药.     

美罗培南治疗腹腔内感染的临床有效性及安全性评价Δ

目的:系统评价美罗培南治疗腹腔内感染的临床有效性及安全性。方法:根据纳入及排除标准,计算机检索Medline、Cochrane图书馆、PubMed、Embase、中国期刊全文数据库(CNKI)、中文科技期刊全文数据库(VIP)和中华医学会数字化期刊(Wanfang),纳入美罗培南治疗腹腔内感染的随机对照试验(RCT)。根据Cochrane手册对纳入的RCT进行治疗评价,并通过RevMan 5.2软件进行Meta分析。结果:本研究共纳入19个RCT,纳入的总样本量为2 486例。Meta分析结果显示,美罗培南的临床有效率优于亚胺培南/西司他丁[RR=1.01,95%CI(0.98,1.04),P=0.61],低于头孢噻肟与甲硝唑联用[RR=0.95,95%CI(0.90,0.99),P=0.01];美罗培南的厌氧菌清除率优于头孢噻肟与甲硝唑联用[RR=1.02,95%CI(0.89,1.17),P=0.78];美罗培南的大肠埃希菌清除率低于亚胺培南/西司他丁[RR=0.96,95%CI(0.88,1.05),P=0.39],优于头孢噻肟与甲硝唑联用[RR=1.04,95%CI(0.83,1.31),P=0.73]以及妥布霉素与克林霉素联用[RR=1.09,95%CI(1.02,1.17),P=0.01];美罗培南的安全性优于亚胺培南/西司他丁[RR=0.89,95%CI(0.69,1.15),P=0.37]及头孢噻肟与甲硝唑联用[RR=0.63,95%CI(0.40,0.97),P=0.04]。除美罗培南临床有效率低于头孢噻肟与甲硝唑联用、大肠埃希菌清除率优于妥布霉素与克林霉素联用、安全性优于头孢噻肟与甲硝唑联用的结果差异有统计学意义(P<0.05)以外,其余结果差异均无统计学意义(P>0.05)。结论:在治疗腹腔感染时,美罗培南的临床有效率和安全性与亚胺培南/西司他丁相当;而美罗培南的临床有效率比头孢噻肟与甲硝唑联用低,但安全性更高。     

Comparison of the Pharmacodynamic Activity of Cefotaxime plus Metronidazole With Cefoxitin and Ampicillin plus Sulbactam

Study Objective . To compare the pharmacokinetic and pharmacodynamic activity of three drug regimens: cefotaxime plus metronidazole, cefoxitin, and ampicillin-sulbactam against two organisms frequently isolated in intraabdominal infection, Escherichia coli and Bacteroides fragilis. Design . Open-label, three-way crossover study. Setting . Hartford Hospital Clinical Research Center. Participants . Nine healthy volunteers. Interventions . Subjects received the following regimens: (1) a single 1-g intravenous dose of cefotaxime plus a single 500-mg oral dose of metronidazole; (2) two intravenous doses of cefoxitin, 2 g each dose given every 6 hours; and (3) two intravenous doses of ampicillin-sulbactam, 3 g each dose given every 6 hours. Measurements and Main Results . Serum bactericidal titers and drug concentrations were measured over a 12-hour period. The cefotaxime-metronidazole regimen showed superior activity against E. coli compared with ampicillin-sulbactam and cefoxitin. The mean areas under the bactericidal activity curve (AUBC) for the three regimens were 550.2, 68.7, and 48.9, respectively (p=0.0001). There was no significant difference in AUBC among the three regimens for B. fragilis. Serum concentrations of cefotaxime remained above the minimum inhibitory concentration (MIC) for E. coli significantly longer than did concentrations of ampicillin-sulbactam and cefoxitin (p=0.0002 and p=0.0023, respectively). Serum concentrations of metronidazole were still at 9 times the MIC for B. fragilis at the end of the 12-hour dosing interval; for ampicillin-sulbactam and cefoxitin concentrations remained above the MIC for one-half and less than one-fourth, respectively, of the dosing interval (p<0.0001). The ratio of AUC:MIC was also favorable for metronidazole (212.2) compared with 63.4 for ampicillin-sulbactam and 9.2 for cefoxitin. Conclusions . The combination of cefotaxime-metronidazole, even at the relatively low doses used in this study, provides coverage against gram-negative and anaerobic pathogens that is at least as effective as that of cefoxitin and ampicillin-sulbactam. In addition, its cost is considerably less expensive than that of the other regimens.     

头孢他啶与头孢噻肟治疗新生儿败血症临床疗效比较

目的:评价头孢他啶和头孢噻肟治疗新生儿败血症的临床效果。方法:以头孢呋辛作对照,回顾性观察头孢他啶和头孢噻肟在新生儿败血症治疗中的疗效及安全性。结果:头孢他啶组、头孢噻肟组的有效率分别为91.30％、94.12％,与对照组头孢呋辛组(89.12％)比较均无显著差异(P>0.05);不良反应发生率也无显著差异(P>0.05);但头孢噻肟钠组与头孢他啶组住院天数均比对照组短(P<0.05)。结论:头孢他啶与头孢噻肟可作为新生儿败血症治疗的首选药物。     

小儿急性阑尾炎细菌学检查及药敏试验的回顾

小儿急性阑尾炎细菌学检查及药敏试验的回顾李岚蔡威陈方张宛陵施诚仁金惠明（上海第二医科大学附属新华医院上海２０００９２）急性阑尾炎是小儿外科常见疾病，病情往往比成人严重，穿孔、腹膜炎的发生率较高，术后正确选用抗菌药物治疗以及防止术后并发症非常重要。引起...     

Assessment of skin barrier function in rosacea patients with a novel 1% metronidazole gel

The skin of patients with rosacea is extremely sensitive and hyper-reactive to dietary, environmental, and topical factors. Accordingly, the management of rosacea involves not only choosing appropriate medication and treatment for daily skin care, but also avoiding known trigger factors. Recently, 1% metronidazole, a mainstay of topical rosacea therapy, was reformulated in a gel vehicle that contains hydrosolubilizing agents (HSA) niacinamide, beta cyclodextrin, and a low concentration of propylene glycol. It is designed to solubilize greater concentrations of metronidazole than is possible in water alone while reducing the potential for irritation and barrier disruption. A 2-week study was undertaken by the author to evaluate the effect of the new 1% metronidazole gel on the skin barrier in 25 women with mild to moderate rosacea. Statistically significant improvement in disease severity, erythema, desquamation, and skin irritation was noted by the investigator by the end of week 1, which continued throughout the study. After 2 weeks, subjects noted improvements in skin condition and rosacea. Results of noninvasive assessments showed no disruption of the skin barrier. Furthermore, there was an increasing trend in skin hydration that approached statistical significance.