高效液相色谱法测定新霉素地塞米松滴眼液中苯扎氯铵的含量

目的 建立了高效液相色谱法(HPLC)测定新霉素地塞米松滴眼液中苯扎氯铵含量的方法.方法 采用C18色谱柱(250 mm × 4.6 mm,5 μm),以0.02 mol·L-1庚烷磺酸钠溶液[含0.1%三乙胺,用磷酸调节pH(3.45±0.1)]-乙腈(20∶80)为流动相,检测波长210 nm,流速1.0 mL·min-1,柱温40 ℃,进样体积20 μL.结果 苯扎氯铵三种同系物在其各自的线性范围内(0.98~126.08、0.85~109.17、0.77~98.25 mg·L-1)内呈良好的线性关系.苯扎氯铵的平均加样回收率为96.53%,RSD为1.75%.结论 该方法准确可靠,操作简单快速,重复性好,灵敏度高,可用于同时测定新霉素地塞米松滴眼液中苯扎氯铵三种同系物的含量,为其安全性考察提供参考.     

普拉洛芬滴眼液中防腐剂苯扎氯铵的含量测定

目的:建立普拉洛芬滴眼液中防腐剂苯扎氯铵的含量测定方法.方法:采用Diamonsfl C18色谱柱,规格为4.6×250mm,粒度为5μm,以0.02mol/L庚烷磺酸钠溶液(含0.1%三乙胺,用磷酸调节pH值3.45±0.1)-乙腈(35:65)为流动相;流速为1.5ml/min;检测波长208nm;柱温:40℃.结...     

硝酸毛果芸香碱滴眼液中苯扎氯铵含量测定

目的:用高效液相色谱法(HPLC)测定硝酸毛果芸香碱滴眼液中苯扎氯铵的含量。方法:色谱柱为CN(HypersilCN,150mm×4.6mm,5μm);流动相为0.03mol/L磷酸二氢钠溶液(用1mol/L氢氧化钠溶液调节pH至7.0)-乙腈(57:43);流速为2mL/min;检测波长为214nm;柱温为35℃;苯扎氯铵C12、C14、C16之间的分离度应符合规定。结果:苯扎氯铵在40～160μg/mL内线性关系良好,Y=12.2281X+6.8814(r=0.9999,n=6),回收率为99.7%～101.9%,RSD=0.66%。结论:该法操作简便,快速、准确、灵敏度高,重复性好,可用于硝酸毛果芸香碱滴眼液中苯扎氯铵的含量测定。     

萘敏维滴眼液中苯扎氯铵的含量测定

目的 建立萘敏维滴眼液中防腐剂苯扎氯铵的含量测定方法. 方法 采用高效液相色谱(HPLC)法,氰基键合硅胶为填充剂,以0.02 mol.L^-1庚烷磺酸钠溶液(含0.1%三乙胺,用磷酸调节pH 3.45±0.10)-乙腈(35:65)为流动相;流速为1.5 mL.min^-1;检测波长210 nm;柱温:45 ℃ . 结果 苯扎氯铵在0.044 4～0.222 0 mg.mL^-1范围内线性关系良好(r=0.999 0,n=5),平均回收率为100.1%,RSD=0.23%. 结论 HPLC法具有灵敏、准确、重复性好的特点,可有效测定萘敏维滴眼液中防腐剂苯扎氯铵的含量.     

HPLC法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量

目的建立一种高效液相色谱法同时测定阿奇霉素滴眼液中阿奇霉素及苯扎氯铵的含量。方法采用十八烷基硅烷键合硅胶色谱柱(4.6 mm×150 mm,5μm),柱温30℃,以乙腈-磷酸盐缓冲液(取0.05 mol.L-1磷酸氢二钾溶液,用20%磷酸调节pH至8.2)(58∶42)为流动相;检测波长210 nm;流速:1.0 mL.min-1。结果阿奇霉素在1.002 8～5.014 0 mg.mL-1的浓度范围内,苯扎氯铵在6.15μg.mL-1～14.35μg.mL-1的浓度范围内均呈线性。阿奇霉素的平均回收率100.68%,RSD为0.50%(n=9);苯扎氯铵的平均回收率100.59%,RSD为0.92%(n=9)。阿奇霉素与苯扎氯铵的定量限分别为750 ng.mL-1、46 ng.mL-1,平均含量分别为106.94%及100.04%,RSD分别为0.94%及0.67%。仪器重复性RSD值均在2.0%以下。结论本方法简单、准确,可同时测定样品中阿奇霉素及苯扎氯铵的含量。     

苯扎氯铵对大鼠结肠神经及平滑肌的影响

目的研究苯扎氯铵对大鼠结肠神经及平滑肌的影响。方法8~9周龄SD大鼠50只,随机分为两组。氯胺酮麻醉下开腹,实验组用0.1%苯扎氯铵处理大鼠降结肠浆膜40min,温盐水冲洗后关腹,对照组用生理盐水代替苯扎氯铵。分别于术后1、2、3、4、8周取处理段结肠行组织学检查,反转录-聚合酶链反应(RT-PCR)检测乙酰胆碱酯酶(AchE)、巢蛋白(nestin)、乙酰胆碱M3受体(Chrm3)的表达,循环水浴药理学检测平滑肌收缩功能变化。结果苯扎氯铵处理后1周,大鼠结肠神经节细胞明显减少、空泡变,3周后完全消失;结肠平滑肌对乙酰胆碱敏感性增强。结论采用0.1%苯扎氯铵可使大鼠结肠产生去神经作用,结肠平滑肌对乙酰胆碱敏感性增强。     

高效液相色谱法测定谷胱甘肽滴眼液中苯扎氯铵的含量

目的:建立测定谷胱甘肽滴眼液中苯扎氯铵含量的方法。方法:采用AgilentZorbaxSB-CN柱(4.6mm×250mm,5μm);流动相:0.1%磷酸水溶液-乙腈-四氢呋喃(52∶38∶10);检测波长:214nm。结果:苯扎氯铵的线性范围为50～250μg/ml,线性回归方程为Y=20674X-79747(r=0.99979)。平均回收率分别为100.9%,RSD为0.19%。结论:该方法简便、快速、准确,具有良好的重复性和回收率,可作为该制剂的质量控制标准。     

苯扎氯铵用于骨科开放性伤口清洗消毒临床效果观察

目的观察苯扎氯铵用于骨科开放性伤口清洗消毒的有效性与安全性。方法选取笔者所在医院60例急症外伤患者,随机分为观察组和对照组各30例。观察组给予0.1%苯扎氯铵溶液冲洗伤口,冲洗顺序为0.1%苯扎氯铵溶液、蒸馏水、双氧水、生理盐水;对照组给予常规碘伏消毒处理创面,消毒液冲洗前后,分别用无菌拭子取创口标本,进行细菌培养,观察菌落生长情况并计数冲洗前、冲洗后菌落数,比较两组消毒效果。结果两组冲洗前测定菌落数差异无统计学意义(P>0.05),但观察组冲洗后菌落数及减少率均明显优于对照组,差异有统计学意义(P<0.05)。结论 0.1%苯扎氯铵溶液用于骨科开放性伤口冲洗,可明显减少伤口细菌数,具有显著的局部杀菌灭菌作用。     

盐酸贝西沙星滴眼液中苯扎氯铵的HPLC法测定

建立了高效液相色谱法测定盐酸贝西沙星滴眼液中苯扎氯铵的含量.采用Kromasil C18柱,5 mmol/L乙酸铵溶液(含1％三乙胺,用冰乙酸调至pH 5.2±0.5)-乙腈(29∶71)为流动相,检测波长为215nm,流速1.0 ml/min.苯扎氯铵在5～15 μg/ml浓度范围内线性关系良好(R2=0.998 3),平均回收率为99.4％ (RSD=-0.42％).     

双氯芬酸钠滴眼液中苯扎氯铵的测定

目的采用HPLC双氯芬酸钠滴眼液中苯扎氯铵的含量。方法乙腈-5 mmol.L-1醋酸铵溶液（含1%三乙胺,用冰醋酸调节pH值至5.0±0.5）（65∶35）为流动相,CNW色谱柱（150 mm×4.6 mm,5μm）,检测波长为214 nm。结果苯扎氯铵的测定在12.50～125.00μg.mL-1与峰面积线性关系良好,苯扎氯铵的平均回收率为99.0%,RSD为1.3%。结论方法简单、灵敏度高,可用于双氯芬酸钠滴眼液中苯扎氯铵的测定。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.