HPLC法测定注射用头孢尼西钠含量及有关物质

目的:用 HPLC 法测定注射用头孢尼西钠的含量及其有关物质。方法:采用 Kromasil C_(18)色谱柱(250 mm×4.6 mm,5μm),以乙腈-水-0.2 mol·mL~(-1)磷酸二氢铵(21:74:5)为流动相,流速1.0 mL·min~(-1),检测波长为254 nm;柱温:40℃。结果:头孢尼西钠与其相邻杂质峰能完全分离,头孢尼西钠在22～132μg·mL~(-1)浓度范围内线性关系良好(r=0.9999)。结论:该法简便、准确、专属性好,可以用于注射用头孢尼西钠的含量测定及有关物质检查。     

注射用头孢尼西钠细菌内毒素检查法的研究

目的研究注射用头孢尼西钠的细菌内毒素检查方法。方法参照《中国药典》2000年版收载的细菌内毒素检查方法及指导原则进行干扰试验。结果注射用头孢尼西钠在药液稀释浓度为1.67mg.ml-1时,对鲎试剂的凝集反应无干扰作用。采用灵敏度为0.25 EU.ml-1的鲎试剂可进行细菌内毒素检查。结论可用细菌内毒素检查法控制注射用头孢尼西钠的质量。本品细菌内毒素限值为0.15EU.mg-1。     

喜炎平配合头孢尼西钠对感染性肺炎患儿的疗效及其对炎症因子水平改善的影响

目的:探究喜炎平配合头孢尼西钠对感染性肺炎患儿临床疗效与炎症因子及其症状的影响。方法:选取2016年12月—2018年12月期间诊治感染性肺炎患儿146例资料,按用药不同将其分为联用组和头孢尼西钠组,每组73例;头孢尼西钠组患者给予单用头孢尼西钠治疗,联用组患者则给予喜炎平与头孢尼西钠联用治疗,比较两组患者治疗后总有效率、症状复常时间的差异,以及血清炎性因子即肿瘤坏死因子-α(Tumor Necrosis Factor-α,以下简称TNF-α)、白介素-6(Interleukin 6,以下简称IL-6)和白介素-1β(Interleukin 1β,以下简称IL-1β)水平改善情况。结果:联用组患者治疗后的总有效率高于头孢尼西钠组(95.89%vs 83.56%,P<0.05),症状(咳嗽、体温和肺部湿啰音)复常时间均早于头孢尼西钠组(P<0.05),TNF-α、IL-6和IL-1β水平测得值均低于头孢尼西钠组(P<0.05)。结论:采用喜炎平配合头孢尼西钠治疗感染性肺炎患儿临床疗效较显著,有效改善了其炎症因子水平和症状。     

头孢尼西钠与4种输液配伍的稳定性

目的考察头孢尼西钠与4种输液配伍的稳定性。方法采用紫外分光光度法测定5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液和0.9%氯化钠注射液中头孢尼西钠的含量。考察混合液的外观性状和pH值变化，测定配伍后头孢尼西钠的含量。结果头孢尼西钠与4种输液混合后，溶液的pH值和外观性状无明显变化，头孢尼西钠的含量稳定。 结论头孢尼西钠和4种输液配伍后在5 h内稳定性无明显变化。     

腹膜透析液中头孢尼西钠的稳定性考察

目的 考察头孢尼西钠在25℃和37℃下与腹膜透析液配伍的稳定性。方法 将头孢尼西钠加入腹膜透析液中混合均匀后，用紫外分光光度法在25℃和37℃下于0，1，2,4，6，8h时测定头孢尼西钠的含量，同时记录配伍液的外观变化和pH值。结果 头孢尼西钠配伍液外观、pH值及含量均无明显变化。结论 在25℃和37℃下0—8h内头孢尼西钠可与腹膜透析液配伍使用。     

头孢尼西钠中相关物质的检测

目的:建立头孢尼西钠中有关物质的HPLC检测方法。方法:采用高效液相色谱法,C18柱(250mm×4.6mm,5μm),以0.01mol/L磷酸二氢钾溶液(冰醋酸调节pH为3.5)-乙腈(79:21)为流动相,检测波长为254nm。结果:头孢尼西与各有关物质达到了较好的分离,1-磺甲基-5-巯基四氮唑二钠与7-氨基头孢烷酸的校正因子分别为0.8829,0.7594,检测限分别为0.02,0.04ng。头孢尼西钠和甲酰基头孢尼西定量限分别为0.08,0.62ng;检测限分别为0.03,0.21ng。结果:本法操作简便、专属性强、准确度高、重复性好,可用于头孢尼西钠中有关物质的测定。     

注射用头孢尼西钠与果糖注射液的配伍稳定性考察

目的:考察注射用头孢尼西钠在室温(25±1)℃下与果糖注射液配伍的稳定性。方法:模拟临床用药浓度,将注射用头孢尼西钠1.0g加入到10mL果糖注射液中,混合均匀后,在室温(25±1)℃下考察6h内配伍液的外观和pH值变化,并采用高效液相色谱法测定头孢尼西的含量,同时考察有无新物质生成。结果:在室温(25±1)℃下,0～6h配伍液的外观、pH值、头孢尼西的含量均无明显变化。结论:注射用头孢尼西钠与果糖注射液配伍,在室温(25±1)℃下6h内配伍稳定。     

注射用头孢尼西钠在更昔洛韦葡萄糖注射液中的配伍稳定性

目的：考察25℃下,注射用头孢尼西钠与更昔洛韦葡萄糖注射液配伍的稳定性.方法：采用HPLC法测定头孢尼西钠与更昔洛韦配伍后0～8h内的含量变化,并观察配伍液的外观及pH.结果：8h内混合液外观、pH及含量均无明显变化.结论：在25℃条件下,注射用头孢尼西钠在更昔洛韦葡萄糖注射液中配伍8h内基本稳定.     

高效分子排阻色谱法分析头孢米诺钠

目的 建立高效分子排阻色谱（HPSEC）法分析头孢米诺钠聚合物等杂质.方法 采用高效凝胶色谱柱（TSKgel G2500 PWxL7.8 mm×300 mm）;流动相为pH 7.0的0.005 mol·L-1磷酸盐缓冲液[0.005 mol·L-1磷酸氢二钠-0.005 mol·L-1磷酸二氢钠（61∶39）];流速为0.5 mL· min-1;检测波长为254 nm;进样量为10μL.结果 头孢米诺的线性范围为2.02～40.36ug·mL-1 （r=0.9999）;定量限为0.8 ng;样品测定的线性范围为0.4～2.5 mg·mL-1 （r=0.9995）.结论 该方法能够较好地分离头孢米诺钠和聚合物等杂质,简便快速、定量准确、重复性好,可用于头孢米诺钠中聚合物等杂质的检验.     

头孢尼西钠残留溶剂检查法的研究

目的建立用气相色谱的顶空进样法测定头孢尼西钠中乙腈、二氯甲烷、四氢呋喃3种残留溶剂.方法用HP-INNOWAX毛细管柱(30m×0·53mm,1·0μm),以氮气为载气,FID检测器,顶空进样,通过外标法计算头孢尼西钠中的残留量.结果头孢尼西钠中3种溶剂残留在6~600μg?ml-1浓度范围有良好的线性关系,r≥0·9997,平均回收率为98·7%~103·2%,RSD为1·3%~1·8%.结论本法快速、简便、灵敏度高,分离度好.     

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.     

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.     

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.     

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.