注射用头孢硫脒与四种常用注射液的配伍稳定性考察

目的 考察注射用头孢硫脒在4种临床常用注射液中的配伍稳定性.方法 根据《中华人民共和国药典》(2010版)规定的注射液pH值的上下限,调节0.9％氯化钠注射液、5％葡萄糖注射液、10％葡萄糖注射液以及5％葡萄糖+0.9％氯化钠注射液的pH值,并按临床常用剂量,配制头孢硫脒与上述注射液及原pH值注射液的配伍溶液,考察上述12种配伍液于0、0.5、1、2、3、4、5、6h的pH值、颜色和澄明度等外观变化,用高效液相色谱法考察在上述时间点下配伍液中头孢硫脒的含量变化.该方法采用BDS-C18(250 mm×4.6 mm,5 μm)色谱柱,磷酸盐缓冲液:乙腈(80∶20)为流动相,检测波长为254 nm,柱温为30℃,进样量1μl.结果 头孢硫脒专属性好,能达到基线分离,线性范围为1～12 mg/ml(R=1.0000),日内精密度相对标准差＜2.0％,12种配伍液在6h内峰面积变化均＜4％.结论 头孢硫脒与不同pH值的0.9％氯化钠注射液、5％葡萄糖注射液、10％葡萄糖注射液以及5％葡萄糖+0.9％氯化钠注射液配伍后稳定,临床上可配伍使用.     

注射用头孢地秦钠与注射用氯诺昔康配伍稳定性考察

目的 考察注射用头孢地秦钠与注射用氯诺昔康在0.9％氯化钠注射液中的配伍稳定性.方法 在(25±1)℃下,采用高效液相色谱法(HPLC)测定配伍液8h内头孢地秦钠与氯诺昔康的含量变化,并观察和检测配伍液的外观、pH值及不溶性微粒变化,结果 在室温下配伍液8h内的含量、pH、不溶性微粒及外观均无明显变化.结论 室温条件下,注射用头孢地秦钠与注射用氯诺昔康在0.9％氯化钠注射液中8h内稳定.     

氟尿嘧啶与氢化可的松注射液配伍稳定性考察

目的考察氟尿嘧啶注射液与氢化可的松注射液的配伍稳定性。方法观察及测定2种注射液在0.9%氯化钠注射液中配伍后于室温放置24h内的外观、pH值及不溶性微粒。结果室温24h内,氟尿嘧啶与氢化可的松混合后加入0.9%氯化钠注射液中的外观、pH值均无明显变化,微粒数目不断减少。结论氟尿嘧啶与氢化可的松注射液以0.9%氯化钠注射液作为溶媒宜配伍。     

盐酸胺碘酮注射液与4种临床常用输液的配伍稳定性考察

目的考察盐酸胺碘酮注射液与临床常用4种输液(5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液及0.9%氯化钠注射液)的配伍稳定性。方法采用Hypersil BDS-C18色谱柱(250 mm×4.6mm,5μm),甲醇∶磷酸-三乙胺缓冲液(pH3.2)(65∶35,V/V)为流动相,柱温30℃,流速1.0 mL/min,检测波长242 nm,测定盐酸胺碘酮注射液与上述4种输液在室温下配伍后6 h内不同时间的含量变化,并观察溶液外观性状及pH值的变化。结果本实验所建立的色谱条件对盐酸胺碘酮的检测专属性好,配伍液中盐酸胺碘酮在0.15～2.4 mg/mL浓度范围内,线性关系良好(R2=1),日内RSD值为0.01%,4种配伍液在6 h内峰面积均无明显变化,RSD值均小于2.0%。结论盐酸胺碘酮注射液与4种输液在室温下配伍后6 h内含量、pH值、外观无明显变化,体外配伍稳定。     

盐酸曲马多注射液与氟哌利多注射液配伍的稳定性研究

目的:考察盐酸曲马多注射液与氟哌利多注射液在0.9％氯化钠注射液中的配伍稳定性.方法:在室温条件下,采用高效液相色谱法(HPLC)测定配伍液72 h内盐酸曲马多与氟哌利多的含量变化,并观察和检测配伍液的外观、不溶性微粒及pH变化.结果:配伍液在72 h内盐酸曲马多与氟哌利多含量、不溶性微粒、外观及pH均无明显变化.结论:盐酸曲马多注射液与氟哌利多注射液在0.9％氯化钠注射液中,室温条件下72 h内保持稳定.     

高效液相色谱法-二极管阵列检测器考察头孢替唑钠与氯诺昔康配伍稳定性

目的 考察注射用头孢替唑钠与注射用氯诺昔康在0.9％氯化钠注射液中的配伍稳定性.方法 在(25±1)℃下,采用高效液相色谱法-二极管阵列检测器测定头孢替唑钠与氯诺昔康配伍后0～6h内的浓度变化,并观察和检测两药配伍液的外观及pH值变化.结果 在室温下配伍液6h内的浓度、pH及外观均无明显变化.结论 室温条件下,注射用头孢替唑钠与注射用氯诺昔康在0.9％氯化钠注射液中6h内保持稳定.     

阿奇霉素与氨溴索的配伍稳定性考察

目的:考察注射用乳糖酸阿奇霉素与盐酸氨溴索注射液的配伍稳定性.方法:观察注射用乳糖酸阿奇霉素与盐酸氨溴索注射液配伍后于室温避光放置24h内的外观、pH及不溶性微粒的变化,并采用高效液相色谱法测定配伍液中阿奇霉素、氨溴索的含量.结果:室温、避光条件下,注射用乳糖酸阿奇霉素、盐酸氨溴索注射液加入5％葡萄糖注射液和0.9％氯化钠注射液中,在24h内配伍液的外观、pH均无明显变化,微粒数目不断减少,含量测定结果显示氨溴索在以5％葡萄糖为溶媒的配伍液和以0.9％氯化钠为溶媒的配伍液中,24h内含量无明显变化;阿奇霉素以5％葡萄糖为溶媒的配伍液中24h内含量无明显变化,但在以0.9％氯化钠为溶媒的配伍液中16 h后含量有所下降.结论:最终浓度分别为4.31,1.03或小于4.31,1.03 mg·ml-1的乳糖酸阿奇霉素和盐酸氨溴索以5％葡萄糖为溶媒的配伍液在24 h内使用较安全,以0.9％氯化钠为溶媒的配伍液建议在8h内使用.     

注射用氯诺昔康与甲磺酸罗哌卡因注射液的配伍相容性研究

目的 考察注射用氯诺昔康与甲磺酸罗哌卡因注射液在0.9％氯化钠注射液中的配伍稳定性.方法 在室温条件下,采用高效液相色谱法测定配伍液48 h内氯诺昔康与甲磺酸罗哌卡因的含量变化,并观察配伍液的外观及pH值变化.结果 配伍液48 h内氯诺昔康与甲磺酸罗哌卡因的含量不断下降,并且配伍液在2h后出现沉淀.结论 室温条件下,注射用氯诺昔康与甲磺酸罗哌卡因注射液在0.9％氯化钠注射液中不稳定,临床不宜配伍应用.     

头孢曲松钠与9种大输液配伍的稳定性

目的 建立HPLC法测定头孢曲松钠含量并考察头孢曲松钠与9种大输液配伍的稳定性.方法 采用Spherisorb ODS柱(4.0 mm×250 mm,5.0μm);柱温25℃;流动相为0.1%三乙胺水溶液∶甲醇(99∶1);流速0.9ml·min-1;检测波长240 nm,内标苯巴比妥.测定配伍液中头孢曲松含量变化,同时观测pH颜色、产气、沉淀和气味变化.结果 头孢曲松钠与10%葡萄糖注射液、0.9%氯化钠注射液、葡萄糖氯化钠注射液、木糖醇注射液、替硝唑葡萄糖注射液、甲硝唑注射液配伍后,25℃6h内含量和pH值稳定,外观变化较小;与碳酸氢钠注射液配伍后,发生产气现象,pH值变化明显.与复方氯化钠注射液、乳酸林格注射液配伍后发生沉淀,6h内含量变化大,降解产物有明显增加趋势.结论 头孢曲松钠与复方氯化钠,乳酸林格氏液、碳酸氢钠注射液不宜配伍.与其它6种输液可配伍使用.     

注射用炎琥宁与注射用头孢他啶配伍的稳定性考察

（1. ［摘要］目的考察注射用炎琥宁与注射用头孢他啶在0.9%氯化钠注射液中的配伍稳定性。方法采用高效液相色谱法,以Hypersil C18色谱柱,乙腈 0.02 mol•L 1磷酸二氢钾（pH值3.5）梯度洗脱,测定注射用炎琥宁与注射用头孢他啶配伍后在室温下8 h内的含量变化,并观察和检测配伍液的外观及pH值变化。结果配伍液外观及含量无明显变化,但pH值随时间变化逐渐上升。结论注射用炎琥宁与注射用头孢他啶在0.9%氯化钠注射液中3 h内稳定。     

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.