头孢哌酮钠皮试液的稳定性及有效期预测

采用恒温加速实验法预测头孢哌酮钠皮试液的稳定性。结果：室温（25℃）有效期约为10d,夏季（37℃）有效期约为1d。同时进行留样观察,与加速实验预测时间基本一致。     

美洛西林钠与卡络磺钠在5%葡萄糖注射液中配伍稳定性考察

目的:考察室温(25℃)下注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中的配伍稳定性。方法:采用反相高效液相色谱法-二极管阵列检测器分别测定美洛西林钠与卡络磺钠在5%葡萄糖注射液中配伍后0～4 h内的含量及pH变化,并观察配伍液的外观变化。结果:4 h内注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中配伍液外观、pH及含量均无明显变化。结论:在室温(25℃)下,注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中4 h内配伍稳定。     

加快美洛西林钠静脉滴注速度致不良反应1例

患者,女,67岁,3d前在外院行左眼翼状胬肉切除术,因局部疼痛伴异物感来我院眼科门诊就诊。查体：T36.9℃,HR80次/min,R20次/min,BP140/90mmHg,左眼术区充血、水肿。考虑左眼翼状胬肉术后感染。拟用美洛西林钠抗感染。询问患者无药物及食物过敏史后进行美洛西林钠皮试,20min观察皮试结果阴性。将美洛西林钠4.0g加入5%葡萄糖氯化钠250ml液体中静脉滴注,30滴/min。     

注射用美洛西林钠在四种常用输液中的稳定性实验

目的：研究注射用美洛西林钠在5％葡萄糖注射液等四种输液中的稳定性,为临床合理用药提供科学依据。方法：在室温(24℃左右)条件下,于0、0．5、l、2h考察配伍液的外观、pH值及美洛西林钠含量的变化。结果：与四种输液配伍后,其外观及pH值变化不大,但美洛西林钠含量下降。0、5h时含量下降10％左右。结论：美洛西林钠在四种常用输液中稳定性较差,临床应用以采用静脉注射为宜。     

3%氯化钠注射液细菌内毒素检查方法的考查

目的:考察不同温度(25℃、37℃)下6h内,美洛西林钠与木糖醇的配伍稳定性。方法:用紫外分光光度法测定配伍液中关洛西林含量,并观察外观、pH值的变化。结果:美洛西林钠与木糖醇输液配伍后6 h内,其外观,pH值以及含量均无明显变化。结论:美洛西林在上述条件下可以与木糖醇输液配伍使用。     

头孢哌酮皮试液的稳定性考察

目的 考察头孢哌酮皮试液的稳定性. 方法 采用经典恒温加速实验法,考察头孢哌酮皮试液的外观、pH值和含量,用高效液相色谱法测定头孢哌酮的含量. 结果 恒温加速实验25 ℃时预测有效期为3 d. 结论 头孢哌酮皮试液热稳定性差,室温保存不宜超过3 d.     

紫虹溶液的稳定性考察

目的：预测医院消毒剂紫虹溶液的稳定性，为临床提供贮存期依据。方法：采用经典恒温加速法和初匀速法，预测其室温（20℃）有效期，同时进行留样观察。结果：其稳定性与温度有关，符合Arrhenius公式。结论：本制剂在室温（20℃）时贮存期为33－34h，与留样观察结果34h基本相符。     

注射用美洛西林钠稳定性考察

目的:研究注射用美洛西林钠稳定性考察。方法:通过在高温40℃±2、高湿90%条件下放置6个月,考察其外观、酸碱度、水分、有关物质及含量。结果:注射用美洛西林钠稳定性良好。     

双氯芬酸钠胶浆的稳定性试验研究

目的研究双氯芬酸钠胶浆的稳定性。方法分别采用留样观察法与化学动力学法，观察双氯芬酸钠胶浆的外观性状、颜色、透明度等变化，同时通过试验求出药物消除速率k值，推算出双氯芬酸钠胶浆的有效期。结果20～25℃室温环境下保存的双氯芬酸钠胶浆稳定性较好，有效期约为1．7年。结论双氯芬酸钠胶浆在避光、室温条件下，能较长时间保存。     

美洛西林钠注射液在6种输液中的稳定性考察

目的 研究注射用美洛西林钠在6种常用输液中的稳定性。方法 用紫外分光光度法考察在30℃时配伍液8h内外观、pH值、含量及紫外光谱变化。结果 在10％葡萄糖注射液和5％碳酸氢钠注射液中颜色略显淡黄，其他输液外观均无变化。紫外光谱和pH值无显改变。除5％碳酸氢钠注射液外，其他5种输液中含量变化不大。结论 美洛西林钠在5％碳酸氢钠注射液中不稳定。     

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.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

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.