注射用泮托拉唑钠与8种常用注射剂的配伍稳定性考察

目的：考察室温条件下注射用泮托唑钠与8种临床常用药物的配伍稳定性。方法：建立了泮托拉唑钠高效液相含量测定方法,模拟临床应用,以0.9%的氯化钠溶液为溶媒,按比例分别将注射用泮托拉唑钠与肌苷注射液、维生素B₆注射液、维生素K₁注射液、注射用辅酶A、氨苯甲酸注射液、酚磺乙胺注射液、门冬氨酸钾镁注射液、注射用ATP 8种临床常见药物混合,在混合后即刻、0.5,1,2 h 4个时间点考察泮托拉唑含量、外观、不溶性微粒、溶液pH值的变化。结果：泮托拉唑钠与氨苯甲酸、酚磺乙胺、维生素B₆配伍后2 h内含量明显下降。结论：泮托拉唑对pH敏感,注射用泮托拉唑钠不宜与氨苯甲酸、酚磺乙胺、维生素B₆配伍,序贯使用时需冲洗管路。     

注射用泮托拉唑钠与3种常用注射液的配伍稳定性考察

目的：考察不同厂家注射用泮托拉唑钠（下称泮托拉唑）在林格注射液及与维生素C和维生素B6配伍后的稳定性。方法：在室温不避光条件下,利用高效液相色谱法测定5h内林格注射液中泮托拉唑的含量及与维生素C和维生素B6配伍后的泮托拉唑含量、观察配伍溶液的外观、澄明度变化并测定pH。结果：在室温不避光条件下5h内,林格注射液中不同厂家泮托拉唑的含量、外观、澄明度和pH均无明显变化;但泮托拉唑与林格注射液及维生素C和维生素B6注射液配伍后泮托拉唑随时间延长含量逐渐降低,配伍液的外观与澄明度和pH未见明显变化。结论：不同厂家泮托拉唑注射液在林格注射液中均稳定,泮托拉唑可以用林格注射液作为稀释剂。但是泮托拉唑注射液不能与维生素C和维生素民注射液配伍。     

喜炎平注射液与溶媒及四种注射剂的配伍稳定性考察

目的考察喜炎平注射液与5%葡萄糖注射液、10%葡萄糖注射液、0.9%氯化钠注射液溶媒不同比例配伍的稳定性,以及与常用联合用药盐酸氨溴索氯化钠注射液、注射用五水头孢唑林钠、注射用炎琥宁、注射用辅酶A的配伍稳定性情况。方法室温下,将喜炎平注射液分别与5%葡萄糖注射液、10%葡萄糖注射液、0.9%氯化钠注射液及盐酸氨溴索氯化钠注射液、注射用五水头孢唑林钠、注射用炎琥宁、注射用辅酶A进行配伍,考察配伍后0～4 h内配伍溶液的性状、pH值、不溶性微粒、主要成分含量的变化情况。结果喜炎平注射液与5%、10%葡萄糖注射液和0.9%氯化钠注射液配伍后,性状、pH值、不溶性微粒、主要成分含量在0～4 h内无显著变化,但以较高浓度30 ml︰250 ml比例配伍后4 h内不溶性微粒超出《中华人民共和国药典》的规定限度。喜炎平注射液与注射用炎琥宁配伍时,pH值在0 h明显升高但在4 h内保持稳定;分别与盐酸氨溴索氯化钠注射液、注射用辅酶A配伍后4 h内的不溶性微粒均出现超出《中华人民共和国药典》规定限度;分别与注射用炎琥宁、注射用辅酶A配伍时,主成分含量均下降约8%。结论喜炎平注射液与5%葡萄糖注射液、10%葡萄糖注射液或0.9%氯化钠注射液配伍后稳定性良好,可配伍使用,但需注意配伍比例,应控制250 ml溶媒配伍的喜炎平注射液用量不大于20 ml;喜炎平注射液与注射用五水头孢唑林钠的配伍稳定性相对较好,与其他三种不宜在配伍时混合使用。     

盐酸川芎嗪注射液与28种药物配伍的稳定性观察

目的；研究盐酸川芎嗪注射液与临床常用28种药物配伍的稳定性。方法：应用紫外分光光度计、pH计、注射液微粒分析仪分别考察了盐酸川芎嗪注射液与临床常用28种药物配伍后的外观、pH、微粒和吸收度变化。结果：盐酸川芎嗪注射液与注射用穿琥宁和注射用头孢哌酮钠配伍后产生沉淀，与氨茶碱注射液配伍后p H逐渐下降，与其他25种药物配伍后无显著改变。结论：盐酸川芎嗪注射液与注射用穿琥宁、注射用头孢哌酮的不宜配伍，与氨茶碱注射液、注射用青霉素、注射用氨苄西林钠、注射用乳糖酸红霉素应谨慎配伍，其余22种药物均可以配伍使用。     

注射用泮托拉唑钠的配伍稳定性考察

对注射用泮托拉唑钠与3种常用输液配伍的稳定性进行初步考察。方法：用HPLC法测定了配伍前后3小时内泮托拉唑的含量,同时测定了pH及外观变化。结果：泮托拉唑与氯化钠注射液配伍时较稳定,而与葡萄糖及氯化钠葡萄糖注射液配合理地则出现含量下降、变色。结论：注射用泮托拉唑与氯化钠注射液可以配伍使用,而不能与葡萄糖及氯化钠葡萄糖注射液配伍使用。     

盐酸法舒地尔与注射用盐酸川芎嗪配伍稳定性考察

目的:考察盐酸法舒地尔(简称法舒地尔)与注射用盐酸川芎嗪(简称川芎嗪)的配伍稳定性。方法:采用HPLC法,测定室温(25℃)条件下8 h内配伍溶液中两药的含量变化,并考察配伍前后外观、性状、pH及无增加不溶性微粒的变化。结果:注射用盐酸法舒地尔与川芎嗪配伍后在室温下放置8 h,配伍溶液的外观、性状、pH无明显变化,不溶性微粒无增加,放置8 h两药的含量仍在97%以上。结论:盐酸法舒地尔注射液与注射用盐酸川芎嗪配伍8 h内稳定。     

注射用丹参多酚酸盐与21种临床常用药品配伍稳定性研究

目的 考察注射用丹参多酚酸盐与21种临床常用药品配伍后的稳定性.方法 模拟临床用药,将注射用丹参多酚酸盐200mg分别与临床21种常用药品,用0.9%氯化钠注射液250 mL或5%葡萄糖注射液稀释配伍,观察溶液外观,测定配伍后4 h内pH、不溶性微粒和含量的变化.结果 注射用丹参多酚酸盐与维生素C注射液、黄芪注射液、单硝酸异山梨酯注射液、盐酸川芎嗪注射液、地塞米松磷酸钠注射液配伍使用时pH超出注射用丹参多酚酸盐厂家质量标准;与香丹注射液配伍在0.9%氯化钠注射液为溶刺的情况下,含量在1 h后下降.注射用丹参多酚酸盐与其他15种临床常用药品配伍,0～4 h内外观、pH、不溶性微粒、含量测定方面均符合规定.结论 注射用丹参多酚酸盐与所选15种,临床常用药品配伍在4 h内基本稳定.但基于中药注射液成分的复杂性,建议临床上单独使用.     

葡萄糖氯化钠钾注射液与注射用盐酸头孢吡肟配伍的稳定性

目的研究在室温下葡萄糖氯化钠钾注射液（简称GNK）与注射用盐酸头孢吡肟配伍后的稳定性。方法采用RP-HPLC法测定配伍后注射用盐酸头孢吡肟的含量变化,同时考察配伍溶液的外观、pH值和不溶性微粒的变化。结果在室温下配伍溶液8 h内均无气体或沉淀产生,pH值、不溶性微粒和含量均无明显变化。结论 GNK与注射用盐酸头孢吡肟配伍后8 h稳定,在8 h内可安全应用于临床。     

HPLC法考察注射用泮托拉唑钠的配伍稳定性

目的:考察注射用泮托拉唑钠与3种常用输液配伍稳定性.方法:应用HPLC法测定药物配伍后6h泮托拉唑的含量,同时观察外观变化及测定pH值.结果:注射用泮托拉唑钠与0.9％生理盐水配伍6h较稳定,而与5％葡萄糖及10％葡萄糖配伍时分别出现纤维状物、变色最后浑浊.结论:注射用泮托拉唑钠与0.9％生理盐水可以配伍稳定,不能与5...     

注射用盐酸川芎嗪与两种输液配伍的稳定性考察

目的考察25℃下8h内注射用盐酸川芎嗪与果糖和木糖醇的配伍稳定性。方法测定溶液的pH值,采用HPLC法测定溶液中注射用盐酸川芎嗪的含量,定时观察溶液的颜色及澄明度。观察注射用盐酸川芎嗪在常用输液5%果糖注射液及5%木糖醇中的稳定性。结果注射用盐酸川芎嗪与果糖和木糖醇常用输液配伍后,pH值、微粒以及含量结果在8h内均无明显变化。结论注射用盐酸川芎嗪可与果糖与木糖醇等常用输液配伍使用。     

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.

---

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.