清开灵注射液与6种药物配伍稳定性考察

目的考察清开灵注射液与注射用青霉素钠、氧氟沙星氯化钠注射液、注射用头孢拉定、注射用阿昔洛韦、注射用更昔洛韦和利巴韦林注射液配伍的稳定性。方法将清开灵注射液与上述6种药物分别配伍，观察配伍后溶液的外观、pH值和含量变化，采用紫外分光光度法进行光谱扫描测定。结果清开灵注射液与青霉素钠和头孢拉定配伍后产生沉淀，颜色加深；与阿昔洛韦配伍后含量显著下降；与阿昔洛韦配伍后2 h内性质稳定，24 h内含量显著下降；与利巴韦林注射液和氧氟沙星氯化钠注射液、更昔洛韦配伍后外观、含量和pH值均无明显变化，配伍后性质稳定。结论清开灵注射液可以和更昔洛韦、氧氟沙星氯化钠注射液、利巴韦林注射液联合使用；与青霉素钠、头孢拉定不能混合使用；与阿昔洛韦配伍应在2 h内滴完。     

果糖注射液与5种药物的配伍稳定性考察

目的:探讨果糖注射液与注射用头孢拉定、利巴韦林注射液、注射用阿昔洛韦、注射用盐酸左氧氟沙星、注射用青霉素钠的配伍稳定性。方法:考察果糖注射液与5种药物分别配伍后的外观、pH值、含量及不溶性微粒的变化,用紫外分光光度法进行光谱扫描。结果:果糖注射液与注射用头孢拉定、利巴韦林注射液、注射用阿昔洛韦、注射用青霉素钠配伍后,外观、含量和pH值均无明显变化,配伍后性质稳定。与注射用盐酸左氧氟沙星配伍后24h内含量显著下降,pH值略有下降,同时混合液出现浑浊现象。结论:果糖注射液与注射用头孢拉定、利巴韦林注射液、注射用阿昔洛韦、注射用青霉素钠在室温下可配伍使用;与注射用盐酸左氧氟沙星的配伍在临床上则应谨慎。     

葡萄糖氯化钠钾注射液与注射用阿昔洛韦、更昔洛韦配伍的稳定性

目的研究在室温下葡萄糖氯化钠钾注射液分别与注射用阿昔洛韦、更昔洛韦配伍后的稳定性。方法采用HPLC法分别测定配伍后阿昔洛韦和更昔洛韦的含量变化,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8h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。结论葡萄糖氯化钠钾注射液与注射用阿昔洛韦、更昔洛韦配伍后8h稳定,在8h内可安全应用于临床。     

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.     

奥硝唑氯化钠注射液与更昔洛韦配伍稳定性考察

目的：对奥硝唑氯化钠注射液与更昔洛韦配伍的稳定性进行考察。方法：采用紫外分光光度法，考察不同时间配伍液中2种药物的含量变化和最大吸收峰峰位变化，并观察配伍液的外观及pH。结果：奥硝唑氯化钠和更昔洛韦在室温下配伍后，8h内药物含量、吸收峰位、外观及pH均无明显变化。结论：奥硝唑氯化钠和更昔洛韦配伍后，在8h内是稳定的，可配伍使用。     

注射用更昔洛韦与4种输液配伍的稳定性考察

目的考察在25℃下注射用更昔洛韦与临床常用的5%葡萄糖氯化钠注射液、10%葡萄糖注射液、乳酸钠林格注射液、果糖注射液配伍后6 h内的稳定性。方法用高效液相色谱(HPLC)法测定注射用更昔洛韦与4种输液配伍后0～6 h的含量,同时考察配伍溶液的外观、pH等。结果 25℃下6 h内,注射用更昔洛韦分别与4种输液配伍后的含量、紫外吸收光谱、外观、pH基本不变。结论注射用更昔洛韦与4种输液不存在配伍禁忌。     

注射用头孢米诺钠与更昔洛韦的配伍稳定性考察

目的考察注射用头孢米诺钠与更昔洛韦在0.9%氯化钠注射液中的配伍稳定性。方法分别于25℃和37℃条件下采用紫外分光光度法测定配伍液中头孢米诺钠与更昔洛韦的含量变化,同时观察配伍液的外观、pH、微粒变化及紫外吸收光谱的变化。结果配伍液在8 h内外观、pH、主药含量及紫外吸收光谱均无显著变化。结论注射用头孢米诺钠与更昔洛韦在0.9%氯化钠注射液中稳定性良好,可配伍使用。     

注射用更昔洛韦与甲硝唑氯化钠注射液配伍稳定性考察

目的探讨注射用更昔洛韦与甲硝唑氯化钠注射液的配伍稳定性。方法采用紫外分光光度法测定注射用更昔洛韦与甲硝唑氯化钠注射液配伍后,在常温20℃下,5.0h内不同时间的含量,观察溶液的色泽及测定PH值。结果在5.0h内,注射用更昔洛韦与甲硝唑氯化钠注射液的配伍液外观、PH值、紫外光谱及含量无明显变化。结论注射用更昔洛韦与甲硝唑氯化钠注射液配伍在5.0h内可以使用。     

更昔洛韦与莪术油葡萄糖注射液配伍的稳定性实验

目的：研究更昔洛韦与莪术油葡萄糖注射液配伍的稳定性。方法：采用高效液相色谱法（HPLC）N定配伍后6h内更昔洛韦的含量变化，用分光光度法测定莪术油中莪术醇的含量变化，同时观察配伍液的外观、pH值和微粒的变化。结果：在4.25和37℃条件下，6h内配伍液全部澄明，pH值、微粒均无明显变化。更昔洛韦的含量〉99％，莪术醇含量〉94％。结论：更昔洛韦与莪术油葡萄糖注射液配伍6h内稳定。     

注射用更昔洛韦与14种药物配伍的稳定性研究

目的 研究注射用更昔洛韦与临床常用14种药物配伍的稳定性.方法 分析注射用更昔洛韦与14种药物在室温下配伍后的外观、Ph值、微粒数和含量.结果 注射用更昔洛韦与0.9%氯化钠注射液、5%葡萄糖注射液、注射用头孢拉定、注射用头孢噻肟钠、克林霉素磷酸酯注射液、替硝唑注射液、西米替丁注射液、地塞米松注射液、维生素B1注射液配伍后无明显变化.结论 注射用更昔洛韦不宜与碳酸氢钠注射液、10%氟罗沙星注射液、盐酸左氧氟沙星注射液、10%葡萄糖注射液配伍使用,与克林霉素磷酸酯注射液、5%葡萄糖氯化钠注射液配伍使用有待进一步研究,可与其他8种药物配伍使用.     

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.

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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.