酒石酸布托啡诺、盐酸曲马多及昂丹司琼注射剂体外配伍稳定性考察

目的:考察酒石酸布托啡诺注射液、盐酸曲马多注射液及盐酸昂丹司琼注射液在0.9%氯化钠注射液中的配伍稳定性。方法:采用HPLC法测定配伍液中三种药物含量,考察三种药物在0.9%氯化钠注射液中,室温条件下72 h内的含量变化,同时观察与检测外观与pH变化。结果:酒石酸布托啡诺注射液、盐酸曲马多注射液及盐酸昂丹司琼注射液的配伍液在72 h内三种药物含量未见明显变化,配伍液外观澄清,pH值保持稳定。结论:酒石酸布托啡诺、盐酸曲马多及盐酸昂丹司琼在0.9%氯化钠注射液中室温条件下、72 h内保持稳定。     

注射用氯诺昔康与盐酸氯胺酮注射液在0.9%氯化钠注射液中的稳定性考察

目的:考察注射用氯诺昔康与盐酸氯胺酮注射液在0.9%氯化钠注射液中的稳定性。方法:采用高效液相色谱法,测定注射用氯诺昔康与盐酸氯胺酮注射液配伍后在室温条件下72h内的含量变化,并观察和检测配伍液的外观及pH变化。结果:配伍液中盐酸氯胺酮含量与pH无明显变化,氯诺昔康的含量逐渐降低,配伍液24h后出现少量沉淀。结论:室温条件下,注射用氯诺昔康与盐酸氯胺酮注射液在0.9%氯化钠注射液中不稳定,临床不宜配伍应用。     

注射用氯诺昔康与盐酸托烷司琼在镇痛泵中配伍稳定性研究

目的考察注射用氯诺昔康与盐酸托烷司琼注射液在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测定配伍溶液72 h内氯诺昔康与盐酸托烷司琼的含量,并观察和检测配伍液的外观和p H值变化。结果配伍溶液中氯诺昔康质量分数和p H值未见明显变化,但盐酸托烷司琼质量分数随时间变化逐渐降低,在2 h后质量分数低于60%,且出现少量针状沉淀。结论在室温条件下,氯诺昔康与盐酸托烷司琼在0.9%氯化钠注射液中不稳定,临床不宜混合使用用于术后镇痛。     

注射用氯诺昔康与盐酸吗啡注射液在0.9%氯化钠注射液中的稳定性

目的 考察注射用氯诺昔康与盐酸吗啡注射液在0.9%氯化钠注射液中的稳定性. 方法 在室温(20±1) ℃避光条件下,观察和检测注射用氯诺昔康与盐酸吗啡注射液在0.9%氯化钠注射液中配伍液在72 h内的外观及pH变化,并用反相高效液相色谱法测定氯诺昔康与盐酸吗啡的含量. 结果配伍液72 h内外观、pH及含量均无明显变化. 结论 室温条件下,注射用氯诺昔康与盐酸吗啡注射液在0.9%氯化钠注射液中72 h内稳定.     

注射用氯诺昔康与芬太尼注射液配伍的稳定性

［摘要］目的考察注射用氯诺昔康与芬太尼注射液在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,测定注射用氯诺昔康与芬太尼注射液配伍后在室温条件下72 h内的含量变化,并观察配伍液的外观,检测pH变化。结果配伍液氯诺昔康含量与pH无明显变化,但芬太尼的含量不断降低,并且配伍液24 h后出现少量沉淀。结论室温条件下,注射用氯诺昔康与芬太尼注射液在0.9%氯化钠注射液中不稳定,临床不宜配伍应用。     

曲马多、芬太尼、昂丹司琼与0.9%氯化钠注射液在镇痛泵中的配伍稳定性考察

目的:考察盐酸曲马多、枸橼酸芬太尼、盐酸昂丹司琼注射液与0.9%氯化钠注射液在镇痛泵中的配伍稳定性。方法:在(25±1)℃室温条件下,将盐酸曲马多、枸橼酸芬太尼与盐酸昂丹司琼注射液置于一次性镇痛泵输液袋内,用0.9%氯化钠注射液稀释至刻度,观察混匀后是否出现沉淀、浑浊及颜色变化,同时测定配伍液的p H值变化,并采用高效液相色谱(HPLC)法测定配伍液中3组分在72 h内的相对百分含量变化。结果:盐酸曲马多、枸橼酸芬太尼与盐酸昂丹司琼配伍液在72 h内外观及p H值均未见明显变化,3组分在72 h内各时间点的相对百分含量均大于97%。结论:盐酸曲马多、枸橼酸芬太尼、盐酸昂丹司琼注射液与0.9%氯化钠注射液配伍液在室温条件下72 h内保持稳定。     

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.     

注射用氯诺昔康在不同pH值氯化钠注射液中的稳定性考察

目的考察注射用氯诺昔康在不同pH值(4.5～7.0)0.9%氯化钠注射液中的稳定性。方法采用高效液相色谱法测定配伍液中氯诺昔康的含量,考察室温条件下氯诺昔康在不同pH值0.9%氯化钠注射液中8 h含量变化,并观察和检测配伍液的外观及pH值变化。结果注射用氯诺昔康在不同pH值0.9%氯化钠注射液中的含量、外观与pH值均无明显变化。结论注射用氯诺昔康在不同pH值0.9%氯化钠注射液中8 h均保持稳定。     

注射用头孢替安与注射用氯诺昔康配伍稳定性考察

目的考察注射用头孢替安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HPLC法测定8 h内配伍液中头孢替安与氯诺昔康的含量变化,观察配伍液的外观,记录pH值。结果 8 h内,配伍液中氯诺昔康的含量无明显变化,头孢替安含量不断下降,8 h含量为80.8%,pH值随时间变化逐渐增大,溶液颜色随时间变化逐渐加深。结论注射用头孢替安与注射用氯诺昔康在0.9%氯化钠注射液中可配伍使用,但应在4 h内用完。     

注射用头孢匹胺与注射用氯诺昔康配伍的稳定性研究

目的考察注射用头孢匹胺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,观察和检测两药配伍液在8 h内的外观及pH值变化,并用高效液相色谱法(HPLC)测定配伍液中头孢匹胺与氯诺昔康的含量变化。结果 8 h内配伍液外观、pH值及氯诺昔康的含量无明显变化,头孢匹胺含量不断下降,8 h含量为96.5%。结论室温条件下,注射用头孢匹胺与注射用氯诺昔康在0.9%氯化钠注射液中8 h内保持稳定。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.