聚氯乙烯输液袋增塑剂的释出和对药物的吸附

聚氯乙烯（PVC）输液袋中使用较多的增塑剂邻苯二甲酸二（2-乙基己基）酯（DEHP）在贮存和使用中会释出至输液中进入人体，药物也可能被PVC输液袋吸附。为此，本研究采用HPLC法测定了PVC输液袋中所释出DEHP的含量，两种PVC输液袋装不同介质后DEHP的释出量，不溶性微粒与DEHP的关系，以及PVC输液袋对硝酸甘油和地西泮的吸附。     

PVC软输液袋对紫杉醇稳定性的影响及其中DEHP溶出量考察

目的考察聚氯乙烯(PVC)软输液袋对紫杉醇稳定性的影响及其中增塑剂邻苯二甲酸二(2-乙基)己酯(DEHP)的溶出情况。方法模拟临床使用紫杉醇的条件,用高效液相色谱法测定整个使用过程中紫杉醇的浓度变化和DEHP的溶出量。结果紫杉醇浓度随时间的延长而下降,DEHP的溶出量随温度的升高和时间的延长而增大。结论目前临床使用的紫杉醇配套输液袋绝大多数为PVC袋,由于紫杉醇浓度下降且溶出的DEHP可直接进入人体,不能保证用药安全,故应高度重视PVC软输液袋的危害性。     

常用注射剂表面活性剂对聚氯乙烯输液器中邻苯二甲酸二辛酯溶出的试验研究

目的:考察常用的5种注射剂表面活性剂对聚氯乙烯(PVC)输液器中邻苯二甲酸二辛酯(DEHP)溶出的影响。方法:分别配制吐温-80、吐温-40、吐温-20、聚氧乙烯蓖麻油、卵磷脂溶液,加入5%葡萄糖注射液中,模拟临床输注方式,用PVC输液器滴注,以高效液相色谱法测定收集液中DEHP峰面积,计算含量,以此考察加入表面活性剂的种类、浓度、输液时间及输液管长度对DEHP溶出的影响。结果:5种表面活性剂对DEHP的溶出能力为吐温-80>吐温-40>吐温-20>聚氧乙烯蓖麻油>卵磷脂,卵磷脂未见溶出DEHP。在表面活性剂种类一定的情况下,DEHP的溶出与其浓度、输液时间以及输液管长度成正相关。结论:本研究可为含有表面活性剂的注射剂选择安全的输液器及药厂生产注射剂时选择表面活性剂提供参考。     

输液用塑料制品对药物的吸附

目前 ,国内、外应用于医药行业的塑料主要有聚氯乙烯(PVC)、聚乙烯 (PE)、聚丙烯 (PP)和聚碳酸酯 (PC)等 ,而供输血、输液用的塑料容器均以软PVC为主体 ,添加增塑剂邻苯二甲酸二辛酯 (DEHP)和稳定剂等加工制成。这种塑料软包装具有体积小、重量轻、便于运输和存放、价格低廉等优点。输液用塑料制品随着在临床的普遍应用 ,其对药物的吸附作用也逐渐引起国内、外学者的重视。本文将就PVC软袋及一次性输液器的吸附作用对不同药物的影响作一综述。1对作用于循环系统药物的吸附1 1对硝酸甘油的吸附将硝酸甘油注射液存放于PVC袋内 ,4h后…     

PVC输液袋存在的问题

PVC输液袋(简称PVC袋)为无毒聚氯乙烯,主要原料为PVC树脂,柠檬酸脂,环氧大豆油等,在净化条件下经塑化热合而成的新型输液生产包装材料。与玻璃瓶包装输液相比有:投资少、生产安全,生产工序少、体积小、重量轻,便于运输、存放,临床应用方便等优点。但在生产、应用中也存在一些问题。     

HPLC测定PVC输液袋中的邻苯二甲酸二(2-乙基己基)酯

目的 测定PVC输液袋中增塑剂邻苯二甲酸二(2-乙基己基)酯(DEHP)的含量.方法 采用HPLC法,流动相为甲醇-水(90:10),流速为1.0 ml·min-1,检测波长为222 nm.结果 峰面积与DEHP浓度的线性关系良好(r=0.9999).结论 所用方法简便,结果准确可靠.     

PVC输液器与药物相容性研究综述

国内临床上广泛使用PVC输液器。研究表明PVC高分子材料对药物有不稳定性,加入邻苯二甲酸二(DEHP)后可能释放对人体有危害的物质进入药液,但大多数不会产生不良反应,对男性胎儿、新生儿和青春发育期的男性等特殊人群有潜在的高危风险,对有些药物的吸附作用使其有效浓度下降而被认为效差或无效。因此,建议研发安全、无吸附的输液器取代PVC输液器,并加强与药物相容性监测,便于指导和监管安全用药。     

3种不同材质输液容器对8种药物的吸附性研究

目的考察8种药品在3种不同材质输液容器（PVC输液袋、M312C非PVC输液袋、玻璃输液瓶）中的吸附性。方法将8种药品溶于上述3种不同材质容器的输液中,分别于混匀后的0、1、3、24、48h取样,采用高效液相色谱法测定药物浓度。结果当药物于输液中混合48h后,药物的含量与0h相比：①在PVC输液袋中,胺碘酮、氯丙嗪的含量下降至76.76%-89.84%之间;②在M312C非PVC输液袋及玻璃输液瓶中,除在水溶液中不稳定的药物外,其他药物含量下降均小于10%。结论PVC输液袋会对一些药物有吸附性,临床应避免这些药物在PVC输液袋中使用。     

3种材质输液容器对药物的相容性及吸附性考察

目的:考察非聚氯乙烯(PVC)多层共挤复合膜输液袋、PVC输液袋和玻璃瓶与大输液的相容性及3种材质输液容器对6种药物的吸附性。方法:将5%葡萄糖注射液(5%GS)、0.9%氯化钠注射液(0.9%NaCl)分别置于3种材质输液容器中存放1y,观察、测定并比较5%GS、0.9%NaCl各质量控制指标及其变化;将一定量6种药品加入3种包装材质输液中,与输液混合均匀后分别于0、1、24h时测定药物浓度,并与0h时比较。结果:与玻璃瓶比较非PVC和PVC材质输液容器中5%GS、0.9%NaCl多数检测指标结果无显著性差异(P>0.05),但PVC材质中2种大输液含量下降(P<0.05);在PVC输液袋中,胰岛素、硝酸异山梨酯和硝酸甘油含量在34.44%～80.80%之间,含量下降百分比与玻璃瓶比较具有统计学差异(P<0.05);在玻璃瓶中,硝酸异山梨酯和硝酸甘油含量为72.83%～81.86%,含量下降百分比与非PVC比较具有统计学差异(P<0.05)。结论:PVC及玻璃瓶材质对部分药物有吸附性,应引起临床注意;非PVC材质与大输液相容性良好,对药物吸附性较小。     

国产直立式聚丙烯输液袋临床实用性考察

目的：考察直立式聚丙烯输液袋的临床应用情况。方法：从全密闭式输液功能、对药物的吸附作用以及输液操作效率等方面对比直立式聚丙烯输液袋与玻璃瓶、PVC软袋、非PVC软袋,考察其,临床应用特点。结果：PVC软袋对胰岛素、硝酸甘油和紫杉醇均有不同程度的吸附,尤其对紫杉醇的吸附率高达90％以上;而玻璃瓶、非PVC软袋和直立式聚丙烯输液袋对上述3种药物几乎无吸附作用。PVC软袋、非PVC软袋和直立式聚丙烯输液袋3种输液的输液持续时间及最终输注速度差异均无统计学意义（P〉0．05）。结论：直立式聚丙烯输液袋具有与PVC软袋、非PVC软袋完全等同的全密闭输液功能,对PVC软袋易吸附的药物无任何吸附作用,便于临床应用,值得推广。     

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.