舒肝宁注射液配伍稳定性的考察

目的 考察不同浓度舒肝宁注射液配制后成品液在不同条件下的质量及稳定性。方法 将10 mL或20 mL舒肝宁注射液与250 mL 10%葡萄糖溶液配伍后,放置于室温、光照（4 500 Lx）、40℃恒温环境下,在不同时间点考察舒肝宁注射液的性状、pH值、不溶性微粒、有效成分（绿原酸、栀子苷和黄芩苷）的含量。结果 舒肝宁注射液成品液在放置过程中性状无明显变化。室温和光照对pH值的影响较小,40℃恒温时低浓度和高浓度溶液随着时间的延长,pH值略有下降。舒肝宁注射液成品液在室温、光照和40℃恒温条件下不溶性微粒24 h内没有超限,符合药典规定。舒肝宁注射液在室温下放置12 h,低浓度和高浓度溶液中3种成分绿原酸、栀子苷、黄芩苷含量变化均不大;24 h光照和40℃恒温条件下3种成分含量均有下降,而40℃恒温对其影响更大。结论 舒肝宁注射液在光照和40℃恒温条件下绿原酸、栀子苷和黄芩苷含量均有下降,室温时比较稳定、下降较少。因此配制后的舒肝宁注射液应放置在室温条件,避免强光照射;建议成品液尽可能在12 h内输注;超过24 h后谨慎使用。     

大株红景天注射液配伍稳定性考察

目的 考察大株红景天注射液配制后溶液在不同条件下的质量稳定性。方法 将10 mL大株红景天注射液与5%葡萄糖注射液250 mL配伍后,放置于室温（10~30℃）、光照（4 500 Lx）、40℃恒温环境下,在不同时间点考察大株红景天注射液的性状、pH值、不溶性微粒和有效成分（红景天苷和酪醇）的含量。结果 大株红景天注射液配伍溶液在放置过程中性状无明显变化,12 h内pH值几乎无变化,24 h内略微下降。光照条件下,溶液在24 h微粒数超出药典规定;其他条件在24 h内微粒数均未超过药典规定。红景天苷含量受光照影响在24 h时下降了5.34%,在室温和40℃恒温条件下放置24 h比较稳定。酪醇24 h内在以上条件下均比较稳定。结论 建议配制后的大株红景天溶液在12 h内输注完毕,超过24 h后需谨慎使用,同时应该避免强光直射。     

注射用艾司奥美拉唑钠配伍稳定性考察

目的 考察注射用艾司奥美拉唑钠与0.9%氯化钠注射液在不同条件下的配伍稳定性。方法 将不同浓度注射用艾司奥美拉唑钠与0.9%氯化钠注射液配伍,然后将配置好的溶液放置于室温、遮光、光照（4 500 Lx）、40℃恒温环境下,定时考察注射用艾司奥美拉唑钠的性状、pH值、不溶性微粒数和艾司奥美拉唑的含量。结果 注射用艾司奥美拉唑钠在放置过程中出现不同程度的颜色变化,变化程度：40℃恒温 > 光照 > 室温 > 遮光。在4种条件下成品液pH值均相对稳定,pH值12 h内几乎无变化,24,48 h内略微下降,40℃恒温下降较多。高浓度溶液在40℃恒温条件下于48 h不溶性微粒数超出药典规定,其他所有溶液的不溶性微粒均符合药典要求。48 h内艾司奥美拉唑的含量也有所下降,40℃恒温条件下降较多。结论 注射用艾司奥美拉唑钠在40℃恒温条件下最不稳定,遮光条件下溶液最稳定。因此建议注射用艾司奥美拉唑成品溶液保存在室温条件下,尽量避光,同时避免高温影响,低浓度溶液（0.4 mg·mL^-1）在配置后12 h内使用,高浓度溶液（1.6 mg·mL^-1）8 h内滴完。     

复方苦参注射液在两种输液中的稳定性考察

摘 要 目的：考察复方苦参配伍液的稳定性,为临床安全用药提供依据。方法: 将复方苦参注射液分别与0.9%氯化钠注射液和5%葡萄糖注射液配伍,在不同条件下放置0,1,2,4,8,12,24,48 h,采用高效液相色谱法,测定配伍液中的4种组分的含量变化,同时考察外观性状、pH、不溶性微粒的变化。结果: 复方苦参注射液在0.9%氯化钠注射液中48 h内稳定,不受光照和温度的影响;在5%葡萄糖注射液中稳定性稍差,室温条件储存不能超过12 h,高温条件下不能超过2 h。结论:复方苦参配伍液的稳定性与溶媒的pH关系密切,建议临床使用0.9%氯化钠注射液作为溶媒,48 h内使用。     

正交试验优选穿琥宁注射液与临床常用输液的配伍条件

目的 研究穿琥宁注射液与临床常用输液的配伍条件。方法 选择温度、光照、放置时间、溶媒种类4个影响因素,以穿琥宁含量、配伍液的pH值变化、不溶性微粒数为检测指标,同时考察不同条件下配伍液中穿琥宁有关物质的限度。结果 在4 h内,穿琥宁注射液与5%葡萄糖注射液及0.9%氯化钠注射液可配伍使用,但不宜与5%的葡萄糖氯化钠注射液配伍。结论 穿琥宁注射液与5%葡萄糖注射液及0.9%氯化钠注射液在4 h内可配伍使用,应尽量避免日光照射与高温环境。     

消癌平注射液与胰岛素在葡萄糖注射液中的配伍稳定性考察

摘 要 目的：考察消癌平注射液与胰岛素在葡萄糖注射液中的配伍稳定性。方法: 观察室温下24h内消癌平注射液与胰岛素在葡萄糖注射液中配伍后溶液外观、不溶性微粒、pH的变化,以及配伍液中绿原酸和胰岛素的含量变化。结果: 配伍液在室温24h内性质稳定、外观、pH无明显变化,无气体沉淀产生、不溶性微粒12h内无明显变化,但24h不溶性微粒数明显升高。主要成分绿原酸及胰岛素的含量均无明显变化。结论: 在该试验条件下,12h内消癌平注射液与胰岛素在5%葡萄糖注射液中配伍稳定。     

注射用红花黄色素与7种输液的配伍稳定性考察

摘 要 目的：考察注射用红花黄色素与果糖注射液,转化糖注射液,转化糖电解质注射液,葡糖糖氯化钠注射液,5%葡萄糖注射液,10%葡萄糖注射液及0.9%氯化钠注射液配伍的稳定性考察。方法: 模拟临床用药浓度,在室温（25±1）℃下放置8 h,以氯化钠配伍液为对照组,分别观察各种配伍液外观,不溶性微粒数量及pH变化,运用高效液相色谱法测定注射用红花黄色素在不同配伍液中的含量变化。结果:注射用红花黄色素与7种输液配伍后在8h内外观,pH和含量均无明显变化,不溶性微粒数符合中国药典2015年版规定。结论:注射用红花黄色素与7种输液配伍在8 h内稳定。     

谷红注射液在临床常用输液中的稳定性考察

摘 要 目的：研究谷红注射液与临床常用输液的配伍稳定性。方法: 采用HPLC DAD法考察谷红注射液与临床常用输液配伍后,分别在5,25,35 ℃,避光,室内光照,紫外线照射条件下,8 h内谷红注射液中7个有效成分乙酰谷酰胺、尿苷、腺苷、鸟苷、紫丁香苷、羟基红花黄色素A 和脱水红花黄色素B的含量变化;采用HPLC法考察乙酰谷酰胺在配伍液中有关物质含量;考察配伍前后溶液外观、不溶性微粒和pH的变化情况。结果: 在8 h内, 各配伍液的外观、pH和不溶性微粒均无明显变化。配伍液中乙酰谷酰胺在紫外光照（35 ℃）的条件下含量有所下降,其余配伍液的各成分含量无明显变化。在避光和室内光照条件下,配伍液的有关物质与配伍前相比无明显变化,杂质的总含量符合有关规定;而在紫外光照射下,随着温度的升高和放置时间的延长,配伍液中的有关物质明显增加。结论:谷红注射液与5%葡萄糖注射液、10%的葡萄糖注射液及氯化钠注射液在4 h内可配伍使用,使用过程中应尽量避免日光照射。     

“即配即用”药物-哌拉西林钠他唑巴坦钠的配伍稳定性考察

摘要：目的 考察“即配即用”药物注射用哌拉西林钠他唑巴坦钠与不同溶媒在不同条件下的配伍稳定性。 方法 注射 用哌拉西林钠他唑巴坦钠与0.9%氯化钠注射液和5%葡萄糖注射液配伍,将配置好的溶液放置于40℃恒温、光照(4500Lx)、遮光 和室温环境下,比较两种规格注射用哌拉西林钠他唑巴坦钠的性状、pH值、不溶性微粒和哌拉西林钠以及他唑巴坦钠的含量随 时间变化情况。结果 注射用哌拉西林钠他唑巴坦钠成品液在放置24h内,颜色未见明显变化。pH值在室温和遮光条件放置24h 后略有下降;高温和光照条件下12h后pH值下降。配置后12h,各配伍液中≥10μm的微粒数目符合2020年版《中华人民共和国 药典》的规定;在40℃恒温条件下,配置后8h配伍液中≥25μm不溶性微粒数目超出药典规定,与2.25g规格注射用哌拉西林钠 他唑巴坦钠配伍液相比,1.25g规格配伍液中≥25μm不溶性微粒数目超出药典规定更多。在室温和遮光条件下两种主要有效成 分的相对百分含量变化不大;在光照(4500 Lx)和40℃恒温条件下放置24h后,两种主要有效成分的相对百分含量均有下降。结 论 配置后8h内,不同规格(2.25g和1.25g)注射用哌拉西林钠他唑巴坦钠的成品输液稳定性无明显差异;配制8h后,2.25g规格配 伍液稳定性优于1.25g规格配伍液;注射用哌拉西林钠他唑巴坦钠与0.9%氯化钠配伍,稳定性更好;高温和光照条件影响其成品 液稳定性,建议注射用哌拉西林钠他唑巴坦钠配置后室温保存,并在8h内输注完毕。     

肾康注射液与5种溶媒配伍的稳定性考察

摘 要 目的： 通过考察肾康注射液与5种常用溶媒配伍的稳定性,选择最佳溶媒配伍方案,以便临床合理用药。方法: 将肾康注射液与5种不同溶媒配伍后,定时考察配伍后溶液的pH、不溶性微粒数、有效物质原儿茶醛的含量变化情况。结果: 5种溶媒按药品说明书比例配伍2 h后不溶性微粒数均有所增加,其中0.9%氯化钠注射液中的不溶性微粒数最多, 且2 h后不溶性微粒数明显增加。5种配伍溶液的pH无明显变化。原儿茶醛的含量随时间的延长而下降,6 h内原儿茶醛的含量变化率：0.9%氯化钠注射液＞5%果糖注射液＞10%转化糖注射液＞5%葡萄糖注射液＞10%葡萄糖注射液,其中0.9%氯化钠注射液中的原儿茶醛含量下降近20%。结论: 肾康注射液在不同溶媒中稳定性不同,用0.9%的氯化钠注射液配伍的注射液中原儿茶醛含量下降明显且不溶性微粒数较多。临床应选择稳定性更好的葡萄糖以及转化糖注射液作为溶媒,配伍后的溶液应尽可能在2 h内用完。     

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.     

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.     

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.