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。     

大株红景天注射液与不同溶媒配伍的不溶性微粒考察

摘 要 目的： 考察大株红景天注射液在常用的4种溶媒（0.9%氯化钠注射液、5%葡萄糖注射液、果糖注射液、木糖醇氯化钠注射液）中配伍的稳定性。方法: 采用《中国药典》2010年版规定的方法考察大株红景天注射液与4种溶媒配伍后分别在0,0.5,1,2,4,8 h内产生不溶性微粒数量和pH的变化。结果: 在8 h内大株红景天注射液与4种溶媒配伍后的外观及pH无明显变化。在0.9%氯化钠注射液,5%葡萄糖注射液中的不溶性微粒数符合药典规定。0.9%氯化钠注射液中不溶性微粒数量小于5%葡萄糖注射液。在果糖注射液中不溶性微粒数超过药典标准,尤其在4h不溶性微粒数明显增多。在木糖醇氯化钠注射液中不溶性微粒数略高于药典标准。结论:建议大株红景天注射液选用0.9%氯化钠注射液,5%葡萄糖注射液做溶媒。不推荐果糖注射液,木糖醇氯化钠注射液做溶媒。虽然说明书未提及大株红景天注射液用0.9%氯化钠注射液做溶媒。本试验可为糖代谢异常患者用药提供一个参考依据。     

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。     

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。     

注射用肌氨肽苷与不同输液配伍的稳定性考察

摘 要 目的：考察注射用肌氨肽苷与不同输液配伍后的稳定性,为临床应用提供依据。方法: 考察注射用肌氨肽苷分别与0.9%氯化钠注射液、5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液的配伍溶液在0,0.5,1,2,4,8 h时的外观、pH、不溶性微粒数及次黄嘌呤和多肽含量的变化情况。 结果: 不同配物溶液均为澄明液体,pH无明显变化,次黄嘌呤和多肽的含量均符合要求。与10%葡萄糖注射液配伍时,≥10 μm的不溶性微粒数最少,符合中国药典2015年版四部规定,与0.9%氯化钠注射液、5%葡萄糖注射液和葡萄糖氯化钠注射液配伍时,个别时间点的≥10 μm不溶性微粒数不符合规定;各配伍溶液≥25 μm的不溶性微粒数均符合规定。结论:注射用肌氨肽苷最适配伍溶媒为10%葡萄糖注射液。     

正交试验法优选灯盏细辛注射液配伍条件及配伍液的稳定性考察

摘 要 目的： 优选灯盏细辛注射液的配伍条件,并考察配伍液的稳定性。方法: 采用正交试验,以不溶性微粒数量和总黄酮含量为指标性成分,考察温度、溶媒种类、溶媒用量3个影响因素,并对试验结果进行综合分析。按正交试验优选的配伍条件,配制3批样品,24 h内通过外观的观察、溶液不溶性微粒数量、pH以及总黄酮含量的变化来考察灯盏细辛注射液的配伍稳定性。结果: 优选出灯盏细辛注射液最佳配伍条件为：温度25℃、取灯盏细辛注射液2支以0.9%氯化钠注射液250 ml作溶媒。24 h内配伍液的外观、不溶性微粒及pH均无明显变化,4 h内总黄酮的含量也无明显变化,而在4 h后总黄酮的含量有一定程度的下降。结论:在临床用药剂量下,灯盏细辛注射液与0.9%氯化钠注射液250 ml 4 h内可稳定配伍。     

3个厂家银杏叶提取物注射液在两种溶媒中的稳定性考察

摘 要 目的：考察3个不同厂家的银杏叶提取物注射液与两种溶媒（0.9%氯化钠注射液和5%葡萄糖注射液）配伍后不同时间和不同条件（常温、高温和光照）下的稳定性。方法: 银杏叶提取物注射液与2种溶媒配伍后,分为常温组、高温组及光照组,考察各组成品输液的外观、不溶性微粒、pH及水解后黄酮类化合物含量变化,其中外观、不溶性微粒按中国药典2015年版四部通则项下特性检查法进行检测,黄酮类化合物含量采用HPLC UV法测定。结果:各成品输液24 h内无明显浑浊和沉淀,色泽无明显变化,为黄色澄清液,pH和微粒值无明显变化;5%葡萄糖注射液的成品输液pH较0.9%氯化钠注射液偏低,但均符合成品输液的pH要求;各成品输液中的槲皮素、异鼠李素于24 h内含量基本保持不变,神威药业的山奈酚含量较其他两个厂家偏高,但均在标准范围内。结论:3个不同厂家的成品输液在不同条件下的含量均较稳定。     

前列地尔脂微球载体制剂在生理盐水和葡萄糖注射液中的稳定性研究

目的 考察前列地尔脂微球载体制剂与生理盐水、5％葡萄糖注射液配伍的稳定性.方法 在室温25℃避光条件下,考察配伍液的pH值及外观的变化,采用高效液相色谱法测定前列地尔配伍液在0～4 h含量及有关物质的变化,并采用静态激光散射计测定配伍液的平均粒径、90％累积粒径的变化.结果 前列地尔脂微球载体制剂分别与生理盐水注射液、5％葡萄糖注射液配伍后4h内pH值、外观、含量、有关物质、平均粒径及90％累积粒径均未发生明显变化.结论 前列地尔脂微球载体制剂在室温避光条件下放置4h内稳定性较好,各项指标均符合国家标准,临床使用时可以依照病人情况选用静脉滴注的方式给药.     

疏血通注射液与5种溶媒配伍的稳定性研究

摘 要 目的：考察疏血通注射液与临床常用5种溶媒配伍的稳定性,以保障临床用药安全。方法: 疏血通注射液分别选择0.9%氯化钠注射液、5%葡萄糖溶液、10%葡萄糖溶液、甘油果糖注射液、木糖醇注射液等5种临床常用溶媒稀释后,考察pH、摩尔渗透压、不溶性微粒、可见异物、有关物质、指纹图谱等指标以及进行热原检查。结果: 这些溶媒与疏血通注射液配伍后,pH、摩尔渗透压、不溶性微粒均在合理的范围内,未检出可见异物和蛋白类物质,且在24 h内基本保持稳定,其指纹图谱与标准对照图谱基本一致。结论: 疏血通注射液与0.9%氯化钠注射液、5%葡萄糖注射液、10%葡萄糖溶液、甘油果糖注射液、木糖醇注射液等配伍后各项检测指标正常;但10%葡萄糖溶液、甘油果糖注射液、木糖醇注射液等的摩尔渗透压本身偏高,不适宜作为疏血通注射液的溶媒,0.9%氯化钠注射液和5%葡萄糖注射液与人体具有等渗环境,适宜临床配伍使用。     

盐酸曲马多与硫酸镁注射液在氯化钠注射液中的配伍稳定性研究

目的 考察盐酸曲马多注射液与硫酸镁注射液配伍的稳定性,为临床用药安全提供依据。方法 模拟临床用药方案,观察盐酸曲马多与硫酸镁注射液在0.9%氯化钠注射液配伍后,在168 h内的外观、pH值及不溶性微粒变化,并采用高效液相色谱法测定盐酸曲马多质量浓度的变化。结果 配伍液在室温条件下外观、pH值及不溶性微粒均无明显变化,两药配伍后盐酸曲马多相对质量浓度>99%。结论 盐酸曲马多注射液与硫酸镁注射液在0.9%氯化钠注射液配伍后,在室温条件下168 h可保持稳定。     

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.

---

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.