HPILC法测定盐酸胺碘酮片的含量

目的 建立盐酸胺碘酮片的含量测定方法.方法 采用C18柱(4.6×250 mm,5μm),以2%三乙胺(用磷酸调pH值至4.0)-甲醇(20:80)为流动相,检测波长241nm,流速为1.0 ml/min.结果 盐酸胺碘酮在9.88～148.20μg/ml范围内与峰面积有良好的线性关系(r=0.9999),平均回收率为99.45%,RSD为0.96%.结论 该方法准确,可靠,可用于盐酸胺碘酮片的质量控制.     

HPILC法测定盐酸胺碘酮片的含量

目的建立盐酸胺碘酮片的含量测定方法。方法采用C18柱(4.6×250 mm,5μm),以2%三乙胺(用磷酸调pH值至4.0)-甲醇(20∶80)为流动相,检测波长241 nm,流速为1.0 ml/min。结果盐酸胺碘酮在9.88~148.20μg/ml范围内与峰面积有良好的线性关系(r=0.9999),平均回收率为99.45%,RSD为0.96%。结论该方法准确,可靠,可用于盐酸胺碘酮片的质量控制。     

氧瓶燃烧—高效液相色谱法测定药物中有机碘含量

目的：高效液相色谱法测定药物中有机碘含量。方法：氧瓶燃烧后,采用高效液相色谱法。Shim-packCLC-NH2柱,1%磷酸二氢钾（pH=4)溶液-甲醇（80：20）为流动相,流速为0.7ml/min,220nm波长检测。结果：测定盐酸胺碘酮,泛影酸与安妥碘中有机碘的含量,重现性好,盐酸胺碘酮的变异系数为1.12%(n=6)。结论：氧瓶燃烧-高效液相色谱法可用于测定药物中有机碘的含量。     

盐酸胺碘酮分散片人体生物等效性研究

目的:研究盐酸胺碘酮分散片的人体生物等效性。方法:采用双周期交叉试验设计,18名健康男性受试者随机交叉单剂量口服盐酸胺碘酮分散片(受试制剂)与盐酸胺碘酮片(参比制剂)400mg,采用液-质联用(LC-MS)法测定人血浆中盐酸胺碘酮经-时血药浓度,利用SPSS10.0统计软件计算药动学参数,评价二制剂的生物等效性。结果:受试制剂与参比制剂的tmax分别为(4.2±1.2)、(3.8±0.9)h,Cmax分别为(420.0±211.7)、(414.8±166.7)ng.mL-1,t1/2分别为(38.8±20.4)、(39.6±12.5)h,AUC0～96分别为(6 375.3±3 093.1)、(6 518.4±3 101.1)ng.h.mL-1,AUC0～∞分别为(7 165.3±3 680.2)、(7 325.5±3478.1)ng.h.mL-1。受试制剂中盐酸胺碘酮的相对生物利用度为(98.4±8.4)%。结论:盐酸胺碘酮分散片与盐酸胺碘酮片具有生物等效性。     

盐酸胺碘酮注射液

本品为盐酸胺碘酮的灭菌水溶液,含盐酸胺碘酮(C₂₅H₂₉I₂NO₅·HCl)应为标示量的90.0~110.0%。[性状]本品为淡黄色的澄明液体。[鉴別]取本品适量(约相当于盐酸胺碘酮0.2g),加氯仿10ml,振摇,氯仿层滤过,滤液蒸干,残渣照盐酸胺碘酮项下的鉴别(1)、(2)、(3)与(5)项(中国药典1990年版二部521页)试验,显相同的结果。     

盐酸胺碘酮注射液与4种临床常用输液的配伍稳定性考察

目的考察盐酸胺碘酮注射液与临床常用4种输液(5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液及0.9%氯化钠注射液)的配伍稳定性。方法采用Hypersil BDS-C18色谱柱(250 mm×4.6mm,5μm),甲醇∶磷酸-三乙胺缓冲液(pH3.2)(65∶35,V/V)为流动相,柱温30℃,流速1.0 mL/min,检测波长242 nm,测定盐酸胺碘酮注射液与上述4种输液在室温下配伍后6 h内不同时间的含量变化,并观察溶液外观性状及pH值的变化。结果本实验所建立的色谱条件对盐酸胺碘酮的检测专属性好,配伍液中盐酸胺碘酮在0.15～2.4 mg/mL浓度范围内,线性关系良好(R2=1),日内RSD值为0.01%,4种配伍液在6 h内峰面积均无明显变化,RSD值均小于2.0%。结论盐酸胺碘酮注射液与4种输液在室温下配伍后6 h内含量、pH值、外观无明显变化,体外配伍稳定。     

盐酸胺碘酮胶囊

本品含盐酸胺碘酮(C₂₅H₂₉I₂NO₃·HCl)应为标示量的90.0~110.0%。[鉴別](1)取本品的内容物适量(约相当于盐酸胺碘酮20mg),加乙醇2ml使溶解,加2,4-二硝基苯肼的高氣酸溶液(取2,4-二硝基苯肼1.2g,加30%高氣酸溶液50ml使溶解)2ml,加水5ml,有黄色沉淀析出。     

精密过滤输液器预防盐酸胺碘酮注射液所致静脉炎的临床观察

盐酸胺碘酮注射液是临床上广泛应用的抗心律失常药物之一,主要用于反复发作、其他药物治疗无效的心房颤动(房颤)、室性心动过速(室速)及心室颤动(室颤)的治疗和预防.盐酸胺碘酮注射液较普通药物所致静脉炎发生率高、发展快[1].有研究表明,外周静脉注射盐酸胺碘酮注射液发生静脉炎的几率可高达88.2%,严重者甚至发生皮肤组织坏死.如何减少盐酸胺碘酮注射液引起的静脉炎,已引起广大护理工作者的重视.我中心于2009年10月～2010年10月对使用盐酸胺碘酮注射液静脉滴注的心律失常患者分别采用普通输液器和精密过滤输液器,并对静脉炎的发生率及严重程度进行对比观察,结果报道如下.     

生殖激素检测在不孕症90例实验诊断中应用

目的 探讨生殖激素检测在不孕症妇女诊断中的应用价值.方法 采用全自动电化学发光分析系统对不孕症90例不同月经周期卵泡刺激素(FSH)、黄体生成素(LH)、雌二醇(E2)、催乳素(PRL)、孕酮(P)、睾酮(T)进行测定,并与正常育龄妇女比较.结果 与正常育龄妇女相比,不孕妇女卵泡期FSH(4.23±2.91 mlu/ml)、E2(38.7±29.6pg/ml)降低,PRL(22.8±24.4ng/ml)升高；排卵期FSH(6.26±3.55 mlu/ml)、LH(8.6±6.48 pg/ml)、E2(87.4±65.8pg/ml)降低；黄体期P(9.6±2.37 (98.9±41.Opg/ml)、LH(5.78±2.03 mlu/ml)升高,差异均有统计学意义(P＜0.05).结论 6项生殖激素的检测对不孕妇女的诊断有重要作用.     

HBeAg阴性HBV感染者不同病毒载量与前S1抗原和大蛋白关系研究

目的 通过定量检测HBeAg阴性HBV感染者血清病毒大蛋白(HBV-LHBS)和前S1(PreS1)抗原,探讨HBV-LHBS和PreS1在反映HBV复制中的作用.方法 收集经荧光定量PCR检测HBV-DNA的120份HBeAg阴性HBV病毒感染者血清,将这些标本按DNA拷贝数分为3组(≥106copies/ml、103～105 copies/ml、≤103 copies/ml),每组各40例,以酶联免疫吸附法(ELISA)检测HBV-LHBS和PreS1抗原.结果 ≥106 copies/ml组,LHBS阳性率和定量检测结果分别为95.0%和(92.12±29.38)ng/ml,103～105 copies/ml组,LHBS阳性率和定量检测结果为72.5%和(33.26±19.44)ng/ml,≤103copies/ml组,LHBS阳性率和定量检测结果为37.5%和(15.02±11.10)ng/ml,3组标本PreS1抗原阳性率依次为80.0%、42.5%、20.0%;LHBS总阳性率为61.6%,PreS1抗原阳性率为38.1%.结论 与PreS1抗原比较,LHBS的测定结果与HBV DNA载量呈现良好的相关性,更能准确地反映HBV感染者体内病毒的复制程度,因此LHBS定量可能成为判断HBV活动的新的血清学指标.     

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.