法莫替丁氯化钠注射液含量的吸收系数法测定

目的:建立吸收系数法用于测定法莫替丁氯化钠注射液的含量.方法:采用紫外分光光度法测定法莫替丁氯化钠注射液中法莫替丁的含量,测定波长为266 nm,D1% cm为315.结果:法莫替丁的平均回收率为100.1%,RSD=1.0%(n=5).结论:本法简便、快速、准确,可作为法莫替丁注射液和法莫替丁氯化钠注射液的含量测定方法.     

高效液相法测定法莫替丁氯化钠注射液中法莫替丁含量

目的为了建立高效液相色谱法测定法莫替丁氯化钠注射液中法莫替丁含量。方法用十八烷基硅烷建合硅胶为填充剂,庚烷磺酸钠溶液—乙腈—甲醇(25:6:1)为流动相,检测波长为254nm,流速为O.8ml/min。结果方法的平均回收率为99.54%RSD 为0.8%。精密度为 RSD为0.2%,法莫替丁回归方程为 Y=1.78127×10~4X十2.26374×10~4 V=0.9999 结论:此法能满足法莫替丁氯化钠注射液中法莫替丁含量测定的要求,峰的分离度及对称性良好。     

高效液相色谱法测定法莫替丁氯化钠注射液的含量

目的:建立一种法莫替丁氯化钠注射液高效液相色谱测定方法,用于生产及市场监控。方法:选用C_(18)(150×4.6mm)5μm色谱柱,庚烷磺酸钠-乙腈-甲醇(25:6:1)为流动相,以外标法按峰面积计算。结果:该法回收率为99.84%,表明用该法测定法莫替丁氯化钠注射液的含量是可行的。结论:该法简便、快捷,结果准确,可用于法莫替丁氯化钠注射液的含量测定和质量控制。     

法莫替丁氯化钠注射液的研制及临床疗效观察

目的 :研制法莫替丁氯化钠注射液。方法 :以门冬氨酸为助溶剂 ,以生理盐水为溶媒制备法莫替丁氯化钠注射液。用HPLC法测定法莫替丁及其有关物质的含量 ,同时考察其稳定性和影响因素 ,并观察其临床疗效。结果 :法莫替丁的含量随温度的升高和时间的延长逐渐下降。加速实验法 :40℃条件下 ,法莫替丁氯化钠注射液放置6mo时 ,法莫替丁的含量为98 6 % ;室温留样观察法 :法莫替丁氯化钠注射液放置1y,法莫替丁的含量为98 4 % ;强光照射法 :在4500Lx光照下d10法莫替丁含量为98 5 % ,但有关物质的含量均小于2 %。法莫替丁氯化钠注射液临床总有效率为93 75 %。结论 :法莫替丁氯化钠注射液性质稳定 ,临床应用简便 ,无污染 ,疗效确切     

法莫替丁氯化钠注射液质量标准的相关研究

目的建立法莫替丁氯化钠注射液中法莫替丁含量及有关物质检测的高效液相色谱方法.方法采用Agilent ZORBAX SB-C18(4.6×250mm,5μm)色谱柱,以0.2%(g·L-1)庚烷磺酸钠溶液(用冰醋酸调pH值为3.7)-乙腈-甲醇(33∶7∶3)为流动相,流速1.2mL·min-1,柱温为35℃,检测波长为254nm.结果法莫替丁的浓度在0.0794～0.238mg·L-1范围内有良好的线性关系,r=0.9999,样品的平均回收率为99.58%,RSD为0.91%.结论高效液相色谱法测定法莫替丁氯化钠注射液中的法莫替丁含量和有关物质,方法准确度、精密度高,适合应用于该制剂的质量控制.     

HPLC法测定法莫替丁葡萄糖注射液中5-羟甲基糠醛的含量

目的建立一种快速、灵敏、准确的高效液相色谱法测定法莫替丁葡萄糖注射液中5-羟甲基糠醛的含量。方法HPLC法,以HypersilODS2 C18(4.6mm×250mm,5μm)为色谱柱,0.01 m o l.L-1庚烷磺酸钠溶液为流动相,流速1.0m l.m in-1,检测波长为284nm。结果5-羟甲基糠醛在0.0456μg.mL-1~0.456μg.mL-1浓度范围与峰面积有良好线性关系,r=0.9994。平均回收率为99.4%。RSD=0.91%(n=9)。结论本方法准确、简便、快捷,排除了法莫替丁的干扰,可用于测定法莫替丁葡萄糖注射液中5-羟甲基糠醛含量。     

紫外分光光度法测定法莫替丁葡萄糖注射液的含量

目的建立法莫替丁葡萄糖注射液中法莫替丁的含量测定方法。方法用紫外分光光度法,以pH为4．5的磷酸盐缓冲液为空白。在266nm波长处测定含量。结果法莫替丁质量浓度在5—30μg／mL范围内与吸光度线性关系良好,回归方程为A=0．03097C＋0．0037,r=0．9999（n=6）,平均回收率为99．66％,RSD为0．43％（n=5）。结论所用方法简便、准确、重现性好,可作为该制剂的质量控制方法。     

HPLC法测定法莫替丁氯化钠注射液的含量

目的:建立法莫替丁的含量测定方法,控制法莫替丁制剂的质量。方法:采用高效液相色谱法,以ODS为固定相,庚烷磺酸钠溶液-乙腈(80:20)为流动相,用外标法计算含量。结果:法莫替丁在20.0～160.0μg·ml~(-1)范围内呈良好线性关系,r =0.999 7,平均回收率为100.4%,日内和日间精密度分别为1.1%和0.7%。结论:本方法操作方便,测定结果准确,可用于注射用法莫替丁的含量测定及质量控制。     

法莫替丁氯化钠注射液中法莫替丁含量测定方法的改进

用高效液相色谱法,测定法莫替丁氯化钠注射液中法莫替丁的含量。十八烷基硅烷键合硅胶(5μm)为分析柱。流动相:庚烷磺酸钠溶液(取庚烷磺酸钠2.0g,加水900mL溶解后,用冰醋酸调节pH值为3.9,加水至1000mL)-乙腈-甲醇(25∶6∶1);流速:1.0mL.min-1;检测波长254nm。在进样量为20μL时,法莫替丁在进样浓度50~200μg·mL-1的范围内,峰面积与进样浓度之间呈良好的线性关系。(r=0.9998),重复进样RSD=0.68%。     

注射用加替沙星与注射用法莫替丁的配伍稳定性考察

目的:考察注射用加替沙星与注射用法莫替丁在0.9%氯化钠注射液和5%葡萄糖注射液中的配伍稳定性。方法:在(20±1)℃条件下,分别观察及测定8h内配伍液的外观、pH值及紫外光谱的变化,并用紫外分光光度法测定加替沙星和法莫替丁的含量。结果:2药配伍后,8h内的pH值及含量均无明显变化;另在0.9%氯化钠注射液中8h内与5%葡萄糖注射液中6h内,配伍液的外观无明显变化。结论:注射用加替沙星与注射用法莫替丁在0.9%氯化钠注射液和5%葡萄糖注射液中配伍稳定。     

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.     

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.