高效液相色谱法测定复方新斯的明滴眼液中甲硫酸新斯的明的含量

目的:建立复方新斯的明滴眼液中甲硫酸新斯的明的测定方法。方法:采用高效液相色谱法,色谱柱为Komasil C18 (150 mm×4．6 mm,5μm),流动相为庚烷磺酸钠溶液(取庚烷磺酸钠4．04 g,磷酸二氢钠2．72 g溶于1 000 ml水中,加三乙胺1．2 ml,用磷酸调节pH=3．0)-乙腈(82∶18),流速为1．0 ml·min-1,检测波长为260 nm。结果:甲硫酸新斯的明在1．01-9．09μg范围内线性关系良好,r=0．999 9,加样回收率为99．7％,RDS为0．93％。结论:该方法具有简便、准确等优点,可用于本制剂的质量控制。     

紫外分光光度法测定新斯的明片中新斯的明的含量

目的:建立测定新斯的明片中新斯的明含量的方法。方法:采用紫外分光光度法。以水为溶剂,在260nm波长下测定新斯的明的含量。结果:新斯的明检测浓度在80～560μg·mL-1范围内与吸光度线性关系良好(r=0.9999);平均回收率为100.7%,RSD=0.65%(n=9)。结论:该法操作简便、精密度好,结果可靠,可用于新斯的明片的含量测定。     

产后康复仪结合新斯的明穴位注射治疗产后尿潴留的疗效观察与护理

目的探讨产后康复仪结合甲硫酸新斯的明穴位注射治疗产后尿潴留的疗效观察与护理。方法对42例产后尿潴留患者随机分成观察组(使用产后康复仪结合甲硫酸新斯的明0.5mg穴位注射)和对照组(单独使用甲硫酸新斯的明0.5mg穴位注射),两组同时进行疗效观察与护理。结果观察组21例,有效19例(90.47%),无效为2例(9.53%);对照组21例,有效10例(47.62%),无效11例(52.38%)。经统计学处理,P<0.01,提示观察组疗效明显优于对照组。结论临床应用产后康复仪结合甲硫酸新斯的明穴位注射治疗产后尿潴留有较好的效果,外加精心的护理,患者更易接受,值得临床推广应用。     

高效液相色谱法测定复方利血平片中4种成分的含量

目的:建立同时测定复方利血平片中硫酸双肼屈嗪、氢氯噻嗪、维生素B_1和维生素B_6含量的高效液相色谱法。方法:采用Hypersil BDS C_(18)柱(200mm×4.6mm,5μm);流动相为0.01mol·L~(-1)庚烷磺酸钠溶液-乙腈-甲醇-三乙胺(65:20:15:0.02),用5%磷酸溶液调节pH至3.6;检测波长为240nm。结果:硫酸双肼屈嗪在32.5～406.7μg·ml~(-1)(r=0.999 2),氢氯噻嗪在24.4～304.4μg·ml~(-1)(r=0.999 4),维生素B_1在8.5～106.6μg·ml~(-1)(r=0.999 3),维生素B_6在8.5～106.0μg·ml~(-1) (r=0.999 1)浓度范围内线性关系良好;硫酸双肼屈嗪回收率为100.2%,RSD为0.8%(n=9),氢氯噻嗪回收率为99.7%,RSD为1.0%(n=9),维生素B_1回收率为100.0%,RSD为0.9%(n=9),维生素B_6回收率为100.5%,RSD为0.9%(n=9)。结论:本法操作简便、快捷,结果准确,可用于复方利血平片的质量控制。     

HPLC测定复方新斯的明眼用凝胶中甲硫酸新斯的明含量

目的：建立甲硫酸新斯的明的含量测定方法。方法：采用HPLC法,色谱柱：Eclipse XDB—C18柱（150mm×4．6mm,5μm）,流动相：甲醇-磷酸二氢铵溶液-水（20：50：30）,检测波长：210nm。结果：线性范围为0．24～3．84μg·ml^-1,r=0．9999（n=5）。平均回收率为101．46％.结论：本方法简便快速、专属性好、重复性好、易操作。     

HPLC 法测定甲硫酸新斯的明注射液的含量

目的：建立 HPLC 法测定甲硫酸新斯的明注射液的含量。方法用 Agilent ZORBAX Eclipse XDB C18（250 mm ×4．6 mm,5μm）,以0．05 moL·L －1磷酸二氢钾溶液（用磷酸调节 pH 为3．0）—乙腈（90∶10）为流动相,流速为1．0 mL·min －1,检测波长为215 nm。结果甲硫酸新斯的明线性范围为在0．102～1．02 g·L －1（r ＝0．9999）;平均回收率为99．57％,RSD 为0．93％。结论该方法灵敏,快速,结果准确,可用于甲硫酸新斯的明注射液的质量控制。     

五香血藤中五味子醇甲与五味子甲素含量测定

目的建立同时测定五香血藤中五味子醇甲与五味子甲素含量的高效液相色谱法。方法采用反相高效液相色谱法,C18色谱柱(4.6 mm×250 mm,5μm),乙腈(A)-水(B)为流动相,梯度洗脱,流速1 mL.min-1,五味子醇甲检测波长216 nm,五味子甲素检测波长209 nm。结果五味子醇甲在0.019 6～0.215 6μg之间线性关系良好,回收率99.11%,RSD=2.02%(n=9);五味子甲素在0.018 4～0.147 2μg之间线性关系良好,回收率102.35%,RSD=1.73%(n=9)。结论该方法简便、准确,可用于五香血藤中五味子醇甲与五味子甲素的含量测定。     

顶空气相色谱法测定溴吡斯的明原料药中的残留溶剂

目的采用顶空气相色谱法测定溴吡斯的明原料药中的残留溶剂。方法色谱柱为PEG-20M(38 mm×0.25mm,0.32μm),氢火焰离子化检测器,载气为氮气,进样口温度为200℃,检测器温度为250℃。柱温为程序升温:初始温度50℃,保持5 min,再以10℃.min-1的速率升温至150℃,保持5 min,顶空条件:顶空平衡温度80℃,平衡时间30 min。结果该方法中溴吡斯的明的残留溶剂得到了较好的分离与测定。丙酮在0.25~0.75 mg.mL-1,乙醇在0.25~0.75 mg.mL-1,甲苯在0.044 5~0.133 5 mg.mL1线性关系良好,相关系数分别为0.999 2、0.998 2、0.995 6。丙酮、乙醇和甲苯的精密度(RSD)分别为3.2%、2.8%、4.1%(n=6),回收率分别为100.5%(RSD=4.6%)、98.4%(RSD=5.5%)和101.2%(RSD=3.7%)(n=6)。结论该方法可用于溴吡斯的明原料药中的残留溶剂测定。     

紫外分光光度法测定溴吡斯的明片中溴吡斯的明的含量

目的:建立测定溴吡斯的明片中溴吡斯的明含量的方法。方法:采用紫外分光光度法,以去离子水为空白,在269nm波长处测定溴吡斯的明的含量。结果:溴吡斯的明检测浓度在16.56～41.40μg·mL-(1r=0.9999)范围内与吸光度呈良好的线性关系;平均回收率为99.87%,RSD=0.19%(n=9)。结论:该法操作简便、精密度好、结果可靠,适用于溴吡斯的明片中溴吡斯的明含量的快速测定。     

RP-HPLC测定注射用甲硫酸新斯的明含量的方法学研究

目的:高效液相色谱法测定注射用甲硫酸新斯的明的含量。方法:SHIMADZU C_8柱(250 mm×4.6 mm,5 μm),以0.05mol·L~(-1)磷酸二氢钾(用磷酸调 pH 至3)-乙腈(87:13),流速为1.0 mL·min~(-1),检测波长为260 nm。结果:高效液相色谱法测定的线性范围为0.32～0.72 mg·mL~(-1),相关系数为0.9997;供试品溶液至少8h 内稳定(RSD=0.70%);方法精密度良好(RSD=0.60%);回收率为99.1%～99.8%,RSD 为0.54%～0.66%;重复性 RSD 为0.49%。结论:本方法结果准确,重复性好,可用于该制剂的质量控制。     

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.     

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.     

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.