果糖注射液的质量控制

目的:探讨果糖注射液的质量控制方法.方法:采用旋光法.结果:果糖浓度在20.022 8～100.114 0 mg/mL范围内旋光度与溶液浓度呈线性关系(r＝0.999 97,n=5),回收率为99.82%,RSD为0.23%(n=4).结论:该制剂稳定,质量控制方法可行.     

旋光法快速测定倍他米松磷酸钠注射液的含量

目的 :建立倍他米松磷酸钠注射液的含量测定方法。方法 :以水为溶剂 ,采用旋光度测定法测定。结果 :倍他米松磷酸钠在 0 .5～ 10 mg/ ml浓度范围内与旋光度值呈良好线性关系 ,回归方程为 :C =10 .8814×α - 0 .0 979( r =0 .9995 ) ,平均回收率 :99.4 % ,RSD=1.0 1%。结论 :该方法简便 ,快速 ,准确。     

旋光法测定硝酸毛果芸香碱滴眼液含量

目的建立旋光法测定硝酸毛果芸香碱滴眼液含量.方法采用旋光法测定.结果硝酸毛果芸香碱浓度为5～25mg·ml-1范围内旋光度与浓度呈良好线性关系,r=1.0000.平均回收率为99.3%,RSD为0.4%(n=5).结论本法快速、准确可靠.     

旋光法测定舒巴坦钠的含量

目的建立旋光法测定舒巴坦钠含量的方法.方法以水为溶剂,运用旋光法对舒巴坦钠进行含量测定.结果舒巴坦钠浓度在1～25 mg/ml范围内与其旋光度呈良好线性关系,回归方程:C=4.0397a-0.0402,r=0.9999,平均回收率99.7%,RSD为0.8%(n=5).结论本法简便易行,结果准确,可作为该原料的质控方法.     

HPLC法和旋光光度法测定布洛芬注射液中精氨酸含量的方法比较

目的采用HPLC法和旋光度法测定布洛芬注射液中精氨酸的含量,并从中选择适宜的方法。方法 HPLC法采用Kromasil NH2色谱柱(250 mm×4.6 mm,5μm),以乙腈-磷酸氢二钾溶液(取磷酸氢二钾4.56 g,加水1 000 mL使溶解,磷酸溶液调节pH值至3.5)(体积比57∶43)为流动相,流速1.0 mL.min-1,检测波长214 nm,柱温30℃;旋光度法照《中华人民共和国药典》2010版附录ⅥE旋光度测定法项下的方法操作直接测定布洛芬注射液的旋光度。结果 HPLC法:主药布洛芬与精氨酸分离度良好,精氨酸质量浓度在0.078～0.780 g.L-1内与峰面积呈良好的线性关系,回归方程为A=8.016×104ρ-1.039×103(r=0.999 8,n=6),方法的最低检测限为150 ng,平均回收率为99.72%,RSD为0.98%(n=9);旋光度法:主药布洛芬不干扰精氨酸测定,溶液质量浓度在63.0101.0 g.L-1内旋光度线性关系良好,回归方程为α=104.5ρ-3.039(r=0.999 7,n=6),平均回收率为99.10%,RSD为0.58%(n=9)。结论两种方法均适用于布洛芬注射液中精氨酸的含量测定,可有效测定精氨酸的含量,测定结果也比较一致。相比较而言,旋光度测定法简便快速。     

旋光法测定薄荷醑中薄荷油的含量

目的:测定10%薄荷醑中薄荷油的含量。方法:用旋光度测定法测定薄荷油含量。结果:薄荷油在8%～12%浓度范围内与旋光度呈良好的线性关系(r=0.999 9),方法的平均回收率为99.6%,RSD=1.4%。结论:本方法操作简便、快速,结果准确,重现性好。     

旋光法测定硫酸阿米卡星注射液含量

目的 :建立硫酸阿米卡星注射液含量测定方法。方法 :以水为溶剂 ,运用旋光法测定硫酸阿米卡星注射液含量。结果 :阿米卡星在 1～ 2 0 mg/ml范围内浓度与旋光度呈良好线性关系 ,回归方程 :C =7.892 7A - 0 .0 35 5 ,r =0 .9999,平均回收率 99.8% ,RSD为 0 .89% (n =5 )。结论 :本法简便易行 ,结果准确 ,可作为该制剂的质控方法     

测定0.5%盐酸麻黄碱滴鼻液含量方法比较分析

目的:选择0.5%盐酸麻黄碱滴鼻液的含量测定方法.方法:将旋光度法,酸碱滴定法,紫外分光光度法测定0.5%盐酸麻黄碱滴鼻液含量的方法进行比较.结果:旋光度法在2.5～20 mg·ml-1之间线性关系良好(r=0.999 8),平均回收率为100.1%,RSD=0.089%.结论:用旋光度法测定0.5%盐酸麻黄碱滴鼻液的含量简便快速,结果可靠.     

旋光度测定法测定硫酸阿米卡星注射液中主药的含量

目的:建立以旋光度测定法测定硫酸阿米卡星注射液中主药含量的方法。方法:以水为溶剂,用1dm测定管测定硫酸阿米卡星注射液在589·4nm波长下的旋光度。结果:阿米卡星检测浓度在1~20mg/ml范围内与旋光度线性关系良好(r=0·9999),平均加样回收率为99·8%(RSD=0·89%,n=5)。结论:本方法简便、快速、准确,可用于本品的质量控制。     

旋光法测定硫酸安普霉素的含量

目的采用旋光测定法检测硫酸安普霉素发酵过程中以及提取分离精制过程中中间体的浓度。方法通过测定硫酸安普霉素的旋光度来计算其浓度。结果平均回收率为99.93%,RSD为0.30%(n=5),硫酸安普霉素的浓度与其旋光度呈现良好的线性关系。线性范围550～2200μg·ml-1(γ=0.9998)。结论该方法测定硫酸安普霉素的浓度,结果准确,重现性好。     

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.