气滞胃痛片质量标准的研究

目的:完善气滞胃痛片的质量标准.方法:采用薄层色谱法鉴别制剂中的延胡索、白芍、甘草、枳壳、香附;采用HPLC法测定制剂中白芍、枳壳、延胡索的含量.白芍、枳壳含量采用Waters C18色谱柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.1％磷酸溶液(14∶ 86),流速为1.0 ml·min-1,检测波长为230 nm,柱温为30℃,进样量为10 μl;延胡索含量采用迪马C18色谱柱(250 mm×4.6 mm,5μm),流动相为甲醇-0.17％磷酸溶液(26∶ 74),检测波长为280 nm,流速为1.0ml·min-1,柱温为30℃,进样量为10 μl.结果:鉴别阴性对照均无干扰;含量测定方法中芍药苷、柚皮苷的线性范围分别为0.098 7～1.973 8μg(r =0.999 9)和0.054 7 ～ 1.641 0μg(r =0.999 9),回收率分别为99.3％(RSD=0.81％,n=6)和99.1％(RSD=0.57％,n=6).含量测定方法中延胡索乙素的线性范围为0.050 6～1.215 6 μg(r =0.999 9),回收率为98.4％ (RSD=1.2％,n=6).结论:所建方法简单、可靠,可用于气滞胃痛片的质量控制.     

HPLC测定金酸萍胶囊中的大黄素

目的 采用HPLC法测定金酸萍胶囊中大黄素的含量.方法 采用Waters C18色谱柱(150 mm ×3.9 mm,5μm),流动相为甲醇-0.1％磷酸溶液(85∶15),柱温30℃,流速1.0 mL·min-1,检测波长254 nm.结果 大黄素的回归方程为:Y=3.149×103X-3.687×103(r =0.9994),0.232～1.86 μg大黄素与峰面积的线性关系良好,平均回收率为97.52％,RSD=2.04％(n=6),精密度和重复性的RSD分别为2.09％、1.64％(n=5).结论 所用方法灵敏度高、结果准确、重复性好,可用于金酸萍胶囊的质量控制.     

HPLC测定毛大丁草中的熊果苷

目的 采用RP-HPLC法测定毛大丁草药材中的熊果苷.方法 色谱柱为DiamonsilTM C18柱(150 mm ×4.6 mm,5 μm),柱温35℃,流动相为甲醇-水(5:95),检测波长280 nm.结果 熊果苷0.739 ～4.434 μg与峰面积线性关系良好;平均加样回收率为99.58％,RSD=1.1％.结论 所用方法专属性强、准确、重复性好,为毛大丁草药材质量标准的提高及完善提供了依据.     

HPLC测定通痹活络丸中的绿原酸

目的 采用RP-HPLC法测定通痹活络丸中绿原酸的含量.方法 采用Agilent Eclipse XDB C18柱(250 mm×4.6 mm,5 μm),流动相为乙腈-0.2％磷酸(9∶91),流速1.0 mL· min-1,检测波长327 nm,柱温35℃.结果 绿原酸0.0176～0.1756 μg与峰面积的线性关系良好(r=0.9999).平均加样回收率为101.5％,RSD =3.2％(n=9).结论 所用方法灵敏、准确、快速,重复性好,可用于通痹活络丸的质量控制.     

HPLC测定易瑞沙中的吉非替尼及有关物质

目的 采用HPLC法测定易瑞沙中吉非替尼及有关物质的含量.方法 色谱柱为Luna C18柱(150 mm ×4.6 mm,5 μm),柱温30℃,流动相为甲醇-水-三氟乙酸(55∶45∶1),流速1 mL· min-1,检测波长为250 nm.结果 吉非替尼0.0816～0.7344 μg与峰面积呈良好的线性关系,回归方程为:y=4.854×103X+ 24.31(r=0.9999),平均回收率为99.80％,RSD=1.03％(n=6),与有关物质分离良好.结论 所用方法快速、简便、准确,可作为控制产品质量的依据.     

HPLC法测定风寒感冒颗粒中5-0-甲基维斯阿米醇苷的含量

目的 建立HPLC法测定风寒感冒颗粒中5-0-甲基维斯阿米醇苷的含量.方法 采用phenomenex Luna -C18柱(200 mm×4.60 mm,5μm),流动相为甲醇-水(35:65),流速为1.00 ml/min,检测波长254 nm,柱温为28℃.结果 5-0-甲基维斯阿米醇苷进样量在0.02804～ 0.3084 μg范围内与峰面积线性关系良好,r =0.9997(n =6),平均回收率为100.42％,RSD为0.99％(n=9).结论 该方法简便、准确、可靠、重现性好,可用于该制剂的质量控制.     

HPLC测定假蒟中的α-细辛脑及其含量的动态积累

目的 采用HPLC法测定假蒟中α-细辛脑的含量,观察其动态积累变化.方法 色谱柱为phenomenex ODS2柱(250mm×4.60 mm,5μm),流动相为乙腈-0.05％磷酸溶液(49∶51),流速1.0 mL· min-1,检测波长313 nm,柱温30℃.结果 α-细辛脑0.0975 ～ 1.9500 μg与峰面积的线性关系良好(r=0.9998),平均回收率为101.59％(RSD=2.10％,n=6).结论 所用方法简便、快捷、重复性好,可作为假蒟药材中α-细辛脑的含量测定方法.     

HPLC测定艳山姜中的去甲氧基醉椒素

目的 采用HPLC测定艳山姜中的去甲氧基醉椒素.方法 色谱柱为Agilent Eclipse XDB-C18柱(150 mm ×4.6 mm,5 μm),流动相为水-乙腈(80:20),流速为1 mL· min-1,检测波长345 nm,柱温25℃.结果 去甲氧基醉椒素0.408 ～2.040 μ g与峰面积的线性关系良好(r=0.9993);平均回收率为99.15％ (RSD=1.20％).结论 所用方法简便、准确,重复性好,可作为艳山姜药材的质量控制方法.     

高效液相色谱法测定养胃宁胶囊中大黄酚含量

目的 建立养胃宁胶囊中大黄酚的含量测定方法.方法 色谱柱为Phenomenex C18柱(250mm×4.6mm,5μm),流动相为甲醇-0.1％磷酸(70∶30),流速为1.0mL/min,柱温为35℃,检测波长为254 nm.结果 大黄酚进样量在41.68～208.4 ng范围内与峰面积线性关系良好,回归方程为Y=5 484.98X-4 707.53(r=0.999 998),平均回收率为99.23％,RSD=1.37％(n=6).结论 所用方法简便、快捷、准确、专属性强,可用于养胃宁胶囊的质量控制.     

HPLC测定小儿热咳口服液中的盐酸麻黄碱

目的 采用HPLC法测定小儿热咳口服液中盐酸麻黄碱的含量.方法 采用Hypersil BDS C18色谱柱(250 mm×4.6μm,5μm),流动相为乙腈-1％磷酸(3∶97),流速1.0 mL· min-1,检测波长206 nm,柱温25 ℃.结果 盐酸麻黄碱对照品的线性范围为12.0 ～ 120.0 μg·mL-1(r =0.9996),平均回收率为97.7％,RSD=1.9％(n=6).结论 所用方法快速、简便、重复性好,可用于小儿热咳口服液的质量控制.     

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.     

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.