乌芪舒筋通络片质量标准的研究

目的 建立乌芪舒筋通络片的质量控制方法。方法 用薄层色谱法鉴定方中续断、黄芪、防已、牛膝,用高效液相色谱法测定方中细辛的细辛脂素含量。结果 续断、黄芪、防已、牛膝的薄层色谱法鉴别专属性强,阴性无干扰;细辛脂素在46.05~460.5 ng（r=1.000）内呈良好的线性关系,平均加样回收率为100.4%（n=9）,RSD为1.86%。结论 本方法简便,专属性强,重复性好,可作为乌芪舒筋通络片的质量标准。     

驱铅颗粒质量标准研究

摘 要 目的:建立驱铅颗粒的质量标准。方法: 采用薄层色谱(TLC)法对制剂中丹参、木香、黄连进行鉴别;采用高效液相色谱(HPLC)法测定制剂中盐酸小檗碱的含量,色谱柱：Hypersil BDS C¹⁸柱（200 mm×4.6 mm,5 μm）柱;流动相：乙腈-0.033 mol·L^-1 KH₂PO4溶液（35∶65）;流速：1.0 ml·min^-1;检测波长：345 nm;柱温：30℃。结果:TLC鉴别丹参酮ⅡA、去氢木香烃内酯、盐酸小檗碱在薄层板上有清晰的斑点,分离效果良好。盐酸小檗碱含量在4.08～130.82 μg·ml^-1浓度范围内线性关系良好(r=0.999 9）,平均回收率为98.1%（RSD=1.46%,n=9）。3批样品中盐酸小檗碱含量分别为0.67,0.71,0.58 mg·g^{-1结论:所建立的薄层鉴别方法专属性强,定量方法简便,准确,可用于驱铅颗粒的质量控制。}     

开胸顺气胶囊质量标准研究

目的 建立开胸顺气胶囊的质量标准。方法 采用薄层色谱法对开胸顺气胶囊中的橙皮苷进行定性鉴别,HPLC测定开胸顺气胶囊中氢溴酸槟榔碱的含量。结果 定性鉴别结果斑点清晰圆整,分离度好,阴性无干扰,易于鉴别;氢溴酸槟榔碱在81.55~1 957.2 μg内线性关系良好(r=1.000),平均回收率为100.6%,RSD为0.88%(n=9)。结论 本法可靠、准确、专属性强,可为开胸顺气胶囊的质量控制提供参考。     

复方汉防己颗粒中野黄芩苷的定性鉴别和含量测定

目的 建立对复方汉防己颗粒中来源于半枝莲的有效成分野黄芩苷的定性鉴别和含量测定方法。方法 采用薄层色谱法对野黄芩苷进行定性鉴别,采用高效液相色谱法进行含量测定。结果 薄层色谱图斑点显色清晰,阴性对照无干扰;含量测定野黄芩苷在22.4~156.8 μg/ml质量浓度范围内与峰面积呈良好线性关系,r=0.9996(n=5),平均加样回收率为97.79%,RSD=0.32%(n=6)。结论 所建立方法专属性强、重现性好,可作为复方汉防己颗粒的质量控制方法。     

HPLC法测定冬柏通淋合剂中盐酸小檗碱的含量

目的 建立HPLC法测定冬柏通淋合剂中盐酸小檗碱的含量。方法 采用 Kromasil C₁₈色谱柱（150 mm×4.6 mm,5 μm）;流动相：乙腈-0.05 mol/L磷酸二氢钠（用磷酸调节pH=3）（28∶72）;流速：1.0 ml/min;柱温：室温（25 ℃）;检测波长：345 nm。结果 盐酸小檗碱在1.00~50.00 μg/ml范围内线性关系良好（r=0.999 6）,平均回收率为104.70%,RSD为1.60%（n=5）。结论 该方法准确、灵敏度高、专属性强、重现性好,对提高冬柏通淋合剂的质量控制标准具有参考意义。     

珍母丸质量标准研究

目的 建立珍母丸的质量标准。方法 采用显微鉴别方法对枸杞子、珍珠母的显微鉴别进行描述，采用薄层色谱法对香附、山茱萸、赤芍进行定性鉴别；采用HPLC测定赤芍中芍药苷的含量，色谱柱为Accurasil C₁₈（250 mm×4.6 mm，5 μm），以乙腈-0.2%磷酸溶液（15∶85）为流动相，流速为1.0 mL·min^-1，检测波长为230 nm，进样量为10 μL。结果 显微、薄层色谱有较强的专属性，赤芍中芍药苷在0.193~2.415 μg内线性关系良好（r=0.999 5），平均回收率为101.56%，RSD为1.45%（n=6）。结论 本方法操作简便，重复性好，可作为珍母丸的质量控制方法。     

康咳灵合剂质量标准研究

目的 建立康咳灵合剂的质量标准。方法 采用薄层色谱法（TLC）对矮地茶、百部进行定性鉴别;采用高效液相色谱法（HPLC）测定岩白菜素的含量。色谱柱为Lichrospher C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：甲醇-水（20：80）;检测波长：275 nm;柱温：30℃;流速：1 ml/min。结果 TLC法能准确鉴别矮地茶和百部,斑点清晰;岩白菜素在0.064 8~0.648 μg（r=0.9998）范围内线性关系良好,平均回收率100.24%（RSD为1.9%,n=6）。结论 本实验建立的方法简便、专属性高、重复性好,结果准确可靠,可用于康咳灵合剂的质量控制。     

复方颠茄合剂质量标准研究

目的 提高复方颠茄合剂的质量控制标准。方法 采用薄层色谱法（TLC）对复方颠茄合剂中的吗啡进行定性鉴别;采用高效液相色谱法（HPLC）测定复方颠茄合剂中吗啡的含量。以WondaSil C₁₈（4.6 mm×150 mm,5 μm）为色谱柱;A相：0.01 mol/L磷酸二氢钾溶液-0.002 5 mol/L庚烷磺酸钠溶液（含0.1%三乙胺,磷酸调pH至2.5）,B相：乙腈,A∶B=90∶10为流动相;流速：1.0 ml/min;检测波长：220 nm;柱温：30 ℃。结果 在TLC图谱中可检出吗啡的特征斑点。吗啡在0.525~10.5 μg/ml范围内与其峰面积线性关系良好（r=0.999 9）,平均回收率为99.44%,RSD= 0.23%（n=9）。结论 本方法简便准确,专属性强,能够用于复方颠茄合剂的含量测定和质量控制。     

清热败毒颗粒剂的质量标准研究

目的 建立清热败毒颗粒剂的质量标准。方法 采用薄层色谱法（TLC）鉴别处方中的板蓝根、连翘、紫花地丁和甘草,采用高效液相色谱法（HPLC）测定绿原酸的含量,色谱柱为Agilent ZORBAX SB-C₁₈柱（4.6 mm×250 mm,5 μm）;流动相为乙腈（A）与含0.2%甲酸的水溶液（B）,梯度洗脱：0~12 min,11%~12%A;流速：1.0 ml/min;柱温：30 ℃;检测波长：327 nm;进样量：20 μl。结果 薄层鉴别色谱中特征斑点明显,专属性强。绿原酸在6.19~396.00 μg/ml浓度范围内呈良好线性关系,其回归方程为Y=60.239 4X+9.096 3（r>0.999 9）,回收率为99.66%（RSD=2.82%）。结论 该法简便、稳定可靠、重复性好,为控制清热败毒颗粒的质量标准提供了可借鉴的依据。     

乳康片质量标准研究

目的 建立乳康片的质量标准.方法 采用薄层色谱法鉴别乳康片中苍术、当归、川芎、香附、连翘,采用高效液相色谱法测定该制剂中盐酸小檗碱含量.结果 薄层色谱定性鉴别分离度好,专属性强;盐酸小檗碱含量测定的线性范围为9.131～73.050 μg,平均回收率为96.41%,RSD＝1.33%（n＝6).结论 所建立的方法可靠、准确、专属性强,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.     

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.