阿咖酚散中游离水杨酸检查方法的改进

摘 要 目的：建立HPLC法检查阿咖酚散中的游离水杨酸。方法: 色谱柱Welch Ultimate C18柱(250 mm×4.6 mm, 5 μm),流动相为乙腈 四氢呋喃 冰醋酸 水（22〖KG*9〗∶〖KG-*2〗5〖KG*9〗∶〖KG-*2〗5〖KG*9〗∶〖KG-*2〗68）,检测波长为303 nm,流速为1.0 ml·min-1。结果: 线性范围为1.500～75.000 μg·ml-1（r=0.999 9）,平均回收率为99.12%,RSD为0.75%（n = 9）,检出限为1.5 ng（S/N=3）。结论: 本方法简便准确、灵敏度高,稳定性比现行标准大幅提高,可用于阿咖酚散中游离水杨酸的检查。     

HPLC法测定不同产地垂盆草药材中木犀草苷的含量

摘 要 目的： 建立反相高效液相色谱法测定垂盆草药材中木犀草苷的含量。方法: 采用Waters SymmetryShield C₁₈ (250 mm×4.6 mm,5 μm) 色谱柱;以四氢呋喃 甲醇 水 磷酸（9〖KG*9〗∶〖KG-*2〗17〖KG*9〗∶〖KG-*2〗74〖KG*9〗∶〖KG-*2〗0.25）为流动相,流速为1.0 ml·min^-1,检测波长为350 nm,柱温为35℃,进样量为10 μl。结果: 木犀草苷在5.2～208.0μg·mL^-1（r=0.999 9）范围内呈现良好的线性关系;平均回收率为99.12％,RSD=0.94%（n=6）。结论:该方法简便、灵敏、准确、专属性强,重复性好,可作为垂盆草药材中木犀草苷含量测定的方法。     

复方枇杷喷托维林颗粒中甘草酸质量标准的建立

摘 要 目的：建立复方枇杷喷托维林颗粒中甘草酸的鉴别和含量测定方法。方法: 采用薄层色谱对甘草酸进行定性鉴别;采用高效液相法测定甘草酸含量,使用Techmate C18（250 mm×4.6 mm,5 μm）色谱柱;流动相为甲醇 0.2 mol·L-1醋酸铵 冰醋酸（60〖KG*9〗∶〖KG-*2〗39〖KG*9〗∶〖KG-*2〗1）;流速：1.0 ml·min-1;检测波长：250 nm,柱温：35℃;进样量：20 μl。结果: 薄层鉴别斑点清晰,阴性对照无干扰。在选定的色谱条件下,甘草酸在0.01～1.01 g·L-1的质量浓度范围内线性关系良好,r=1.000 0,平均加样回收率103.2%,RSD=1.8%（n=9）。结论: 本方法简便、准确,可用于该制剂的质量控制。     

增光片质量标准的改进

摘 要 目的：提高完善增光片的质量标准。方法: 修订了原标准的显微鉴别法;采用TLC法对石菖蒲、枸杞子、远志进行鉴别;采用HPLC法测定五味子醇甲的含量,色谱柱为Hypersil BDS C18 (250 mm×4.6 mm,5 μm）,流动相为甲醇 水 (1〖KG*9〗∶〖KG-*2〗1),流速为1.0 ml·min^-1,检测波长为250 nm,柱温为35℃,进样量为10 μl。结果: 显微鉴别法专属性强;TLC色谱斑点清晰,专属性强,重复性良好。五味子醇甲对照品在21.17～423.40 ng范围内线性关系良好（r=0.999 9）,平均回收率为99.7%,RSD为1.4%（n=6）。结论: 所建立的增光片质量标准全面、完善,能有效控制该品种的质量。     

HPLC法测定米诺地尔微乳中米诺地尔的含量

摘 要 目的：建立高效液相色谱法测定米诺地尔微乳中米诺地尔的含量。方法: 色谱柱:Diamonsil C18柱（200 mm×4.6 mm,5 μm）,流动相:甲醇 水 冰醋酸 十二烷基硫酸钠 (70 ∶〖KG-*4〗30 ∶〖KG-*4〗0.03 ∶〖KG-*4〗0.045)(v/v/v/w),流速：1.0 ml·min-1,检测波长：280 nm,进样量：10 μl,柱温：30℃。结果: 米诺地尔在5.00~100.00 μg·ml-1线性关系良好（r=0.999 7）,平均回收率为99.12%,RSD为1.60%（n=9）。结论: 该方法简便,准确,灵敏,重复性好,专属性强,可用于该制剂的含量测定。     

止咳祛痰口服液质量标准的建立

摘 要 目的：建立止咳祛痰口服液的质量标准。方法: 采用TLC法对桔梗、甘草进行定性鉴别;采用HPLC法对射干的有效成分射干苷进行定量测定,色谱柱为Waters Symmetry C18柱（150 mm×4.6 mm,3.5 μm）,流动相为乙腈 水（14〖KG*9〗∶〖KG-*2〗86）,流速1.0 ml·min-1,柱温35℃,检测波长为265 nm。结果: 薄层色谱斑点清晰,阴性无干扰。射干苷在0.115～2.880 μg范围内线性关系良好（r=0.999 9）,平均回收率为92.44%,RSD为1.83%(n=6)。结论: 所建立的方法简便、快速、重复性好,可用于止咳祛痰口服液的质量控制。     

乳浆草药材质量标准的建立

摘 要 目的：建立乳浆草药材的质量标准。方法: 采用薄层色谱法对乳浆草药材进行定性鉴别;采用HPLC法测定乳浆草药材中槲皮素含量,色谱柱为AlltimaTM C18柱（150 mm×4.6 mm,5 μm）,流动相为乙腈 0.4%磷酸溶液（30〖KG*9〗∶〖KG-*2〗70）,流速为1.0 ml·min-1,检测波长为360 nm,柱温为35℃。结果: TLC色谱中,供试品溶液在与对照药材色谱相同的位置上显相同颜色的斑点。HPLC法中槲皮素浓度在3.194～102.208 μg·mL^-1范围内时与峰面积呈良好的线性关系（r=0.999 9）,平均回收率为99.0%,RSD=1.68%（n=6）。结论: 该方法快速、简便,结果准确,可用于乳浆草药材的质量控制。     

小儿汗停颗粒质量标准研究

摘 要 目的：建立小儿汗停颗粒的质量标准。方法: 采用TLC法对制剂中黄芪、白术（炒）、防风进行定性鉴别。采用HPLC法对制剂中毛蕊异黄酮葡萄糖苷含量进行测定,Cosmosil C18柱（250 mm×4.6 mm,5 μm）分离,以乙腈 0.2%甲酸溶液 (16〖KG*9〗∶〖KG-*2〗84)为流动相;流速为1.0 ml·min-1,检测波长为260 nm。结果: TLC色谱分别检出黄芪中的黄芪甲苷,与白术、防风对照药材有相同清晰斑点且阴性无干扰。毛蕊异黄酮葡萄糖苷对照品在0.061～0.613 μg范围内与峰面积呈良好的线性关系（r=0.999 9）,平均加样回收率结果为99.4%,RSD为1.29%（n=6）。 结论: 该方法准确、快速、稳定、可靠,重复性好,可用于小儿汗停颗粒的质量控制及评价。     

三草安神胶囊的质量标准

摘 要 目的：建立三草安神胶囊的质量标准。方法: 采用TLC法对三草安神胶囊中缬草、夏枯草、黄芩、黄连进行定性鉴别;采用HPLC法对三草安神胶囊中的迷迭香酸进行定量分析。色谱柱：Hypersil ODS2 C18（250 mm×4.6 mm,5 μm）,流动相为乙腈（A） 0.1%三氟乙酸（B）（30∶〖KG-*2〗70）,等度洗脱,流速：1.0 ml·min^-1 ,柱温：25℃,检测波长：330 nm,进样量:20 μl。结果: TLC鉴别色谱中斑点清晰,阴性无干扰;迷迭香酸进样量在0.105～2.104 μg（r=0.999 3）范围内线性关系良好,平均回收率为99.5%,RSD为0.80% (n=6)。结论: 该方法简便、准确、可靠,可用于三草安神胶囊的质量控制。     

HPLC法测定吲哚美辛呋喃唑酮栓中两组分的含量

摘 要 目的：建立同时测定吲哚美辛呋喃唑酮栓中两组分含量的HPLC法。方法: 采用XTerra RP18色谱柱(250 mm×4.6 mm,5 μm),以甲醇为流动相A,0.01 mol·K^-1磷酸二氢钾溶液 三乙胺(100〖KG*9〗∶〖KG-*2〗0.02)为流动相B,梯度洗脱,流速1.0 ml·min^-1,柱温30 ℃,检测波长263 nm,进样量10 μl。结果: 吲哚美辛呋喃唑酮栓中呋喃唑酮和吲哚美辛的分离度符合要求;线性范围分别为5.12~81.87 μg·ml^-1 (r=1.000 0)和3.78~60.45 μg·ml^-1 (r=1.000 0);平均回收率分别为99.6% (RSD=1.5%,n=6)和100.3% (RSD=1.6%,n=6);定量限分别为0.02 μg·ml^-1和0.05 μg·ml^-1。结论:该法经方法学验证,适用于吲哚美辛呋喃唑酮栓的质量评价。     

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.