HPLC法测定盐酸异丙肾上腺素气雾剂雾滴分布、每揿主药含量的探讨

目的：建立HPLC法测定盐酸异丙肾上腺素气雾剂雾滴分布、每揿主药含量和含量。方法：采用ShimPackVP—ODS（250mm×4．6mm，5μm）色谱柱；流动相为含1．76g庚烷磺酸钠的水溶液-甲醇（800：200），用1mol·L^-1磷酸调节pH至3．0；检测波长：280nm。结果：在3．5～700μg·mL^-1浓度范围，盐酸异丙肾上腺素的峰面积与浓度呈良好线性关系（r=0．9999），平均加样回收率分别为99．3％，98．7％，98．2％（n=9）。结论：本法测定盐酸异丙肾上腺素气雾剂雾滴分布、每揿主药含量和含量简捷、灵敏、准确度高，不受辅料干扰。考察结果显示，国内盐酸异丙肾上腺素气雾剂的质量有待进一步提高。     

高效液相色谱法测定盐酸氯丙嗪片的含量与溶出度

目的：建立HPLC法测定盐酸氯丙嗪片的含量与溶出度。方法：采用EclipseXDBC18色谱柱（4．6mm×250mm，5μm），流动相：0．1mol·L^-1磷酸二氢钾（pH3．0）-乙腈（60：40），流速1．0mL·min，检测波长254F11TI，柱温35℃。结果：盐酸氯丙嗪在1～100mg·L^-1范围内线性关系良好（r=0．9999，n=7），平均回收率为97．8％（n=9）。结论：本方法简便、快速、准确，专属性好，可用于盐酸氯丙嗪片含量和溶出度的测定。     

RP—HPLC法同时测定当归龙荟片中黄芩苷、盐酸巴马汀和盐酸小檗碱的含量

目的：建立同时测定当归龙荟片中黄芩苷、盐酸巴马汀和盐酸小檗碱含量的RP—HPLC法。方法：以当归龙荟片为研究对象，采用Diamonsil C18柱（200mm×4．6mm，5μm）分离，流动相为乙腈-甲醇-0．05mol·L-1磷酸二氢钠溶液-三乙胺（25：7：76：0．23，磷酸凋pH3．1），流速1．0mL·min-1，检测波长265mm，柱温35℃。结果：黄芩苷、盐酸巴马汀和盐酸小檗碱浓度分别在0．91～18．16mg·L-1（r=0．9994，n=5），0．16—3．14mg·L-1（r=0．9999，n=5），0．47～9．40mg·L-1（r=0．9999，n=5）范围内与峰面积呈良好线性关系；平均加样回收率（n=9）分别为100．3％，99．3％，99．2％。结论：本测定方法简便、快捷、准确，为当归龙荟片质量评价提供依据。     

高效液相色谱法测定盐酸异丙肾上腺素注射液的含量

目的建立高效液相色谱（HPLC）法用于测定盐酸异丙肾上腺素注射液的含量。方法以Agilent Eclipse XDB-C18柱（250mm×4．6mm,5μm）为分析柱,以用磷酸调pH=3．0的0．14％庚烷磺酸钠溶液-甲醇（65：35）为流动相,流速为1．0mL／min,检测波长为280nm,柱温为室温。结果盐酸异丙肾上腺素质量浓度在25．0～625．2μg／mL范围内与峰面积线性关系良好,回归方程为A=565563．275C-2．625,r=0．9999（n=7）,平均回收率为99．76％,RSD为0．51％（n=6）。结论HPLC法操作简便、结果准确、重现性好,可用于盐酸异丙肾上腺素注射液的含量测定。     

HPLC法测定盐酸左旋咪唑糖浆的含量

目的：采用高效液相色谱法测定盐酸左旋咪唑糖浆的含量。方法：采用Agilent TC—C18色谱柱（4．6mm×150mm，5μm）；以0．05mol·L^-1磷酸二氢钾溶液（二乙胺调节pH7．0）-乙腈（60：40）为流动相；流速1．0mL·min^-1；检测波长为215nm；柱温：室温。结果：盐酸左旋咪唑线性范围为5．14～25．70μg·mL^-1（r=0．9998），平均回收率（n=6）为98．3％，RSD为0．56％。结论：本方法简便、准确、重现性好，可用于测定盐酸左旋咪唑糖浆的含量。     

HPLC测定黄藤素片剂及注射液中盐酸巴马汀的含量

目的：利用反相高效液相色谱法测定黄藤素片剂及黄藤素注射液中盐酸巴马汀的含量。方法：采用Agilent1100型液相色谱仪，色谱柱为Agilent Ecplise XDB—C18（5μm，4．6mm×150mm），流动相为：甲醇-0．04mol·L^-1磷酸二氢钠溶液（35：65），流速1mL·min^-1，检测波长254nm，柱温30℃。结果：巴马汀在0．427～2．136μg范围内，线性关系良好（r=0．9996）；片剂及注射液的回收率（n=5）分别为106．3％（RSD为0．33％），103．4％（RSD为0．28％）。结论：本法简单、快捷，能够满足质量检测的需求。     

HPLC法测定盐酸尼卡地平缓释片的含量

建立高效液相色谱法测定盐酸尼卡地平缓释片的含量。采用高效液相色谱法，色谱柱为Waters XTerra^TM RP18柱；以甲醇-0．01mol·L^-1磷酸二氢钾溶液（72：28）为流动相，流速为1．0mL·min^-1；检测波长为236nm；柱温为35℃。浓度在5．008-95．152μg·mL^-1（r=0.9999）范围内具有良好线性关系，平均回收率为99．28％，RSD为0．46％（n=9）。方法可靠、简单可行，可用于测定盐酸尼卡地平缓释片的含量。     

HPLC法测定黄藤素注射液中盐酸巴马汀的含量

目的：建立测定黄藤素注射液中盐酸巴马汀含量的HPLC方法。方法：采用岛津shim-pack VP—ODS（150mm×4．6mm,4．6um）柱;流动相：乙腈-0．4％磷酸溶液（32：68）;流速：1．0ml·min^-1;检测波长：345nm;柱温：30℃。结果：盐酸巴马汀在9．2～45．8ug·ml^-1范围内呈良好的线性关系（r=0．9999）,平均回收率为99．8％（n=6）（RSD=0．27％）。结论：本法操作简单、灵敏、准确,可用于黄藤素注射液的质量控制。     

HPLC法测定小儿消咳片中小檗碱的含量

目的：建立HPLC法测定小儿消咳片中盐酸小檗碱的含量方法。方法：以迪马钻石C18（250mm×4．6mm，5μm）为色谱柱；流动相：乙腈-0．1％磷酸溶液（每100ml中加入0．1g十二烷基磺酸钠）（50：50）；流速：1．0ml·min^-1；柱温：30℃；检测波长349nm。结果：盐酸小檗碱线性范围为2～21μg·ml^-1（r=0．9996），平均回收率为98．4％，RSD为0．9％（n=6）。结论：方法适用于小儿消咳片中盐酸小檗碱的含量测定。     

RP-HPLC法测定盐酸洛美沙星胶囊的含量及有关物质

目的：采用高效液相色谱法测定盐酸洛美沙星胶囊中盐酸洛美沙星的含量及其有关物质。方法：用Lichospher ODS C18柱（250mm×4．6mm，5μm）；以0．05mol·L^-1枸橼酸溶液（用三乙胺调节pH至4．0）-乙腈（87：13）为流动相；检测波长287nm。结果：盐酸洛美沙星的线性范围为20～200μg·ml^-1（r=0．9995），平均回收率为99．7％（n=9）。结论：方法重复性好，准确度高，适于盐酸洛美沙星胶囊的质量控制。     

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.     

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.