复方虎杖凝胶剂的制备及质量控制

目的制备复方虎杖凝胶剂，建立其质量控制方法。方法以壳聚糖为凝胶材料，按药剂学原理制备凝胶剂；用高效液相色谱法测定制剂中的大黄素含量。结果大黄素质量浓度与峰面积的线性范围为10～80μg／mL，平均回收率为100.65％，RSD为0．56％（n=6）。结论凝胶剂制备工艺简单，含量测定方法准确，重现性好。     

五虎壳聚糖凝胶剂的制备与临床应用

目的：研宄五虎壳聚糖凝胶剂的制备方法与临床应用。方法：含挥发油的药材采用蒸馏法提取挥发油，其他药材采用水煎煮法提取，以壳聚糖为凝胶材料制备五虎壳聚糖凝胺剂；用薄层层析法进行鉴别，用高效液相色谱法测定含量．结果：该凝胶剂制备工艺简单，质量控制方法可行。临床疗效可靠。结论：该制剂符合《中国药典》凝胶剂项下有关规定.     

复方乳酸左氧氟沙星壳聚糖凝胶剂的制备与质量控制

目的:制备复方乳酸左氧氟沙星壳聚糖凝胶剂,建立其质量控制方法.方法:以壳聚糖、羧甲基纤维素为凝胶材料制备复方乳酸左氧氟沙星壳聚糖凝胶剂;采用紫外分光度法测量乳酸左氧氟沙星含量,采用容量法测定谷氨酸锌含量.结果:乳酸左氧氟沙星的线性范围为4.5～20.5 μg·ml-1,平均回收率为100.2%,RSD为0.18%(n=9).结论:该凝胶剂制备工艺简单,质量控制方法可靠,质量稳定.     

复方加替沙星壳聚糖凝胶的制备与质量控制

［摘要］目的研究复方加替沙星壳聚糖凝胶剂的制备工艺，建立质量控制方法。方法以壳聚糖、卡波姆为凝胶材料制备复方加替沙星壳聚糖凝胶剂；采用紫外分光光度法测定加替沙星含量；采用容量法测定谷氨酸锌含量。结果该凝胶剂制备工艺简单，质量控制方法可行，质量稳定。结论该凝胶剂符合《中华人民共和国药典》凝胶项下有关规定。     

氟比洛芬凝胶剂的制备与质量控制

目的研制氟比洛芬凝胶剂，并建立其质量控制方法。方法选用壳聚糖为凝胶材料制备氟比洛芬凝胶剂，采用紫外分光光度法进行定性鉴别，采用高效液相色谱法测定氟比洛芬含量。结果氟比洛芬质量浓度在10～100μg／mL范围内与峰面积线性关系良好，平均回收率为99．93％，RSD为1．15％。结论该制剂制备工艺合理，质量控制方法可靠。     

2种不同制备工艺在复方苦参止痒液中的应用研究

目的探讨2种不同制备工艺在复方苦参止痒液中的应用。方法采用ZTC1＋1澄清剂沉淀法的新工艺制备复方苦参止痒液,并与原水醇法制备工艺进行比较。结果 2种工艺制备的样品均稳定、澄明、不混浊、色泽相近,无明显变化,苦参碱的含量相对稳定。结论吸附澄清剂工艺不仅能够使君药的含量增加,而且可缩短生产周期,减少回收乙醇程序,降低成本,值得推广。     

复方止痒凝胶剂的制备与临床应用

目的 研制以苦参、黄柏等多味中药为原料．治疗瘙痒症的复方止痒凝胶剂的制备与临床应用。方法 制备复方止痒凝胶剂并进行136例临床疗效观察。结果 总有效率达94．12％。结论 本制剂处方合理．治疗瘙痒症疗效显著。     

来氟米特凝胶剂的制备与质量控制

目的制备来氟米特凝胶剂，并建立其质量控制方法。方法以壳聚糖为凝胶材料制备来氟米特凝胶剂，采用高效液相色谱法测定来氟米特含量。结果来氟米特质量浓度在10～100μg／mL范围内与峰面积线性关系良好，平均回收率为100．3％，RSD为0．67％（n=6）。结论制备工艺合理、简单，含量测定方法可行，制剂质量稳定。     

复方酮康唑凝胶剂的制备

目的：制备复方酮康唑凝胶剂。方法：将酮康唑用羟丙基-β-环糊精包合，以卡波姆-940为凝胶基质，以制剂外观、稳定性和体外释放率为指标，进行凝胶剂处方和制备工艺的优选。结果：复方酮康唑凝胶剂的优化处方组成为1．0％酮康唑、0．0025％丙酸氯倍他索、1．0％硫酸新霉素、2．0％卡波姆、20％羟丙基廿环糊精、1．0％硫代硫酸钠、10％甘油、5％聚乙二醇-400、适量三乙醇胺。结论：采用优化处方制备的复方酮康唑凝胶剂，外观透明、均匀细腻，黏附性与稳定性良好。     

复方甘草酸铵凝胶剂制备

目的:制备复方甘草酸铵凝胶剂。方法:以甘草酸铵、苦参碱为主药,卡泊姆为基质制备凝胶剂。用紫外分光光度法分别测定甘草酸铵和苦参碱的含量并进行稳定性试验。结果:甘草酸铵的线性范围为10～70μg·ml~(-1)平均回收率为100.38%;苦参碱的线性范围为10～100μg·ml~(-1)平均回收率为100.6%。结论:该制剂制备工艺可行,凝胶性质稳定,质控方法简单、可靠。     

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.     

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.     

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.     

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.