阿奇霉素胶囊溶出度测定方法的改进

目的:以茜素红荷移分光光度法改进阿奇霉素胶囊溶出度的测定方法.方法:依<中国药典>二部附录X C溶出度测定方法项下二法,以600 mL pH 5.0的磷酸盐缓冲液为溶剂,转速为100 r·min-1.经45 min取样,以茜素红荷移分光光度法在524 nm处测定阿奇霉素胶囊的溶出度,限度为75%.结果:阿奇霉素在12.5～62.0 mg·L-1范围内线性关系良好(r=0.991 3),平均回收率为100.3%.结论:该方法准确、简便,可用于阿奇霉素胶囊溶出度的测定.     

茜素红荷移分光光度法测定罗红霉素片溶出度

目的建立茜素红荷移分光光度法测定罗红霉素片溶出度。方法采用中国药典附录XC第一法及第三法,以600 ml或250 ml 0.01M的磷酸氢二钠缓冲液pH值（5.0±0.05）为溶出介质,转速为100 r/min,经45 min取样,茜素红荷移分光光度法在525±2 nm处测定罗红霉素片的溶出度,限度为75%。结果罗红霉素在50.00-200.0μg/ml范围内,吸光度（A）与浓度（C）呈良好的线性,r=0.9994,平均回收率：101.1%。结论该方法简便、准确、专属,可用于该片的质量控制。     

阿奇霉素颗粒溶出度测定法研究

目的建立阿奇霉素颗粒的溶出度测定方法。方法采用桨法,以0．1mol／L盐酸溶液900ml为溶出介质,转速为50r／min,以硫酸溶液（75→100）为显色剂,用分光光度法进行测定。结果可以用硫酸显色法测定阿奇霉素颗粒溶出度。结论本方法简便、准确可信,可用于阿奇霉素颗粒溶出度的测定。     

茜素红荷移分光光度法测定克拉霉素胶囊溶出度

目的建立茜素红荷移分光光度法测定克拉霉素胶囊溶出度的方法。方法采用中国药典附录XC第三法,以0.05 mol/l pH5.0的磷酸盐缓冲液250 ml为溶剂,转速为100 r/min,经45 min取样,在525 nm处测定克拉霉素胶囊的溶出度,限度为标示量的75%。结果克拉霉素浓度在60.4～151.0μg/ml范围内线性关系良好,r=0.999 8,平均回收率100.6%,RSD为0.8%。结论该方法准确、简便,可用于克拉霉素胶囊溶出度的测定。     

阿奇霉素分散片与其普通片溶出度比较考察

目的 考察阿奇霉素分散片的溶出度。方法 以硫酸溶液(75→100)为显色剂，用分光光度法测定其溶出度，并与阿奇霉素普通片比较。结果 测定3批样品的累积溶出百分率在10min内可达90％，但批与批之间存在差异。结论 阿奇霉素分散片的溶出度比普通片快。     

茜素红的荷移分光光度法测定罗红霉素胶囊的溶出度

目的:建立茜素红荷移分光光度法测定罗红霉素胶囊溶出度的方法.方法:采用中国药典方法(附录ⅩC第一法),以盐酸溶液(1→1 00)900 mL为溶出介质,分别以硫酸显色分光光度法、茜素红荷移分光光度法测定罗红霉素的溶出度. 结果:经过对2种方法的比较本文方法在20-120 mg*L-1范围内线性关系良好r=0.999 6,平均回收率为97.98%.结论:该方法简便、快捷,可用于罗红霉素溶出度的测定.     

阿奇霉素片的茜素红荷移分光光度法测定

阿奇霉素与茜素红在乙醇-水溶液中发生荷移反应,由此建立了荷移分光光度法测定阿奇霉素片的含量.荷移反应生成1:2型络合物,最大吸收波长为538 nm,摩尔吸收系数为1.23×10 4L·mol-1·cm-1.阿奇霉素在10～60μg/ml浓度范围内线性关系良好.含量测定结果与HPLC法结果基本相符.     

阿奇霉素颗粒溶出度检查方法研究

目的建立阿奇霉素颗粒中主药溶出度的测定方法。方法采用紫外分光光度法,在482nm波长处测定阿奇霉素颗粒中主药的吸收度,并计算回收率和溶出度。结果阿奇霉素检测浓度线性范围为13．79—110．32mg·L^-1（r=0．9990）;平均回收率为99．2％（RSD=1．12％,n=9）;3批样品在45min溶出量均在75％以上。结论本方法准确、可靠,可用于该制剂的溶出度测定。     

复方利福平片溶出度测定方法的研究

目的 建立复方利福平片的溶出度测定方法。方法 采用溶出度测定法第二法，以水为溶剂，转速为50r／min，经45min取样，紫外分光光度法在474nm处测定利福平的溶出量，溶出限度为标示量的75％。结果利福平在10．3—36．1μg／ml范围内线性关系良好(r＝1．0000)，平均回收率99．8％。结论 本方法准确、快速、简便。通过测定复方利福平片的溶出度可有效检测其制剂工艺水平。     

阿奇霉素分散片与其普通片溶出度比较考察

目的　考察阿奇霉素分散片的溶出度。方法　以硫酸溶液 (75→ 10 0 )为显色剂 ,用分光光度法测定其溶出度 ,并与阿奇霉素普通片比较。结果　测定 3批样品的累积溶出百分率在 10min内可达 90 % ,但批与批之间存在差异。结论　阿奇霉素分散片的溶出度比普通片快。     

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.     

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.     

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.