双波长紫外分光光度法测定复方氧氟沙星喷雾剂中盐酸达克罗宁和氧氟沙星的含量

目的 建立双波长紫外分光光度法测定复方氧氟沙星喷雾剂中盐酸达克罗宁和氧氟沙星的含量.方法 盐酸达克罗宁以282nm为测定波长,300.7nm为参比波长;氧氟沙星以225nm测定其波长.结果 盐酸达克罗宁在3.0054～8.0114μg·mL-1范围内线性关系良好,相关系数r=0.9994,平均回收率100.8%,RSD=0.97%;氧氟沙星在1.4973～3.9928μg·mL-1范围内相关系数良好,r=0.9992,平均回收率为100.4%,RSD=0.92%.结论 该方法简便,结果准确,适用于复方氧氟沙星喷雾剂中盐酸达克罗宁和氧氟沙星的含量测定.     

RP-HPLC法测定伪麻那敏缓释胶囊中的有效成分及释放度

目的建立伪麻那敏缓释胶囊中盐酸伪麻黄碱和马来酸氯苯那敏分析方法,测定进口和自制伪麻那敏缓释胶囊的体外释放度.方法 RP-HPLC法用苯基柱,流动相为甲醇-磷酸缓冲液(60∶40),检测波长为254 nm.结果盐酸伪麻黄碱在5.78～723.00 μg·mL-1线性关系良好(r=1.000),马来酸氯苯那敏在0.41～51.00 μg·mL-1线性关系良好(r=1.000).样品的回收率分别为100.4%(RSD=1.1%,n=15)和98.7%(RSD=1.6%,n=15).结论采用RP-HPLC法控制产品质量准确、迅速,累计释放曲线符合一级方程:ln(1-Mt/M∞)=-kt.     

盐酸莫西沙星片在健康志愿者体内两种条件下的药动学研究

目的 研究盐酸莫西沙星片在健康志愿者体内两种条件下的药动学.方法 采用随机交叉自身对照试验设计,24名健康男性志愿者随机交叉单剂量空腹(或餐后)口服400 mg盐酸莫西沙星片.采用HPLC-UV法测定受试者血浆中莫西沙星的浓度,计算药动学参数,评价制剂在两种条件下的药动学行为.结果 空腹条件下,盐酸莫西沙星片的主要药动学参数为:Tmax =1.55 ±0.96 h,Cmax=3.45±0.88 μg·mL-1,AUC0-t=58.77±13.02 μg·mL-1·h,AUC0-∞=60.50±13.71 μg·mL-1·h;餐后条件下,盐酸莫西沙星片的主要药动学参数为:Tmax =2.66±1.48 h,Cmax=3.16±0.70 μg·mL-1,AUC0-t=57.01±9.95μg· mL-1·h,AUC0-∞=59.00± 10.60 μg·mL-1· h.结论 餐后与空腹条件相比,除了Tmax有所延迟外,其余药动学参数均无太大差别,表明食物可能会减缓盐酸莫西沙星的吸收.     

达克罗宁凝胶剂的制备与临床应用

目的制备达克罗宁凝胶剂并建立其质量控制标淮。方法拟定达克罗宁凝胶剂的处方和制备工艺;采用紫外分光光度法测定盐酸达克罗宁含量;并进行临床疗效观察。结果盐酸达克罗宁在4~20μg.mL-1范围内有良好的线性关系,r=0.999 7,平均回收率为99.85%,RSD为0.74%;临床总有效率为96%。结论制剂工艺简单,质量控制可靠,临床疗效确切。     

HPLC法同时测定盐酸奈福泮萘普生胶囊中2种成分的含量

目的 建立同时测定盐酸奈福泮萘普生胶囊中盐酸奈福泮和萘普生含量的高效液相色谱方法.方法 采用Apollo C18色谱柱,以庚烷磺酸钠溶液-乙腈(53:47)为流动相,流速为1.0 mL·min-1,检测波长为215 nm.结果 盐酸奈福泮浓度在15.8～47.5 μg·mL-1范围内与峰面积线性关系良好(r=0.9997),平均回收率为99.43％,RSD为1.31％(n=3);萘普生在54.7～164.2 μg·mL-1范围内线性关系良好(r=0.9999),平均回收率为99.72％,RSD为0.80％(n=3).结论 该方法操作简便,结果准确,精密度高,可用于控制盐酸奈福泮萘普生胶囊的质量.     

HPLC法测定氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量

目的 建立测定氯麻滴鼻液中氯霉素和盐酸麻黄碱含量的高效液相色谱法.方法 采用Waters C18色谱柱（4.6mm×250 mm,5μm）,流动相为0.01 mol·L-1磷酸二氢钾溶液（用磷酸和三乙胺调节pH=3.0）-乙腈（60∶40）,流速为1.0 mL· min-1,检测波长为220 nm,柱温为30℃.结果 氯霉素在9.84～98.45 μg·mL-1范围内线性关系良好,盐酸麻黄碱在40.24～402.39 μg·mL-1范围内线性关系良好.氯霉素平均回收率为100.89％,RSD=0.21％;盐酸麻黄碱平均回收率为100.33％,RSD=0.83％.结论 本方法灵敏度高、操作简便、准确可靠,可用于氯麻滴鼻液中氯霉素和盐酸麻黄碱的含量测定.     

HPLC法测定复方盐酸达克罗宁乳膏的含量

目的:建立HPLC法测定复方盐酸达克罗宁乳膏中盐酸达克罗宁含量的方法.方法:Agilent Extend C18色谱柱(250×4.6 mm,5μm),以乙腈-0.02 mol·L-磷酸二氢钾溶液(用磷酸调pH至3.0)(35∶65)为流动相,流速为1.0 ml· min-1,检测波长为282 nm,柱温为30℃.结果:盐酸达克罗宁进样量在0.1196 ～0.5980 μg的范围内线性关系良好(r=0.9999),平均回收率为99.2％,RSD =0.49％ (n =9).结论:本试验方法简单,结果准确,重复性好,可用于该制剂的质量控制.     

注射用盐酸帕洛诺司琼的制备、质量控制及稳定性考察

目的:制备注射用盐酸帕洛诺司琼,建立其质量控制方法并考察其稳定性.方法:制备注射用盐酸帕洛诺司琼;采用高效液相色谱法测定其含量及有关物质,并对制剂进行稳定性试验.结果:本品处方以10%甘露醇作为填充剂,用磷酸二氢钠调节溶液pH值为4.5～6.0;盐酸帕洛诺司琼在 12.00 μg·mL-1～150.01 μg·mL-1浓度范围内线性关系良好(r＝0.999 9),恒温加速试验6个月及长期留样18个月时主药含量及有关物质未见明显变化.结论:该制剂处方工艺可行,质量可控,稳定性良好;所建立的含量测定方法重复性好,专属性强,结果准确可靠.     

多效内窥镜乳的制备及质量控制

目的：研制一种能同时起到多种作用的内窥镜检查用的口服制剂,并建立制剂的质量标准。方法：拟定内窥镜乳的处方组成与制备工艺,进行性状、鉴别、有关物质检查等质量控制方法,采用紫外分光光度法测定盐酸达克罗宁含量。结果：盐酸达克罗宁在4.0～24.0μg·mL-1范围内呈良好的线性关系。盐酸达克罗宁的平均回收率为99.7%（RSD=0.74%）。结论：本制剂制备工艺简便可行,质量稳定可控。     

增强化学发光法测定盐酸恩诺沙星的含量

目的 采用增强化学发光法快速测定痕量盐酸恩诺沙星.方法 利用加入Tb3+和盐酸恩诺沙星后可以使Ce4+-Na2SO3体系的化学发光显著增强的原理,测定盐酸恩诺沙星的含量.结果 增强的化学发光强度与盐酸恩诺沙星0.1～10μg·mL-1和10～100μg·mL-1呈良好的线性关系(r分别为0.9984、0.9980),检测限为0.033 μg·mL-1,RSD=1.29%(n=11).结论 所建方法快捷、简便、灵敏度高,测定了自制牛奶样品中盐酸恩诺沙星的含量,结果满意.     

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.