HPLC测定扎西他宾薄膜衣片的溶出度

目的 建立定量测定扎西他宾薄膜衣片溶出度的方法. 方法采用HPLC法,AlphaBond-C18柱 (150 mm×3.9 mm,10 μm),流动相为磷酸缓冲液-甲醇-乙腈(96:4:3),检测波长270 nm. 结果 0.005～20.000 μg·ml-1的线性方程为:A＝4.455×105C 1.770×104 (r＝0.9999);平均回收率为99.28%,RSD＝0.83% (n＝9);5批样品溶出迅速,批间差异小. 结论所建方法简单,专属性强,可测定扎西他宾薄膜衣片的溶出度.自制片剂和进口参比制剂溶出度相似.     

HPLC法测定氯诺昔康口腔崩解片的含量

目的:建立HPLC法测氯诺昔康口腔崩解片的含量。方法:色谱柱为,Linksil C18(4.6mm×250mm,5μm),流动相为0.05mol·L-1磷酸二氢钾溶液(用磷酸调pH值至3.1)-乙腈-甲醇(60∶30∶10),流速为1.0ml·min-1;检测波长为264nm;柱温为40℃。结果:氯诺昔康的线性范围为4.0~60.0mg·L-1,r=0.9998;平均回收率为99.8%,RSD=0.63%。结论:本方法方便、快速、准确,可用于该制剂的质量控制。     

HPLC法测定盐酸噻诺啡片的含量及其溶出度

目的:建立一种HPLC法测定盐酸噻诺啡片的含量及溶出度.方法:采用Phenex prodigy C18色谱柱(250mm×4.6mm,5μm),以乙腈-甲醇-0.02mol·L-1磷酸盐缓冲液(pH=3,含0.2%的三乙胺)(40:15:45)为流动相,220nm为检测波长,测定了盐酸噻诺啡片的含量和溶出度.结果:本法测定盐酸噻诺啡的线性范围为0.5～10μg·mL-1(r=0.999 9);日内精密度和日间精密度均小于2%(n=5);回收率在98%～102%之间.结论:本法精密、准确,适用于盐酸噻诺啡片的含量及溶出度测定.     

高效液相色谱法测定氯诺昔康速释片的含量

目的建立了氯诺昔康速释片含量的HPLC测定法。方法采用C18色谱柱,柱温35℃,流动相为0.1mol·L-1醋酸钠溶液-甲醇(1∶1),检测波长为378nm。结果氯诺昔康在9.5μg·mL~285.5μg·mL范围内线性良好,相关系数r=1.0000(n=5);平均回收率为99.69%(n=6,RSD为0.9%)。结论HPLC法可以测定氯诺昔康速释片的含量。     

氯诺昔康口腔崩解片的质量控制

目的:建立氯诺昔康口腔崩解片的质量控制方法。方法:利用自制崩解装置测定氯诺昔康口腔崩解片的崩解时限;以紫外-可见分光光度法测定溶出度;采用高效液相色谱法进行含量测定。结果:氯诺昔康口腔崩解片的崩解时间不超过20s,标示含量达到99.2%以上,10min内溶出度在90%以上。结论:建立的质量控制方法简便可靠,可用于该制剂的质量控制。     

高效液相色谱法测定氟氯西林钠片的溶出度

目的:建立氟氯西林钠片溶出度的测定方法.方法:高效液相色谱法,色谱柱为Hypersil BDS C18柱(200mm×4.6mm, 5μm),流动相为0.02mol·L-1磷酸二氢钾缓冲液(用稀NaOH调节pH至5.0)-乙腈(70:30),检测波长为225nm,流速为1.0ml·min-1,柱温为25℃.照中国药典2005年版二部附录"溶出度测定法"第二法测定溶出度.结果:3批样品溶出量均为标示量的94%.结论:该法简便、准确,结果可靠.可用于氟氯西林钠片的溶出度测定.     

紫外-可见分光光度法测定氯诺昔康颗粒的溶出度

目的: 建立测定氯诺昔康颗粒溶出度的方法。方法: 照《中国药典》2010年版二部溶出度测定第二法,以磷酸盐缓冲液(pH 7.4)900 mL为溶出介质,转速50 rpm,15 min取样,用紫外-可见分光光度法测定溶出量,检测波长为376 nm。结果: 氯诺昔康在1.105～22.100 g·L^-1浓度范围内吸光度线性关系良好(r=0.999 9,n=5),平均回收率为99.7%(RSD=0.63%)。结论: 本方法简便,准确可靠,能满足质量控制的要求。     

氯诺昔康口腔崩解片的制备

目的:对氯诺昔康口腔崩解片的处方及制备工艺进行研究,并评价其质量。方法:以片剂崩解时限、口感为指标,采用正交试验设计优化处方。通过直接压片法制备氯诺昔康口腔崩解片,并测定了其体外崩解时间、溶出度等质量指标。结果:所得片剂完整光洁、口感良好,能在20 s内崩解完全,5 min内体外溶出度超过85%。结论:氯诺昔康口腔崩解片达到了设计要求,方便患者服药。     

紫外分光光度法测定氯诺昔康注射液的含量

目的 采用分光光度法测定氯诺昔康注射液的含量。方法 以水为溶媒，测定波长378nm的条件下，对氯诺昔康注射液进行含量测定，另外还对样品的测定条件进行了优选。结果 氯诺昔康浓度在4μg-20μg范围内线性良好，以标准曲线法得其回收率为99.7%(n=5),RSD为0.78%。结论 该方法稳定可靠，重现性好，辅料及杂质无干扰。     

炔诺酮片溶出度测定方法学研究

目的建立炔诺酮片溶出度检查方法。方法采用桨法进行溶出度实验,高效液相色谱法测定介质中药物含量。结果溶出度检查方法为桨法,以5g.L-1十二烷基硫酸钠溶液500mL为溶出介质,转速为75r.min-1,取样时间为45min(薄膜衣片)或60min(糖衣片)。含量测定方法的线性方程为Y=64 743 X-208(r=1.000 0),在0.12～1.84μg.mL-1质量浓度范围内线性关系良好(r=1.000);A企业样品平均回收率为100.1%,RSD为1.3%,B企业样品平均回收率为100.8%,RSD为0.7%。结论该方法准确可靠,适用于该制剂的质量控制。     

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.     

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.