产舒康颗粒中盐酸水苏碱的高效液相色谱法定量

目的建立产舒康颗粒中盐酸水苏碱的高效液相色谱法定量方法。方法通过强酸性阳离子交换树脂柱得到产舒康颗粒中盐酸水苏碱。高效液相色谱法测定条件:Spherisorb SCX柱150mm×4.6mm,5μm;流动相:甲醇-水(60:40)含0.05mol.L-1磷酸二氢钾;检测波长:215nm。结果盐酸水苏碱在1.0～5.0μg内线性关系良好,平均回收率96.21%,RSD=2.22%,三批颗粒中盐酸水苏碱含量分别为0.0304%,0.0276%,0.0191%。结论该方法简便、灵敏、准确,为控制产舒康颗粒的质量提供依据。     

薄层扫描法测定血尿康颗粒中盐酸水苏碱的含量

目的:建立以薄层扫描法测定血尿康颗粒中盐酸水苏碱含量的方法。方法:采用硅胶G薄层板,展开剂为正丁醇-盐酸-醋酸乙酯(8∶3∶1),显色剂为稀碘化铋钾试液,测定波长为515nm,参比波长为700nm,狭缝大小为6.00mm×0.45mm。结果:盐酸水苏碱点样量在5.06μg～25.32μg范围内与斑点峰面积积分值呈良好的线性关系(r=0.9978),平均加样回收率为96.67%(RSD=2.01%)。结论:本方法简便、灵敏度高、重现性好,可用于血尿康颗粒的含量测定与质量控制。     

薄层扫描法测定肾宁颗粒中盐酸水苏碱的含量

目的:建立以薄层扫描法测定肾宁颗粒中盐酸水苏碱含量的方法。方法:展开剂为丙酮-无水乙醇-盐酸(10∶6∶1) ,显色剂为碘化铋钾试液-1%三氯化铁无水乙醇溶液(2∶1) ,测定波长为530nm ,参比波长为670nm ,狭缝大小为0.4mm×0. 4mm ,线性化参数Sx=3。结果:盐酸水苏碱点样量在2.412μg～6.432μg范围内斑点峰面积积分值呈良好的线形关系(r=0.9972) ,平均回收率为98.93% (RSD=1.15 % )。结论:本方法简便、准确、重现性好,可用于肾宁颗粒的质量控制     

薄层扫描法测定咳喘平颗粒中盐酸麻黄碱含量

目的:测定咳喘平颗粒中盐酸麻黄碱的含量.方法:薄层扫描法,展开剂:氯仿-甲醇-浓氨水(20:5:0.5),显色剂:0.3%茚三酮,检测波长λs=505 nm.结果:盐酸麻黄碱在0.34～1.70μg范围内线性良好,r=0.998 0,平均回收率为98.7%,RSD为1.89%.结论:本法适用于咳喘平颗粒中盐酸麻黄碱含量测定.     

薄层扫描法测定化痰降气胶囊中盐酸麻黄碱含量

目的 测定化痰降气胶囊中盐酸麻黄碱的含量.方法薄层扫描法,展开剂:氯仿-甲醇-浓氨水(20∶5∶0.5),显色剂:0.3%茚三酮,检测波长λs=490 nm.结果 盐酸麻黄碱在0.336～1.680 μg范围内线性良好,相关系数r=0.9978,平均回收率为99.22%,RSD=1.94%.结论 本法适用于化痰降气胶囊中盐酸麻黄碱含量测定.     

HPLC法测定八珍益母片中盐酸水苏碱的含量

目的:建立测定八珍益母片中盐酸水苏碱含量的方法。方法:采用高效液相色谱法。色谱柱为Kromasil NH2(200 mm×4.6 mm,5μm),流动相为乙腈-水(75∶25,V/V),流速为1.0 ml/min,柱温为30℃,检测波长为192 nm,进样量为10μl。结果:盐酸水苏碱的进样量在0.626 3⁵.219 0μg范围内与峰面积积分值呈良好的线性关系(r=0.999 9);精密度、稳定性、重复性试验的RSD≤0.41%;平均加样回收率为98.50%,RSD=0.73%(n=6)。结论:本方法准确、快速、简便、可靠,可用于八珍益母片中盐酸水苏碱的含量测定。     

薄层扫描法测定复宫胶囊中盐酸水苏碱的含量

目的:建立复宫胶囊中主药益母草中水苏碱含量测定方法.方法:薄层扫描法,λs=510 nm,λR=590 rm.结果:样品平均回收率为98.12%,RSD为2.15%.结论:以上方法简单、可靠,有效地控制了制剂的质量.     

益母草颗粒中盐酸水苏碱的含量测定

目的建立测定益母草颗粒中盐酸水苏碱的含量方法。方法采用雷氏盐剩余比色法测定盐酸水苏碱的含量,测定波长为520nm。结果本方法在0~12m g范围内线性关系良好,r=0.9992。平均回收率为99.2%,RSD=1.20。结论本法操作简便、灵敏度高、专属性好,可作为该制剂质量控制方法。     

薄层扫描法测定新生化颗粒中盐酸水苏碱的含量

目的:测定新生化颗粒中盐酸水苏碱的含量.方法:采用薄层扫描法.结果:盐酸水苏碱在2.04～10.20μg呈线性关系,平均加样回收率为97.4%,精密度RSD=1.6%.结论:本法可以用于该药品的质量控制.     

HPLC测定复方益母口服液中的盐酸水苏碱

目的 采用HPLC测定复方益母口服液中盐酸水苏碱的含量,并与TLC法比较.方法 采用Kromasil C_(18)(250 mm×4.6 mm,5 μm)色谱柱,流动相为乙腈-0.05 mol·L~(-1)磷酸二氢钾溶液(18:82,pH5.5),流速1.0 mL·min~(-1),柱温35 ℃,检测波长215 nm,以外标法计算含量.结果 盐酸水苏碱1.05～26.25 μg与峰面积具良好的线性关系(r=0.9997),平均加样回收率为98.3%(n=9),RSD=1.17%.结论 所用方法简便、准确、重复性好,可替代TLC法控制该制剂的质量.     

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.     

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.