紫外分光光度法测定盐酸环丙沙星的含量

目的：用紫外分光光度法测定盐酸环丙沙星的含量。方法：以0．01mol/L盐酸为溶剂采用紫外分光光度法进行含量测定，建立含量测定的质量控制方法。结果：盐酸环丙沙星含量测定平均回收率为100．15％，RSD为0．85％（n=6)。结论：用本法测定盐酸环丙沙星含量简便、快速，测定结果与药典方法基本一致。     

复方泮托拉唑钠胃内漂浮片的制备及含量测定

目的制备复方泮托拉唑钠胃内漂浮片并对其含量进行测定。方法采用直接压片法制备，以高效液相色谱法测定其含量。结果制备的泮托拉唑钠胃内漂浮片体外漂浮性能良好；含量测定线性范围为0．275-1．650μg，r=0，9999，平均回收率为99．2％，RSD=0．41％。结论该制备方法简单、易操作。含量测定方法简便、准确，回收率高，可用于泮托拉唑钠胃内漂浮片的制备及含量测定。     

泮托拉唑钠口腔崩解片的制备及质量控制

目的：制备泮托拉唑钠口腔崩解片并对其含量进行测定。方法：采用直接压片法制备，HPLC法测定其含量。结果：制备的泮托拉唑钠口腔崩解片外观光洁，硬度为3kg，崩解时间小于30s；含量测定线性范围为0．275-1．650μg，r=0．9999，平均回收率为99．7％，RSD=0．35％。结论：该制备方法简单，含量测定方法简便、准确，回收率高，可用于泮托拉唑钠口崩片的制备及含量测定。     

导数光谱法测定复方苯甲酸醇溶液中两组分含量

目的建立测定复方苯甲酸醇溶液中苯甲酸和水杨酸含量的方法。方法采用二阶导数光谱法在233nm波长处测定苯甲酸的含量，在319nm波长处测定水杨酸含量。结果苯甲酸、水杨酸质量浓度分别在12．16～60．80μg／mL和6．72—33．60μg／mL范围内二阶导数振幅线性关系良好（r=-0．9998和r=-0．99996），平均回收率分别为100．9％和100．5％，RSD分别为1．01％和1．00％（n=5）。结论所用方法简便、快速、准确，可用于复方苯甲酸醇溶液中苯甲酸和水杨酸的含量测定。     

紫外分光光度法测定复方薄荷脑滴鼻液中樟脑含量

目的建立测定复方薄荷脑滴鼻液中樟脑含量的方法。方法采用紫外分光光度法，在289nm波长处测定樟脑的含量。结果樟脑质量浓度在1．50～3．50mg／mL范围内与吸光度线性关系良好，回归方程为A=0．217C-0．0303（r=0．9999），平均回收率为100．1％，RSD=1．4％（n=9）。方法精密度的RSD=1．7％（n=5）。结论所建方法简便、准确、重现性好，可用于复方薄荷脑滴鼻液的樟脑含量测定。     

HPLC法测定三两半药酒中齐墩果酸与阿魏酸的含量

完善三两半药酒含量的测定。方法采用HPLC对本品当归中阿魏酸、牛膝中齐敦果酸进行含量测定。结果HPLC测定齐墩果酸，线性范围为9．6～40．0μg／ml（r=0．9998），平均加样回收率为97．8％；HPLC测定阿魏酸，线性范围为0．125～0．75μg/ml（r=0．998）平均加样回收率99．8％。结论本实验方法简便、灵敏、重现性好，可作为该制剂含量的控制方法。     

薄层扫描法测定伤科乳膏中大黄素的含量

目的 建立伤科乳膏中大黄素的含量测定方法。方法 采用薄层扫描法对伤科乳膏叶1的大黄素进行含量测定。结果 大黄素在0．392～1．96ug范周内线性关系良好，r=0．99998，平均回收率为97．28％，RSD=1．08％。空白无干扰。结论 方法简便、重现性好，可作为该制剂中大黄素的含量测定方法。     

高效液相色谱法测定翻白草中熊果酸含量

目的 建立测定翻白草中熊果酸含量的方法。方法 利用高效液相色谱法（HPLC法）测定在最佳工艺条件下（即采用70％乙醇，料液比为1：12,4次回流，水浴回流时间为2．5h）提取的熊果酸含量。结果 翻白草中熊果酸的含量为0．02436mg／g（n=3），翻白草根中的含量为0．02157mg／g（n=3），方法回收率为99．21％，RSD为1．13％（n=5）。结论 HPLC法简便、精确、精密度高。     

复方氧氟沙星滴耳液的制备及质量控制

目的制备复方氧氟沙星滴耳液，并建立其含量测定方法。方法以氧氟沙星、替硝唑为主药，配制成滴耳液，并采用双波长分光光度法测定其含量。结果氧氟沙星的平均回收率为100．11％，RSD为0．48％（n=5）；替硝唑的平均回收率为100．04％，RSD为0．70％（n=5）。结论该制剂制备方法简便，质量稳定，含量测定方法简单、快速、可靠。     

络合滴定法测定鞣酸鱼肝油软膏中的鞣酸含量

目的：制订鞣酸鱼肝油软膏中鞣酸含量的质控标准。方法：采用锌标准液测定鞣酸，乙二胺四乙酸钠回滴过量锌离子的络合滴定法对鞣酸作含量测定。结果：鞣酸鱼肝油软膏中鞣酸含量平均为4．77％，RSD=2．41％；方法回收率为102．41，RSD=2．52％。结论：该方法简便、快速、准确；可控制该制剂质量。     

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.     

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.