复方呋喃西林滴鼻凝胶剂的制备

目的：制备复方呋喃西林滴鼻凝胶并对其含量进行测定。方法：以卡波姆-40为乳化剂，三乙醇胺调节pH，制备水溶性透明凝胶。用紫外分光光度法和旋光度法分别测定凝胶剂中呋喃西林和盐酸麻黄碱的含量。结果：制备的凝胶均匀细腻，稠度适宜。呋喃西林的平均含量为98．56％，RSD为1．24％。平均回收率为99．36％，RSD为0．83％，盐酸麻黄碱的平均含量为97．93％，RSD为1．32％。平均回收率为100．36％，RSD为0．67％。结论：该制剂性质稳定，容易吸收，无刺激性，使用方便，测定方法简单易行，快速准确。     

复方妇炎康栓的制备及质量控制

目的:制备复方妇炎康栓剂并建立其质量标准、方法:以替硝唑、呋喃西林等为主药制备栓剂;以高效液相色谱法控制含量。结果:复方妇炎康栓中替硝唑和呋喃西林分别在192.0 480μg/ml～448.1 120μg/ml(r替=0.9 999)和9.6 672μg/ml～22.5 568μg/ml(r呋=0.9 998)浓度范围内线性关系良好;平均回收率分别为100.37％、101.45％,相对标准差分别为1.171％(n=5)、1.771％(n=5)。结论:复方妇炎康栓性质稳定,质量控制方法简便,含量测定准确、可靠。     

苦柏痔瘘栓的制备及其中小檗碱的含量测定

目的制备苦柏痔瘘栓剂,并对该栓中小檗碱进行含量测定。方法用水提醇沉法提取、纯化药物,使用丙二醇单硬脂酸酯做基质制备栓剂;采用紫外分光光度法测定小檗碱含量,测定波长为420nm。结果含药栓剂在37℃能够融化,盐酸小檗碱含量测定方法在2—10μg/ml范围内线性良好Y=0．0714X-0．0624（R2=0．9973,n=5）,平均回收率为99．77％RSD=1．8％（n=6）。结论此法可制备出性状优良的苦柏痔瘘栓,紫外分光光度法测定盐酸小檗碱含量稳定性好,操作快捷、经济实用。     

平阳霉素栓的制备及临床应用

目的：制备平阳霉素栓剂,治疗尖锐湿疣。方法：利用硬脂酸聚烃氧（40）酯为基质制备平阳霉素栓剂。并用紫外分光光度法进行含量测定。结果：平阳霉素溶液,在10－70μg.ml^-1范围内吸收民与浓度有良好线关系。平均回收率为（n=5）为100．095,RSD＝0．74％,临床应用对尖锐湿疣治愈率为93．94％,结论：平阳霉素栓剂性质稳定,紫外分光光度法测定快捷准确,治疗尖锐湿疣具有良好疗效。     

0．02％呋喃西林溶液的贮存期预测

目的预测0．02％呋喃西林溶液的贮存期。方法用分光光度法于波长376nm处测定0．02％呋喃西林溶液的含量,采用经典恒温实验法预测其在25℃时的贮存期。结果测得0．02％呋喃西林溶液25℃预测贮存期为130d,与留样观察结果相符。结论0．02％呋喃西林溶液的贮存期可定为4个月,以10～25℃、避光条件下贮存为宜。     

奥硝唑生物粘附性缓释栓的制备及质量控制

目的：制备治疗滴虫感染的奥硝唑生物粘附性缓释栓，并制定其质量控制标准。方法：以PEG—600，PEG—6000，CMC—Na为栓剂基质，奥硝唑为主药制成栓剂，并用紫外分光光度法测定主药的含量。结果：低、中、高3种浓度的平均回收率分别为99.92％，98．76％，100．61％，RSD分别为0．08％，1．24％，0．61％。结论：奥硝唑生物粘附性缓释栓制备工艺简单，栓剂成型性好，含量剩定方法可行，结果可靠。     

呋喃西林溶液处方和制备方法的改进及其质量控制

目的探讨呋喃西林溶液的处方和制备方法改进及其含量测定方法方法按改进的处方组成，将苯甲酸钠先配制成浓溶液，加入呋喃西林使完全溶解后，再加入其他药物配制。采用高效液相色谱（HPLC）法测定呋喃西林溶液中呋喃西林的含量。结果改进后的处方和配制方法所制备的呋喃西林溶液稳定性好，放置6个月以上不析出沉淀。呋喃西林质量浓度在10．2～101．6mg／L范围内与峰面积线性关系良好（r=0．9999），平均回收率N98．9％，RSD为1．24％。结论改进后的处方科学，配制方法操作简单、准确，具有很好的实用价值。     

HPLC测定复方甲硝唑含漱液中甲硝唑和呋喃西林的含量

目的：建立复方甲硝唑含漱液中甲硝唑和呋喃西林的含量测定方法。方法：色谱柱为Lichrospher C18（250mm×4．6mm,5μm）;流动相为乙腈-1％磷酸溶液（三乙胺调pH3．8）（20：80）;检测波长为263nm;柱温为35℃。结果：甲硝唑和呋喃西林的线性范围分别为606～1414μg·ml^-1,9．36-21．84μg·ml^-1,r=0．9999。甲硝唑平均回收率为100．8％,RSD为0．41％;呋喃西林平均回收率为99．5％,RSD为0．20％。结论：本方法简便、测定稳定、测定结果准确,能有效控制该制剂的质量。     

呋柳泡腾片中呋喃西林的定量研究

目的 建立呋柳泡腾片中呋喃西林的含量测定方法。方法采用紫外分光光度法在375nm处测定呋柳泡腾片中呋喃西林的含量。结果呋喃西林的线性范围为2.05μg-10.25μg／ml，回归方程为A=80878.05C-0．0084，r=1．0000；加样回收率为100．15％，RSD=0.7％。结论紫外分光光度法可用于测定呋柳泡腾片中呋喃西林的含量，方法准确，处方其他成分无干扰，重现性好。     

复方雌三醇栓的制备及质量控制

目的：研究复方雌三醇栓的制备方法及质量控制。方法：以半合成脂肪玻甘油酯为基质制备栓剂，并对制剂质量控制造行研究。结果：采用本法制备的栓剂质量稳定可靠，雌三醇平均回收率100．01％(n＝6)，RSD＝0．33％。结论：该制剂制备工艺简便，制出的栓剂比较理想；所用质量控制方法可行。     

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.