外障眼药水的质量标准研究

目的 建立外障眼药水的质量标准.方法 对制剂中的黄连进行薄层色谱法鉴别;采用高效液相色谱法测定盐酸小檗碱的含量.结果 薄层色谱法检出盐酸小檗碱;盐酸小檗碱在0.2425 μg～1.94 μg线性关系良好,相关系数r=0.9999,平均回收率为99.98%,RSD=1.00%(n=9).结论 该方法简便、灵敏,重现性好,可用于控制外障眼药水的质量.     

胃安丸的质量标准研究

目的对胃安丸进行质量标准的研究.方法采用薄层色谱法对处方中的浙贝母、三七进行定性鉴别;采用高效液相色谱法对黄连(吴茱萸制)中的盐酸小檗碱进行含量测定.结果在薄层色谱中均可检出浙贝母、三七的特征斑点;盐酸小檗碱在0.0702～0.6318μg间线性关系良好,r=0.9999,平均加样回收率为97.31%(RSD=1.25%,n=5).结论本方法简便可行、重复性好,能有效控制该制剂的质量.     

复方健胃颗粒质量标准的研究

目的建立复方健胃颗粒的质量标准。方法采用薄层色谱法对制剂中的厚朴、黄柏、陈皮进行定性鉴别,采用高效液相色谱法测定制剂中的盐酸小檗碱。结果薄层图谱清晰,阴性对照无干扰,盐酸小檗碱进样量在0.4284².1420μg范围内线性关系良好(r=0.9998)。结论本方法简便、重现性好,可有效控制制剂的质量。     

四方胃片质量标准研究

目的:建立四方胃片的质量控制方法。方法:采用薄层色谱法对制剂中的延胡索和浙贝母进行定性鉴别,采用高效液相色谱法测定四方胃片中盐酸小檗碱的含量。结果:定性鉴别专属性强;盐酸小檗碱进样量在0.06～1.8μg范围内与峰面积积分值呈良好线性关系(r=0.9999),平均回收率为97.1%,RSD=1.6%(n=6)。结论:所建标准能有效控制该制剂的质量。     

复方黄连肠炎宁胶囊定性定量标准研究

目的建立复方黄连肠炎宁胶囊的质量标准。方法采用薄层色谱法对该制剂中黄连、黄芪、地榆、补骨脂进行定性鉴别;采用高效液相色谱法测定复方黄连肠炎宁胶囊中盐酸小檗碱的含量。结果薄层色谱斑点清晰、分离度好,专属性强,盐酸小檗碱在0.420 0~3.502 5μg线性关系良好,平均回收率为99.8%,RSD=0.2%(n=6)。结论所建立的方法简便可靠,重复性好,可用于复方黄连肠炎宁胶囊的质量控制。     

葛连解糖颗粒的质量标准研究

目的:建立葛连解糖颗粒的定性鉴别和含量测定方法。方法:采用薄层色谱法对葛连解糖颗粒中葛根、黄连、胡芦巴、枸杞子、地黄等进行定性分析;采用高效液相法,建立葛连解糖颗粒中葛根素、盐酸小檗碱的含量测定方法。结果:建立的薄层色谱鉴别方法,分别能检出葛根、黄连、枸杞子、地黄、胡芦巴药材,薄层斑点清晰,阴性对照均无干扰。葛根素进样量在21.1～337.6 ng(r=0.999 9),盐酸小檗碱进样量在43.1～689.9 ng范围内线性关系良好(r=0.999 9);葛根素平均回收率为97.21%,RSD为1.41%(n=6),盐酸小檗碱平均回收率为96.18%,RSD为1.22%(n=6)。结论:所建方法定性专属性强,定量准确度高,可用于葛连解糖颗粒的质量控制。     

肠炎清合剂的质量控制方法研究

目的:建立肠炎清合剂中君药黄连的鉴别及盐酸小檗碱、盐酸巴马汀含量测定方法。方法:采用薄层色谱法对合剂中黄连进行定性鉴别;采用HPLC进行含量测定。结果:薄层色谱均能明显的检出黄连的特征有效成分盐酸小檗碱和盐酸巴马汀;HPLC法中,盐酸小檗碱在1.34～42.8μg.mL-1内线性关系良好(r=0.9999),平均回收率99.3%,RSD=0.92%(n=9);盐酸巴马汀在1.24～39.8μg.mL-1内线性关系良好(r=0.9999),平均回收率98.6%,RSD=0.82%(n=9)。结论:本法简便、快速、灵敏、准确,重现性好,可以作为该合剂的质量控制方法。     

藏药八味獐牙菜丸的质量标准研究

目的：建立测定藏药八味獐牙菜丸中盐酸小檗碱含量的方法。方法：采用薄层色谱法和高效液相色谱法。结果：建立了八味獐牙菜丸中兔耳草和小檗皮的薄层色谱鉴别方法,并采用HPLC测定了该藏药制剂中小檗皮的有效成分盐酸小檗碱的含量,其回归方程为：y=4629102.46x-136034.70,r=0.9995,盐酸小檗碱的平均回收率为97.30%,RSD=1.57%（n=6）。结论：该方法测定快速、重现性好,可用于八味獐牙菜丸的质量控制。     

香蔹痔疮栓质量标准研究

目的:建立香蔹痔疮栓的质量标准。方法:采用薄层色谱法对方中黄连、五倍子、冰片进行定性鉴别;采用高效液相色谱法对盐酸小檗碱进行含量测定。结果:薄层鉴别斑点清晰,阴性无干扰;含量测定中盐酸小檗碱在0.18272μg~1.8272μg范围内与峰面积线性关系良好。结论:所建立方法可作为该制剂的质量标准。     

肾保康胶囊的质量标准

目的:建立肾保康胶囊的质量控制方法.方法:用薄层色谱法对肾保康胶囊中的金银花、发酵虫草菌粉进行定性鉴别;采用高效液相色谱法测定盐酸小檗碱的含量.结果:薄层色谱中斑点清晰,易于识别;盐酸小檗碱线性范围为0.0351～0.263μg,r=0.9999,平均回收率为96.30%,RSD为1.45%.结论:本方法简便,灵敏度高,可有效地控制肾保康胶囊的质量.     

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.