金叶败毒颗粒质量标准的实验研究

目的：建立金叶败毒颗粒的质量标准。方法：采用薄层色谱法鉴别其中绿原酸、靛玉红;采用高效液相色谱法,在ＹＷＧＣ１８柱（４．６ｍｍ×２５０ｍｍ）上,以乙腈水冰醋酸（３∶４６∶１）为流动相,流速１．５ｍｌ·ｍｉｎ－１,检测波长为３２８ｎｍ,测定其中绿原酸的含量。结果：绿原酸、靛玉红的薄层色谱鉴别方法有良好的重现性、专属性;绿原酸在０．３０～３．００μｇ呈良好的线性关系（ｒ＝０．９９９６）,其含量测定方法稳定、精确,平均回收率达９６．３％±１．５％。结论：制定的质量标准可以保证金叶败毒颗粒的质量。     

痔痛消中苦参碱的含量测定

目的：用薄层扫描法对痔痛消中苦参碱进行了含量测定。方法：以氯仿甲醇氨水（５∶０．６∶０．２）为展开剂,在ＣＳ９２０薄层扫描仪上以反射式锯齿扫描方式进行测定,λｓ＝５１２ｎｍ。结果：样品含量在５～２５μｇ范围内呈良好线性关系,ｒ＝０．９９６５（ｎ＝５）,平均回收率９９．９０％,ＲＳＤ＝０．９５％。结论：方法简便、精确、快速、重现性好,可作为痔痛消的质量控制标准。     

反相高效液相色谱法测定萘普生钠血浆浓度

目的：建立用高效液相色谱法测定萘普生钠血浆浓度的方法。方法：血浆样品在酸性条件下,以１,２二氯乙烷提取,吲哚美辛为内标,采用ＬｉｃｈｒｏｓｏｒｂＣ１８（５μｍ）柱,流动相为甲醇∶醋酸醋酸铵缓冲液（ｐＨ４．５）＝７４∶２６,流速为１．０ｍｌ·ｍｉｎ－１,检测波长３１８ｎｍ,萘普生和内标的保留时间分别为３．３５和４．７１ｍｉｎ。结果：线性范围在１～９０μｇ·ｍｌ－１（ｒ＝０．９９９９,最低检测浓度为０．４μｇ·ｍｌ－１血浆,ＲＳＤ％＜３．５。结论：本方法可用于萘普生钠的药物动力学研究     

高效液相色谱法测定雷登泰口服液中创木酚甘油醚,盐酸伪麻黄？…

采用高效液相色谱外标法测定雷登泰口服液中愈创木酚甘油醚，盐酸伪麻黄碱，氢溴酸右美沙芬的含量。色谱柱为ＳｐｈｅｒｉｓｏｒｂＣ８ ５μｍ４．６ｍｍ２５０ｍｍ，流动相为０．００２５ｍｏｌ．Ｌ＾－１己烷磺酸甲醇溶液－水（含２％三乙胺）－３ｍｏｌ．Ｌ＾－１磷酸（１．４：１．０：０．０６３），紫外检测器，检测波长２５７ｎｍ。结果愈创木酚甘油醚进样量在２．０－１０．０μｇ，盐酸为伪麻黄碱在０．３－１．５μｇ，氢     

金叶败毒颗粒质量的实验研究

目的;建立金叶败毒粒的质量标准。方法：采用薄层色谱法鉴别其中绿原酸、靛玉红;采用高效上色谱地,在ＹＷＧＣ１８柱（４．６ｍｍ×２５０ｍｍ）上,以乙腈－水－冰醋酸（３：４６：１）为流动相,流束这１．５ｍｌ·ｍｉｎ＾－１,检测汉长为３２８ｎｍ,测定其中绿原酸的含量。结果：绿原酸、靛玉红的薄层色谱鉴别方法有良好的重现性、专属性;绿原酸在０．３０－３．００μｇ呈良好的线性关系。其含量测定方法稳定、精确,平均     

高效液相色谱法测定头孢氨苄胶囊含量

目的：介绍一种用反相高效液相色谱法测定头孢氨苄胶囊含量的方法。方法：以ＳｈｉｍｐａｃｋＣＬＣＯＤＳ（１５０ｍｍ×６ｍｍ,１０μｍ）为色谱柱,甲醇水（７０∶３０）为流动相,检测波长为２６２ｎｍ,外标法定量。结果：头孢氨苄浓度线性范围为１００～９００μｇ·ｍｌ－１,相关系数ｒ＝０．９９９９,方法回收率为９９．７％,ＲＳＤ为０．８９％。结论：方法简便快速,结果准确可靠,可作为头孢氨苄制剂的质量控制方法。     

高效液相色谱法测定罗红霉素颗粒剂的含量

目的：探讨反相高效液相色谱法测定罗红霉素颗粒剂含量的方法。方法：在Ｃ１８柱上以乙腈０．０８３ｍｏｌ·Ｌ－１醋酸铵甲醇（５５∶２３∶２８）,并以醋酸调节ｐＨ６．８为流动相,在２１５ｎｍ波长处检测。结果：在０．５～７ｍｇ·ｍｌ－１浓度范围内,浓度与样品峰面积呈良好线性关系（ｒ＝０．９９９５）,样品回收率为９９．９２％（ｎ＝６,ＲＳＤ０．８９％）。结论：方法简便可靠,能够满足颗粒剂含量测定的要求     

An expressional system of human cytochrome P-450 CYP1A1 gene transcription

目的：在人ＨｅｐＧ２细胞系上，建立人细胞色素Ｐ４５０ＣＹＰ１Ａ１（ＣＹＰ１Ａ１）基因转录的表达系统．方法：瞬时转染含人ＣＹＰ１Ａ１启动子的质粒（ｐＭＣ６３Ｋ）、ＥＬＩＳＡ法测定报道基因氯霉素乙酰转移酶（ＣＡＴ）的含量和酶学测定ＣＹＰ１Ａ１活性．结果：β萘黄酮２．５μｍｏｌ·Ｌ－１明显增强ＣＡＴ表达和ＣＹＰ１Ａ１活性（Ｐ＜０．０１）；在２．５－１０μｍｏｌ·Ｌ－１范围内，ＣＡＴ表达随浓度增高而不断增强，而ＣＹＰ１Ａ１活性则接近最高水平；１０μｍｏｌ·Ｌ－１时它们的作用强度分别为对照组的９４．３和２．８倍．用这种方法对八种含不同侧链的芥子油苷进行检测的结果表明，芸苔苷的水解产物（而非吲哚３原醇）诱导ＣＹＰ１Ａ１基因表达．结论：ＣＹＰ１Ａ１基因转录表达系统具有较高的可靠性和灵敏度     

HPLC法测定通脉活血口服液中葛根素含量

目的：测定通脉活血口服液中葛根素含量。方法：ＨＰＬＣ法,色谱条件：ＣＬＣ－ ＯＤＳ柱（１５０ｍｍ×６ｍｍ ,５μｍ）,流动相：５％ 醋酸溶液－ 甲醇（８０∶２０） ,检测波长：２７６ｎｍ 。结果：进样量在０－２４ ～１－２２μｇ 范围内线性关系良好,ｒ＝ ０－９９９８。平均回收率１００－１４％ ,ＲＳＤ＝１－１％ （ｎ ＝６）。结论：方法简便、准确、灵敏度高,可作为本品含量测定方法。     

薄层扫描法测定抗炎灵口服液中连翘苷的含量

目的：采用双波长薄层扫描法测定抗炎灵口服液中连翘苷含量。方法：连翘苷测定波长λＳ＝５１０ｎｍ,参比波长λＲ＝７００ｎｍ;展开剂为：环己烷氯仿苯甲醇（５∶３∶５∶３）,显色剂为１０％硫酸乙醇液;用反射式锯齿扫描测定。结果：连翘苷的平均回收率为９５．２％,ＲＳＤ为１．２％。结论：该法分离效果好,简便,结果准确,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.     

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.