高效液相色谱法测定茵栀黄软胶囊的稳定性

目的 建立茵栀黄软胶囊中黄芩苷的高效液相色谱含量测定方法。并用此方法对茵栀黄软胶囊进行稳定性考察。方法 含量测定采用反相高效液相色谱法，Diamonsil—C18色谱柱，流动相为甲醇-0．4％磷酸（51：49），检测波长为277nm，流速为1．0ml／min，柱温为40℃。稳定性研究采用加速实验法。结果黄芩苷进样浓度在0.05149～0．574mg／ml范围内与峰面积呈良好线性关系（r=0．9999），该制剂中黄芩苷的平均加样回收率为98．4％，RSD=0．69％（n=5）。自制茵栀黄软胶囊经过3个月加速实验，黄芩苷相对含量无明显变化。结论 HPLC法能很好地分离、检测茵栀黄软胶囊中的黄芩苷，可用于该制剂中黄芩苷的含量测定；自制茵栀黄软胶囊的稳定性较好。     

高效液相色谱法测定黄连上清片中黄芩苷含量

目的用高效液相色谱法测定黄连上清片中黄芩苷含量。方法色谱柱为Diamonsil（钻石）C18柱（150mm×4．6mm，5μm），流动相为甲醇-2％醋酸溶液（55：45），检测波长为274nm，流速为1．0mL／min，柱温为26℃。结果黄芩苷进样量线性范围是0．11—2．20μg（r=0．9999），平均加样回收率为100．77％，RSD=1.32％（n=6）。结论该方法简便、灵敏，可用于制剂的质量控制。     

银黄口腔崩解片中黄芩苷含量的测定

目的测定银黄口腔崩解片中黄芩苷的含量。方法采用高效液相色谱法，色谱柱为Hypersil C18柱，流动相为甲醇-水-磷酸（50：50：0．2）。结果黄芩苷进样量线性范围为24．68～86．38μg／mL，r=0．9997，平均回收率为97．2％，RSD为0．97％（n=5）。结论该方法简便、准确、重现性好，可作为该制剂的含量测定方法。     

高效液相色谱法定量分析黄芩苷粗品中4种黄酮类成分

目的：建立黄芩苷粗品中黄芩苷、黄芩素、汉黄芩苷和汉黄芩素含量的高效液相色谱（HPLC）测定方法，以便控制其质量。方法：固定相用Agilent ZORBAX SB-C18柱（5μm，4．6mm×250mm），苷流动相为甲醇-水-冰醋酸（49：51：0．2），苷元流动相为甲醇-水-冰醋酸（61：39：0．2），检测波长为275nm。结果：黄芩苷、黄芩素、汉黄芩苷和汉黄芩素线性范围分别是0．102～1．020μg（r=0．9997），0．051～0．510μg（r=0．9994），0．01～0．51μg（r=0．9995），0．02～0．20μg（r=0．9999）；平均回收率（n=5）分别为99．12％（RSD为1．55％），101．60％（RSD为2．67％），102．27％（RSD为1．92％／40）和98．51％（RSD为3．13％）。结论：本方法简便、准确，可用于黄芩苷粗品的质量控制。     

高效液相色谱法测定双黄消炎片中黄芩苷和盐酸小檗碱的含量

目的 建立高效液相色谱法同时测定双黄消炎片中黄芩苷和盐酸小檗碱含量的方法。方法采用ODS C18（200mm×4．6mm，5μm）色谱柱，流动相为乙腈0．05mol·L^-1磷酸二氢钾溶液三乙胺（25：75：0．05），流速为1．0mL·min^-1，检测波长为265nm。结果黄芩苷和盐酸小檗碱分别在19．0-380．0μg·mL^-1（r=0．9999）、1．01-20．18μg·mL^-1（r=0．9999）内线性关系良好，平均加样回收率（n=6）分别为100．1％和98．5％。结论该方法简便、准确、重复性好，可同时测定双黄消炎片中黄芩苷和盐酸小檗碱的含量。     

高效液相色谱法测定复方鱼腥草口服液中黄芩苷和绿原酸含量

目的建立复方鱼腥草口服液中黄芩苷和绿原酸的含量测定方法。方法采用Shimadzu C18柱（250mm×4．6mm,5μm）,黄芩苷测定以甲醇-水-磷酸（45：55：0．2）为流动相,检测波长为315nm;绿原酸测定以乙腈-0．4％磷酸溶液（13：87）为流动相,检测波长为327nm。结果黄芩苷进样量在0．2654—1．3270μg范围内与峰面积线性关系良好,r=0．99996（n=5）,平均回收率为100．5％,RSD=1．08％（n=6）;绿原酸进样量在0．1072～0．5360μg范围内与峰面积线性关系良好,r=0．99998（n=5）,平均回收率为97．26％,RSD=1．41％（n=6）。结论该方法快速准确、结果可靠。     

反相高效液相色谱法测定争光抗菌片中黄芩苷的含量

目的：反相高效液相色谱法测定争光抗菌片中黄芩苷的含量，方法：HYPERSIL C18柱，流相为甲醇－水－磷酸（52：48：0．2），于280nm波长处检测。结果：黄芩苷的线性范围为0．116－1．856ug,r=0.9997，平均加样回收率为98．1％，RSD＝0．52％（n=3)，结论：方法简便，精密度和稳定性良好，适用于测定争光抗菌片中黄芩苷的含量。     

高效液相色谱法测定复方金银花颗粒中绿原酸和黄芩苷含量

目的：采用高效液相色谱法测定复方金银花颗粒中绿原酸和黄芩苷的含量。方法：色谱柱为Zorbax SB—C18（250mm×4．6mm，5μm），流动相为含1％乙酸的水-甲醇梯度洗脱，检测波长为280nm；柱温为25℃。结果：绿原酸在0．0465～0、2324μg范围内线性关系良好（r=0．9998），平均加样回收率为100．6％，RSD为0．6％；黄芩苷在0．2505～1．2525μg范围内线性关系良好（r=0．9995），平均加样回收率为100．1％，RSD为1．1％。结论：该方法简便、准确、重现性好，可作为复方金银花颗粒含量控制方法。     

RP-HPLC法测定珍黄丸中黄芩苷的含量

目的建立HPLC法测定珍黄丸中黄芩苷的含量质量控制方法。方法采用SinochromODSCIs柱，以甲醇一水_磷酸溶液（55：45：0．2）为流动相；流速为1．0ml·min-1；检测波长为280nm。结果黄芩苷在7．824—39．12μg范围内线性关系良好，r=0．9999；平均加样回收率为99．46％，RSD为1．3％（n=5）。结论本法专属性强，准确度高，重现性好，可作为该产品质量控制的方法。     

RP-HPLC法测定黄连上清丸中黄芩苷的含量

目的：采用高效液相色谱法测定黄连上清丸中黄芩苷的含量，以控制该制剂的质量。方法：以C18化学键合硅胶柱分离黄芩苷，以甲醇－水－醋酸（40：60：1）为流动相，UV检测波长274nm进行测定。结果：黄芩苷峰与其它组分峰能够基线分离，理论板数以黄芩苷峰计算为3500，方法的平均加样回收率为100．8％（n=5),5次独立测定的相对偏差RSD＝0．92％，黄芩苷在0．25－2．5μg范围内，进样量与吸收面积值呈良好的线性关系。结论：本法测定黄连上清丸中黄芩苷的含量。结果准确，重复性好。     

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.