玄麦甘桔口服液质量标准的提高

摘 要 目的：建立玄麦甘桔口服液的质量提高标准。方法: 采用TLC色谱法对菊花、甘草进行定性鉴别;采用HPLC色谱法定量测定菊花中木犀草苷的含量,以EcosIL C18柱为色谱柱（250 mm×4.6 mm,5 μm）,流动相为乙腈 0.1%乙酸溶液梯度洗脱,检测波长为350 nm,流速为1.0 ml·min-1,进样量为10 μl,柱温为30℃。 结果: TLC鉴别斑点清晰,阴性样品无干扰;木犀草苷进样量在58.65～586.50 ng之间, 线性良好 (r=1.000 0), 平均回收率为104.1%, RSD为1.4% (n=6) 。 结论: 本方法结果可靠, 操作简便, 可用于玄麦甘桔口服液的质量控制。     

补血益母颗粒质量标准的提高

摘 要 目的：提高完善补血益母颗粒的质量标准。方法: 采用TLC法对当归、黄芪进行鉴别;采用HPLC法测定黄芪中黄芪甲苷的含量,色谱柱为Agilent Zorbax SB C18柱(250 mm×4.6 mm,5 μm),流动相为乙腈 水（32∶68）,柱温为35℃,流速为1.0 ml·min-1,检测器为ELSD。结果:薄层色谱均斑点清晰,分离度较好;黄芪甲苷对照品在1.577～13.140 μg范围内线性关系良好（r=0.999 2）,平均回收率为96.88%,RSD=3.01%（n=6）。结论:本方法操作简便、准确可靠、重复性好,可用于该制剂的质量控制。     

止咳祛痰口服液质量标准的建立

摘 要 目的：建立止咳祛痰口服液的质量标准。方法: 采用TLC法对桔梗、甘草进行定性鉴别;采用HPLC法对射干的有效成分射干苷进行定量测定,色谱柱为Waters Symmetry C18柱（150 mm×4.6 mm,3.5 μm）,流动相为乙腈 水（14〖KG*9〗∶〖KG-*2〗86）,流速1.0 ml·min-1,柱温35℃,检测波长为265 nm。结果: 薄层色谱斑点清晰,阴性无干扰。射干苷在0.115～2.880 μg范围内线性关系良好（r=0.999 9）,平均回收率为92.44%,RSD为1.83%(n=6)。结论: 所建立的方法简便、快速、重复性好,可用于止咳祛痰口服液的质量控制。     

复方黄槐片质量标准的提高

摘 要 目的：提高并完善复方黄槐片的质量标准。方法: 采用TLC法对制剂中槐米、黄芩、赤芍、大黄、白茅根、鸡血藤、薏苡仁、夏枯草等8味药材进行定性鉴别;采用HPLC法测定芦丁的含量：色谱柱为DIKMA Spursil C18柱（250 mm×4.6 mm,5 μm),以甲醇 0.2%磷酸（45∶〖KG-*2〗55）为流动相;检测波长为350 nm;柱温为25℃;流速为1.0 ml·min^-1 ,进样量为20 μl。结果: TLC鉴别斑点清晰,阴性对照无干扰;芦丁在0.011 6～0.185 9 mg·ml^-1的浓度范围内有良好的线性关系(r=0.999 9),平均回收率为98.93%（RSD=1.14%,n=6）。结论: 提高后的质量标准具有操作简单、专属性强、重复性好的特点,可用于该制剂的质量控制。     

加味小柴胡颗粒质量标准的建立

摘 要 目的：建立加味小柴胡颗粒的质量标准。方法: 采用TLC法对制剂中柴胡、黄芩、黄连进行定性鉴别;采用UPLC法对制剂中甘草苷、黄芩苷、盐酸小檗碱、汉黄芩苷、黄芩素、甘草酸单铵盐进行定量分析。色谱柱：Aglient ZORBAX Eclipse Plus C18（50 mm×2.1 mm,1.8 μm）,流动相：乙腈（A） 0.1%磷酸水（B）,流速：0.4 μml·min-1,检测波长： [0~11 min:270 nm;11~12 min:254 nm],柱温：35 ℃,进样量：2 μl。结果: 柴胡、黄芩、黄连的TLC图谱斑点清晰,分离度好;甘草苷、黄芩苷、盐酸小檗碱、汉黄芩苷、黄芩素、甘草酸单铵盐质量浓度分别在1.764~28.224 μg·ml-1（r=0.999 9）、12.390~198.240 μg·ml-1（r=0.999 7）、2.496~39.936 μg·ml-1（r=0.999 9）、4.200~67.200 μg·ml-1（r=0.999 5）、0.940~15.040 μg·ml-1（r=0.999 9）、1.872~29.950 μg·ml-1（r=0.999 6）浓度范围内线性关系良好;平均回收率分别为103.26%,101.36%,97.66%,103.27%,101.37%,102.44%,RSD分别为0.71%,0.81%,2.53%,1.58%,2.31%,3.34%（n=6）。结论: 所建质量标准能有效控制加味小柴胡颗粒的质量。     

蓝玉簪颗粒的质量标准提高

摘 要 目的：建立蓝玉簪颗粒的质量提高标准。 方法: 采用TLC法定性鉴别蓝玉簪龙胆和三七总皂苷;采用HPLC法定量测定龙胆苦苷的含量。色谱柱为Promosil C18柱(250 mm×4.6 mm,5 μm),以甲醇 水（27∶73）为流动相,检测波长为270 nm,流速为1.0 ml·min-1,进样量为10 μl,柱温25℃。 结果: 薄层鉴别斑点清晰,阴性对照无干扰;龙胆苦苷含量在25.00～1 000.00 μg·ml-1之间线性良好(r=0.999 9),平均回收率为98.24%,RSD为3.04%(n=6)。 结论: 本方法结果可靠,操作简便,可用于蓝玉簪颗粒的质量控制。     

金黄连口服液质量标准的提高

摘 要 目的：建立金黄连口服液的质量提高标准。方法: 采用TLC法对金银花、黄芩、连翘中的绿原酸、黄芩苷、连翘苷进行定性鉴别;采用HPLC法定量测定金银花中绿原酸的含量,色谱柱：Promosil C18色谱柱(250 mm×4.6 mm,5 μm,Agela technologies公司);流动相：乙腈 0.4%磷酸（10∶90）;检测波长为327 nm;流速：1.0 ml·min^-1;进样量：10 μl,柱温：25℃。结果: 薄层鉴别斑点清晰,在与对照药材相同的位置上,显相同颜色的荧光斑点,阴性样品无干扰;绿原酸含量在5.325～170.400 μg·m-1之间,线性良好(r=0.999 8),平均回收率为97.95%,RSD为2.04%(n=6)。结论: 本方法结果可靠,操作简便,可作为金黄连口服液的质量控制方法。     

HPLC法测定氨糖美辛肠溶片的含量

摘 要 目的：建立HPLC法测定氨糖美辛肠溶片中吲哚美辛和盐酸氨基葡萄糖含量。方法: 采用Waters BridgeC18 (250 mm×4.6 mm,5 μm)色谱柱,以磷酸二氢铵(以磷酸调节pH至3.0)（A）,乙腈(B)为流动相,梯度洗脱,流速为0.7 ml·min-1,检测波长195 nm,进样量为20 μl,柱温30℃。结果: 盐酸氨基葡萄糖在0.030 0～1.500 8 mg·ml-1（r=0.999 1）,吲哚美辛在0.010 3～0.513 0 mg·ml-1（r=0.999 9）范围内线性关系良好;平均回收率分别为98.3% （RSD=0.33%,n=6）;99.9% （RSD=0.06%,n=6）。结论: 此方法准确、快速、灵敏、专属性强,可较好地控制该产品的质量。     

甘草浸膏胶囊质量标准的建立

摘 要 目的：建立甘草浸膏胶囊中两种有效成分质量控制标准。方法: 采用TLC法对方中甘草进行鉴别;测定样品中甘草苷和甘草酸铵的含量。色谱条件：色谱柱为Inertsil C18柱(150 mm×4.6 mm,5 μm);流动相：乙腈(A) 0.2%磷酸(B) (0～8 min:20%A～20%A;8～34 min:20%A～50%A;34～35 min:50%A～100%A;35～40 min:100%A～20%A);流速为1.0 ml·min-1;检测波长：237 nm;柱温：25℃。结果: 薄层定性鉴别的斑点清晰,分离效果良好;甘草苷在0.002 0～0.100 0 mg·mL^-1浓度范围内线性关系良好（r=0.999 5）,平均加样回收率为100.29％,RSD为2.94％(n=6);甘草酸铵在0.002 0～0.100 0 mg·mL^-1浓度范围内线性关系良好（r=0.999 8）,平均加样回收率为101.46％,RSD为2.33％(n=6)。结论: 所建立方法快速简便,重复性好,专属性强,可作为该制剂的质量控制方法。     

HPLC法测定米诺地尔洗剂含量及温度对含量影响的考察

摘 要 目的：建立高效液相色谱法同时测定化瘀祛斑胶囊中芍药苷、黄芩苷和黄芩素的含量。方法: 色谱柱为Agilent Zorbax SB C18柱（150 mm×4.6 mm,5 μm）;流动相为甲醇 0.1%磷酸溶液,梯度洗脱;流速为1.0 ml·min-1;检测波长为230 nm（0~15 min）,277 nm（15~45 min）;柱温为25℃;进样量为10 μl。结果: 芍药苷、黄芩苷和黄芩素的线性范围分别为1.295～25.890 μg·ml-1（r=0.999 9）、30.050～601.000 μg·ml-1（r=0.999 9）、1.874~37.480 μg·ml-1（r=0.999 9）,平均回收率分别为100.9%,100.3%,99.31%,RSD分别为0.92%,1.30%,0.89%。结论: 该法简便、快捷、结果准确、重复性好、实用性强,可以用于化瘀祛斑胶囊的质量控制。     

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.     

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.