通便灵的生产工艺改革

为了提高通便灵胶囊中番泻苷的含量,改进通便灵生产工艺.根据番泻苷的性质进行提取,用可见紫外分光光度法对番泻苷B进行测定.     

高效液相色谱法测定肠必清肠溶颗粒剂中番泻苷的含量

目的 :建立高效液相色谱法测定肠必清肠溶颗粒剂中番泻苷A、B含量的方法。方法 :以C18 柱为分析柱 ,以50 %乙腈 (含0 25mmol/L十六烷基三甲基溴化铵和0 25mmol/L磷酸氢二钠 ,每200ml加入冰醋酸75μl)为流动相 ,流速为1ml/min ,检测波长为270nm。结果 :在0 25μg/ml～80 0μg/ml浓度范围内呈线性关系 (番泻苷A :r=0 9997 ;番泻苷B :r=0 9997) ,番泻苷A、B测定方法重现性较好 (RSD<2 % )的精密度均<2 % ,回收率均>98 %。结论 :本方法简单、准确、重现性好 ,可以用于肠必清肠溶颗粒剂的质量控制     

通便灵胶囊中松果菊苷的含量测定及质量情况分析

目的：建立通便灵胶囊中肉苁蓉有效成分松果菊苷的含量测定方法,了解通便灵胶囊的整体质量情况,保障公众用药安全有效。方法：采用高效液相色谱法(HPLC)测定松果菊苷的含量,流动相为甲醇-0.1%甲酸溶液,梯度洗脱,检测波长为340 nm。结果：松果菊苷在2.867～286.742 μg/mL 之间呈良好的线性关系(r=0.999 9),回收率为102.1%,RSD为0.8%。通过对45批次通便灵胶囊的松果菊苷含量测定,发现各批次之间质量状况存在差异,提示部分生产厂家存在少投或用劣质药材(饮片)投料的现象。结论：该方法操作简便、结果准确,为通便灵胶囊的全面质量控制提供了科学依据。     

通便灵胶囊质量标准改进

目的提高通便灵胶囊的质量控制标准。方法参照2005年版《中国药典（一部）》番泻叶的质量要求，对该产品的质量进行全面检测，并用薄层色谱法对其番泻苷进行定性鉴别，用紫外分光光度法对总番泻苷含量进行测定。结果采用薄层定性方法，斑点清晰，分离完全，易于区别。含量测定方法的精密度为1．8％，平均回收率为99．43％，RSD=1．05％（n=6）。结论建立的定性及定量方法准确、可靠、重现性好。可作为通便灵胶囊的质量控制方法。     

HPLC法测定通便灵胶囊中番泻苷A的含量

目的测定通便灵胶囊中番泻苷A的含量。方法采用Discovery C18为色谱柱,乙腈-0.1%磷酸溶液(18∶82)为流动相,检测波长为271nm。结果平均回收率为99.72%,RSD=1.0%(n=9),线性范围为0.10~2.05μg,相关系数为1.0000。结论该方法简便、准确、可靠。     

HPLC法测定通滞苏润江胶囊中番泻苷A、B的含量

目的：建立通滞苏润江胶囊中番泻苷A、B的含量测定方法.方法：采用HPLC法对通滞苏润江胶囊中的番泻苷A、B含量进行测定,SinoChrom ODS BP色谱柱（250 mm×4.6 mm,5μm）,流动相乙腈-5 mmol·L-1四庚基溴化铵的醋酸.醋酸钠缓冲液（pH5.0）（1→10）（37：63）,流速：1.0 ml·min-1,柱温：40℃,检测波长：340 nm.结果：番泻苷A进样量在41.971～2 098.552 ng的范围内线性关系良好（r=0.999 9）,平均回收率为99.52％（RSD=1.39％,n=6）;番泻苷B进样量在42.781～2 139.046ng的范围内线性关系良好（r=0.999 9）,平均回收率为99.36％（RSD=1.45％,n=6）.结论：方法简便快捷,适用于该制剂中番泻苷A、B的含量测定.     

HPLC法测定番泻叶中番泻苷A及番泻苷B的含量

目的：鉴于用紫外分光光度法测定番泻叶中的番泻苷总含量，操作流程长，操作较为复杂，繁琐，操作条件要求苛刻，因此建立用HPLC法测定番泻苷A，番泻苷B的方法。用ODS色谱柱，检测波长340nm，流动相为乙腈-1mol/L醋酸-醋酸钠缓冲液（pH5.0)(1→10)(35:65)该混合液1000ml中，加入四庚基溴化铵2.45g，外标法。结果：加样回收率：番泻苷A98.72%RSD=1.62%，番泻苷B100.15%RSD=1.49%。线性范围：SA0.0464-0.6960μgrA=0.9999,SB0.0973-1.4600μgrB=0.9999。该方法操作简便，可靠，易行。     

抗癌平胶囊中野黄芩苷含量的HPLC研究

目的：建立抗癌平胶囊中野黄芩苷的含量测定方法。方法：采用高效液相色谱法,ODS C_(18)柱(250×4．6mm,5μm)；流动相：甲醇—0．04%磷酸水溶液(35：65)；检测波长：270mm。结果：野黄芩苷在4～138μg/ml范围内与峰面积呈现良好的线性关系,y=0．019X 0．2688,r=1．0000,平均回收率为99．61%,RSD值为1．05%。结论：该方法方便,准确可靠、重视性好,可作为抗癌平胶囊中野黄芩苷的含量测定方法。     

RIP-HPLC法测定通便胶囊中二苯乙烯苷的含量

目的：建立测定通便胶囊中二苯乙烯苷含量的反相高效液相色谱法。方法：采用ZORBAX ODS C18色谱柱（250mm×4．6mm,5μm）,流动相：乙腈-水（25：75）;流速：1．0ml·min^-1;检测波长：320nm;柱温：30℃。结果：二苯乙烯苷在1—250μg·ml^-1 线性关系良好（r=0．9999）;平均回收率为98．9％,RSD1．7％（n=6）。结论：该方法操作简便、快速,适用于通便胶囊中二苯乙烯苷的含量测定。     

高效液相色谱法测定通便灵胶囊中大黄酸的含量

目的 :建立 HPL C法测定通便灵胶囊中大黄酸含量的方法。方法 :采用 Shim- pack VP- ODS(15 0 mm× 4 .6mm,5 μm)色谱柱 ;流动相为甲醇 -水 (70∶ 30 ,磷酸调至 p H=3) ;柱温 :2 4 o C;流速 :1.0 ml/ min;检测波长 :4 37nm。结果 :大黄酸线性范围为 0 .132～ 2 .6 4 μg,r=0 .9991,平均回收率 =10 0 .34% ,RSD=1.2 9%。结论 :此方法可做为通便灵胶囊中大黄酸含量测定的方法 ,为制定该制剂的质量控制标准提供了依据。     

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.