一阶导数光谱法测定偏头宁滴鼻剂中盐酸利多卡因的含量

目的：探讨偏头宁滴鼻剂中盐酸利多卡因含量的测定方法。方法：采用一阶导数光谱法。结果：盐酸利多卡因浓度在0.1-0.5mg/mL范围内与在λ=270nm处所测得的振幅值呈良好的线性关系，平均回收率为100.04%，RSD=0.5%(n=6)。结论：方法简便、准确，可用于偏头宁滴鼻剂的质量控制。     

对呋麻滴鼻液中麻黄碱含量的检测

呋喃西林、盐酸麻黄碱滴鼻剂治疗急、慢性鼻炎长期使用于临床。该制剂配方中含呋喃西林0.02％、盐酸麻黄碱2％。在质检过程中由于使用乙醚提取、酸碱中和化测法测定呋麻滴鼻液中盐酸麻黄碱含量不易判定终点,因此改用751G型紫外仪,分别测定二组份在λ200～240nm范围,△λ为2nm的A值,通过导数解析法将其零阶导数光谱图绘制成一阶导数光谱图,由一阶导数谷零法摒除滴鼻剂中呋喃西林对盐酸麻黄碱含量测定的干扰,定量分析麻黄碱成分。此方     

-阶导数光谱法测定偏头宁滴鼻剂中盐酸利多卡因的含量

目的:探讨偏头宁滴鼻剂中盐酸利多卡因含量的测定方法。方法:采用-阶导数光谱法。结果:盐酸利多卡因浓度在0.1～0.5mg/mL范围内与在λ=270nm处所测得的振幅值呈良好的线性关系,平均回收率为100.04％,RSD=0.5％（n=6）。结论:方法简便、准确,可用于偏头宁滴鼻剂的质量控制。     

二阶导数光谱法同时测定葛根芩连微丸盐酸小檗碱和黄芩甙含量

目的建立葛根芩连微丸中盐酸小檗碱和黄芩苷的含量测定方法.方法采用二阶导数光谱法,以无水乙醇为溶剂,测定波长分别为(365 ±1) nm和(274 ±1) nm.结果盐酸小檗碱在4～12 μg·ml-1浓度范围内线性关系良好 (r＝0.9996) ,平均回收率为100.5%(n=5,RSD1.65%);黄芩苷在 5～15 μg·     

双波长二阶导数光谱法测定盐酸苯海拉明糖浆的含量

本文采用双波长二阶导数光谱法直接测定盐酸苯海拉明糖浆中盐酸苯海拉明的含量,其浓度在2.5～25.0μg/ml 范围内呈较好的线性关系,标准曲线方程为Δ((dαA)/(dλ~2))=0.00658c-0.00095,r=0.9999。在三种不同浓度下的回收率(n=3)分别为100.13%,99.56%,100.33%;CV%为0.11%,0.84%、0.64%。     

二阶导数光谱法测定海仙灵口服液中甲硝唑含量

目的:建立二阶导数光谱法测定海仙灵口服液中甲硝唑含量的方法。方法:用二阶导数光谱法直接测定海仙灵口服液中甲硝唑含量,276.8nm波长处测定振幅D值。结果:甲硝唑在5.15～25.75μg·ml~(-1)范围呈良好线性关系;其回归方程为D=0.835×10~(-4)C-1.1×10~(-4)(r=0.9970),平均回收率99.71%、RSD=2.39%(n=5)。结论:本方法操作简单、准确,可用于测定海仙灵口服液中甲硝唑含量。     

二阶导数光谱法测定复方异丙嗪糖浆中盐酸异丙嗪的含量

目的用紫外分光光度法不经分离直接测定复方异丙嗪糖浆中盐酸异丙嗪的含量。方法二阶导数光谱法,测定波长为256nm。结果盐酸异丙嗪在5．21～31．26ug/ml浓度范围内线性关系良好,峰零间振幅D对浓度C的回归方程C=-651．25×D＋0．3256,r=1．0000,平均回收率为101．10％,相对标准偏差为0．98％。结论二阶导数光谱法测定复方异丙嗪糖浆中盐酸异丙嗪含量简便、快速、结果准确。     

HPLC法同时测定重酒石酸去甲肾上腺素注射液和盐酸去氧肾上腺素注射液的含量及有关物质

目的:建立测定重酒石酸去甲肾上腺素注射液和盐酸去氧肾上腺素注射液含量及有关物质的方法.方法:采用高效液相色谱法,色谱柱:Kromasil C18色谱柱(4.6 mm×250 mm,5 μm);流动相:甲醇-乙腈-庚烷磺酸钠溶液(1∶1∶8);检测波长:280 nm;流速:1 ml/min;柱温:30 ℃.结果:重酒石酸去甲肾上腺素在80～320 μg/ml范围内与峰面积呈良好的线性关系,r=0.999 8;高、中、低3种浓度的平均回收率为101.2%,RSD为0.18%(n=9).重酒石酸去甲肾上腺素的最小检测限为152.3 ng/ml.盐酸去氧肾上腺素在100～400 μg/ml范围内与峰面积呈良好的线性关系,r=0.999 6;高、中、低3种浓度的平均回收率为98.1%,RSD为0.051%(n=9).盐酸去氧肾上腺素的最小检测限为103.8 ng/ml.结论:该法简便、准确、灵敏度高,重现性好,可用于重酒石酸去甲肾上腺素注射液和盐酸去氧肾上腺素注射液的含量测定和有关物质检查.     

氧麻滴鼻剂的制备

目的:研究氧麻滴鼻剂的制备方法和含量测定方法。方法:氧麻滴鼻剂用溶解法制备;采用初匀速法进行稳定性考察:氧麻滴鼻剂中氧氟沙星的含量测定采用紫外分光光度法,先绘制标准曲线,得回归方程,然后进行回收率实验和含量测定;盐酸麻黄碱采用旋光法测定含量。结果:在25℃条件下,氧麻滴鼻剂的贮存期为2.32年。氧氟沙星的回归方程为:C=11.0545A 0.1875(r=0.9992,n=12),回收率为99.60％,RSD为1.02％(n=6)。盐酸麻黄碱回收率为99.87％,RSD为0.63％(n=6)。结论:氧麻滴鼻剂稳定性较好。所建立的含量测定方法,操作简便,结果准确,能够达到制荆质量控制的要求。     

用加校正因子的主成分自身对照法测定盐酸去氧肾上腺素中杂质C的含量

目的建立加校正因子的主成分自身对照法测定盐酸去氧肾上腺素中杂质C的含量。方法采用C18柱(4.6 mm×250 mm,5μm),以乙腈∶0.325%磺酸钠(用磷酸调节p H值为2.8)(10∶90)为流动相,梯度洗脱,流速为1.5 m L·min-1,柱温为45℃,检测波长为215 nm,进样量为20μL。测定杂质C相对于盐酸去氧肾上腺素的相对出峰时间及校正因子,并计算其含量。结果杂质C在0.065 1~1.626 9μg·m L-1,盐酸去氧肾上腺素在0.064 7~1.618 4μg·m L-1浓度范围内,峰面积与浓度呈良好的线性关系;杂质C相对于盐酸去氧肾上腺素的相对保留时间为1.3,校正因子为0.50。结论本方法专属性强,结果准确可靠,无需提供杂质对照品,能够准确测定盐酸去氧肾上腺素中杂质C的含量。     

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.