黑膏药风湿骨痛贴的皮肤安全性评价

目的:考察黑膏药风湿骨痛贴经皮给药的安全性.方法:采用健康家兔皮肤刺激性试验、健康豚鼠皮肤过敏性试验,观察风湿骨痛贴对动物经皮给药的刺激性和过敏性.结果:风湿骨痛贴对家兔完整皮肤和破损皮肤均无刺激性,对豚鼠皮肤无致敏性.结论:在本试验条件下风湿骨痛贴经皮给药无明显不良反应.     

风湿骨痛胶囊的制备与临床观察

目的:研制风湿骨痛胶囊,建立质量控制方法及观察临床疗效.方法:通过治疗风湿性关节炎及类风湿关节炎进行临床验证,采用化学法及薄层色谱法进行质量控制.结果:临床观察397例,总有效率87.6%.薄层色谱结果显现供试品色谱与对照药材色谱在相应的位置上,显相同颜色斑点.结论:风湿骨痛胶囊组方合理,制备方法简便,疗效确切,质量控制方法准确,灵敏,重现性好且简单易行.     

风湿骨痛贴膏的工艺探讨

目的优选风湿骨痛贴膏生产工艺的最佳工艺参数。方法:通过正交试验,以风湿骨痛贴膏成品率为指标。结果选用水与提取膏的比例为:2:1,加水后浸泡24hr,提取膏比重为1.25。结论风湿骨痛贴膏成品率高,制剂稳定性好,适合于工业生产。     

反相高效液相色谱法测定风湿骨痛颗粒中甘草酸的含量

目的　研究风湿骨痛颗粒中甘草酸的定量分析方法。方法　采用高效液相色谱法。色谱柱。shim packclc ODS(15 0mm× 4 6mm ) ;流动相 :甲醇 -水 -冰醋酸 -三乙胺(6 0∶38∶1∶0 3) ;检测波长 :2 5 0nm ;柱温 :30℃ ;结果　甘草酸含量测定的线性范围为 16 4 2～ 82 10 μg(r =0 9999,n =5 ) ,平均加样回收率为 98 0 2 % ,RSD为 1 4 2 %。结论　该方法简便、快速准确 ,可作为该制剂的质量控制方法     

风湿骨痛胶囊配合扶他林治疗双膝退行性骨关节炎的临床观察

目的探讨风湿骨痛胶囊配合扶他林对双膝关节退行性骨关节炎(DOA)的疗效和安全性.方法将75例DOA患者随机分3组治疗,试验组同时内服风湿骨痛胶囊及扶他林片.对照1组单纯内服风湿骨痛胶囊,对照2组单纯内服扶他林,观察其临床疗效、停药2周后复发惰况和不良反应.结果试验组的总有效率为92%,显效率为64%;对照1组的总有效率为72%,显效率为20%;对照2组的总有效率为80%,显效率为36%.试验组与对照1、2组比较总有效率无显著性差异(P＞0.05),显效率存在显著性差异(P<0.05).停药后复发率分别为8.7%、38.9%、50%,试验组与对照1、2组比较存在显著性差异(P<0.05).不良反应无显著性差异.结论风湿骨痛胶囊和扶他林配合使用能提高显效率,防止症状复发,而不良反应并没有相应增加.     

近红外光谱一致性检验方法快速鉴别风湿骨痛胶囊真伪

目的建立快速鉴别风湿骨痛胶囊真伪的近红外光谱一致性检验方法。方法采集风湿骨痛胶囊原料、正品胶囊及内容物的近红外光谱,用OPUS分析软件进行处理,建立风湿骨痛胶囊的近红外光谱一致性检验方法,用风湿骨痛胶囊伪品的近红外光谱进行验证。结果建立的近红外光谱一致性检验方法可快速、准确地判断风湿骨痛胶囊真伪。结论该方法是一种简便、快速、准确的分析技术,可以用于药品快速检测车的筛查和抽样。     

SPE技术在风湿骨痛片麻黄含量测定中的应用

目的采用SPE-HPLC联用技术测定风湿骨痛片麻黄中盐酸麻黄碱和盐酸伪麻黄碱的含量。方法采用Oasis MCX-SPE阳离子固相萃取小柱对样品进行前处理,Welch XDB-C18(250mm×4.6mm,5μm)为色谱柱,以乙腈-0.1mL·L~(-1)磷酸(用三乙胺调pH值至3.0)(5∶95)为流动相等度洗脱,流速1.0mL·min~(-1),检测波长207nm,柱温30℃。结果该实验条件下,盐酸麻黄碱和盐酸伪麻黄碱分离度好。盐酸麻黄碱进样量在22.99~1 150ng、盐酸伪麻黄碱进样量在14.60~730.2ng范围内线性关系良好,盐酸麻黄碱平均回收率为100.8%(RSD=2.8%),盐酸伪麻黄碱平均回收率为98.6%(RSD=2.4%)。结论该方法简便、专属性好,能有效消除复方中其他干扰,可用于风湿骨痛片中麻黄的质量控制。     

LC-MS/MS法对风湿骨痛宁胶囊中非法添加双氯芬酸的检查

目的采用LC-MS/MS联用技术,建立风湿骨痛宁胶囊中非法添加双氯芬酸的鉴别方法。方法色谱柱为SHIMADZU shim-pack VP-ODS,(0.02mol.-L1乙酸铵-0.1%乙酸)水溶液-乙腈(55:45)为流动相,流速为1.0mL.min-1,检测波长为280nm;Agilent 6310离子阱质谱仪,电喷雾离子源(ESI),雾化气压力为40psi,干燥气温度为350℃,流速为9mL.min-1,扫描范围150~500m.z-1。结果在高效液相色谱、质谱中,样品出现与双氯芬酸成分一致的色谱峰、质谱峰。结论本方法简单可行,结果准确可靠,可用于风湿骨痛宁胶囊中添加双氯芬酸成分的定性鉴别。     

反相高效液相色谱法测定风湿骨康片中士的宁的含量

目的:建立RP-HPLC法测定风湿骨康片中士的宁的含量,完善质量标准.方法:采用Hyper-C18柱,0.03mol·L-1甲酸溶液(用三乙胺调节pH至3.0±0.1)-乙腈(78∶22)为流动相,254nm为检测波长.结果:测得线性范围0.416μg～4.992μg(r=0.9998),平均回收率98.65%,RSD为1.88%(n=5).结论:本法简便,准确,专属性强.     

高效液相色谱法测定风湿骨康片中士的宁的含量

目的建立风湿骨康片中士的宁的测定法。方法采用高效液相色谱法,色谱柱为C18柱(250mm×4.6mm,5μm);流动相为乙腈-水-磷酸(28∶72∶0.1)含0.005mol·L-1庚烷磺酸钠溶液;流速1.0mL·min-1;柱温为30℃;检测波长为254nm。结果士的宁进样量在0.248~1.24μg范围内线性关系良好,r=0.9989,平均回收率为98.1%,RSD为2.2%。结论该方法简便可行,灵敏度高,重现性好,可作为风湿骨康片的质量控制标准。     

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.