塞来昔布凝胶剂的制备及含量测定

目的：制备塞来昔布凝胶并建立测定塞来昔布凝胶剂含量的方法。方法：以卡波姆940为凝胶基质制备塞来昔布凝胶剂;采用高效液相色谱法测定主药含量。结果：本法制得的凝胶均匀细腻,易涂布;塞来昔布在2．05～205．20μg·ml^-1浓度范围内线性关系良好（r=0．9999）,平均回收率为100．01％,RSD=0．18％。结论：该方法操作简便,准确可靠。     

复方环麻滴鼻凝胶剂的制备及质量控制

目的：制备复方环麻滴鼻凝胶剂有其质量控制。方法：以卡波姆－940为乳化剂，三乙醇胺调节pH,制备水溶性透明凝胶。用紫外分光光工法和旋光度分别测定凝胶剂中盐酸丙沙星和盐酸麻黄碱的含量。结果：制备的凝胶均匀细腻，稠度适宜。盐酸环丙沙星的含量平均值为102．3％，RSD为1．86％；平均回收率为99．4％，RSD为0．26％。盐酸麻黄碱的平均含量为103．7％，RSD为2．8％；平均回收率为99．7％，RSD为0．81％。结论：该制剂性能稳定，无刺激性，测定方法简单易行，快速准确，适合医院制剂。     

复方氯霉素凝胶的研制及质量控制

目的：制备复方氯霉素凝胶剂。方法：以氯霉素、己烯雌酚、硫酸锌为主药，卡泊姆为凝胶基质，制备复方氯霉素凝胶。用导数光谱法控制主药氯霉素的含量。结果：氯霉素的平均回收率为100．74％，RSD为0．29％。结论：该凝胶剂制备工艺简单，凝胶性质稳定，质量可控，可满足临床需求。     

尼美舒利透明质酸凝胶的制备及质量控制

目的：研究尼美舒利透明质酸凝胶的制备及质量控制。方法：采用卡波姆等为基质制成凝胶剂，用紫外分光光度法测定凝胶中尼美舒利的含量，检测波长296nm。结果：含量测定平均回收率为99．8％，RSD为1．1%(n=5)。结论：该制剂处方合理，制备工艺简便，稳定性好，质量易于控制。     

复方加替沙星壳聚糖凝胶的制备与质量控制

［摘要］目的研究复方加替沙星壳聚糖凝胶剂的制备工艺，建立质量控制方法。方法以壳聚糖、卡波姆为凝胶材料制备复方加替沙星壳聚糖凝胶剂；采用紫外分光光度法测定加替沙星含量；采用容量法测定谷氨酸锌含量。结果该凝胶剂制备工艺简单，质量控制方法可行，质量稳定。结论该凝胶剂符合《中华人民共和国药典》凝胶项下有关规定。     

盐酸丁卡因凝胶剂的研制和质量控制

目的 制备盐酸丁卡因凝胶剂，并建立质量控制标准。方法 以正交试验法筛选基质最佳处方，并建立了酸碱度、含量测定等质量控制标准。结果 含量测定平均回收率为99．86％，RSD为0．36％。结论 制备该凝胶剂工艺简单，质量可控。     

五虎壳聚糖凝胶剂的制备与临床应用

目的：研宄五虎壳聚糖凝胶剂的制备方法与临床应用。方法：含挥发油的药材采用蒸馏法提取挥发油，其他药材采用水煎煮法提取，以壳聚糖为凝胶材料制备五虎壳聚糖凝胺剂；用薄层层析法进行鉴别，用高效液相色谱法测定含量．结果：该凝胶剂制备工艺简单，质量控制方法可行。临床疗效可靠。结论：该制剂符合《中国药典》凝胶剂项下有关规定.     

赤黄肝康口服液的制备和质量控制

目的：建立赤黄肝康口服液的制备工艺和质量控制方法。方法：以赤芍、大黄、茵陈、五味子和丹参制备赤黄肝康口服液，采用薄层色谱（TLC）对该制剂中赤芍和大黄进行鉴别，采用高效液相法（HPLC）测定芍药苷的含量。结果：制备的赤黄肝康口服液符合制剂要求；TLC鉴别有专属性；芍药苷的平均回收率为99．53％，RSD为0．47％。结论：该制剂制备工艺简单可行，质量控制方法准确可靠。     

氟比洛芬凝胶剂的制备与质量控制

目的研制氟比洛芬凝胶剂，并建立其质量控制方法。方法选用壳聚糖为凝胶材料制备氟比洛芬凝胶剂，采用紫外分光光度法进行定性鉴别，采用高效液相色谱法测定氟比洛芬含量。结果氟比洛芬质量浓度在10～100μg／mL范围内与峰面积线性关系良好，平均回收率为99．93％，RSD为1．15％。结论该制剂制备工艺合理，质量控制方法可靠。     

左氧氟沙星凝胶的制备及质量控制

目的 建立制备左氧氟沙星凝胶剂及质量控制的方法。方法 用聚乙烯醇124作凝胶基质，制备左氧氟沙星凝胶；采用紫外分光光度法进行含量测定，测定波长为293nm；一元线性回归分析．线性范围为2.0～12．0mg／L，r=0．9999．结果 含量测定平均回收率为99．8％．RSD=0．15％(n=5)。结论 制备该凝胶工艺简单，质量稳定，测定方法可靠，应用无刺激，可供临床应用。     

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.