正交试验优选雷公藤涂膜剂的基质组成

目的优选雷公藤涂膜剂基质的组成和配比。方法采用正交试验法,以外观质量、成膜时间为指标,确定基质中不同辅料的最佳配比。结果以聚乙烯醇-124、CMC-Na、甘油比例为4∶1∶2制得的涂膜剂最稳定。结论优选得到的配方设计合理,制备工艺简单,质量可控,可以为工业生产提供理论基础。     

复方酮康唑涂膜剂的制备与疗效观察

目的 制备复方酮康唑涂膜剂并观察其临床疗效。方法 以聚乙烯醇-124为成膜材料制备涂膜剂，并观察其对102例手足癣、体癣或股癣患者的临床疗效．结果 涂膜剂成膜性能好，质量稳定，对皮挟无刺激性，临床总有效率达100％。结论 复方酮康唑涂膜剂制剂工艺可行，临床疗效可靠.     

复方芩E涂膜剂的制备与质量控制

目的 制备复方芩E涂膜剂,并对其质量进行控制.方法 以聚乙烯醇-124为成膜材料,按药剂学原理制备复方芩E涂膜剂,建立质量控制方法 并对主成分含量测定方法 进行了方法 学验证.结果 制备工艺合理、简单,质量控制方法 可行,制剂质量稳定,对家兔皮肤无刺激.结论 符合涂膜剂质量标准和要求,可供临床应用.     

磺胺嘧啶银涂膜剂的研制

目的研制磺胺嘧啶银涂膜剂并建立质量控制方法。方法拟定处方组成及制备工艺,以羧甲基壳聚糖、聚乙烯醇为辅料制备涂膜剂;用永停滴定法测定主药含量。结果羧甲基壳聚糖、聚乙烯醇不影响主药理化性质,对含量测定无干扰。主药平均回收率为100．6％,RSD=0．81（n=9）。结论该制剂制备工艺简单,含量测定方法准确,质量可控。     

用于治疗糖尿病足的中药复方涂膜剂制备工艺研究

目的：确定糖足康涂膜剂的制备工艺。方法：采用正交试验法,以聚乙烯醇用量、甘油用量、乙醇用量为考察因素,以成膜时间为考察指标,优选糖足康涂膜剂的最佳制备工艺。结果：本研究所得糖足康涂膜剂的最佳制备工艺为：聚乙烯醇用量为4g,甘油用量为1.5mL,乙醇用量为30mL。结论：本研究确定的糖足康涂膜剂的制备工艺合理、可靠,为糖足康涂膜剂的进一步研究提供理论基础。     

褐藻胶浆在皮肤外用制剂中的应用——Ⅰ.涂膜材料的研究

本文以自行研制的褐藻胶浆作成膜材料,制备了药物涂膜剂,并以褐藻酸钠,聚乙烯醇的相同药物制剂作对照,进行了抑菌,稳定性,药物释放等实验研究。结果表明,褐藻胶浆是一较理想的皮肤外用制剂新辅料。以该原料制备的制剂治疗渗出性皮肤病,疗效满意。     

丹参祛痘涂膜剂制备工艺及其抗炎作用

目的优选丹参祛痘涂膜剂提取工艺条件和制备方法,并对其抗炎作用进行观察。方法采用L_9(3)~4正交实验法考察温度、溶剂浓度、提取时间及提取次数对隐丹参酮和丹参酮ⅡA提取率的影响,优选醇提条件;正交实验优选出涂膜剂的基质组方;采用二甲苯所致小鼠耳廓肿胀模型研究该涂膜剂的抗炎作用。结果醇提工艺条件为8倍量90%乙醇75℃回流提取3次;时间分别为2、1、1 h,制备涂膜剂的基质最优组方为聚乙烯醇(PVA)∶甘油∶西黄蓍胶=1.0 g∶2.5 mL∶1.0 g;与基质对照组比较,祛痘涂膜剂中剂量(1%)与高剂量(2%)具有抗炎作用,能显著降低小鼠耳廓肿胀度(P<0.05)。结论丹参祛痘涂膜剂提取与制备工艺稳定可控,成膜性好,无刺激性,无毒,具有较显著的的抗炎作用。     

复方黄芩涂膜剂的制备及临床应用

目的　研究复方黄芩涂膜剂的制备与临床疗效。方法　制定复方黄芩涂膜剂的工艺 ,采用薄层层析法进行质量控制并作临床观察。结果　制剂质量稳定 ,质量控制方法可靠 ,疗效确切。结论　本制剂设计合理 ,稳定性好 ,可用于临床治疗。     

复方黄芩涂膜剂的制备及临床应用

目的 研究复方黄芩涂膜剂的制备与临床疗效。方法 制定复方黄芩涂膜剂的工艺，采用薄层层析法进行质量控制并作临床观察。结果 制剂质量稳定，质量控制方法可靠，疗效确切。结论 本制剂设计合理，稳定性好，可用于临床治疗。     

复方氧氟沙星涂膜剂的制备与临床疗效观察

目的：制备复方氧氟沙星涂膜剂并进行疗效观察。方法：采用壳聚糖为基质，制备含氧氟沙星、盐酸丁卡因等药物的涂膜剂，建立制剂质量控制方法，并进行临床疗效观察。结果：该制剂制备工艺简单，质量可靠，治疗复发性口疮有效率达98．8％。结论：该制剂制备工艺简单，疗效确切，临床使用安全可靠。     

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.