依诺沙星壳聚糖阴道栓的研制

目的研究依诺沙星壳聚糖阴道栓的处方、制备工艺、质量控制、刺激性。方法以壳聚糖、明胶、甘油为基质制备依诺沙星阴道栓 ,采用紫外分光光度法测定栓剂中依诺沙星的含量 ,并用家兔进行刺激性试验。结果依诺沙星含量测定平均回收率为 99.97% ,RSD为 0 .34% (n =6 )。栓剂对家兔直肠无刺激。结论处方设计合理、制备简单、质量稳定 ,适合于临床推广应用     

依诺沙星滴眼液质量评价

目的通过对4家生产企业的50批依诺沙星滴眼液的质量分析,评价依诺沙星滴眼液的质量现状。方法采用现行法定标准及探索性研究的检测方法,分析pH对依诺沙星溶解性的影响、有关物质、抑菌剂使用的合理性等项目,探讨依诺沙星滴眼剂处方及工艺的合理性。结果按法定标准检验50批依诺沙星滴眼液,合格率为100%;但探索性研究发现,仅66%的产品中抑菌剂的含量在处方量的80%~120%范围,两家企业处方中的抑菌剂含量偏高,部分处方不合理。结论国内依诺沙星滴眼液整体质量亟待提高。     

复方依诺沙星滴眼液的制备与质量控制

目的在依诺沙星滴眼剂中加入地塞米松、聚乙烯吡咯烷酮制备复方依诺沙星滴眼剂,为临床提供高效、缓释、低毒、方便的新型制剂。方法用依诺沙星、地塞米松为主药,以聚乙烯吡咯烷酮、羟苯乙酯为辅料,制备复方依诺沙星滴眼剂,采用高效液相色谱法测定其中主药含量,并考察制剂稳定性和刺激性。结果所制备的滴眼液为微黄色澄明液体;进样量在10～100 μg•mL 1范围内与峰面积线性关系良好,平均回收率100.5%（RSD＝0.51%）;该滴眼剂稳定且无刺激性,眼用安全。结论该制剂制备方法简单,生产周期短,质量可控。     

聚甲酚磺醛阴道栓联合依诺沙星治疗宫颈柱状上皮异位效果分析

目的：探讨聚甲酚磺醛阴道栓联合依诺沙星治疗宫颈柱状上皮异位的疗效。方法选取该院收治的240例宫颈柱状上皮异位患者,按治疗方案不同分为对照组和观察组各120例。对照组给予依诺沙星治疗,观察组联合应用聚甲酚磺醛阴道栓治疗。比较组间疗效、症状改善情况及不良反应发生情况。结果观察组总有效率和症状改善率显著高于对照组,且两组不良反应发生率比较差异无统计学意义。结论聚甲酚磺醛阴道栓联合依诺沙星治疗宫颈柱状上皮异位效果良好,能够提高疗效,改善临床症状,且不增加不良反应。     

甲苯磺酸妥舒沙星滴眼液的制备与稳定性考察

目的 研究甲苯磺酸妥舒沙星滴眼液的制备及质量控制方法 ,并考察其稳定性.方法 以甲苯磺酸妥舒沙星为主药,加入氯化钠、羟苯乙酯等制备甲苯磺酸妥舒沙星滴眼液.采用紫外分光光度法测定甲苯磺酸妥舒沙星含量.结果 甲苯磺酸妥舒沙星在10～60 μg•mL-1范围内线性关系良好, r＝0.999 9.平均回收率为100.17%,RSD为1.15%(n＝9).在40 ℃避光条件下放置90 d稳定,常温避光条件下放置180 d稳定.结论 该滴眼液处方工艺简单,质控方法 可靠.     

复方司帕沙星中空栓的制备及质量控制

目的:制备复方司帕沙星中空栓并建立其质量控制方法。方法:以司帕沙星、替硝唑为主药,半合成脂肪酸甘油酯为基质制备中空栓;采用双波长分光光度法测定其中主药含量,并考察室温留样6个月内的制剂稳定性,同时用家兔做阴道黏膜刺激性实验。结果:司帕沙星、替硝唑检测浓度的线性范围分别为2.0～10.0(r=0.9998)、4.0～20.0μg.mL-1(r=0.9995),平均回收率分别为98.41%(RSD=1.40%)、98.62%(RSD=0.40%);该制剂对阴道黏膜的刺激性小,室温贮存6个月内质量稳定。结论:该制剂制备及含量测定方法简单可行,且质量稳定、刺激性小,易于推广。     

复方加替沙星泡腾栓的制备与临床应用

目的 制备复方加替沙星泡腾栓,方便临床用药. 方法 以甘油明胶为基质制备复方加替沙星泡腾栓,建立质量控制并对其进行临床疗效观察. 结果 加替沙星浓度在2～12 μg•L^-1（r＝0.999 9）范围内呈良好的线性关系. 平均回收率为99.98%（RSD＝0.24 %）. 临床用于77例感染性阴道炎,全部有效. 结论 复方加替沙星泡腾栓制备简单,质量可控,疗效显著,可用于临床.     

依诺沙星泡腾片的研制及在妇科的临床应用

目的制备依诺沙星阴道泡腾片并建立质量控制方法。方法选用合适的药物辅料制备依诺沙星阴道泡腾片，用紫外分光光度法测定依诺沙星的含量，考察制剂的稳定性，并进行临床疗效观察。结果本泡腾片处方合理，制备工艺简便，质量控制易行，稳定性良好。该制剂对细菌性阴道病有效率为92．78％，治愈率为84．52％。对淋菌性阴道炎治愈率为75％。结论本泡腾片剂有望成为临床治疗阴道炎症的较理想的新制剂。     

复方司帕沙星滴眼液的制备

［摘要］目的研究复方司帕沙星滴眼液的制备及质量控制方法。方法以司帕沙星为主药配伍地塞米松磷酸钠等制备复方司帕沙星滴眼液,采用高效液相色谱法测定司帕沙星、地塞米松磷酸钠的含量。结果所制备的复方滴眼液中,司帕沙星和地塞米松磷酸钠的浓度线性范围分别为10～120和5～80 μg•mL 1,平均回收率分别为100.31%（RSD＝0.83%）和100.32%（RSD＝1.33%）。结论复方司帕沙星滴眼液的制备工艺简单,质控方法可靠。     

依诺沙星治疗社区获得性肺炎21例临床疗效观察

目的探讨依诺沙星对社区获得性肺炎的临床疗效。方法采用随机、对照治疗方案,分依诺沙星组和阿奇霉素组,每天分别静点依诺沙星400mg、阿奇霉素500mg,两组疗程均7～10d。结果依诺沙星组用药5d后临床有效率为85.7%,并且依诺沙星组临床总有效率90.4%,均显著高于阿奇霉素组。结论依诺沙星静点治疗社区获得性肺炎疗效高,优于阿奇霉素,不良反应轻微,可以临床普遍使用。     

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.

---

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.