塞克硝唑泡腾片的制备与质量控制

目的设计抗真菌药物塞克硝唑阴道泡腾片的处方和制备工艺建立制剂含量的测定方法。方法采用紫外分光光度法测定塞克硝唑的含量。结果泡腾片中其它成分不干扰测定。平均回收率100．8％．RSD0．58％。结论制剂稳定含量测定方法简便。灵敏、准确、重现性好。     

塞克硝唑阴道泡腾片的制备及质量研究

目的对塞克硝唑阴道泡腾片的制剂工艺和质量进行研究。方法采用非水溶剂法,以pH值、崩解时限、发泡量为指标对处方进行筛选,并且利用高效液相色谱法测定主药塞克硝唑的含量。结果制备的塞克硝唑阴道泡腾片经过加速和长期实验,质量符合要求,塞克硝唑的质量浓度在5.051⁴5.459μg·mL-1范围内线性关系良好,r为0.999 98。结论该制剂设计合理,稳定性好,建立的含量测定方法准确可靠。     

塞克硝唑阴道泡腾片的制剂工艺和质量研究

目的 :对塞克硝唑阴道泡腾片的制剂工艺和质量进行研究。方法 :采用紫外分光光度法测定主药塞克硝唑的含量。结果 :线性范围为 5 1 5～ 36 0 5μg/ml,相关系数为 0 9999,线性关系良好 ,平均回收率为 1 0 0 3 % ,RSD为 0 36 % (n =9)。结论 :本制剂设计合理 ,稳定性好 ,可满足临床需要     

塞克硝唑阴道泡腾片的制剂工艺和质量研究

目的：对塞克硝唑阴道泡腾片的制剂工艺和质量进行研究。方法：采用紫外分光光度法测定主药塞克硝唑的含量。结果：线性范围为5.15-36.05μg/ml，相关系数为0.9999。线性关系良好，平均回收率为100.3%,RSD为0.36%(n=9)。结论：本制剂设计合理，稳定性好。可满足临床需要。     

塞克硝唑温敏性水凝胶的处方设计与含量测定

目的:筛选塞克硝唑温敏性水凝胶的最佳处方,并建立其含量测定方法。方法:以基质泊洛沙姆P407/P188(A)、溶剂乙醇(B)及黏附剂海藻酸钠(C)的用量为因素,以主药塞克硝唑含量为指标,采用正交设计筛选处方;在277nm波长下采用紫外分光光度法测定主药含量。结果:最佳处方为A15g/15g、B20mL、C0.6g。塞克硝唑检测浓度线性范围为4.618～46.18mg·L-(1r=0.9998),平均回收率为98.27%,日内RSD<1.8%,日间RSD<2.1%。结论:该处方设计合理,制备工艺可靠,质量稳定。     

塞克硝唑凝胶剂的研制与含量测定

目的:制备塞克硝唑凝胶剂并建立含量测定方法.方法:应用聚羧乙烯941作辅料制备塞克硝唑凝胶剂,用一阶导数分光光度法测定凝胶剂中塞克硝唑的含量;结果:塞克硝唑凝胶剂平均回收率99.9%,RSD 0.206%.结论:聚羧乙烯可作为辅料制备塞克硝唑凝胶剂,一阶导数分光光度法测定准确可靠.     

阴道用塞克硝唑温敏型原位凝胶的研制

目的:以温敏性聚合物泊洛沙姆407和黏附性聚合物羟丙基甲基纤维素为载体制备阴道用塞克硝唑温敏型原位凝胶,使凝胶在阴道壁原位凝胶化并迅速黏附于黏膜表面,延长药物在黏膜表面吸收时间。方法:采用单因素考察泊洛沙姆407浓度及药物对凝胶相变温度的影响,确定最佳处方;采用冷法制备载塞克硝唑温敏型原位凝胶,考察凝胶的流变学特性;采用紫外分光光度法测定原位凝胶中药物的含量。结果:当泊洛沙姆407浓度为20%时,载塞克硝唑温敏型凝胶的胶凝相变温度为(31.7±0.5)℃,可满足阴道用药后迅速相变为凝胶的条件,流变学行为显示塞克硝唑阴道凝胶的黏度随温度的变化均呈S形曲线,相变温度与转子法测得值相近。含量测方法在4.99~24.96mg.L-1范围内线性关系良好,平均回收率为98.47%,RSD为2.73%(n=6)。结论:阴道用塞克硝唑温敏型原位凝胶制备工艺简单,能在生理温度下迅速原位凝胶化,建立的含量测定方法简便可靠。     

奥硝唑阴道泡腾片的制备及临床应用

目的：将奥硝唑制成阴道泡腾片剂。方法：选用枸橼酸、碳酸氢钠、黏合剂等药物辅料制备奥硝唑阴道泡腾片，用紫外分光光度法测定奥硝唑的含量，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、滴虫性阴道炎的总有效率分别为91．2％，95．71％。结论：泡腾片剂有望成为临床治疗细菌性阴道病、滴虫性阴道炎理想的新制剂。     

左奥硝唑分散片的研制及溶出度测定方法的研究

目的对左奥硝唑分散片进行处方分析,并建立溶出度测定方法。方法以崩解时限为指标,优选左奥硝唑分散片的处方;采用紫外分光光度法测定溶出度。结果确定了左奥硝唑分散片的处方,分散片于3 min时均已溶出90%以上。建立了溶出度测定方法,在5.329～26.645μg/mL浓度范围内,其吸收度值与浓度呈良好的线性关系(r=1.0),方法回收率为99.8%,精密度好(RSD=0.2%)。结论筛选的处方合理,制得的左奥硝唑分散片分散快、溶出快。用紫外分光光度法测定左奥硝唑分散片溶出度,方法简单、可靠。     

呋柳泡腾片中呋喃西林的定量研究

目的 建立呋柳泡腾片中呋喃西林的含量测定方法。方法采用紫外分光光度法在375nm处测定呋柳泡腾片中呋喃西林的含量。结果呋喃西林的线性范围为2.05μg-10.25μg／ml，回归方程为A=80878.05C-0．0084，r=1．0000；加样回收率为100．15％，RSD=0.7％。结论紫外分光光度法可用于测定呋柳泡腾片中呋喃西林的含量，方法准确，处方其他成分无干扰，重现性好。     

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.