复方氧氟沙星滴鼻液的制备及临床应用

以氧氟沙星,地主松磷腔钠和盐酸苯海拉明为主要原料的复方氧氟沙星滴鼻剂,用紫 不铫度法,高效液相法和滴定法测定氧氟沙星,地塞米松磷酸钠和盐酸苯海拉明的含量,初均速法预测有效期。３种主药含量测定的平均回收率和ＲＳＤ分别为１０１．５１％（ＲＳＤ＝０．４４％）,９７．６２％（ＲＳＤ＝０．７９％）和９８．２３％（ＲＳＤ＝０．５８％）。室温贮期Ｔ０．９＾２８Ｃ＝３．６７年。     

复方替硝唑口腔膜剂的制备及质量控制

目的：本文研究复方替硝唑口腔膜剂的处方和制备工艺,并建立制剂的含量测定方法。方法：以替硝唑与氧氟沙星为主药,并用双波长分光光度法测定两主药的含量。结果：替硝唑和氧氟沙星的平均回收率分别为９８．６％（ＲＳＤ＝０．６１％）和９８．９％（ＲＳＤ＝０．４９％）。结论：该制剂的配制及质控方法是可行的。     

多波长吸收度比值差法氯麻滴鼻液的含量

应用多波长吸收度比值差法测定了氯麻滴鼻液中盐酸麻黄碱的含量，同时用单波长法测定氯霉素的含量。平均回收率：氯霉素１００．１％，ＲＳＤ＝０．２０％；盐酸麻黄碱１００．３％，ＲＳＤ＝０．４９％。     

复方氧氟沙星鼻喷剂的稳定性实验

本文报告了复方氧氟沙星鼻喷剂的配制及其稳定性考察。结果表明，制剂中两种主药氧氟沙星和盐酸麻黄碱的室温有效期均在２．２ａ以上，远超过呋麻滴鼻液的室温贮存期。该制剂可取代呋麻滴鼻液用于临床。     

“鼻炎愈”的药剂学研究

目的：研制以氧氟沙星（ＯＦＬＸ）、盐酸麻黄碱为主药并配伍透明质酸（ＨＡ）的滴鼻剂。方法：ＨＰＬＣ法测定含量、稳定性试验及临床观察。结果：ＯＦＬＸ和盐酸麻黄碱含量测定的标准曲线分别是Ｃ＝１．４５５Ａ－０．００８９,＝０．９９９４（ｎ＝３）和Ｃ＝０．０３８７－０．０００１,＝０．９９９４（ｎ＝３）,回收率（ｘ±ｓ）分别为１０１．１±１．８０％（ｎ＝３）和１０１．０±０．４８％（ｎ＝３）。稳定性试验显示,处方中氧氟沙星对光较敏感,制剂在４０℃、７５％ＲＨ条件下３个月无明显变化。３所医院临床疗效观察１３０例,总有效率９１．９％。结论：本制剂处方合理,质控方法可靠,疗效满意。贮存期暂定２年。     

紫外分光光度法测定氧氟沙星颗粒剂的含量

本文以盐酸液（０．１ｍｏｌ／Ｌ）为溶剂，采用紫外分光光度法测定氧氟沙星颗粒剂的含量。考察了光照和温对含量测定的影响，并与ＨＰＬＣ法（部标准）作了比较试验。方法平均回收率为９８．７１％，ＲＳＤ＝０．０６％，ｎ＝９；样品含量测定的平均ＲＳＤ为０．９９％，ｎ＝６。与ＨＰＬＣ法相比，无显著性差异。     

氧麻滴鼻液的制备及质量控制

目的：介绍氧麻滴鼻液的制备及其质量控制方法。方法：以氧氟沙星、甲硝唑和盐酸麻黄碱为原料制备氧麻滴鼻液，采用双波长分光光度法直接测定主药氧氟沙星及甲硝唑含量，用容量法测定盐酸麻黄碱含量，留样观察法考察其稳定性。结果：本制剂中两主药氧氟沙星及甲硝唑平均回收率分别为98．85％和99．96％。结论：本制剂制备工艺简单。性质稳定，含量测定方法简便快速，适宜于医院制剂室配制和应用。     

紫外分光光度法测定氯麻滴鼻剂含量

采用双波长分光光度法同时测定氯霉素盐酸麻黄碱滴鼻剂中氯霉素和盐酸麻黄碱的含量,氯霉素和盐酸麻黄碱的测定波长分别为２７６ｎｍ 和２５６ｎｍ ,平均回收率分别为９９－８５ ％ 、ＲＳＤ＝ ０ ．６５２ ％ 和１００－３ ％ 、ＲＳＤ＝ ０ ．２８ ％ 。     

双波长分光光度法测定地麻滴鼻液中地塞米松磷酸钠、盐酸麻黄碱的含量

本文采用双波长分光光度法不经分离直接测定地麻滴鼻液中地塞米松磷酸钠、盐酸麻黄碱的含量。地塞米松磷酸钠的测定波长为２４２．０ｎｍ，参比波长为２６５．３ｎｍ，盐酸麻黄碱测定波长为２５６．０ｎｍ，参比波长２２６．５ｎｍ。地塞米松磷酸钠的平均回收率为１０１．１５％，ＲＳＤ为０．９６％；盐酸麻黄碱的平均回收率为９９．４２％，ＲＳＤ为０．５８％。本法快速、简便、结果准确，适用于该制剂质量控制。     

导数比率法测定复方呋喃西林滴鼻液中盐酸麻黄碱的含量

应用导数比率法消除盐酸麻黄碱及呋喃西林之间的相互干扰，测定呋麻液中盐酸麻黄碱的含量，平均回收率为：１００．８±０．４７％（ＲＳＤ），ｎ＝５。     

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.