妥布霉素地塞米松磷酸钠滴眼液的制备及质量控制

目的制备妥布霉素地塞米松磷酸钠滴眼液并建立其质量控制方法。方法以妥布霉素、地塞米松磷酸钠为主药配制滴眼液，采用抗生素微生物检定法测定妥布霉素，高效液相色谱法测定地塞米松磷酸钠的含量，并考察加速试验、室温留样12个月内的药物含量及稳定性。结果所制制剂为无色澄明液体，且鉴别、检查等均符合2005版《中国药典》相关规定：地塞米松磷酸钠检测浓度的线性范围6．25～200μg／ml（r=0．9997），平均回收率100．01％（RSD=0．23％）：加速试验及室温留样12个月内妥布霉素和地塞米松磷酸钠的含量均稳定。结论该制剂处方工艺简单可行，质量稳定。     

复方妥布霉素滴眼掖的制备及临床疗效观察

目的 介绍复方妥布霉素滴眼液的处方组成、配制方法、质量控制和临床应用。方法 采用抗生素微生物检定法测定其含量选择白内障术后病人和细菌性结膜炎病人共183例，分为本院自制复方妥布霉素滴眼液组(试验组)102例，进口复方妥布霉素滴眼液组(对照组)81例，采用随机对照方法进行治疗。结果 该制剂制备工艺和质量控制方法可行，试验组对照组临床总有效率均为100％，细菌清除率和阴转率均为100％，统计学分析两组无显著性差异(P＞0．05)。结论 本滴眼剂处方及制备方法合理，疗效确切，是一种很好的医院眼科制剂。     

妥布霉素口服液的制备及质量控制

目的：制备妥布霉素口服液并建立其质量标准。方法：以妥布霉素为主药，甜菊糖苷为矫味剂制备妥布霉素口服液，采用旋光法测定妥布霉素含量。结果：方法平均回收率为100．1％，RSD为0．4％（n=5）。结论：制剂处方及制备工艺合理，质量可控。     

妥布霉素滴眼液的制备及临床观察

目的：对我院妥布霉素滴眼液进行制备和临床疗效观察,评价其生产的可行性与确切的临床疗效。方法：７７例外眼细菌性感染患者,随机分成两组,以托百士滴眼液作为阳性药物进行对照试验,参照 Ｇｗｏｎ观察项目和计分的得分形式给予评价。结果：妥布霉素滴眼液和托百士滴眼液总有效率为９２．７％和９４．４％,相互对照,无显著性差异（Ｐ＜０．０５）。结论：妥布霉素滴眼液制备工艺简单,疗效确切,可作为医院制剂推广。     

复方妥布霉素滴眼液的制备及临床疗效观察

目的介绍复方妥布霉素滴眼液的处方组成、配制方法、质量控制和临床应用.方法采用抗生素微生物检定法测定其含量;选择白内障术后病人和细菌性结膜炎病人共18 3例,分为本院自制复方妥布霉素滴眼液组(试验组)102例,进口复方妥布霉素滴眼液组(对照组)81例,采用随机对照方法进行治疗.结果该制剂制备工艺和质量控制方法可行;试验组对照组临床总有效率均为100%,细菌清除率和阴转率均为100%,统计学分析两组无显著性差异(P＞0.05).结论本滴眼利处方及制备方法合理,疗效确切,是一种很好的医院眼科制剂.     

阿昔洛韦妥布霉素滴眼液的制备及疗效观察

目的：制备阿昔洛韦妥布霉素滴眼液并观察其疗效。方法：采用抗生素微生物检定法测定妥布霉素的含量，紫外分光光度法测定阿昔洛韦的含量，检测波长为252nm，并对其进行临床疗效观察。结果：通过50例原因暂不明确的临床眼部急性感染病人的应用，总有效率为98.0%。结论：制剂质量易于控制，疗效安全可靠。     

复方妥布霉素-氟米龙滴眼液的研制及质量控制

目的:研制复方妥布霉素-氟米龙滴眼液并探讨其质量控制方法.方法:根据各种原辅料不同的溶解特性,采取分步调剂并灭菌的制备方法.采用高效液相色谱法及抗生素微生物检定法分别测定氟米龙及妥布霉素的含量,并建立了质量标准.结果:制得的复方妥布霉素-氟米龙滴眼液质量稳定可控,含量测定方法准确可靠.结论:制备工艺合理,质量控制方法可行.     

微生物比浊法测定妥布霉素、硫酸妥布霉素注射液及妥布霉素滴眼液的效价

目的：建立妥布霉素、硫酸妥布霉素注射液及妥布霉素滴眼液效价的微生物比浊法。方法：分别采用微生物比浊法和管碟法对妥布霉素、硫酸妥布霉素注射液及妥布霉素滴眼液的含量进行测定和比较研究。结果：妥布霉素效价测定的线性范围为0.4~1.0 U/ml;R2=0.991 3,硫酸妥布霉素注射液平均回收率为100.2%,RSD为2.6%（n=9）;妥布霉素滴眼液平均回收率为99.6%,RSD为1.5%（n=9）。结论：微生物比浊法具有简便、精确、快速的特点,可应用于产品的控制。     

复方妥布霉素混悬滴眼剂的研制

目的:制备稳定的复方妥布霉素混悬滴眼剂。方法:以沉降容积比、粘度为指标,对可用于该制剂的助悬剂进行筛选。结果:经加速试验3个月,药物含量稳定,用库尔特计数仪测定粒径分布,5μm以下的颗粒无明显变化。结论:本方法工艺简便,质量便于控制,用本方法制备的复方妥布霉素混悬滴眼剂稳定性好。     

复方妥布霉素滴眼液的制备及临床疗效观察

目的 介绍复方妥布霉素滴眼液的处方组成、配制方法、质量控制和临床应用。方法 采用抗生素微生物检定法测定其含量;选择白内障术后病人和细菌性结膜炎病人共183例,分为本院自制复方安布霉素滴眼液组(试验组)102例,进口复方妥布霉素滴眼液组(对照组)81例,采用随机对照方法进行治疗。结果 该制剂制备工艺和质量控制方法可行;试验组对照组临床总有效率均为100％,细菌清除率和阴转率均为100％,统计学分析两组无显著性差异(P>0.05)。结论 本滴眼剂处方及制备方法合理,疗效确切,是一种很好的医院眼科制剂。     

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.