5种中药重金属的检测研究

目的:探讨紫外分光光度法在监测中药重金属含量中的应用.方法:采用紫外分光光度法测定桔梗、丹参、党参、川芎、地龙重金属的含量.结果:对照品重金属的检测浓度在0～5μg·ml-1,质量浓度范围内与吸收度呈良好线性关系(r=0.9993);平均回收率为98.46%,RSD=1.49%(n=6);桔梗、丹参、党参的重金属含量为25.60、27.12、24.44μg·g-1;川芎、地龙的重金属含量偏高,分别为47.38、50.56μg·g-1.结论:紫外分分光光度法可用于检测中药重金属的含量.     

氟康唑阴道泡腾片的研制和质量标准

目的氟康唑阴道泡腾片的制剂、质量标准的研究.方法采用紫外分光光度法测定主药氟康唑的含量.结果线性范围为25～250μg·ml-1,r=0.9999,平均回收率为99.96%,RSD为0.28%(n=6).结论该制剂制备工艺简单,值得临床推广使用.     

人工泪液氯霉素滴眼液的含量测定和稳定性考察

目的:制定人工泪液氯霉素滴眼液含量测定方法并预测室温存放的有效期.方法:以双波长紫外分光光度法测定氯霉素含量,银量法测定含氯量,采用Q10法预测人工泪液氯霉素滴眼液的有效期.结果:氯霉素浓度在5～40μg·ml-1的范围内与吸收度差值呈良好的线性关系,氯霉素平均回收率为100.77%,RSD为0.37%.人工泪液氯霉素滴眼液在室温25℃下的有效期(t0.9)为9.3个月.结论:含量测定及贮存期预测方法简便、快速、准确可靠,适用于医院制剂的质量控制.     

安乃近片含量测定方法的探讨

目的:探讨安乃近片的含量测定方法.方法:采用紫外分光光度法测定安乃近片中安乃近的含量,测定波长为(257±1)nm.结果:安乃近在10～30μg·ml-1的浓度范围内,吸收度A与浓度C呈良好的线形关系(r=0.999 9,n=5),平均回收率为100.01%,RSD为0.91%(n=5).结论:紫外分光光度法干扰因素少,准确可靠,可用于安乃近片的含量测定.     

紫外分光光度法测定盐酸丁卡因滴眼液的含量

目的 建立一种测定盐酸醒丁卡因滴眼液含量的方法.方法 采用紫外分光光度法,检测波长:311 nm.结果 盐酸丁卡因在2.18～13.08 μg·ml-1 的浓度范围内有良好的线性关系,平均回收率为98.5%.结论 本法简便、快速、准确.     

紫外分光光度法测定伊曲康唑注射液的含量

目的建立紫外分光光度法测定伊曲康唑注射液含量的测定方法。方法采用紫外分光光度法测定伊曲康唑注射液的含量,测定波长为262nm。结果线性范围0~38.08μg·ml-1,伊曲康唑的平均回收率为99.1%,RSD为0.24%,r=0.9999(n=6)。结论该法方便快速准确,可作为伊曲康唑注射液含量测定的方法。     

紫外分光光度法测定半边旗二萜类化合物5F滴眼液的含量

目的:建立半边旗二萜类化合物5F滴眼液的含量测定方法.方法:采用紫外分光光度法测定滴眼液中5F的含量,检测波长为242 nm.结果:线性范围为20～100μg/mL(r=0.999 4),日内、日间RSD为1.0%～2.0%,平均回收率为100.6%.结论:紫外分光光度法专属性好,操作简便,能准确检测出滴眼液中5F的含量.     

复方氟康唑滴耳剂的制备及质量控制

目的:制备复方氟康唑滴耳剂,并对其进行质量控制。方法:运用紫外分光光度法测定含量(双波长分光光度法测定氟康唑含量,单波长分光光度法测定替硝唑含量)。结果:氟康唑的线性范围为60～300μg/mL,回归方程C=-0.5989±714.365△A(r=0.9999,n=6),回收率为98.18%～102.39%;替硝唑的线性范围为5～25μg/mL,回归方程C=0.049±28.128A(r=0.9999,n=6),回收率为97.50%～102.73%。结论:复方氟康唑滴耳剂制备简单,质量稳定,无刺激性。     

紫外分光光度法测定硫酸庆大霉素滴眼液的含量

目的 :研究硫酸庆大霉素滴眼液含量测定的紫外分光光度法。方法 :将硫酸庆大霉素进行衍生化反应后 ,在356nm波长处测定吸收度 ,并绘制标准曲线 ,求出回归方程 ,计算其含量。结果 :硫酸庆大霉素经衍生化反应后 ,可采用紫外分光光度法测定其含量 ,线性范围 :0 5～40 0μg·L-1,回归方程 :A=0.005585C 0.0049,(r=0.9997)。结论 :紫外分光光度法测定硫酸庆大霉素滴眼液的含量 ,操作简便 ,方法可行 ,可推广应用。     

甲磺酸培氟沙星滴眼液的研制及临床应用

:目的 :研制甲磺酸培氟沙星滴眼液。方法 :采用紫外分光光度法测定含量。对170例门诊眼部重症感染患者应用该滴眼液后进行疗效观察。结果 :线性范围为2～14μg/ml,回归方程为A=0.1018C,r=0.9999(n=7)。该方法测得平均回收率为99 64 % ,RSD为0 43 %。经治疗痊愈150例 ,有效16例 ,无效4例 ,总有效率达97 6 %。结论 :该滴眼液疗效确切 ,紫外分光光度法测定含量方法简便、快速、准确 ,不需要特殊试剂     

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.     

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.