磺胺嘧啶银凝胶的制备及质量控制

目的设计磺胺嘧啶银凝胶处方,并进行质量控制。方法以CMC-Na,甘油为基质,制备磺胺嘧啶银凝胶,用永停滴定法测定其含量,并留样观察其稳定性。结果所得凝胶质量稳定,含量准确,平均加样回收率为101.2%,RSD=1.1%(n=6)。结论该凝胶制剂处方简单,质量可控,为一种理想的医院制剂。     

甲磺酸加替沙星凝胶的制备与质量控制

目的:制备甲磺酸加替沙星凝胶剂,建立其质量控制方法.方法:以甲壳胺作凝胶基质制备甲磺酸加替沙星凝胶,用紫外分光光度法在入=292 nm处测定甲磺酸加替沙星凝胶的含量.并且建立了性状、鉴别、pH值、卫生学等质量控制方法.结果:甲磺酸加替沙星的pH值5.0～6.5,卫生学检查合格,线性范围为2.0～12.0μg·ml-1,含量测定平均回收率99.83%、RSD=0.42%(n=9).结论:该凝胶设计合理,工艺简单,质量控制方法可靠,质量稳定,具有应用方便,作用持久的特点,适于临床应用.     

泰麻鼻用凝胶的制备与质量控制

目的 设计泰麻鼻用凝胶处方,并进行质量控制.方法 以卡波姆-940、甘油为主要辅料,三乙醇胺调节pH值,制备泰麻鼻用凝胶,分别采用紫外分光光度法和旋光法对凝胶中氧氟沙星和盐酸麻黄碱的含量进行测定.结果 所得凝胶质量稳定,含量准确,氧氟沙星的平均回收率为100.87%,RSD 0.85%(n=6);盐酸麻黄碱平均回收率为100.74%,RSD=1.96%(n=6).结论 该制剂处方简单,质量可控,为一种理想的医院制剂.     

复方乳酸左氧氟沙星壳聚糖凝胶剂的制备与质量控制

目的:制备复方乳酸左氧氟沙星壳聚糖凝胶剂,建立其质量控制方法.方法:以壳聚糖、羧甲基纤维素为凝胶材料制备复方乳酸左氧氟沙星壳聚糖凝胶剂;采用紫外分光度法测量乳酸左氧氟沙星含量,采用容量法测定谷氨酸锌含量.结果:乳酸左氧氟沙星的线性范围为4.5～20.5 μg·ml-1,平均回收率为100.2%,RSD为0.18%(n=9).结论:该凝胶剂制备工艺简单,质量控制方法可靠,质量稳定.     

西替利嗪凝胶的制备和质量评价

目的:制备西替利嗪凝胶剂,并建立质量控制方法.方法:以卡波姆940为基质制备凝胶,采用紫外分光光度法测定西替利嗪含量,并考察其稳定性.结果:西替利嗪线性范围为6～16 mg·L-1(r=0.996 7),平均回收率为98.23%,RSD为0.69%(n=5),凝胶稳定性良好.结论:该凝胶制备工艺可行,性质稳定.     

双氯芬酸钾壳聚糖凝胶剂的制备与质量控制

目的 研制双氯芬酸钾壳聚糖凝胶剂,并建立其含量测定方法.方法 以卡波姆和壳聚糖作为凝胶基质制备双氯芬酸钾壳聚糖凝胶剂,采用高效液相色谱法进行含量测定.结果 双氯芬酸钾在40.4～323.2 μg·mL^-1浓度范围内线性关系良好，r=0.999 8，平均回收率为99.72%，RSD为0.80%.结论 该凝胶剂制备工艺简单,质量稳定,质量控制方法准确可靠.     

茶多酚阴道栓的制备及体外抑菌试验

目的:制备茶多酚阴道栓,建立其质量控制方法,并考察其体外抑菌作用。方法:以明胶、甘油等为辅料制备栓剂;以紫外分光光度法测定其中茶多酚含量;通过体外抑菌试验考察其对各阴道致病菌的有效抑菌浓度(MIC)。结果:所得制剂成模性好;茶多酚检测浓度在0.01～0.09mg.mL-1范围内呈良好的线性关系(r=0.9994),平均回收率为101.0%(RSD=0.84%);主药浓度在10mg.mL-1以上即对几种主要阴道致病菌均有抑制作用。结论:该制剂制备方便,质量易控,体外抑菌作用较强,可供临床使用。     

替硝唑口腔凝胶剂的制备及临床应用

目的:制备替硝唑口腔凝胶剂,观察临床疗效.方法:将替硝唑制成口腔凝胶剂,用紫外分光光度法对替硝唑进行含量测定.将165例牙病患者随机分为治疗组85例和对照组80例,2组均用朵贝氏液嗽口后再分别用替硝唑口腔凝胶和冰硼散,3次/d,平均用药4d.结果:替硝唑口腔凝胶的含量测定方法简便可行.治疗组与对照组的总有效率分别为98.8%和97.5%(P＞0.05),治疗组与对照组的显效率分别为96.5%和75.0%(P＜0.01).结论:该制剂工艺合理,质量可控,临床疗效满意.     

尿囊素凝胶的制备及含量测定

目的:制备尿囊素凝胶并建立其含量测定方法。方法:以尿囊素为主药,卡波姆-940为基质制备凝胶;采用高效液相色谱法测定其中主药含量。结果:所制凝胶涂展性好;尿囊素检测浓度的线性范围为12.78～68.16μg.mL-1(r=0.9999),平均回收率为99.7%(RSD=0.36%)。结论:本制剂制备工艺简便可行,含量测定方法准确、快速,可用于该制剂的质量控制。     

甲磺酸帕珠沙星凝胶的制备与质量控制

目的:制备甲磺酸帕珠沙星凝胶,建立质量控制方法。方法:以卡波姆934为基质制备凝胶,采用高效液相色谱法测定甲磺酸帕珠沙星含量,并考察其稳定性。结果:甲磺酸帕珠沙星线性范围为20.0~80.0μg.mL-1(r=0.9999),平均回收率为98.1%,RSD=1.77%(n=6),凝胶稳定性良好。结论:该处方设计合理,质量控制方法准确可靠,制剂稳定性好。     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.     

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.