不同厂家盐酸西替利嗪包衣片体外溶出度的比较

目的:比较两个厂家不同批号的盐酸西替利嗪包衣片溶出度.方法:采用转篮法测定盐酸西替利嗪包衣片的体外溶出度,并进行溶出参数方差分析.结果:两个厂家不同批号的盐酸西替利嗪包衣片体外溶出度均符合中国药典2000年版的规定.比较其T50、Td数值并进行方差分析,得出国外产品批间不存在显著差异(P>0.05),国内产品批间存在极显著差异(P<0.01),国外产品与国内产品间存在极显著差异(P<0.01).结论:国外产品与国内产品之间T50、Td存在极显著差异(P<0.01).     

不同厂家安定片的体外溶出度比较

采用转篮法研究了四个厂家6个批号安定片的体外溶出度,实验数据用威布尔分布模型拟合,求得T_d、T₅₀、m.结果表明:不同厂家生产的安定片溶出度差异显著(P<0.01),而同一厂家生产的不同批号的安定片溶出度无明显差异。     

罗红霉素片的体外溶出度研究

对国内外不同厂家生产的罗红霉素片进行体外溶出度比较，并分析各溶出参数，以评价产品的内在质量。方法：用分光光度法测定样品在pH5.8的磷酸盐缓冲液中的溶出度。结果：根据威布尔（Weibull)分布模型，计算出Td,T50,m的溶出参数。结论：国产罗红霉素片与进口罗红霉素片相比较，溶出度有显著差异。     

4厂家吡格列酮片体外溶出度比较

目的:比较4厂家吡格列酮片的体外溶出度,为临床用药提供参考。方法:采用转篮法结合高效液相色谱法,分别测定4厂家吡格列酮片的累积溶出度,并以威布尔公式计算参数Td、T50、m值,再进行方差分析。结果:4厂家吡格列酮片溶出度均符合《中国药典》规定,除北京产品与江苏产品、杭州产品与天津产品的Td、T50比较无显著性差异外(P>0.05),其余两两之间Td、T50比较均存在显著性差异(P<0.05)。结论:同一品种不同来源的药品之间溶出度具有差异,临床用药时应考虑相关情况。     

不同厂家格列齐特片溶出度考察

目的 :比较6厂家格列齐特片的溶出度 ,为临床选用提供参考。方法 :采用分光光度法分别测定A、B、C、D、E、F厂格列齐特片的累积溶出度 ,绘制其溶出曲线 ,计算参数T50、Td、m的值 ,并对T50、Td 值进行两两比较。结果 :E厂格列齐特片的T50、Td 值与其它5厂有显著性差异 (P<0 01) ,其余5厂格列齐特片的T50、Td 值间无显著性差异 (P>0 05)。其中 ,E厂格列齐特片在180min时的累积溶出率<75 %,不符合《中国药典》规定 ,其它5厂格列齐特片的溶出度均符合规定。结论 :建议有关厂家对影响制剂溶出度的辅料及生产工艺进行改进 ,以提高产品质量。     

不同厂家替米沙坦片体外溶出度的考察

目的比较5厂家替米沙坦片的溶出度。方法采用紫外分光光度法分别测定A,B,C,D和E厂替米沙坦片的累积溶出度,绘制其溶出曲线,计算参数m、T50、Td的值,并对T50、Td值进行两两比较。结果A厂和E厂替米沙坦片的T50、Td值与其它3厂有显著性差异(P<0.05),其余3厂替米沙坦片的T50、Td值间无显著性差异(P>0.05);其中,E厂替米沙坦片在60min时的累积溶出率小于65%,不符合中国药典规定,其它4厂替米沙坦片的溶出度均符合规定。结论建议有关厂家对影响制剂溶出度的辅料及生产工艺进行改进,以提高产品质量。     

五厂家罗红霉素制剂的溶出度比较

目的：比较不同厂家罗红霉素制剂的溶出度。方法：以对二甲氨基苯甲醛为显色剂，用分光光度法测罗红霉素的含量并用转篮法测罗红霉素的溶出度，计算溶出参数并进行方差分析。结果：B，C，D，E厂的样品均在30min内溶出80%以上，T50分别为5.24,2.28,2.05,0.001min,Td分别为8.56,3.06,2.37,0.05min，A厂样品在1h内未崩解。结论：B、C、D，E厂的样品溶出度无显差异，A厂样品溶出度不合格。     

高效液相色谱法测定盐酸西替利嗪片的含量及溶出度

目的建立盐酸西替利嗪片的含量及溶出度测定方法;比较不同厂家不同批号盐酸西替利嗪片的溶出度。方法采用C18色谱柱(4.6nm×250nm,5μm),流动相为甲醇-0.01mol/L磷酸二氢钠(60∶40),流速:1mL/m in,检验波长230nm,柱温:室温;转篮法测定药品体外溶出度。结果本法简便灵敏准确,盐酸西替利嗪在10~100μg/mL浓度内呈良好线形关系,回收率为99.2%.RSD为1.58%(n=6)。结论三个厂家盐酸西替利嗪片之间T50和Td存在极显著差异(P<0.01),同一厂家不同批次间不存在极显著差异(P>0.05)。此方法可用于盐酸西替利嗪片的质量控制。     

两种国产盐酸西替利嗪片溶出度比较

目的考察盐酸西替利嗪片的体外溶出度,为评价其质量提供参考。方法 采用转篮法测定溶出度,用威布尔(Wcibull)分布模型拟合溶出曲线,并对溶出参数m、T50、Td等采用t检验进行统计分析。结果 两厂家盐酸西替利嗪片的溶出参数无显著性差异(P>0.05)。结论 两国产厂家制剂的溶出度均符合规定。     

硝苯地平片的溶出度研究

本文采用来法对国产6个厂家7个批号的硝苯地平片进行了溶出度测定。结果表明：不同厂家及同一厂家不同批号样品的溶出参数（T50、Td、m）有显著性差别。建议对该产品进行溶出度检查，以控制产品质量，保证临床疗效。     

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.