联立方程组新解法在含氟罗沙星复方制剂分析中的应用

目的 :测定复方氟罗沙星栓及复方氟罗沙星滴耳液中2组分含量。方法 :采用联立方程组新解法不经分离直接测定复方氟罗沙星栓及复方氟罗沙星滴耳液中氟罗沙星、替硝唑及氟罗沙星、甲硝唑的含量。结果 :以286、317nm分别为复方氟罗沙星栓中2组分的测定波长 ,以蒸馏水为空白 ,氟罗沙星和替硝唑的平均回收率及RSD分别为100 17 %、0 44 %和99 96 %、0 37 % ;以286、318nm分别为复方氟罗沙星滴耳液中2组分的测定波长 ,以蒸馏水为空白 ,氟罗沙星和甲硝唑的平均回收率及RSD分别为100 65 %、0 65 %和99 92 %、0 21 %。结论 :本法操作简便快速 ,重现性好 ,可消除各处方中2组分的相互干扰 ,结果满意     

高效毛细管电泳法测定人尿中氟罗沙星的含量

目的　建立高效毛细管电泳法测定人尿中氟罗沙星的含量。方法　采用高效毛细管电泳法 ,电泳缓冲液为磷酸盐 (5 0mmol·L-1) -SDS(10mmol·L-1) ,pH 4 .7,检测波长为 2 78nm。结果　在 5 0 .0～ 2 5 0 .0 μg·ml-1范围内线性良好 ,r =0 .9992。加样回收率在 94 .6 %～ 10 5 .9%之间 ,日内和日间RSD分别为 3.1%和 3.8% ,氟罗沙星的检测限为 2 .3μg·ml-1。结论　所用方法能快速、简便、经济地测定人尿中氟罗沙星的含量 ,可用于临床检验和药物制剂的质量控制     

RP-HPLC同时测定复方氟罗沙星栓中氟罗沙星和替硝唑的含量

目的 :测定复方氟罗沙星栓中氟罗沙星和替硝唑的含量。方法 :采用反相高效液相色谱法 (RP-HPLC) ,以ODS-C18 色谱柱分离 ,以0 05mol/L柠檬酸 -乙腈 (65∶35 ,用三乙胺调pH为4 0)为流动相 ,流速为0 8ml/L ,外标法定量 ,检测波长为300nm。结果 :氟罗沙星在9 92～79.36μg/ml,替硝唑在20 32～162 56μg/ml的浓度范围内峰面积与浓度呈良好的线性关系 ,r分别为0 9974、0 9995,平均回收率分别为101 6%、100 1 % ,RSD分别为1 4 %、1 2 %。结论 :方法简便、快速、准确 ,适于该制剂的含量测定     

荧光分光光度法测定人尿中氟罗沙星的含量

目的:建立灵敏、准确、简便、快速的方法测定人尿中氟罗沙星的含量.方法:以290 nm为激发波长,以458 nm为发射波长,用荧光分光光度法测定人尿中氟罗沙星的排出速率.结果:氟罗沙星浓度在0.05～0.5 mg*L-1范围内,荧光强度与浓度呈良好的线性关系,检测限为0.03 mg*L-1.精密度为日内RSD<1.10%,日间RSD<2.98%(n=5),回收率为(98.6±1.3)%.结论:采用此法测定了2名健康受试者口服氟罗沙星片后的尿药排出速率.尿中药物排出速率最高是在服药后6～8 h,24 h内尿药累积排出率为56.12%,0～24 h内尿药浓度为(69.3±40.6)mg*L-1,显著高于大多数常见致病菌的MIC90,表明有效尿药浓度至少可维持24 h.     

氟替中空泡腾栓的研制

目的 :建立氟罗沙星 -替硝唑中空泡腾栓的制备及质量控制方法。方法 :用36型半合成脂肪酸酯作基质制备氟罗沙星 -替硝唑中空泡腾栓 ;采用双波长紫外分光光度法同时测定氟罗沙星和替硝唑的含量。结果 :氟罗沙星和替硝唑平均回收率分别为99 72 %、99 08% (n=5) ,精密度分别为0 95%、1 02 %。结论 :本方法设计合理 ,工艺可行     

培氟沙星与氟罗沙星治疗慢性阻塞性肺疾病急性发作期病人疗效比较

目的 :评价培氟沙星和氟罗沙星治疗慢性阻塞性肺疾病 (COPD)急性发作期病人的临床疗效。方法 :COPD病人 68例 ,男性 41例 ,女性 2 7例 ,年龄 67a±s 3a。在常规治疗基础上分别使用培氟沙星 40 0mg·d- 1(A组 3 6例 ) ,氟罗沙星 40 0mg·d- 1(B组 3 2例 )均静脉滴注 ,疗程 7～ 10d。结果 :A ,B 2组治疗总有效率分别为 80 %和 81% (P>0 .0 5 ) ,细菌清除率分别为 76%和 78% (P >0 .0 5 )。结论 :培氟沙星临床疗效与氟罗沙星相近。     

高效液相色谱法同时测定口洁灵含漱剂中甲硝唑和醋酸氯己定的含量

目的 :建立口洁灵含漱剂中甲硝唑和醋酸氯己定的高效液相色谱测定方法。方法 :色谱柱YWG -C18柱(10 μm,4 .0mm× 15 0mm) ,流动相为甲醇 0 .0 1mol·L-1磷酸二氢钾液 (1∶ 1,用磷酸调 pH至2 .80 ) ,流速 1.0mL·min-1,检测波长为 2 5 4nm ,柱温为室温。结果 :甲硝唑和醋酸氯己定的线性范围分别为 12 .5～ 10 0mg·L-1和 2 .5～2 0mg·L-1,r值分别为 0 .99998和 0 .9995 2 ,平均回收率(n =5 )分别为 99.6 4 %和 99.90 % ,RSD分别为 0 .4 3%和0 .2 4 %。结论 :本法适用于本制剂的质量控制     

氟罗沙星葡萄糖注射液处方工艺改进

目的　制备符合注射剂质量要求的 2 g· L-1氟罗沙星葡萄糖注射液。方法　去掉原处方中作为抗氧剂的维生素 C,而加入 0 .0 5 g·L-1EDTA- 2 Na作为金属离子络合剂 ;原处方中含量为 2 7.5 g· L-1的葡萄糖调整为 5 0 g· L-1。结果　改进后的 2 g· L-1氟罗沙星葡萄糖注射液质量符合要求。结论　改进后的处方合理 ,制备工艺简单 ,质量稳定。临床用药安全、有效     

氟罗沙星片的人体生物等效性

目的:研究氟罗沙星片的人体相对生物利用度,评价受试制剂与参比制剂的人体生物等效性。方法:20名男性健康志愿者采用随机交叉给药方案,单次口服400mg国产氟罗沙星片受试制剂和参比制剂,采用高效液相色谱法(HPLC)定量测定血浆氟罗沙星浓度,用DAS1.0程序计算两者生物利用度参数,并作出生物等效性评价。结果:单次口服400mg氟罗沙星受试制剂和参比制剂的主要生物利用度参数AUC0→t分别为(76 245.4±9 991.0)μg.h.L-1和(78 295.9±10 566.8)μg.h.L-1,AUC0→∞分别为(79 792.1±10 599.3)μg.h.L-1和(81 037.9±10 807.6)μg.h.L-1;Cmax分别为(5 218.8±1 493.8)μg.L-1和(4 983.9±910.7)μg.L-1;tmax分别为(1.8±1.0)h和(2.0±1.0)h。AUC0→t、AUC0→∞和Cmax经方差分析和双单侧t检验以及tmax经秩和检验表明两制剂的差异无显著性(P>0.05)。结论:两种制剂具有生物等效性,以AUC0→t计算受试制剂相对生物利用度为(98.4±13.4)%。     

氟罗沙星与氧氟沙星治疗泌尿生殖系统感染的比较

目的 :观察评价氟罗沙星与氧氟沙星治疗泌尿生殖系感染的疗效及安全性。方法 :72例病人随机分成 2组 ,治疗组 3 9例 ,用氟罗沙星 0 2～ 0 4g,po ,qd ;对照组 3 3例 ,用氧氟沙星 0 1～ 0 2g ,po,bid ;疗程均为 7～ 1 4d。结果 :治疗组临床有效率 92 3 % ,细菌消除率 90 4% ;对照组分别为90 9%和 93 2 % ;2组间无显著性差异 (P >0 0 5 )。结论 :氟罗沙星治疗泌尿生殖系感染疗效满意 ,安全方便 ,无显著不良反应。     

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.     

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.     

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.     

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.