萘普生混悬液的制备和疗效观察

萘普生(naproxen)是非甾体类抗炎药,具有抗炎、解热、镇痛作用,口服吸收迅速完全,1次给药2～4h血浆药物浓度达峰值,T1/2为13～14h,约95%自尿中以原形及代谢物排出.目前应用剂型有片剂、胶囊剂、颗粒剂、栓剂等.为便于儿童用药,我们研制了萘普生混悬液,同时观察了萘普生混悬液的退热疗效.     

萘普生与β-环糊精包合降低致溃疡性

萘普生是一非甾体消炎药并有解热、止痛作用,经常用于治疗风湿性关节炎及骨关节炎。由于它的酸性及低溶解度,药物缓慢溶解,刺激和损伤胃壁,如以高剂量长期口服治疗会引起溃疡。萘普生和β-环糊精1∶1混合物于蒸馏水中,加少量氨增加溶解度,搅拌24h,冷冻干燥。经相溶解度图、IR 谱及 DSC 扫描曲线证明冻干物为包合物。把体重180～210g 的雄性大鼠分成三组。给药4天,每天口服20mg/ml 混悬液,     

萘普生钠注射液的药物动力学研究

以萘普生钠水溶液作对照,研究了萘普生钠注射液在家兔体内药物动力学。结果表明萘普生钠注射液的T_(max)(1.32±0.25h)较萘普生钠水溶液(4.7±1.4h)短;C_(max)(327±27μg/ml)较水溶液(168±28μg/ml)高;而Ka和Ke(0.55±0.18h~(-1),0.107±0.025h~(-1))较水溶液(0.40±0.20h~(-1),0.050±0.014h~(-1))大。以萘普生钠水溶液作“标准”制剂,计算注射液的相对生物利用度为102.96%。说明萘普生钠注射液肌注给药比口服水溶液吸收快,排泄也快,吸收程度高。     

萘普生锌给药剂量与药效关系的探讨

以生理盐水和萘普生悬浮液为对照,对萘普生锌悬浮液在镇痛,抗炎和解热作用方面的用药剂量与药效关系进行了探讨。结果表明,萘普生和萘普生锌在镇痛、抗炎、解热方面的作用与生理盐水比较,有显著性差异。但同等剂量的奈普生和萘普生锌在镇痛,抗炎,解热方面的作用无显著性差异。且二者的用药剂量与药效之间呈现量效关系。     

萘普生及其钠盐、锌盐栓剂抗炎镇痛作用的比较

萘普生及其钠盐、锌盐栓剂抗炎镇痛作用的比较贾海鹰（内蒙古医学院药学系呼和浩特０１００５９）王玉和（内蒙古呼铁局工程处中心卫生所）徐俐峰路广秀成瑞（内蒙古医学院第一附属医院）萘普生是一种非甾体的抗炎镇痛药物，我们试制其钠盐及锌盐栓剂，并以萘普生栓剂为对...     

萘普生钠片的人体生物等效性

目的 :比较国产和进口萘普生钠片在 2 0名男性健康受试者间的药物动力学和生物等效性。方法 :随机交叉单剂量口服萘普生钠片 0 .5 5 g后 ,采用高效液相色谱 -荧光检测法测定血药浓度。结果 :国产和进口萘普生钠片的药物动力学参数如下 :AUC0 - t分别为 (975 .36± 176 .5 1)、(982 .5 5± 141.0 4) ︼g· h/ ml;cmax分别为 (72 .0 5± 13.95 )、(75 .6 2± 15 .0 5 ) ︼g/ m l;tmax分别为 (1.6 0± 1.17)、(1.15± 0 .5 9) h;T1 / 2 分别为 (11.6 9± 1.47)、(11.82± 1.38) h。经统计学处理 ,上述各项参数间差别均无统计学意义 (P>0 .0 5 )。国产萘普生钠片相对生物利用度为 (99.18± 9.93) %。结论 :萘普生钠片国产片与进口片具有生物等效性     

高效低毒新药萘普生钠

萘普生钠(英文名:Naproxen Sodium,国外商品名:Anaprox)属非甾体类抗炎镇痛药物(NASID),国外七十年代末合成,八十年代初已有商品在欧美等国上市,一九八五年收载于美国药典双ⅩⅩⅠ版。[药物合成] 本品系萘普生的钠盐(?)C_(11)-H_(13)NaO_3=252.4],由萘普生与氢氧化钠或碳酸钠在弱碱性环境下反应而成。     

萘普生-β-环糊精包合物抗类镇痛作用测定及数据分析

采用电刺激痛阈值法、扭体反应法及足跖肿胀法测定萘普生及萘普生－β－环糊精包合物对大鼠和小鼠的抗炎镇痛作用,结果表明,萘普生－β－环糊精包合物有显著的镇痛、抗炎作用（Ｐ＜ ０．０１,Ｐ＜ ０．０１）,其镇痛作用优于萘普生单体（Ｐ＜ ０．０５）     

萘普生钠经口灌胃给药长期毒性研究

萘普生钠经口灌胃给药长期毒性研究张继芳，张桥，陈铁江，邓丽霞，钟小明萘普生钠是非甾体有机酸类的一种抗炎镇痛药，主要用于类风湿关节炎，风湿性关节炎，痛风等，其主要作用机理是抑制前列腺素的合成，关于萘普生钠的毒性作用尚未完全清楚，为此我们进行了萘普生钠对...     

萘普生口服微乳的制备及质量评价

目的：研制萘普生口服微乳制剂,并对其质量进行评价。方法考察萘普生在不同油相、表面活性剂和助表面活性剂中的溶解度,并通过滴定法绘制伪三元相图,根据相图优选处方,并初步考察微乳制剂的稳定性、形态粒径和理化性质。结果适宜的油相、表面活性剂和助表面活性剂分别为中链甘油三酯（ MCT）、聚山梨酸酯80（吐温80）和PEG400,三者之间的最适比例是1∶4.5∶1.5。结论该普生口服微乳制备简单,性质稳定,可显著增加萘普生的溶解度,为开发萘普生口服微乳提供了依据。     

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.