HPLC法测定益肾灵颗粒中补骨脂素、异补骨脂素的含量

目的：建立益肾灵颗粒中补骨脂素、异补骨脂素的含量测定方法。方法：采用反相高效液相色谱法，Diamonds色谱法，流动相为甲醇。水（48：52），检测波长246nm，流速为0．8mL·min^-1。结果：该方法的补骨脂素的回收率为98．94％（RSD=0．89％，n=5）；畀补骨脂素的回收率为100．27％（RSD=1．83％，n=5）。结论：本法简便、灵敏、准确，可用于本品补骨脂素、异补骨脂素的含量测定。     

甲氧补骨脂素搽剂中8-甲氧补骨脂素的含量测定

目的建立甲氧补骨脂素搽剂中8-甲氧补骨脂素的含量测定方法.方法采用HPLC法,以甲醇-0.02molL/L磷酸二氢钠溶液(5050)为流动相,检测波长为249nm,测定该制剂中8-甲氧补骨脂素的含量.结果平均回收率为99.84%,RSD为0.44(n=5),回归方程为y=1.5172+1.142X×10-5r=1.结论方法简便、快速、准确,适合作该制剂中8-甲氧补骨脂素的含量监控.     

HPLC法同时测定复方萘酚喹片中磷酸萘酚喹和甲氧苄啶的含量

目的：建立同时测定复方萘酚喹片中磷酸萘酚喹和甲氧苄啶含量的方法。方法：高效液相色谱法。固定相为十八烷基硅烷键合硅胶;流动相为乙腈－0．25％二乙胺（30：70,混合后用磷酸调pH至2．5）;检测波长271nm。结果：线性范围：磷酸萘酚喹75．9－227．8μg/ml,r=0.9999,甲氧苄啶26．7－80．2μg/mol,r=0.9999;方法回收率;磷酸萘酚喹100．5％,RSD 0．3％,n=6,甲氧苄啶99．7％,RSD0．7％,n=6。结论：该方法操作简便,结果准确,适用于该制剂的含量测定。     

8-甲氧补骨脂素治疗寻常性斑块型银屑病随机双盲平行对照临床研究

目的评价比较进口与国产的8-甲氧补骨脂素片口服结合UVA UVB照射治疗寻常性斑块型银屑病的临床疗效及安全性。方法用随机双盲、平行对照试验方法,60例患者随机口服进口或国产8-甲氧补骨脂素片,剂量为0.6 mg·kg-1,2h后照射UVA和UVB,每周3次,疗程8周,观察疗效与安全性。结果通过8周的治疗,进口8-氧补骨脂素组PASI总分下降了96.3％,基愈率为92.9％,有效率为100％;国产8-甲氧补骨素组PASI总分下降98.5％,基愈率和有效率均为100％,两组间基愈率和有效率比较无显著性差异(P>0.05)。进口8-甲氧补骨脂素片药物不良反应发生率为46.4％,国产8-甲氧补骨脂素组为40％。药物不良反应多为轻中度消化道及皮肤瘙痒、色素沉着等。结论进口与国产8-甲氧补骨脂素片在进行银屑病PUVA疗法中都具有良好疗效及安全性。     

头孢羟氨苄甲氧苄啶胶囊溶出度测定

目的：建立头孢羟氨苄甲氧苄啶胶囊溶出度测定方法。方法：以盐酸溶液（9→1000）为溶出介质,采用高效液相色谱法测定其溶出度。结果：头孢羟氨苄的浓度在38．6～192．8μg·ml^-1内呈良好的线性关系,r=1．0000,平均回收率为99．1％（RSD=0．3％,n=10）;;甲氧苄啶的浓度在7．8～39．0μg·ml^-1内呈良好的线性关系,r=0．9999,平均回收率为98．9％（RSD=0．5％,n=10）.结论：方法准确、简便,可作为制剂的溶出度测定方法。     

复方8-甲氧补骨脂素凝胶的研制及临床疗效

目的 对8-甲氧补骨脂素／醋酸地塞米松凝胶的制备和质量控制进行研究，并观察其临床疗效。方法 采用新型辅料卡波姆-980等为基质制成凝胶剂，用HPLC测定两主药含量，并对其外观、稳定性、临床疗效等进行考察。结果 复方8-甲氧补骨脂素凝胶外观均匀细腻，两主药平均回收率分别为100．1％和99．9％，RSD分别为0．33％和0．42％。治疗组临床疗效优于对照组。结论 该制剂处方合理，制备工艺简便，稳定性好，质量易于控制，且临床疗效较好。     

补骨脂酊中补骨脂素、异补骨脂素的含量测定

目的建立补骨脂酊中补骨脂素、异补骨脂素的含量测定方法。方法采用高效液相色谱法,色谱柱为Agilent Eclipse XDB-C18柱（150mm×4．6mm,5μm）．流动相为甲醇-水（40：60）．流速为1．0mL·min^-1;检测波长为246nm。结果补骨脂素在0．022～0．44μg（r=0．9999）,异补骨脂素在0．02388～0．4776μg（r=0．9999）具有良好线性关系。补骨脂素平均回收率为98．10％（n=9．RSD=1．20%）,异补骨脂素平均回收率为97．74％（n=9,RSD=1．10％）。结论本方法简便、准确、可靠,可用于补骨脂酊中补骨脂素、异补骨脂素的含量测定。     

离子对分配色谱法测定复方磺胺甲噁唑片中两组分的含量

目的建立离子对分配色谱法测定复方磺胺甲噁唑片中磺胺甲噁唑和甲氧苄啶的含量。方法流动相为甲醇：0．34％磷酸二氢钾：0．05mol／L四丁基溴化铵（55：45：5）。ODS C18柱为色谱柱。柱温25℃，流速1．0ml／min。检测波长240nm。结果磺胺甲噁唑在40-200μg／ml（r=0．9999）、甲氧苄啶在8-40μg／ml（r=0．9998）的浓度范围内呈线性关系。平均回收率分别为100．3％、100．6％；RSD分别为0．29％、0．32％。结论该法专属性强，操作简便，结果准确。     

HPLC法测定无花果叶中补骨脂素的含量

目的：目的：建立无花果叶中补骨脂素含量测定的HPLC法。方法：色谱柱为Diamonsil C18柱（150mm×-4．6mm，5μm）；流动相为：甲醇：水（62：38），流速1．0ml·min^-1，检测波长245nm，柱温35℃。结果：补骨脂素在0．16～1.60μg范围内与峰面积呈良好线性关系（r=0．9999），平均回收率为96．8％，RSD为0．91％。结论：本方法简单、灵敏、准确，可作为无花果叶中补骨脂素含量的测定方法。     

HPLC法测定不同来源补骨脂中补骨脂素和异补骨脂素的含量

目的：建立HPLC法测定不同来源补骨脂中补骨脂素和异补骨脂素含量的方法。方法：选用Hypersil C18柱（250mm×4．6mm,5μm）,以甲醇：0．015％磷酸溶液（40：60）为流动相,流速1．0ml·min^-1,检测波长246／1／11,柱温25℃。结果：补骨脂素在4．16～14．56μg·ml^-1间呈良好的线性关系（r=0．9997）,平均加样回收率为99．9％（RSD=0．90％,n=9）;异补骨脂素在4．16～14．56μg·ml^-1间呈良好的线性关系（r=0．9996）,平均加样回收率为98．0％（RSD=0．78％,n=9）。结论：该方法快速、准确,可用于补骨脂的质量控制。     

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.