高效液相色谱法测定复方健疗霜中三组分含量

目的：测定复方健疗霜中曲安奈德、盐酸苯海拉明和硝酸咪康唑的含量。方法：高效液相色谱法,在ＳｈｉｍｐａｃｋＣＬＣ－ｐｈｅｎｙｌ柱上,以甲醇－水相（三乙胺２ｍＬ,加水至３００ｍＬ,磷酸调ｐＨ至７６）为流动相,检测波长：２３０ｎｍ。结果：本文可同时测定三组分的含量。曲安奈德００２０～００８０ｇ·Ｌ－１,盐酸苯海拉明００８０～０３２０ｇ·Ｌ－１,硝酸咪康唑０１６０～０６４０ｇ·Ｌ－１范围内,峰面积与其浓度呈良好线性关系;平均回收率依次为１００４％,ＲＳＤ＝１０２％;１００６％;ＲＳＤ＝０９１％;１００５％,ＲＳＤ＝０６０％。结论：方法简便、快速、准确,可作为样品的检测方法。     

反相高效液相色谱法测定人血浆中氨溴索浓度

目的：建立测定血浆中氨溴索浓度的反相高效液相色谱法。方法：血浆样品用乙醚提取,醚层经００１ｍｏｌ·Ｌ－１盐酸提取后进样,色谱柱为ＲｅｓｏｌｖｅＣ１８４６ｍｍ×２５０ｍｍ（５μｍ）,流动相为乙腈－甲醇－００１ｍｏｌ·Ｌ－１ｐＨ７０磷酸盐缓冲液－四氢呋喃（３５０∶３５０∶２７５∶２５）,流速１５ｍＬ·ｍｉｎ－１,检测波长２４２ｎｍ,外标法峰高定量。结果：本法最低检测浓度５ｎｇ·ｍＬ－１,线性范围１０～３２０ｎｇ·ｍＬ－１,回归方程为Ｈ＝２４５＋１６４Ｃ,ｒ＝０９９９５,日内ＲＳＤ为２７％～５３％,日间ＲＳＤ为３２％～８２％。结论：该法适用于盐酸氨溴索片的药代动力学研究。     

HPLC法测定复方福尔可定糖浆的含量

目的： 应用高效液相色谱法, 测定复方福尔可定糖浆的含量。方法： 采用ＯＤＳ 柱（２００ ｍ ｍ×４－６ ｍ ｍ） , 以０－０２ ｍｏｌ·Ｌ－ １ 庚烷磺酸钠甲醇溶液－ ０－０５ ｍｏｌ·Ｌ－ １ 磷酸二氢钾溶液－ 三乙胺（３０∶７０∶１ , 用磷酸调ｐＨ 为３－０） 为流动相, 检测波长为２１０ ｎｍ 。结果： 平均回收率（ ｎ ＝ ５） 福尔可定为９９－３ ％ , ＲＳＤ＝ ０－７ ％ ; 愈创木酚甘油醚为９９－８ ％ , ＲＳＤ＝ ０－５ ％ ; 盐酸麻黄碱为９９－５ ％ , ＲＳＤ＝ ０－４ ％ 。结论： 实验结果表明, 该方法简便, 准确, 灵敏度高, 重现性好。     

高效液相色谱法测定静注吡洛地尔兔血药浓度及药物动力学参数

本文应用反相高效液相色谱法测定兔静注吡洛地尔（１５ｍｇ／ｋｇ）血药浓度，样品用正庚烷提取。流动相以１０％三乙胺：甲醇液（甲醇：水＝９：１）＝５：９５。紫外检测波长为２５４ｎｍ，回收率８１．４％，日内和日间的ＲＳＤ值为２．４％、３．５％。最低检测血浓为２０ｎｇ／ｍｌ。用３Ｐ８７程序拟合为二室模型。α＝３．０８ｈ－１，β＝０．１８ｈ－１，Ｔ１／２＝４．０７ｈ，Ｋ１０＝０．９１ｈ－１，Ｋ１０＝０．６１ｈ－１，Ｖｃ＝１１．４５ＡＬ／ｋｇ，ＣＬ＝６．７３Ｌ／（ｋｇ·ｈ），ＡＵＣ＝２．２１（μｇ·ｈ）／Ｌ。     

HPLC法测定万辉化痰止咳露中磷酸可待因、盐酸麻黄碱和马来酸氯苯那敏的含量

目的： 建立一种采用高效液相色谱分离检测多组分复方制剂中磷酸可待因、盐酸麻黄碱和马来酸氯苯那敏含量的方法。方法： 以ＯＤＳ为固定相,０－０５ ｍｏｌ·Ｌ－ １ 磷酸二氢钾（ 含１％ 三乙胺, 用磷酸调ｐＨ＝ ３） － ０－００５ｍｏｌ·Ｌ－１ ＩＰＲ－ Ｂ６ 甲醇溶液（１－２∶１） 为流动相, ＵＶ 检测波长为２５４ ｎｍ 。结果： 磷酸可待因、盐酸麻黄碱和马来酸氯苯那敏３ 种成分的回收率分别为１０１－６％ , ９９－６ ％ , １０１－７ ％ ; ＲＳＤ 分别为１－１％ , １－２％ , １－９％ （ ｎ ＝５） 。结论： 方法简便, 结果准确可靠。     

高效液相色谱法测定盐酸阿洛司琼胶囊溶出度

目的：建立用反相高效液相色谱法测定盐酸阿洛司琼胶囊溶出度的方法。方法：采用ＳＵＰＥＬＯＣ Ｃ１８柱,０．０１ｍｏｌ／Ｌ醋酸铵（用冰醋酸调节ｐＨ＝４．０）－甲醇－四氢呋喃（７０：２４：６）为流动相,检测波长２９５ｎｍ。结果：盐酸阿洛司琼在２．４３～１７．０１ｕｇ·ｍｌ＾－１浓度范围内呈现良好的线性关系（ｒ＝０．９９９９）,平均回收率为９９．４８％,ＲＳＤ＝１．３％（ｎ＝５）。结论：本方法操作简便,准     

Pharmacokinetics of bendazac lysine in 10 Chinese young men

比较国产和进口苄达赖氨酸（ＢＬ）片在人体内的药物动力学．方法：１０名男性汉族健康志愿者随机交叉口服单剂量５００ｍｇ国产和进口苄达赖氨酸（ＢＬ）片剂后，用高效液相紫外法测定血浆药物浓度．结果：血药浓度时间曲线拟合表明该药体内过程符合口服二室开放模型，国产和进口片剂的主要药代动力学参数：Ｃｍａｘ６６±１６ａｎｄ６５±８ｍｇ·Ｌ－１；Ｔｍａｘ０９８±０２２ａｎｄ０９８±０２１ｈ；Ｔ１２β６２±１８ａｎｄ６２±１７ｈ；ＡＵＣ３３５±４７ａｎｄ３３７±５８ｍｇ·ｈ·Ｌ－１．经ｔ检验无显著性差异，国产片对进口片的相对生物利用度为９９±１２％．结论：两种片剂具有生物等效性．     

高效液相色谱法测定复方盐酸万乃洛韦滴眼液的含量

目的：测定复方盐酸万乃洛韦滴眼液中盐酸万乃洛韦和氧氟沙星的含量。方法：采用高效液相色谱法,色谱柱为Ａｌｌｔｉｍａ Ｃ８柱;相为０．０２ｍｏｌ．Ｌ＾－１,磷酸二氢钾－乙腈（４：１）,流速为１ｍｌ．ｍｉｎ＾－１,检测波长为２５０ｎｍ。结果：盐酸万乃洛韦和氧氟沙星的回收率分别为９９．４％,ＲＳＤ＝０．９８％,１００．２％,ＲＳＤ＝０．５７％,结论：方法快速,准确,可作为该制剂的质控标准。     

高效液相色谱法测定盐酸氟桂利嗪血浆浓度及其药物动力学

以高效液相色谱法测定血浆中的盐酸氟桂利嗪浓度。色谱条件：紫外检测波长２１０ｎｍ；柱ＳｐｈｅｒｉｓｏｒｂＣ８１５０×４．６ｍｍ；流动相：甲醇（８０％）∶水（１５％）∶（０．０５ｍｏｌ·Ｌ－１ＮＨ４Ｈ２ＰＯ４＋０．０２５ｍｏｌ·Ｌ－１Ｈ３ＰＯ４）缓冲液（５％）。最低检测限１０ｎｇ·ｍｌ－１。药物动力学为一室模型，其参数（Ｔ１／２（Ｋ）２．３８～２．６４ｈ，Ｔｍａｘ２．３０～２．４３ｈ，Ｃｍａｘ１３５．１３～１４３．９６ｎｇ·ｍｌ－１。     

家兔静注水杨醛-N'-(2-呋喃硫羰基)腙铜配合物的药物动力学

目的：研究水杨醛－Ｎ′－（２－呋喃硫羰基）腙铜配合物（ＣＳＦＣ）在兔体内的药物动力学。方法：１０只家兔静脉注射ＣＳＦＣ５ｍｇ·ｋｇ－１，用反相ＨＰＬＣ法测定血清药物浓度。结果：ＣＳＦＣ的血药浓度－时间曲线符合二室开放模型，主要药动学参数为：Ｔ１２α＝３．４±１．７ｍｉｎ，Ｔ１２β＝６５．５±１４．６ｍｉｎ，Ｋ１２＝０．１１８３±０．０６６９ｍｉｎ－１，Ｋ２１＝０．０２２８±０．００６５ｍｉｎ－１，Ｋ１０＝０．１２０２±０．０４０７ｍｉｎ－１，Ｖ０＝０．３０５±０．１８４Ｌ·ｋｇ－１，ＣＬ＝１．８９６±０．４７０Ｌ·ｋｇ－１·ｈ－１，ＡＵＣ＝１７０．１±５７．０ｍｇ·ｍｉｎ－１·Ｌ－１。结论：ＣＳＦＣ在兔体内分布迅速而广泛，消除也较快。家兔静注５ｍｇ·ｋｇ－１，可维持抗结核杆菌有效血浓度６ｈ。     

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.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

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.