HPLC法测定米诺地尔搽剂中米诺地尔的含量

目的建立用于测定米诺地尔搽剂中米诺地尔含量的HPLE法。方法采用HPLC法测定,色谱柱：Hypersil ODS2 （250mm×4．6mm,5μm）,流动相：V（甲醇）：V（0．1％三乙胺水溶液）=25：75,检测波长285nm,柱温30℃,流速1mL·min^-1。结果米诺地尔在质量浓度6．6—39．6mg·L^-1内与峰面积之间呈现良好的线性关系（r=0．9996）,平均回收率为107．99％,RSD为0．99％。结论本方法简便、灵敏度高,能准确检测米诺地尔搽剂中米诺地尔的含量,可作为米诺地尔搽剂质量控制的有效测量方法。     

复方桑参米诺地尔搽剂中米诺地尔的HPLCLC定

建立了高效液相色谱法测定复方桑参米诺地尔搽剂中米诺地尔的含量。采用C18柱，流动相为甲醇．乙腈·水（40：10：50），流速1．2ml／min，检测波长230nm，内标为对乙酰氨基酚。米诺地尔在3．649。6μg／ml浓度范围内线性关系良好（r=0．9999），回收率大于98％，日内和日间RSD均小于1％。     

5%米诺地尔搽剂的制备及稳定性

米诺地尔（minoxidil）局部外用可用于治疗簇状脱发（斑秃）和雄激素所致脱发（男性化脱发），常用浓度为2％，但近年发现5％米诺地尔的效果明显优于2％的米诺地尔，且无明显的毒副作用。本研究介绍了5％米诺地尔搽剂的制备方法、质量控制方法及其稳定性。     

高效液相色谱法测定米诺地尔搽剂中米诺地尔的含量

目的建立测定米诺地尔搽剂中米诺地尔含量的高效液相色谱(HPLC)检验方法。方法采用Nova-PaKC18色谱柱(150mm×4.6mm,5μm),流动相为甲醇-水(70∶30),流速为1.0mL/min,检测波长为285nm。结果米诺地尔在2.5～20mg/L浓度范围内含量与峰面积比呈现良好的线性关系(r=0.9999),平均回收率为99.5%,RSD为1.85%,最低检出浓度为0.5mg/L。结论本法能准确检测米诺地尔搽剂中米诺地尔的含量,因此可作为米诺地尔搽剂质量控制的有效测量方法。     

紫外分光光度法测定复方长压啶搽剂中两组份的含量

建立复方长压啶搽剂中米诺地尔和维甲酸的含量测定方法。方法：要用紫外分光光度法同时测定复方长压啶搽剂中米诺地尔和维甲酸的含量,以一阶导数２７８．５ｎｍ处的振幅值测定米诺地尔,以零阶导数３３７ｎｍｔｈ ｒ ｋｅ ｉｑ ｙａ ｉｍｊ ｐｇ ｘｗｙｇｌｈｎｈｓｃｔ     

米诺地尔凝胶的制备及临床疗效观察

目的：研制米诺地尔凝胶，治疗雄激素脱发。方法：以卡波普作为凝胶基质制备米诺地尔凝胶，用紫外分光光度法进行含量测定。结果：米诺地尔在287nm波长处，4～16μg／ml浓度范围内，浓度与吸收度之间线性关系良好。其回归方程C=21．1487A 0．01177，r=0．9994，平均回收率为99．88％，RSD=0．72％(n=5)，临床有效率63．04％。结论：米诺地尔凝胶性质稳定，具有良好的临床疗效，未发现毒副作用。     

米诺地尔生发液的制备及稳定性考察

目的 探讨米诺地尔生发液的制备及质量控制方法，并预测其有效期。方法 采用紫外分光光度法测定含量，以初均速法考察稳定性。结果 检测波长为280nm；米诺地尔浓度在2～10μg/mL范围内与吸收度呈良好线性关系，C=9．1291A-0.1472，r=0.9999（n=6）平均回收率为100．38％（n=9）；在室温（20℃）条件下，2％，5％米诺地尔生发液有效期分别为13个月和10个月。结论 该制剂稳定，制备简便，含量测定方法简便、准确，其稳定性与温度有关，符合Arrhenius公式。     

紫外分光光度法测定米诺地尔洗剂中米诺地尔的含量

目的 建立米诺地尔洗剂的含量测定方法。方法 采用紫外分光光度法测定洗剂中米诺地尔的含量。结果 测定波长231nm，在1～7μg／ml浓度范围内吸收度与浓度线性关系良好(r=0．9998)，平均回收率99．29％，RSD 0．05％(n=4)。结论 本法方便快捷，结果准确，可用于米诺地尔洗剂的质量控制。     

紫外分光光度法测定醋酸氟轻松搽剂中醋酸氟轻松的含量

目的：建立醋酸氟轻松搽剂中醋酸氟轻松含量的测定方法。方法：采用紫外分光光度法测定醋酸氟轻松搽剂中醋酸氟轻松的含量。结果：采用紫外分光光度法以238．4nm为检测波长，其回归方程为A=0．0326C 0．0002，r=0．9998。平均回收率=99．17％；RSD=2．55％。同时采用对照品比值法进行回收试验，其平均回收率=100．3％；RSD=0．85％。结论：采用紫外分光光度法测定醋酸氟轻松搽剂中醋酸氟轻松的含量，方法快捷，准确，可行。     

紫外分光光度法测定米诺地尔酊的含量

目的：用紫外分光光度法测米诺地尔酊中米诺地尔的含量,为该药提供质量控制方法。方法：紫外分光光度法。结果：米诺地尔浓度在０．５～６μｇ·ｍｌ－１范围内吸收度与溶液浓度呈线性关系（ｒ＝０．９９９９,ｎ＝５）,回收率为１００．４％,ＲＳＤ为０．１０％（ｎ＝５）。结论：该法能作为米诺地尔酊含量测定的方法,而且简便、准确、快速。     

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.