导数—分光光度法测定小儿胺散的含量

Sulfaguanidine (Ⅰ) and sulfadimidine (Ⅱ) in infantile co-sulfadimidine powders were determined using derivative-spectrophotometry. Ⅰ and Ⅱ were extracted with 10 ml dilute HCl, and added 0.1 mol/L HC1 to 100 ml. Ⅰ was analyzed with spectrophotometry at 220 nm. Ⅱ was analyzed with derivative-spectrophotometry at 321, 324 nm. Recoveries of Ⅰ and Ⅱ were 100.2±0.33% and 100.3±0.55% respectivly.     

PLS—紫外分光光度法同时测定复方阿斯匹林片中三组分含量

本文研究了复方阿斯匹林片中阿斯匹林、非那西丁和咖啡因含量同时测定的紫外分光光度法的最佳实验条件,并简述偏最小二乘法(PLS)在多组分同时测定中的基本原理和应用。三组分模拟试样回收率平均值的置信区间分别为100.1±0.23%,100.0±0.25%和100.1±0.33%(置信度95%)。PLS法是一种理想的多组分测定方法,计算速度较快,结果更准确可靠,尤其适用于成批试样的分析,为微机控制的紫外可见分光光度计提供了一种新方法。     

国产丙硫氧嘧啶片在中国男性志愿者的人体药动学及生物等效性研究

目的 :研究健康男性自愿者口服国产丙硫氧嘧啶片的人体相对生物利用度及生物等效性。方法 :2 0名健康男性志愿者随机交叉自身对照分别单次口服丙硫氧嘧啶国产及进口片剂各 2 0 0mg。用HPLC法检测血药浓度 ,以内标法定量。结果 :峰浓度Cmax分别为 (5 .7± 1.5 )及 (5 .8± 1.8)mg·L- 1;达峰时间Tmax分别为 (1.4± 0 .8)及 (1.4± 0 .7)h ;消除相半衰期t1/2 分别为 (1.7± 0 .3)及 (1.7± 0 .2 )h ;AUC0 -t分别为 (18.0± 4 .4 )及 (17.8± 4 .6 )mg·h·L- 1;AUC0 -∞ 分别为 (18.1± 4 .5 )及 (17.9± 4 .7)mg·h·L- 1。受试片相对于参比片的生物利用度为(10 1.9± 13.2 ) %。结论 :丙硫氧嘧啶片国产片和进口片具有生物等效性     

AKC矩阵分光光度法同时测定增效联

本文应用加非零截矩校正的AKC矩阵分光光度法。选取238～266nm间的8个波长点为测定波长，测得增效联磺片中三组分的含量。方法的平均回收率±相对标准偏差分别为：磺胺嘧啶99.7％±0.88％.磺胺甲基异恶唑100．8％±0．97％.甲氧苄胺嘧啶99．6％±0．86％。方法简便．准确。     

丙硫氧嘧啶肠溶胶囊人体相对生物利用度研究

目的 :评价国产丙硫氧嘧啶肠溶胶囊的人体相对生物利用度。方法 :采用改进的高效液相色谱法测定20名男性健康受试者单剂量口服100mg丙硫氧嘧啶肠溶胶囊 (受试制剂 )和进口的丙硫氧嘧啶片 (参比制剂 )后的血药浓度 ,应用CRFB生物利用度统计程序对数据进行拟合。结果 :受试制剂和参比制剂的AUC0～t 分别为 (9 13±1 53)、(8 80±1 37) (μg·h)/ml,Cmax 分别为(3 02±0 71)、(3 03±0 66) μg/ml ,tmax 分别为 (4 51±0 24)、(1 13±0 44)h。两组参数均无统计学差异 (P>0 05) ,受试制剂的相对生物利用度为 (104 37±12 16) %。结论 :国产丙硫氧嘧啶肠溶胶囊与进口丙硫氧嘧啶片具有生物等效性。     

银锌霜的制备和临床应用

目的研制银锌霜,并观察该药的临床疗效。方法采用硬脂酸为乳化剂制成的基质加入磺胺嘧啶银和磺胺嘧啶锌制成乳膏剂,观察90例烧烫伤病人的治疗效果。结果临床观察90例Ⅱ°、Ⅲ°烧烫伤病人,有效率达100%。结论本制剂制备工艺合理,稠度适宜,易于涂布,吸水性好,质量可靠,疗效确切,值得推广。     

磺胺甲噁唑及其乙酰化代谢物的药代动力学研究

目的测定20名中国男性缝康受试者口服复方新诺明片(含磺胺甲噁唑800 mg)后磺胺甲噁唑(SMZ)和N4-乙酰基-磺胺甲噁唑(N4-Ac-SMZ)的血药物浓度,进行药代动力学研究.方法用反相高效液相色谱法同时测定磺胺甲噁唑和N4-乙酰基-磺胺甲噁唑的血浆浓度,并计算药代动力学参数.结果磺胺甲噁唑和N4-乙酰基-磺胺甲噁唑的tmax分别为1.83±0.71 h和8.10±2.94 h,Cmax分别为37.57±13.52mg.L-1和5.89±2.90 mg.L-1,t1/2分别为10.25±1.16 h和12.65±1.44 h,AUC0-34h分别为486.0±183.6 mg2h·L-1和131.7±64.1mg.h.     

磺胺嘧啶速释片的相对生物利用度研究

目的　研究磺胺嘧啶速释片在健康人体的相对生物利用度。 方法　8名健康受试者单剂量随机交叉口服磺胺嘧啶速释片标准参比制剂和待测制剂 10 0 0mg ,采用HPLC法测定用药后不同时间的血药浓度。结果　 两种制剂的体内过程均符合一房室开放模型 ,AUC分别为 (5 6 9 1± 94 8)mg·h·L-1和 (5 71.8± 79.1)mg·h·L-1,Cmax分别为 (2 8.5± 4 .1)mg·L-1和 (30 .1± 4 .4 )mg·L-1,Tmax分别为 (4 .5 9± 1.2 8)h和 (4 .4 8± 1.4 3)h。待测制剂的相对生物利用度为 (10 1.4± 11.4 ) %。 结论　 用NDST软件对两种制剂的AUC、Cmax、Tmax等进行双向单侧t检验 ,表明两种制剂具有生物等效性     

双波长法测定增效黄连素片中甲氧苄氨嘧啶的含量

本文采用双波长法可消除黄连素的干扰而直接测定该片中甲氧苄氨嘧啶的含量,其检测波长为271±1nm,参考波长为339±1nm。平均回收率为100.7%;变异系数为1.23%。增效黄连素片每片含盐酸黄连素0.1g,甲氧(艹卡)氨嘧啶(以下简称Tmp)0.05g,淀粉(包括淀粉浆)约0.09g及微量硬脂酸镁组成片蕊,     

翻白草对高血糖动物模型的作用研究

目的　研究翻白草的降血糖作用。方法　将翻白草煎剂配伍组 (另加优降糖 0 6 6mg·kg-1)高、中、低三个剂量 ,分别对 3组正常小鼠和 3组小鼠模型ig ,给药 15d ,观察正常和模型小鼠血糖变化。结果　翻白草低剂量 (2 5g·kg-1)配伍组 ,对正常小鼠血糖有明显影响 ,血糖平均值(3 10± 0 14 )mmol·L-1,对照组为 (4 4 6± 0 12 )mmol·L-1(P <0 0 1)。翻白草配伍组 3个剂量对四氧嘧啶糖尿病小鼠模型组都有降糖作用 ,其中低剂量配伍组最为明显 ,血糖平均值为 (6 2 5± 0 4 4 )mmol·L-1,模型对照组为 (11 84±1 0 7)mmol·L-1(P <0 0 1)。结论　翻白草配伍组对正常和高血糖模型小鼠均有降血糖作用     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.