高效液相色谱法测定中药升麻中阿魏酸和异阿魏酸的含量

目的 :测定中药升麻中阿魏酸和异阿魏酸的含量。方法 :反相高效液相色谱法。HypersilODS分析柱(2 5 0mm× 4 6mm ,5 μm) ,流动相 :甲醇 -水 -磷酸 (5 0∶15 0∶0 1) ,紫外检测波长 :32 0nm ,灵敏度 :1 0AUFS ,柱温 :2 4℃ ,流速 :1mL·min-1。结果 :阿魏酸在 0 0 42～ 2 10 μg (r =0 9993) ,异阿魏酸在 0 0 43～ 2 14μg (r =0 9994)范围内呈线性 ,阿魏酸和异阿魏酸平均回收率 (n =5 )分别为 98 76 % (RSD =1 6 % )和 98 32 % (RSD =1 8% )。结论 :本方法简便、精确、可靠。     

反相高效液相色谱法对不同产地川芎中阿魏酸的测定

目的 :对中药川芎中阿魏酸的含量分析进行方法学研究 ,并测定川芎的不同产地、不同品种的阿魏酸的含量。方法 :采用RP HPLC技术对 5个品种 15个样品进行测定。流动相为甲醇 水 36 %乙酸 (30 :6 7:3) ,流速为 1.0ml/min。UV检测波长32 2nm。结果 :本方法测定阿魏酸在 4 .0 16～ 2 0 .0 8μg/ml范围内呈良好的线形关系 ,回归方程为A =2 .2 1199C 1936 .16 (r =0 .9999)。阿魏酸的平均回收率±RSD为 99.90 %± 5 .12 % (n =3)。不同产地、不同品种的川芎其阿魏酸的含量为 0 .6 5 30～1.32 71mg/g。 结论 :川芎由于产地不同其阿魏酸的含量相差悬殊。以四川川芎中阿魏酸的含量为最高。本测定为筛选优良品种提供了简便易行的方法     

反相高效液相色谱法测定生肌膏中阿魏酸的含量

目的 :测定生肌膏中阿魏酸的含量。方法 :反相高效液相色谱法。色谱柱为Nova PakC18柱 (4μm ,30 0mm×4 .0mm) ,流动相为甲醇 水 乙酸 (46∶5 3∶1) ,检测波长为 32 3nm。结果 :阿魏酸浓度在 4 .39～ 30 .74mg·L-1范围内与色谱峰面积呈良好的线性关系 (r =0 .9999)。平均加样回收率为 97.0 8% ,RSD为 1.2 6 % (n =6 )。结论 :本法简便 ,准确 ,灵敏度高 ,重现性好 ,可用于生肌膏中阿魏酸含量的测定。     

高效液相色谱法测定小儿咳喘灵冲剂中麻黄碱的含量

目的 :建立高效液相色谱法测定小儿咳喘灵冲剂中麻黄碱的含量。方法 :采用 phenomenex C1 8柱 (4 .6 mm×2 5 0 mm,5μm) ,流动相为 0 .0 1mol/ L磷酸二氢钾溶液 (用磷酸调 p H至 2 .4 0 ) -甲醇 (92 :8) ,流速 1.0 0 ml/ min,检测波长2 10 nm。结果 :盐酸麻黄碱进样量为 0 .0 84～ 0 .6 72μg范围内呈良好的线性关系 (r =0 .9990 ) ,平均回收率 10 4 .2 % ,RSD为 2 .32 %。结论 :本法简便、准确、重复性好 ,可用于该制剂的质量控制。     

肠舒胶囊中阿魏酸含量的HPLC法测定

目的　建立肠舒胶囊中阿魏酸含量的HPL C测定方法。方法　选用 Hypersil C18分析柱(15 0 mm× 4 .6 mm,5μm) ,以甲醇为提取溶剂 ,甲醇- 10 m L· L-1冰醋酸 (2 3∶ 77)为流动相 ,检测波长32 0 nm,流速 1.0 m L· min-1。结果　线性范围 2 0～10 0 mg· L-1(r =0 .9999) ,平均回收率 97.5 % ,RSD 1.6 6 % (n =5 )。结论　本法测定肠舒胶囊中阿魏酸的含量 ,方法准确 ,简便 ,适用     

高效液相色谱法测定盐酸平阳霉素软膏的含量

目的 :采用高效液相色谱法测定平阳霉素软膏中盐酸平阳霉素含量。方法 :Kromasil C8( 2 5 0 mm× 4 .6 mm,5μm)柱为色谱柱 ;流动相为戊烷磺酸钠溶液 -甲醇 -乙腈 ( 81∶ 13∶ 6 ) ;柱温 4 0 o C;流速 0 .8ml/ min;检测波长 2 5 4 nm;峰面积外标法。结果 :平阳霉素在 17.3～ 86 .6μg/ ml范围内呈良好的线性关系 ,r =0 .9998,平均回收率为 10 0 .0 % ( n =9) ,结论 :本方法简便、快速 ,结果准确 ,重现性好     

高效液相色谱法测定瑞巴匹特的含量

目的 :建立高效液相色谱法测定瑞巴匹特含量的方法。方法 :采用 C1 8柱 (2 5 0 mm× 4 .6 mm,5 μm) ,以甲醇 -醋酸 /醋酸钠缓冲溶液 (49∶ 5 1)为流动相 ,流速为 1.0 ml/min,检测波长为 32 7nm。结果 :瑞巴匹特浓度在 0 .1～ 0 .6mg/ml范围内 ,线性关系良好 ,r=0 .9999。回收率为 99.5 % ,RSD为 0 .8% (n=5 )。结论 :本方法简便、准确、专属 ,可用于本品的含量测定及质量控制。     

多波长高效液相色谱法测定四季三黄胶囊中4种主药成分含量

目的 :同时测定四季三黄胶囊中大黄酸、黄芩苷、盐酸小檗碱和栀子苷的含量。方法 :紫外 -可见四波长同时检测的高效液相色谱法。色谱柱为 Diamonsil C1 8柱 (2 5 0 mm× 4 .6 mm ,5μm) ;流动相为甲醇 (A)水 (B) (含 0 .0 33mol/ L磷酸二氢钾 ,0 .3%磷酸 ) ;流速为 1ml/ min;柱温为 32 o C;检测波长为 2 2 8nm(大黄酸 ) ,2 78nm(黄芩苷 ) ,35 0 nm(盐酸小檗碱 ) ,2 36 nm(栀子苷 ) ;线形梯度洗脱。结果 :平均回收率分别为大黄酸 97.9%、黄芩苷 98.4 %、盐酸小檗碱 10 2 .2 %、栀子苷 99.3%。结论 :为四季三黄胶囊提供了更全面、有效的质控方法。     

高效液相色谱法测定康媛颗粒中阿魏酸的含量

建立高效液相色谱法测定康媛颗粒中阿魏酸的含量。色谱柱LichrospherC18(5 μm ,2 5 0mm×4 6mm) ,流动相 :甲醇 - 0 16 %醋酸溶液 (38∶6 2 ) ;检测波长 :32 3nm ;阿魏酸的线性范围为 7～ 35 μg·ml-1(r=0 9995 ) ,平均回收率为 96 89% ,RSD为 1 34% (n =5 )。本法操作简单 ,快速 ,准确 ,可行。     

HPLC测定人血浆中螺旋霉素的浓度及其药代动力学研究

目的 :建立人血浆中螺旋霉素 (SPM )浓度的测定方法及进行人体药代动力学的研究。方法 :采用高效液相色谱法 ,色谱柱 :phenomenex C1 8色谱柱 (5 μm,2 5 0 mm× 4 .6 mm) ,以乙腈∶磷酸二氢钾缓冲液(0 .0 5 mol/ L,p H为 2 .86 ) =5∶ 18(v/ v)为流动相 ,以乳酸司帕沙星为内标 ,流速 1.0 ml/ min,柱温为 2 0℃ ,紫外检测波长 2 32 nm,用螺旋霉素与内标的峰面积比进行定量。线性范围 2 5～ 32 0 0μg/ L ,最低检测浓度为2 0μg/ L ,对 18名健康受试者单次口服 4 5 0万 u螺旋霉素片剂后的药代动力学进行研究。结果 :18名健康受试者的血药浓度数据经 3p97拟合 ,符合血管外给药一室模型 ,AU C0～ t为 (44 72 .0± 6 74 .3) μg· h/ L,Cmax为(16 14 .4± 2 98.2 ) μg/ L,Tmax为 (2 .75± 0 .31) h,T1 /2 ke为 (2 .6 4± 0 .70 ) h。结论 :该方法简便 ,稳定性好 ,噪音小 ,灵敏度和准确度高 ,能够满足人体内低浓度药物的测定及药代动力学研究的要求。     

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.     

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.     

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.