盐酸达克罗宁凝胶的制备与质量控制

目的 :研制盐酸达克罗宁凝胶剂 ,并制定合适的质量控制。方法 :以卡波姆 94 0为凝胶基质制备盐酸达克较宁凝胶剂 ,用一阶导数光度法进行含量测定。结果 :盐酸达克罗宁溶液在 2～ 16 μg·ml-1范围内 ,浓度C与振幅D有良好的线性关系 ,其回归方程为C =- 0 .0 2 6 1+1.0 70 1D(r =0 .9997) ,平均回收率为 99.8% ,RSD为 0 .5 % (n =6 )。结论 :盐酸达克罗宁凝胶制备工艺简单 ,用一阶导数光度法测定含量快捷、简便、准确。     

复方醋酸氯己定凝胶的制备和质量控制

目的：制备复方醋酸氯己定凝胶,并建立其质量控制方法。方法：以醋酸氯己定、盐酸达克罗宁、薄荷脑、曲安奈德为主药,以甲基纤维素4500为基质制备凝胶;采用高效液相色谱法测定醋酸氯己定、盐酸达克罗宁的含量。结果：制备的凝胶均匀细腻,分散性好;醋酸氯己定浓度在0.08152～0.40760μg范围内呈良好的线性关系（r=0.9999,n=5）,平均回收率为98.82%,RSD为1.19（n=9）;盐酸达克罗宁在0.1636～0.8180μg范围内呈良好的线性关系（r=0.9999,n=5）,平均回收率为98.85%,RSD为1.13（n=9）。结论：本制剂组方合理,制备工艺简便可行,质量稳定可控。     

局麻止痛膜的制备及质量控制

目的:制备局麻止痛膜并建立其质量控制方法。方法:以聚乙烯醇-124为基质制备局麻止痛膜,并采用高效液相色谱法测定其中主药盐酸达克罗宁的含量。结果:盐酸达克罗宁检测浓度在40.8~408μg/ml范围内与峰面积线性关系良好(r=0.9 998),平均回收率为101.3%(RSD=1.3%,n=6)。结论:局麻止痛膜的制备工艺简单,质量稳定,控制方法可行。     

盐酸林可霉素甘油涂剂的制备及含量测定

目的:制备治疗口腔黏膜溃疡的盐酸林可霉素甘油涂剂,并建立其含量测定方法。方法:以盐酸林可霉素、盐酸达克罗宁为主药制备涂剂;采用高效液相色谱法测定其中2种主药的含量。结果:盐酸林可霉素、盐酸达克罗宁的线性范围分别为20～200(r=0.9998)、10～100μg·mL-1(r=0.9999);平均回收率分别为99.61%、99.28%(n=5),RSD分别为0.439%、0.818%。结论:该制剂制备及含量测定方法简便、可行。     

HPLC法测定复方氯己定凝胶中醋酸氯己定和盐酸达克罗宁含量

目的建立高效液相色谱(HPLC)法测定复方氯己定凝胶中醋酸氯己定和盐酸达克罗宁的含量。方法选用Inertsil ODS-SP色谱柱,0.5%三乙胺(用冰醋酸调pH值至3.8)-乙腈(68∶32)为流动相,流速1.0 mL/min,检测波长270 nm。结果醋酸氯己定在0.081 52～0.489 10μg时呈良好的线性关系(r=0.999 9,n=6),平均回收率为98.82%,相对标准偏差(RSD)为1.19%(n=9);盐酸达克罗宁在0.163 6～0.981 6μg时呈良好的线性关系(r=0.999 9,n=6),平均回收率为98.85%,RSD为1.13%(n=9)。结论 HPLC法操作简便、灵敏度高、重复性好,可用于该制剂中醋酸氯己定和盐酸达克罗宁的含量测定。     

达克罗宁氯己定硫软膏中盐酸达克罗宁的含量测定

目的建立测定达克罗宁氯己定硫软膏中盐酸达克罗宁含量的高效液相色谱法。方法采用C18柱(150mm×4.6mm,5μm),以乙腈-水-三乙胺-冰醋酸(35∶65∶0.5∶0.25)为流动相,检测波长为282nm。结果盐酸达克罗宁的进样质量浓度在5.345～213.8μg/mL范围内与峰面积呈良好的线性关系,r=0.9999,平均回收率为99.93%,RSD为1.04%。结论该法快速、准确,可用于达克罗宁氯己定硫软膏中盐酸达克罗宁的质量控制。     

高效液相色谱法测定复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的含量

目的建立高效液相色谱法测定复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠含量的方法。方法采用高效液相色谱法。色谱柱为VP-ODS C18柱(250 mm×4.6 mm,5μm);流动相为磷酸缓冲液-乙腈(80∶20);流速:1.0 mL.min-1;测定波长:240 nm;柱温:30℃:进样:10μL。结果该方法不受处方中基质干扰。盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的线性范围分别为0.100 3~0.702 1μg(r=0.999 8,n=6),0.028 56~0.199 9μg(r=0.999 9,n=6),0.006 694~0.046 85μg(r=0.999 7,n=6),平均回收率分别为98.8%、99.0%、99.0%,RSD分别为0.97%、1.3%、0.98%(n=9)。结论该方法操作简便,灵敏度高,重现性好,可用于复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的含量测定。     

RP-HPLC法测定盐酸达克罗宁乳膏中盐酸达克罗宁的含量

目的 建立盐酸达克罗宁乳膏中盐酸达克罗宁含量的RP-HPLC法测定.方法 采用反相高效液相色谱法,使用C18柱,乙腈∶水∶三乙胺∶冰醋酸(35∶ 65∶ 0.5∶ 0.25)为流动相,检测波长:279 nm.结果 此方法线性关系良好,盐酸达克罗宁的加样回收率为99.11%,RSD为0.78%.结论 方法简便快速,分离度好,结果稳定,可用于盐酸达克罗宁乳膏的质量控制.     

复方乳酸左氧氟沙星烧伤凝胶的制备及质量控制

目的:制备复方乳酸左氧氟沙星烧伤凝胶,并建立其质量控制方法.方法:以乳酸左氧氟沙星、盐酸达克罗宁和硫酸锌为主药,以壳聚糖等为辅料制备凝胶;采用双波长紫外分光光度法测定乳酸左氧氟沙星和盐酸达克罗宁的含量,配位滴定法测定硫酸锌的含量.结果:制备的凝胶均匀细腻,分散性好;乳酸左氧氟沙星检测质量浓度在2～8 mg·L1范围内线性关系良好(r=0.999 9,n=6),平均回收率为99.79%,RSD为0.33%(n=9);盐酸达克罗宁检测质量浓度在4～16mg·L-1范围内线性关系良好(r=0.999 8,n=6),平均回收率为99.43%,RSD为0.81%(n=9).结论:本制剂组方合理,制备工艺简便可行,质量稳定可控.     

达克罗宁凝胶剂的制备与临床应用

目的制备达克罗宁凝胶剂并建立其质量控制标淮。方法拟定达克罗宁凝胶剂的处方和制备工艺;采用紫外分光光度法测定盐酸达克罗宁含量;并进行临床疗效观察。结果盐酸达克罗宁在4~20μg.mL-1范围内有良好的线性关系,r=0.999 7,平均回收率为99.85%,RSD为0.74%;临床总有效率为96%。结论制剂工艺简单,质量控制可靠,临床疗效确切。     

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.