阿奇霉素滴耳液的研制及质量控制

目的:制备阿奇霉素滴耳液.方法:以阿奇霉素为主药,采用硫酸呈色分光光度法测定制剂中阿奇霉素的含量.并进行了制剂的稳定性试验和刺激性试验.结果:阿奇霉素滴耳液的平均回收率为(100.79±0.54)%.90 d内制剂中阿奇霉素含量在合格范围内,外观无明显变化.刺激性试验结果表明无明显刺激性.结论:该制剂制备工艺简单,性质稳定,质量可靠,可满足临床需求.     

眼用阿奇霉素脂质体原位凝胶的制备及体外释药行为

目的制备眼用阿奇霉素脂质体原位凝胶,并对其体外释放行为和刺激性进行考察。方法薄膜分散法制备阿奇霉素脂质体,将其分散于泊洛沙姆407(P407)中制备阿奇霉素脂质体凝胶,根据胶凝温度筛选P407浓度,双室法对该制剂的体外释药行为进行考察,荧光示踪法测定制剂眼部滞留时间,同体自身对照观察制剂的眼部刺激性。结果处方中P407最佳浓度为20%,脂质体凝胶中药物的释放明显慢于其他制剂,眼部滞留时间(28.1±5.5)min,明显长于其他三种剂型(P<0.05),且对兔眼无刺激。结论 P407原位脂质体凝胶缓释特性突出、刺激性低,适合作为阿奇霉素眼用给药载体。     

门冬氨酸阿奇霉素耳丸的制备和质量控制

目的:制备门冬氨酸阿奇霉素耳丸,并确定其质量标准.方法:以聚乙二醇 4 000为载体制备门冬氨酸阿奇霉素耳丸,用四苯硼钠滴定法测定其含量.结果:所制备的门冬氨酸阿奇霉素耳丸质量稳定,含量测定方法准确可靠.结论:本制剂治疗化脓性中耳炎,疗效确切,有临床使用价值.     

阿奇霉素原位凝胶滴眼液眼部滞留性和刺激性研究

摘要目的考察阿奇霉素原位凝胶滴眼液在家兔眼部的滞留性和刺激性。方法采用γ 闪烁扫描示踪技术,以放射强度为指标,评价制剂在眼部的滞留时间,应用Draize评分标准法考察阿奇霉素原位凝胶滴眼液单次给药和多次给药后对家兔眼部的刺激性。结果与普通滴眼液相比,阿奇霉素原位凝胶滴眼液的眼部滞留时间延长了约2.5倍,角膜刺激性评价实验表明制剂眼部相容性良好。结论阿奇霉素原位凝胶滴眼液眼部刺激性小,滞留时间长,具有广阔的研究开发前景。     

阿奇霉素乳膏的制备及质量控制

目的介绍阿奇霉素乳膏的制备及质量控制方法。方法以阿奇霉素为原料制备阿奇霉素乳膏,采用二剂量法进行含量测定及稳定性考察。结果制剂中主药阿奇霉素平均回收率为99.88%,RSD为0.28%。结论该制剂制备工艺简单、性质稳定,适用于医院制剂室配制和临床使用。     

硫磺克林霉素凝胶剂的研制及临床应用

目的:制备硫磺克林霉素凝胶剂并观察其临床应用效果。方法:以卡波姆为凝胶材料制备硫磺克林霉素凝胶剂,以碘量法、HPLC法分别测定硫磺和克林霉素含量,并以克林霉素磷酸酯凝胶作对照,观察临床疗效。结果:使用该制剂治疗300例寻常性痤疮患者,总有效率90.6%,明显高于克林霉素磷酸酯凝胶对照组。结论:该制剂配制简便,质量可控,疗效可靠。     

乳糖酸阿奇霉素阴道泡腾片的研制

目的 研制乳糖酸阿奇霉素阴道泡腾片. 方法以乳糖酸阿奇霉素为主药,选用碳酸氢钠和磷酸二氢钠作为泡腾剂,内加淀粉作为崩解剂,建立性状、鉴别、含量测定等质控方法. 结果 制备的泡腾片符合工艺要求. 以硫酸呈色分光光度法测定乳糖酸阿奇霉素阴道泡腾片的含量,平均回收率为100.28%,RSD=0.68%(n=9). 结论 该制剂制备工艺可行,测定方法简便、准确.     

克林霉素-过氧苯甲酰凝胶的制备及其急性毒性试验

目的:制备克林霉素.过氧苯甲酰凝胶并考察其急性毒性。方法:以克林霉素磷酸酯、过氧苯甲酰为主药,卡波姆- 940为主要凝胶基质制备凝胶并建立其质量控制方法;观察家兔完整皮肤及破损皮肤短时间接触克林霉素-过氧苯甲酰凝胶后所产生的毒性反应情况。结果:制备的凝胶质地均匀,粘稠度适中。在观察期内,各组动物无全身中毒及死亡情况,各项观察内容正常。结论:该制剂性质稳定,急性毒性较低。     

阿奇霉素软胶囊的制备工艺研究

目的 确定阿奇霉素软胶囊的最佳制备工艺,降低工业生产成本,缩短生产周期. 方法 采用单因素考察和正交实验设计的 方法 确定阿奇霉素软胶囊的最佳工艺. 结果 阿奇霉素软胶囊的最佳制备工艺为:阿奇霉素:聚乙二醇600=1:3,囊壳的最佳配比为明胶:甘油:水=2:1:1.5,溶胶温度为60 ℃. 相对湿度在30%～45%的环境下,并在35 ℃时鼓风干燥6～8 h. 结论 该方法制备的阿奇霉素软胶囊工艺操作可行,质量稳定,可控.     

阿奇霉素原位凝胶滴眼液的制备及体外释放机制考察

目的:研制阿奇霉素温敏原位凝胶滴眼液。方法:以凝胶基质与泪液混合前后的相变温度变化筛选适宜的处方,基于阿奇霉素与硫酸显色的原理,建立UV法测定其体外释放度,以阐明其释放机制。结果:硫酸显色方法能够准确测定阿奇霉素在泪液中的体外释放度,该原位凝胶在8 h内能稳定释放,释放机制为扩散和凝胶溶蚀共同作用。结论:与普通阿奇霉素滴眼液相比较,原位凝胶滴眼液能够达到较好的缓释效果,体外释放稳定,有广泛的应用前景。     

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.     

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.     

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.