乳糖酸阿奇霉素缓释阴道栓的研制

目的:制备乳糖酸阿奇霉素缓释阴道栓。方法:以硬脂酸聚烃氧酯(S-40)为基质,羟丙基甲基纤维素(HPMC)为缓释材料采用热熔法制备栓剂,建立了性状、鉴别、含量测定等质控方法,并进行了稳定性试验、黏膜刺激性试验。结果:以硫酸呈色分光光度法测定乳糖酸阿奇霉素的含量平均回收率为99.60%,RSD为1.96%(n=9),栓剂稳定,无变化,黏膜刺激性小。结论:该制剂制备工艺可行,性质稳定,测定方法简便准确。     

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。     

阿奇霉素滴眼剂的制备及质量控制

目的:制备阿奇霉素滴眼剂并对其质量进行控制。方法:以海藻糖为渗透压调节剂、柠檬酸为助溶剂、氢氧化钠调节pH、尼泊金乙酯为抑菌剂,制备阿奇霉素滴眼剂。采用高效液相色谱法,测定药物含量,初步考察其稳定性和家兔眼部刺激性。结果:制备的阿奇霉素滴眼剂为无色澄明液体,pH为6.7⁶.9,渗透压为0.2876.9,渗透压为0.287⁰.296 Osmol/kg,与泪液等渗,鉴别、检查项均符合《中国药典》中的相关规定;阿奇霉素检测质量浓度的线性范围为2000.296 Osmol/kg,与泪液等渗,鉴别、检查项均符合《中国药典》中的相关规定;阿奇霉素检测质量浓度的线性范围为200¹ 200μg/ml(r=0.999 8),回收率为99.15%1 200μg/ml(r=0.999 8),回收率为99.15%¹00.4%,RSD为1.047%100.4%,RSD为1.047%¹.909%;与0时比较,高温、高湿、强光、加速、长期试验下该制剂检查指标均无明显变化;该制剂对家兔眼部刺激性评分均小于1。结论:该制剂制备工艺简单可行,质量稳定可控,有效期初步预测为2年,对眼无刺激性。     

阿奇霉素凝胶的制备及质量控制

目的:制备阿奇霉素凝胶并建立质量标准.方法:研制阿奇霉素凝胶,采用硫酸呈色分光光度法测定制剂中阿奇霉素的含量.结果:阿奇霉素凝胶的平均回收率为(98.77±0.93)%.结论:该制剂制备工艺简单,性质稳定,质量可靠.     

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.     

阿奇霉素凝胶的制备及质量控制

目的：建立阿奇霉素凝胶的制备及质量控制方法。方法：用卡波姆－940作凝胶基质制备阿奇霉素凝胶。进行了酸碱度及卫生学、稳定性、透皮吸收、皮肤刺激性等试验及含量测定。结果：pH值6．5－7．5,卫生学检查符合规定，凝胶稳定无变化无刺激性，含量测定平均回收率为100．7％。结论：本方法设计合理，稳定性好，可满足临床需要。     

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。     

复方加替沙星滴耳液的制备及质量控制

目的:建立复方加替沙星滴耳液的制备及质量控制方法.方法:以甘油和乙醇为溶剂制备滴耳液,采用双波长分光光度法于263.2 nm和360.0 nm波长处测定硝酸益康唑含量,于293.0 nm波长处测定盐酸加替沙星含量,并进行稳定性、刺激性考察.结果:硝酸益康唑和盐酸加替沙星的平均回收率分别为101.0%(RSD=0.80% )和 99.8%(RSD=0.70% ).结论:本制剂制备工艺合理,质量控制方法可行.     

门冬氨酸阿奇霉素滴眼液的制备及临床应用

目的：研制门冬氨酸阿奇霉素滴眼液用于治疗各种感染性眼部疾病。方法：制定门冬氨酸阿奇霉素滴眼液的制备工艺，质量标准，考察该制剂的稳定性，刺激性和临床应用。结果：该制剂处方合理，性状稳定，临床总有效率为98％。结论：该制剂易于制备，疗效好，值得推广应用。     

复方克林霉素凝胶的研制及疗效观察

目的:研究一种治疗寻常痤疮的外用制剂处方、设计制备工艺、建立制剂的含量测定方法、并对制剂进行临床疗效观察.方法:处方中选用盐酸克林霉素和替硝唑为主药,新型药用辅料卡波姆为基质,用HPLC法测定含量,结果可靠.结果:通过临床验证认为疗效确切,无刺激性,处方配伍合理,质量可控.结论:该制剂配制、含量测定方法可靠,临床疗效较好,值得推广应用.     

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.

     

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.     

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.     

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.