In vitro hemolysis of rat erythrocytes by selenium compounds

Rat erythrocytes were incubated in vitro with various selenium compounds at 37°. Hemolysis occurred with some selenium compounds but not with corresponding sulfur analogues. Selenite induced more rapid loss of intracellular glutathione (GSH) than did selenocystine but was less hemolytic. Cystine caused neither loss of intracellular GSH nor hemolysis. Addition of GSH to the incubation medium enhanced hemolysis by selenite and selenium dioxide but inhibited hemolysis by selenocystine. Inclusion of glucose in the incubation medium also inhibited selenocystine-induced lysis of erythrocytes from both selenium-supplemented rats and selenium-deficient rats. The results suggest a relationship between the oxidation of intracellular GSH and the hemolysis by selenocystine, selenite and selenium dioxide,     

Frederick Belding Power 1853–1927: Pioneer pharmaceutical scientist

When Frederick Belding Power died in 1927, the editor of the Journal of the American Pharmaceutical Association wrote that Power was “an honor to pharmacy and an inspiration to scientists and is entitled to a place in Pharmacy’s Hall of Fame.” A year earlier, Carl Alsberg, who had succeeded Harvey Wiley as the chief of the Bureau of Chemistry (today’s Food and Drug Administration), wrote that Power performed great service in creating fundamental knowledge about medicinal plants, was a force in industry through his work with Wellcome Chemical Research Laboratories, and was an educator of first rank among scientists. In 1924, Ivor Griffith, editor of the American Journal of Pharmacy and later dean and president of the Philadelphia College of Pharmacy (PCP), reviewed Power’s publications and noted that the “extent of his work and his incalculable services to his profession may be judged by surveying this brilliant record of his scientific contributions.”     

In vivo-in vitro correlations: predicting pulmonary drug deposition from pharmaceutical aerosols

In order to answer the question "what research remains to be done?" we review the current state of the art in pharmaceutical aerosol deposition modeling and explore possible in vivo- in vitro correlations (IVIVC) linking drug deposition in the human lung to predictions made using in vitro physical airway models and in silico computer models. The use of physical replicas of portions of the respiratory tract is considered, alongside the advantages and disadvantages of the different imaging methods used to obtain their dimensions. The use of airway replicas to determine drug deposition in vitro is discussed and compared with the predictions from different empirical curve fits to long-standing in vivo deposition data for monodisperse aerosols. The use of improved computational models and three-dimensional computational fluid dynamics (CFD) to predict aerosol deposition within the respiratory tract is examined. CFD's ability to predict both drug deposition from pharmaceutical aerosol sprays and powder behavior in dry powder inhalers is examined; both were highlighted as important areas for future research. Although the authors note the abilities of current in vitro and in silico methods to predict in vivo data, a number of limitations remain. These include our present inability to either image or replicate all but the most proximal airways in sufficient spatial and temporal detail to allow full capture of the fluid and aerosol mechanics in these regions. In addition, the highly complex microscale behavior of aerosols within inhalers and the respiratory tract places extreme computational demands on in silico methods. When the complexity of variations in respiratory tract geometry is associated with additional factors such as breathing pattern, age, disease state, postural position, and patient-device interaction are all considered, it is clear that further research is required before the prediction of all aspects of inhaled pharmaceutical aerosol deposition is possible.     

In vitro pharmacodynamic properties of a fluoroquinolone pharmaceutical derivative: hydrochloride of ciprofloxacin-aluminium complex

Some in vitro pharmacodynamic properties of a new aqueous soluble ciprofloxacin (CIPX) derivative, the hydrochloride of its aluminum complex: (HCl.CIPX)(3)Al, are reported. Although (HCl.CIPX)(3)Al had the same MIC as CIPX, the minimum bactericidal activity against Escherichia coli was 2-fold higher than that of CIPX and the rate of killing was slightly delayed compared with time-kill curves obtained with CIPX. (HCl.CIPX)(3)Al showed a longer post-antibiotic effect (PAE). As pharmacodynamic properties of CIPX are not drastically affected by being complexed with aluminium, the increased aqueous compatibility of the complex remains as the main formulation factor for liquid dosage forms.     

解读《药物刺激性、过敏性和溶血性研究技术指导原则》

《药物刺激性、过敏性和溶血性研究技术指导原则》在2014年2月经国家食品药品监督管理总局正式发布。本文通过介绍修订前后主要内容的变化,结合申报资料中常见问题,重点说明试验设计中需要关注的内容。     

In vitro preclinical lead optimisation technologies (PLOTs) in pharmaceutical development

The explosion of genuine high throughput technologies has allowed large compound libraries to be screened with ever increasing biological specificity, exacerbating the problem of lead candidate selection for subsequent drug development. To avoid creating a bottleneck, compounds identified from the high throughput screens undergo lead optimisation, a medium-throughput screen which allows ranking in terms of their basic absorption, distribution, metabolism, excretion (ADME) and toxicological properties. The historical role of the preclinical scientist in the drug discovery/development continuum has been to perform ADME and toxicology studies, simply to support the regulatory submission of lead candidates. This situation is, however, changing with the development of preclinical lead optimisation technologies (Approaches to High Throughput Toxicity Screening, London, Atterwill et al., 1999) facilitating the selection of leading candidates, thereby bridging the gap between high throughput efficacy screens and traditional safety assessment programmes.     

吐温80体外溶血研究

目的 考察吐温80的体外溶血作用,为制剂生产和临床安全用药提供依据.方法在570 nm波长下,采用紫外分光光度法评价吐温80对家兔红细胞的体外溶血作用.结果吐温80可引起家兔红细胞体外溶血和红细胞形态改变.结论 吐温80具有一定的体外溶血性.     

甘油在体外的溶血特性

目的：分析甘油在体外的溶血特性,方法：将正常人的红细胞加入到含不同浓度甘同的溶液中,在没时间后测定剩余的红细胞数量,计算溶血的程度。结果：在0．9％氯化钠和5％葡萄糖等渗液中,浓度40％以下的甘油无溶血作用,80％甘油有溶血作用,在蒸馏水中,20％甘油能短暂对抗蒸馏水引起的溶血作用,在0．3％氯化钠和1．7％葡萄糖低液中,10％和20％甘油可对抗低渗溶液引起的溶血作用,结论：甘油在体内的溶血作用可能是输入大剂量甘油引起肾脏损伤所致,而不是在输注时甘油与血液接触所致。     

Recommendations and guidance for providing pharmaceutical care services during COVID-19 pandemic: A China perspective

BackgroundThe novel coronavirus pneumonia (COVID-19), which was first detected in Wuhan City, has now became a pandemic that affecting patients around the world. Particularly, the community patient population are at high risk of infection and are facing potential failure of proper medication use during the pandemic.ObjectiveTo discuss community pharmacists’ role and the content of pharmaceutical care (PC) during the novel coronavirus pandemic to promote effective prevention and control and safe drug use of the community patient population.MethodCollect and summarize the experience Chinese community pharmacies gained from providing pharmacy services during the COVID-19 outbreak, and taking patients' PC needs into consideration, analyze and discuss the methods and strategies that community pharmacies and pharmacists shall use to provide PC during the pandemic.ResultsCommunity pharmacy management teams shall support PC services by providing adequate supply of COVID-19 related medications and preventative products, following environment regulations, and providing sufficient staff trainings. Pharmacists shall use various approaches to provide PC services in drug dispensing, consulting and referrals, chronic disease management, safe use of infusions, patient education, home care guidance and psychological support to promote the COVID-19 pandemic control and ensure safe medication use of community patients during the pandemic.ConclusionPC services in communities during the COVID-19 shall possess different properties due to disease characteristics and related change in patients' need. Community pharmacies shall work as a strong supporter of patient's medication and protective equipment supply. Community pharmacists shall be prepared to provide skilled and effective PC services for community patient population to ensure medication safety and promote the overall COVID-19 pandemic control.     

In situ gelling hydrogels for pharmaceutical and biomedical applications

Since Wichterle et al. introduced hydrogels as novel materials possibly suitable for a variety of biomedical applications, hydrogel research has become a fast-developing and exciting research field. The soft and hydrophilic nature of hydrogels makes them particularly suitable as protein delivery system or as cell-entrapping scaffold in tissue engineering. Traditional hydrogels were formed by chemical crosslinking of water-soluble polymers or by polymerization (of mixtures) of water-soluble monomers. Because of incompatibility of these crosslinking methods with fragile molecules like pharmaceutical proteins and living cells, in recent years research interest has been focused on hydrogels that gel spontaneously under physiological conditions. In these systems, hydrogel formation occurs in situ, at the site of injection, without the aid of potentially toxic or denaturizing crosslinking agents. This review provides an overview of in situ gelling systems and their potential in biomedical applications. Both photopolymerizable as well as self-assembling hydrogels, based on either chemical crosslinks or physical interactions will be addressed.     

Novel Biomaterial for Transdermal Application: In vitro and In vivo Characterization

The objective of the present study was to evaluate a novel film forming biomaterial for its potential application in the preparation of unilaminate transdermal adhesive matrix systems. The biomaterial, Damar Batu (DB), was tried alone and in combination with Eudragit RL100 as a matrixing agent in the preparation of transdermal patches. Developed transdermal patches of Diltiazem hydrochloride (DH) were evaluated for thickness uniformity, weight uniformity, folding endurance and drug content. USP dissolution apparatus V was used for in vitro drug release studies. Modified Franz diffusion cell used for permeation study using excised human cadaver skin. Total 6 formulations were developed and on the basis of in vitro drug release and in vitro skin permeation profile F5 composed of DB: Eudragit RL100 (60:40) and carrying 20 %w/w DH was selected as an optimized formulation for in vivo study. The in vivo study results showed that F5 achieved the Cmax of about 269.76?±?1.52?ng/mL in 6?h and sustained the release of the drug till 24?h. The skin irritation study results proved that the novel biomaterial is non-sensitizing and non-irritating. Drug-polymer interaction study carried out to check the compatibility of drug and polymer showed the intactness of the drug in the formulation proving the compatibility of the polymer. It can be proposed from the outcome of the present study that by applying suitable adhesive layer and backing membrane, DB: Eudragit RL100 (60:40) transdermal patches can be of potential therapeutic use.