1例肺间质纤维化合并感染患者的药学监护

摘 要 目的:探讨肺间质纤维化合并感染患者的抗菌药物选择和药学监护。方法：结合糖皮质激素类药物临床应用指导原则,分析药物治疗方案,为1例肺间质纤维化合并感染患者制订个体化药学监护计划并全程实施,同时根据治疗情况适时调整药学监护方案。结果：临床药师以糖皮质激素类药物及抗菌药物合理应用作为切入点,制定、实施药学监护方案。结论：对肺间质纤维化合并感染患者实施药学监护,可优化治疗方案,避免出现药物治疗问题及不良后果,提高药物治疗的安全性和有效性。     

药物流行病学在临床药学研究领域的可视化引文分析

摘 要 目的:针对药物流行病学在临床药学中的研究领域开展可视化引文分析。 方法：借助可视化引文分析工具HistCite,以Web of Science核心合集的科学引文索引数据库扩展版为数据源,综合运用文献计量分析、引文分析和可视化技术,分析药物流行病学在临床药学研究文献中的核心期刊和当前研究的热点,并用可视化方法展示临床药学研究的发展历史。结果：得到了Pharmacoepidemiology and Drug Safety等10种药物流行病学在临床药学领域的核心期刊,确定了药物流行病学研究的热门研究主题,并用引文编年图直观地展示药物流行病学在临床药学研究领域的发展历史和阶段。结论：药物流行病学在临床药学研究领域发展迅速,HistCite能够快速、直观地展现药物流行病学在临床药学研究领域的发展轨迹。     

非层状液晶在经皮传递系统中的应用概述

摘 要 目的：综述非层状液晶作为药物载体在经皮传递系统中的应用进展。方法: 根据国内外发表的最新文献,对非层状液晶在经皮传递系统中的作用机制以及应用进行分析与讨论。结果: 非层状液晶作为药物载体在经皮传递系统的应用越来越广泛,该载体具有增溶、包封、保护药物;促进药物渗透;提高载药量;提高药物的稳定性等作用。结论:非层状液晶作为药物经皮传递载体在医药卫生等领域具有较好的发展前景。     

临床药师参与心血管内科临床治疗实践的回顾性研究及思路探讨

目的 研究和探讨临床药师在心血管内科开展药学服务的类别和内容,为药师参与临床治疗提供思路。方法 通过统计临床用药干预建议的类别及接受率,结合病例分析临床药师参与临床工作的内容与方法。结果 临床干预建议中,非专科用药干预建议略多于专科用药,分别占53.5%和46.5%;其中非专科用药接受率比专科用药略高,为90.8%。结论 临床药师应掌握专科主要病种的治疗药物,熟悉常见合并症非专科治疗用药的使用方法,具备良好的沟通技能,以便为临床提供多种形式的药学服务,促进药物应用更加安全、有效。     

6种黄槿倍半萜类成分的衍生化改造和体外抗肿瘤活性研究

目的 对黄槿中6种天然倍半萜类成分进行衍生化改造,并对所得衍生物进行体外抗肿瘤活性评价,分析其构效关系。方法 选取各种芳胺对黄槿中发现的6种倍半萜成分进行席夫碱修饰,采用噻唑蓝(MTT)法考察合成的目标化合物对HeLa、HepG2和MCG-803细胞的体外抗增殖活性。结果 衍生改造了19个不同的倍半萜类衍生物,结合¹H-NMR、¹³C-NMR、HR-MS确定其结构,其中17个衍生物首次得到。部分衍生物表现出良好的抗肿瘤活性,苄胺基团对此类骨架化合物的结构修饰能够较好地提高其抗肿瘤活性。结论 部分衍生物表现出良好的抗肿瘤活性,特别对HepG2细胞活性有较大的提高,化合物12、22、23具有进一步研究价值。     

1例结肠癌合并静脉血栓病例临床用药分析和药学监护

目的 探讨临床药师在结肠癌合并静脉血栓患者治疗过程中发挥的个体化药学服务作用。方法 临床药师通过临床药学查房、详细的药学问诊、会诊、查阅文献和交流讨论等，参与患者抗凝治疗，抗感染治疗，对低分子肝素（LMWH）在围手术期的使用以及术后出血的原因进行分析，提出处理意见，对患者进行用药教育。结果 对结肠癌合并静脉血栓患者的治疗以及围手术期的处理应该权衡利弊进行个体化管理，同时警惕低分子肝素导致的出血性不良反应。结论 临床药师积极高效参与患者治疗过程，提供个体化药学服务，协助医师制定治疗方案，有利于抗凝药物和抗感染药物的合理、安全使用。     

1位芳基取代的青藤碱衍生物的合成和抗炎活性研究

目的 进行1位取代芳基的青藤碱衍生物的合成及体外抗炎活性研究。方法 以青藤碱为先导化合物,首先1位溴取代反应,然后通过Suzuki偶联反应对A环1位进行修饰,制得一系列取代芳基的青藤碱衍生物,所有化合物均经¹H-NMR、¹³C-NMR、MS结构确认;采用报告基因法研究青藤碱衍生物对NF-κB转录活性的影响。结果 Suzuki偶联反应得到的一系列化合物活性均优于对照药青藤碱。结论 筛选到的4f和4g可作为候选药物进行深入研究,对研发治疗风湿性关节炎药物具有重要意义。     

壳聚糖及其衍生物在药物载体中的应用

摘 要壳聚糖及其衍生物具有无毒、良好的生物相容性和可降解性、黏膜黏附性和促渗性等优点,在药物载体领域具有较为广阔的研究及应用前景。本文结合国内外最新发表的相关文献,对壳聚糖及其衍生物作为相关药物载体的应用以及作用机制进行分析讨论,并对其作为抗肿瘤药物靶向载体、缓控释药物载体、眼用药物载体、基因载体和凝胶基质的应用及研究进展进行综述。     

1例Ⅱ型血小板减少症的药学监护并文献复习

目的 探讨低分子肝素诱导的Ⅱ型血小板减少症（HIT）患者的药学服务要点,从而为临床药师参与此类患者的临床治疗提供参考。方法 临床药师对1例急性肺栓塞使用低分子肝素钠抗凝治疗导致Ⅱ型血小板减少症的患者进行用药分析及药学监护。检索近年来国内外的相关文献,并结合本病例进行相关性评价,帮助临床医生制订治疗方案。结果 急性肺栓塞患者治疗安全有效,血小板计数等指标恢复正常。结论 临床药师应用循证医学证据,充分发挥药学专业特长,积极参与临床Ⅱ型HIT患者的治疗监护,提高药物治疗的安全有效性。     

论军事药学学科体系与分类

目的 探讨军事药学学科体系与分类。方法 运用系统分析和系统结构化法,在对军事药学的学科定位、分类现状、分类思路和分类方法进行全面梳理、分析、归纳的基础上,描述军事药学学科体系。结果 军事药学学科体系可划分为军事药学基础学科、军事药学技术学科、军事药学工程学科、军事药学管理学科四大类及若干小类。结论 加强军事药学学科体系的研究将完善学科体系分类,有助于提高军事药学学科整体认知水平、推进军事药学学科的发展。     

Heparosan,a promising ‘naturally good’ polymeric conjugating vehicle for delivery of injectable therapeutics

Many therapeutics have issues with delivery due to nonoptimal pharmacokinetics and/or detrimental side effects due to their nonhuman nature. Injectable biologic drugs are one class that often needs assistance. The pharma industry has employed a variety of delivery strategies and this Editorial focuses on drug–polymer conjugates, in particular those utilizing a newly introduced system using a natural carbohydrate called heparosan. This molecule, the biosynthetic precursor to the well-known drug heparin, appears tolerated due to its ‘self’ nature as well as exhibits intrinsically favorable behavior in the bloodstream and tissues. The polysaccharide is stable in the extracellular spaces of mammals, but degraded by lysosomal enzymes following entry into the cell. Heparosan manufacture utilizes a novel synchronized, stoichiometrically controlled reaction employing a sugar-polymerizing enzyme in an aqueous buffer system that results in a quasi-monodisperse product. Heparosan is predicted to serve as a conjugating vehicle to extend the plasma half-life of biologics without liabilities of polydispersity, immunogenicity and/or unwanted accumulation in the body that are observed for other types of polymer such as PEG, hydroxyethyl starch, or poly(sialic acid).     

PIC/S实时放行检测相关要求的研究与借鉴

目的：通过分析药品检查合作计划（PIC/S）药品生产质量管理规范（GMP）指南及实时放行检测（RTRT）附录的要求,为我国制药行业实时放行检测技术的发展和应用提供思路和建议。方法：对PIC/S的GMP指南及RTRT附录进行深入研究,并结合国内外RTRT相关法规、文献,探讨RTRT在我国制药行业的可行性及对我国药品监管的启示。结果与结论：建议我国药监部门尽早对标PIC/S相关技术要求,结合参数放行的试点经验及我国制药行业发展特点,出台符合国情的RTRT指南,保障RTRT在我国制药行业落地,为我国加入PIC/S,更好地与国际接轨奠定基础。     

Redox-responsive biocompatible nanocarriers based on novel heparosan polysaccharides for intracellular anticancer drug delivery

Heparosan is a natural precursor of heparin biosynthesis in mammals. It is stable in blood circulation but can be degraded in lysosomes, showing good biocompatibility and long circulation features. So heparosan can be designed as anticancer drug carriers to increase tumor selectivity and improve the therapeutic effect. A novel redox-sensitive heparosancystamine-vitamin E succinate(KSV) micelle system was constructed for intracellular delivery of doxorubicin(DOX). Simultaneously, the redox-insensitive heparosan-adipic acid dihydrazide-vitamin E succinate copolymer(KV) was synthesized as control. DOX-loaded micelles(DOX/KSV) with an average particle size of 90–120 nm had good serum stability and redox-triggered depolymerization. In vitro drug release test showed that DOX/KSV micelles presented obvious redox-triggered release behavior compared with DOX/KV. Cytotoxicity and cell uptake were investigated using MGC80-3 tumor cells and COS7 fibroblast-like cells. The cell survival rate of blank micelles was more than 90%, and the cytotoxicity of DOX/KSV in MGC80-3 cells was higher than in COS7 cells, indicating that the carrier has better biocompatibility and less toxicity side effect. The cytotoxicity of DOX/KSV against MGC80-3 cells was significantly greater than that of free DOX and DOX/KV. Furthermore, compared with DOX/KV in MGC80-3 cells, DOX/KSV micelles uptook more anticancer drugs and then released DOX faster into the cell nucleus. The micelles were endocytosed by multiple pathways, but clathrin-mediated endocytosis was the main pathway. Therefore, heparosan polysaccharide could be a potential option as anticancer carrier for enhancing efficacy and mitigating toxicity.     

An overview of late-stage functionalization in today’s drug discovery

ABSTRACT

Introduction: Late-stage functionalization (LSF) can introduce important chemical groups in the very last steps of the synthesis. LSF has the potential to speed up the preparation of novel chemical entities and diverse chemical libraries and have a major impact on drug discovery. Functional group tolerance and mild conditions allows access to new molecules not easily accessible by conventional approaches without the need for laborious de novo chemical synthesis.

Areas Covered: A historical overview of late-stage functionalization and its applicability to drug discovery is provided. Pioneering methodologies that laid the foundations for the field are briefly covered and archetypal examples of their application to drug discovery are discussed. Novel methodologies reported in the past few years mainly stemming from the recent renaissances of photoredox catalysis and radical chemistry are reviewed and their application to drug discovery considered.

Expert opinion: It is envisioned that late-stage functionalization will improve the efficiency and efficacy of drug discovery. There is evidence of the widespread uptake of LSF by the medicinal chemistry community and it is expected that the recent and continuing endeavors of many academic laboratories and pharmaceutical companies will soon have an impact on drug development.     

药包材关联审评审批申报资料技术要求的对比分析

目的：详细解读药包材关联审评审批申报资料的技术要求。方法：通过对比分析药包材注册管理和关联审评审批两种管理模式中申报资料的技术要求,剖析新管理模式的技术特点。结果：关联审评审批管理进一步加强了药品制剂和药包材之间的联系,明确在药包材使用过程中的责任主体,极大地体现了药包材是药品的一个组成部分的重要理念,在研发、生产、质量控制、安全性等方面,对药包材与药品制剂提出了同等要求。结论：关联审评审批管理模式改革是药包材行业健康发展的巨大机遇,必将推动药包材行业水平发生质的飞跃。     

Chitosan-based nanoparticles as drug delivery systems: a review on two decades of research

Abstract

Chitosan (CS) is one of the most functional natural biopolymer widely used in the pharmaceutical field due to its biocompatibility and biodegradability. These privileges lead to its application in the synthesis of nanoparticles for the drug during the last two decades. This article gives rise to a general review of the different chitosan nanoparticles (CSNPs) preparation techniques: Ionic gelation, emulsion cross-linking, spray-drying, emulsion-droplet coalescence method, nanoprecipitation, reverse micellar method, desolvation method, modified ionic gelation with radial polymerisation and emulsion solvent diffusion, from the point of view of the methodological and mechanistic aspects involved. The physicochemical behaviour of CSNPs including drug loading, drug release, particles size, zeta potential and stability are briefly discussed. This review also directs to bring an outline of the major applications of CSNPs in drug delivery according to drug and route of administration. Finally, derivatives of CSNPs and CS nano-complexes are also discussed.     

医院药事管理信息化建设的发展

目的：探讨药事管理信息化建设对医院药学发展的促进作用。方法：以信息建设为依托,分析我院信息系统对医院药事管理工作的影响。结果：我院在药库、住院药房、门诊药房、静配中心实施信息化管理后,工作效率和质量都得到了大幅度提升,合理用药软件使检索医嘱的合理性更加准确、方便,为患者安全用药提供了药学保障。结论：医院药品合理使用信息管理平台能够及时、有效地规范临床医师的用药行为,提高医院合理用药水平和药事管理工作效率     

药用辅料行业发展现状分析与思考

目的：促进药用辅料行业健康发展,确保药品质量和用药安全。方法：回顾分析我国药品辅料的发展,结合目前国内药用辅料标准收载及药用辅料与药品关联审评对辅料的要求,分析辅料行业存在的问题,提出相关建议和对策。结果与结论：药用辅料行业发展相对落后,提高药用辅料标准,加强辅料的开发和生产应用,是确保药用辅料质量安全的有效措施。     

Oleanolic acid derivatives for pharmaceutical use: a patent review

Introduction: Oleanolic acid belongs to the pentacyclic triterpene family. In China, oleanolic acid has been used as an over the counter (OTC) hepatoprotective drug for decades. Oleanolic acid and its derivatives present a wide variety of biological activities, supporting their pharmaceutical uses for multiple diseases.

Areas covered: Representative patent publications (1971-2015) covering the preparation, pharmaceutical compositions, and medical uses of oleanolic acid and its derivatives are analyzed, with focus on their anticancer, anti-osteoporosis, anti-obesity, anti-diabetic, lipid-lowering, anti-inflammatory, antioxidant, immune-regulatory, and hepatoprotective effects. A large number of Chinese patents have been given particular attention in this review.

Expert opinion: Detailed efficacy studies are highly worth doing to undoubtedly confirm the clinical potential of oleanolic acid and its derivatives. Based on that, it would be critical to identify the key protein targets of the drugs so as to promote drug development and search for new lead compounds. Together, there is a huge potential for drug-repositioning of oleanolic acid, particularly in the areas of metabolic disease and immunological disorders.     

凸显药学服务能力的执业药师职业资格考试改革尝试

目的：通过分析普通高等学校药学专业类项下,包括临床药学专业在内的各专业毕业生参加执业药师职业资格考试成绩,观察执业药师职业资格考试内容改革与执业药师具备药学服务知识和能力的契合程度。方法：提取2020-2022年度参加药学类执业药师职业资格考试的全日制本科学历药学专业类参考人员的考试成绩,进行统计分析。结果：在药学专业科目考试中,临床药学专业参考人员的成绩显著高于药学、药物制剂、药事管理等专业参考人员的成绩。结论：执业药师职业资格考试改革后,考试内容基本实现了面向患者安全用药的转移,凸显了临床药学的知识与技能,初步满足了药品监督管理对药学服务的要求。