药用辅料聚乙烯醇质量标准对比研究

目的 时比研究药用辅料级聚乙烯醇国内外质量标准,为其国内质量标准的提高提供参考,对进一步规范国内厂家药用级聚乙烯醇的生产、认证、检查提出意见及建议.方法 参考《中国药典》(2010版)、《美国药典》(36版)和《欧洲药典》(7.0版)及其他质量标准的要求,从溶液颜色及澄清度、砷盐、水不溶物、皂化值、水解度、残留溶剂等方面进行了研究.结果 《中国药典》(2010版)在对药用聚乙烯醇标准规定上不如国外标准,本文研究内容对国内部分标准进行了修订和补充.结论 药用辅料聚乙烯醇国内质量标准有待进一步的完善和提高.     

药用辅料蔗糖硬脂酸酯的质量标准研究

目的：修订《中华人民共和国药典》2020年版四部中蔗糖硬脂酸酯的质量标准。方法：比较国内外蔗糖硬脂酸酯质量标准,建立了HPLC法对其进行含量测定,并结合试样结果,对其分型、性状、酸值、游离蔗糖、水分、脂肪酸组成等进行增修订。结果：根据不同产品的质量和制剂中的实际应用情况,比国外药典多制订了一个分型和相应的单、二、三酯及以上多酯的限度,并对国外药典中含量测定计算公式的错误进行纠正,修订后的蔗糖硬脂酸酯质量标准已完成公示。结论：本质量标准的建立,将为蔗糖硬脂酸酯在药品中的应用提供质量保障。     

制剂企业药用辅料内控质量标准的研究

药用辅料是药物制剂的重要组成成分,药用辅料质量与成品质量息息相关,本文结合国内外药典收载情况及作者自己工作经验,浅谈药用辅料内控质量标准的制定,为药品制剂企业药用辅料内控质量标准的建立提供参考。     

药用气雾剂辅料抛射剂质量标准概述

药用气雾剂是一种特别的药物剂型,在治疗支气管哮喘、慢性阻塞性肺病等呼吸系统疾病方面具有其他剂型不可替代的优势;抛射剂是药用气雾剂中药液雾化的动力,也是溶解或分散药物的介质,作为药用气雾剂中的重要辅料,抛射剂的质量直接影响到药品的安全性和有效性。现对几类常见的药用气雾剂辅料抛射剂国内外质量标准进行概括比较,为我国药用气雾剂辅料抛射剂质量标准的制修订工作提供参考。     

药用辅料氨丁三醇质量标准研究及改进

目的：提升《中国药典》2020年版收载药用辅料氨丁三醇的质量标准。方法：比较国内外氨丁三醇质量标准，对现行药典标准中全部检验项目进行考察，并结合试验结果提出改进方案。结果：对性状中的外观和溶解度、化学反应鉴别、溶液的澄清度与颜色、有关物质及铁盐检查提出修订建议，将熔点第二法修改为第一法，解决了本品在乙醇中溶解度与现行标准规定不一致的问题。结论：本方案从安全性和规范性上提高并完善了氨丁三醇质量标准，为加强本品的质量控制和进一步修订质量标准提供理论参考。     

药用辅料黑氧化铁质量标准探讨与改进

目的:提升《中国药典》2020年版收载药用辅料黑氧化铁的质量标准.方法:参考USP43/NF38和相关文献,对药典标准已有项目进行修订,补充必要的检验项目,建立合适的方法,并进行方法验证.结果:对原标准中铅的检测方法进行了修订,建立了石墨炉原子吸收(GFAAS)测定黑氧化铁中镍的方法以及等离子体发射光谱(ICP-AES...     

关联审评制度下药用辅料质量标准浅析

目的：研究关联审评制度下药用辅料质量标准现状，帮助理解关联审评制度下药用辅料质量标准内涵和各质量标准间存在的关系。方法：详细介绍关联审评制度下药用辅料质量标准的分类及特点，着重对现行药用辅料备案管理制度和药用辅料备案标准的制定要求、状态、变更、效力和现状等进行系统归纳、阐述，同时也对药用辅料备案标准和药典标准间的关系进行了分析、探讨。结果与结论：药品辅料的质量标准是药用辅料质量的重要衡量尺度，包括药典标准、注册标准、备案标准和内控标准等，其中药用辅料药典标准是对该辅料质量控制的基本标准和门槛；关联审评新制度下产生的药用辅料备案标准是监管机构确认辅料质量的重要文件。在关联审评制度的新时期，在进一步加深对药用辅料各质量标准的内涵和关系理解的同时，一方面需要企业对其备案的药用辅料进行更加广泛、深入的研究，以便给审评人员在关联审评时提供更多的参考依据；另一方面需要监管机构持续完善我国药用辅料药典标准体系，促进国内药用辅料质量标准整体提升，有助于提高我国制剂整体质量、推进制剂创新发展。     

药用辅料管理：探究药用辅料的科学监管

药用辅料作为药物制剂的重要组成成分。它具有保护、支持、加强药品的稳定性、生物利用度或病人的顺应性,有助于药品的识别,在储存或使用期间增强药品的总体安全性和有效性等作用。然而长期以来,辅料都被视为惰性物质,它并没有得到企业和研究机构甚至监管部门的重视,直至近年的“齐二药”事件中,假辅料让“良药”变“毒药”,才使药用辅料的重要性开始被人们重视起来。国家药品监管部门也加大法规建设的力度,例如,《药用辅料注册管理办法》,《药用辅料生产质量管理规范》,《药用辅料质量标准》等系列法规的颁布,但是,目前药用辅料行业仍然存在很多问题,探究药用辅料的科学监管成为既重要又紧迫的课题。     

Managing the microbiological quality of pharmaceutical excipients

The microbiological quality of the pharmaceutical excipients used to manufacture pharmaceutical and over-the-counter drug products may significantly affect the outcome of individual processing steps and the microbiological attributes of the final drug products. Unlike active pharmaceutical ingredients, excipients are purchased from multiple suppliers and in many cases are produced for the food, cosmetics, consumer products, photographic, and paint industries and not specifically for the pharmaceutical industry, so the management of their microbiological quality is less straight- forward. This article discusses the qualification of suppliers, excipient production methods, compendial standards, regulatory controls, and microbial limits testing of excipients. Emphasis is given to risk assessment associated with pharmaceutical excipients.     

药用辅料三氯叔丁醇有关物质检查方法研究及标准制定

目的：建立三氯叔丁醇有关物质测定的气相色谱分析法,对该辅料质量标准进行修订。方法：以聚乙二醇（PEG-20M）为固定液的毛细管柱。起始温度为35℃,保持5 min,以20℃/min的速率升温至135℃并保持10 min;检测器温度为280℃;进样口温度为260℃;。检测器分别为FID（丙酮）和ECD（三氯甲烷）;进样分别采用顶空进样（丙酮）和直接进样1μL（三氯甲烷）;顶空平衡温度90℃,平衡时间为20min。结果：丙酮和三氯甲烷分别在0.5～40μg?mL-1和5～500ng?mL-1范围内峰面积与浓度呈良好的线性关系(r值分别为 0.9997和0.9995);丙酮和三氯甲烷平均回收率分别为93.9%.和106.9%,均符合方法学研究要求;按该方法对2批样品进行有关物质检查,丙酮含量分别为0.008%和0.004%,三氯甲烷含量分别为0.0008%和0.0003%,。结论：建立方法可增订入中国药典质量标准,用于三氯叔丁醇质量控制。     

辛酸钠药用辅料的制备及质量控制

目的 制备药用辅料辛酸钠.方法 以正辛酸及氢氧化钠为原料,控制反应终点pH 8～10,喷雾干燥.结果 所制辛酸钠经结构确证和质量分析,符合药用辅料要求.结论 合成方法简便易行,质量控制指标可用于工业化生产.     

The safety of pharmaceutical excipients

The most important part of a medicine as far as its weight is concerned, is constituted by its excipients, which have the important functions of guaranteeing the dosage, stability and bioavailability of the active principle. The components employed as excipients must present the characteristics required by their technological function but, as with any substance administered to man, they must also correspond to suitable safety requirements. In fact, in the past the importance of evaluating the possible adverse effects of excipients was underestimated, because their inertia and innocuity were taken for granted. The safety profile of these substances is more deeply researched as regards the toxicological aspect only if they are also employed in the food industry (anti-oxidants, sweeteners, colouring agents, etc.). Indeed, in this case, the International Toxicological Committees (among which the Joint Expert Committee on Food Additives, a mixed committee of the WHO/FAO) demand thorough studies in laboratory animals, with the intent of protecting the consumer's safety. Tackling the question of the toxicity of excipients thoroughly is not a simple matter for several reasons: the large number of substances on the market and the diversity of their chemical profiles, their sources, their technological functions, and the presence of secondary products and/or contaminants that may be the true causes of adverse effects. In this article we shall review the principal classes of excipients and their respective side effects. Then we shall proceed to their toxicological evaluation, giving examples of: (a) intrinsic toxicity, or adverse effects that may be encountered in the whole population; and (b) specific toxicity, which manifests only in people who are carriers of a transmissible disease or who are genetically predisposed, such as people with allergies and intolerances.     

药用辅料对药品安全性的影响

药用辅料和药物活性成分共同组成了我们日常使用的药品,药用辅料同药物活性成分一样全程参与了体内的吸收、分布、代谢、排泄过程,所以药用辅料的安全性直接影响到了药物制剂的安全性,本文从药用辅料本身的毒副作用、药用辅料同药物活性物质(API)的配伍禁忌、药用辅料有毒副作用的杂质以及其他引起的药品安全性问题的辅料因素等四个方面阐述了药用辅料同药品安全性的关系。     

The effects of pharmaceutical excipients on drug disposition

Many new chemical entities are poorly soluble, requiring the use of co-solvents or excipients to produce suitable intravenous formulations for early pre-clinical development studies. There is some evidence in the literature that these formulation components can have significant physiological and physicochemical effects which may alter the distribution and elimination of co-administered drugs. Such effects have the potential to influence the results of pre-clinical pharmacokinetic studies, giving a false impression of a compound's intrinsic pharmacokinetics and frustrating attempts to predict the drug's ultimate clinical pharmacokinetics. This review describes the reported effects of commonly used co-solvents and excipients on drug pharmacokinetics and on physiological systems which are likely to influence drug disposition. Such information will be useful in study design and evaluating data from pharmacokinetic experiments, so that the potential influence of formulation components can be minimised.