【作者】 崔宝国；

【导师】 黄桂华；

【作者基本信息】 山东大学 ， 制药工程， 2007， 硕士

【摘要】 药用辅料包括多种赋形剂与添加剂，是药物制剂的基础材料和重要的组成部分，在制剂成型的发展和生产中起着很重要的作用，它不仅赋予药物一定剂型用于临床，并且与提高药物的疗效，降低毒副作用有很大的关系。此外，在常规剂型的处方设计和确定最佳处方时以及研制开发新剂型、新品种时，都离不开辅料的选择和应用。特别是近一、二十年来，由于新剂型的研究推动了新辅料的开发，新辅料的应用又促进了新剂型的发展。本文首先论述了药用辅料在药剂中的重要作用，对辅料与剂型的关系、辅料与吸收的关系以及药用辅料引起的不良反应进行综述。药物和辅料之间相互影响，辅料对药物的实际应用和疗效的发挥，起着积极的关键性的作用，其中溶剂、稀释剂、粘合剂、崩解剂、润滑剂以及土体分散载体材料的水溶性高分子材料等辅料对药物的吸收都有很大的影响。辅料并非惰性或者非活性物质，不合理的应用会引起一系列的不良反应，本文对一些辅料所引起的不良反应和对辅料在儿童用剂型设计中的注意事项进行了综述。其次论述了我国辅料在品种规格及使用频率方面、质量标准方面、检测手段方面、科研开发方面、应用研究方面以及生产经营方面和国外药用辅料的差别。通过在品种规格及使用频率上的对比，分析了国产制剂质量较进口产品差的原因；国内辅料缺乏统一的质量标准，虽然出台了《药用辅料GMP指南》，但和国外仍有很大的差距，并且检测方法单一和检测仪器落后，这就造成了辅料质量差异太大；通过对比在辅料开发和应用研究方面的特点以及药用辅料生产企业的状况，发现我国新辅料均属仿制且开发集中于传统老剂型，低水平重复开发较严重，研究的深度也不够，应用机制理论的研究则还是一片空白，有待于进一步巩固和发展，辅料生产厂家的多样化，专门的药用辅料企业过少，这就使我国药用辅料和国外有了更大的差距。再者，对药用新辅料在新药新剂型开发中的应用方面进行了综述，列举了药剂辅料在固体制剂包衣与包合物方面的应用、在控释、透皮制剂与靶向制剂中的应用、在缓控释制剂中的应用、在固体分散体与粘膜吸收剂中的应用，详细介绍了羟丙甲纤维素、微晶纤维素、聚丙烯酸树脂等几种药剂中常用的新辅料的具体应用和最新的研究进展。最后对我国药剂辅料工业的发展提出了几点建议，希望我国药用辅料生产企业不断在提高产品质量，提高自主的研究开发能力，寻找出适合国内企业发展的道路，使新型辅料不断得到开发与应用，通过产品质量和应用技术的服务提高竞争力实力，顺应生产专业化、品种系列化、应用科学化、服务优质化、市场国际化的发展趋势，使药用辅料在新药新剂型开发中发挥更大作用，以取得更佳社会效益和经济效益。更多还原

【Abstract】 The pharmaceutical are composed of various diluents bases and adjuncts, which are essential materials and important parts in pharmaceutics. They play a key role in developing dosage forms and pharmaceutical industry production. Pharmaceutical excipients can not only provide some dosage forms of drug, but also increase therapeutic effects and reduce side effects. Further, the optimization and design of formulation as well as the research and development of dosage form all depend strongly on the selection of excipients. The study of new dosage forms advances the development of new excipients in recent forty years, so they have a close relation and depend strongly on each other.This review paper discussed the important function of excipients on dosage forms, and described the relationship between excipients and absorption, and the adverse drug reactions caused by excipients as well. There is a positive correlation between drug and excipients, and the excipients play an important and positive role in applications of drugs. Some pharmaceutical excipients, such as solvent, attenuant, adhesive material, disintegrating agent, lubrication and water soluble polymer of solid dispersion, have a considerable impact on drug absorption. Adverse drug reaction could be caused by the non-rational use of some excipients, thereby; the article summarized some adverse drug reactions induced by excipients and the attention for the use of excipients in dosage form design.Comparison has been carried out between domestic and foreign excipients, including the description, usage frequency, quality standard, detecting methods, scientific research, application study and production operations.Through the contrast research on the description and usage frequency, the causes of domestic preparations inferior to foreign ones were analyzed. Although the Medical Subsidiary GMPGuide was issued, domestic excipients are scant of unified quality standards, and there is still a big gap compared with foreign ones. The detection methods for excipients are single and detecting instruments are backward, which cause a great quality discrepancy among the excipients.Through the contrast research on the application study and production operations, the paper finds that domestic excipients are all imitations, and the research is mostly concentrated traditional old dosage form and repeated at low level. Besides the research depth is not inadequate, and theoretical research of application is still blank,which need to be further investigated.Application of the excipients in dosage forms development, e.g. in the solid preparation as well as inclusion compound, sustained/controlled release preparations, transdermal and targeting drug delivery systems, solid dispersion and mucosal absorbefacient, were introduced in this review. The article also presents the applications of some new supplementary agents such as hypromellose, cellulose microcrystallisate, polyacrylic resin in detail, and the development suggestions on also were described.In the end, the paper gives some advice on the development of supplementary agents industry in China. We hope that China’s pharmaceutical excipients manufacturers will improve the product quality constantly, enhance independence innovation ability, find out for the development of domestic enterprises, and enabled new excipients continued development and application. Through the quality.control and the application of technology services, the competitiveness of strength and service competitiveness strength are hoped to be improved and enhanced. Then some measucements, e.g. specialization and multi-variety series of production, application of scientific, and quality service, international market development trends, must to be administered to enable the pharmaceutical excipients play a greater role in development of new dosage form, and achieve better social and economic benefits.更多还原