摘要:
多肽药物具有相对成本低、生物活性强、毒副作用小、作用靶点专一等优点，因而被广泛使用。目前，多肽药物市场的增速是其他药物市场增速的2倍。大多数的多肽药物是通过固相肽合成技术来获得。多肽药物在合成和储存过程，容易形成相关结构杂质，如氨基酸丢失、氨基酸插入、保护基残留、氧化/还原等。很多相关结构杂质不但没有药物疗效，反而具有毒副作用。本文系统地对合成多肽药物中相关结构杂质分析进行了综述，将有助于建立相关药物质量管理规范，最终提高多肽药物质量。
Abstract:
Peptide medicines have been widely used because of the advantages of relatively low cost, high biological activity, low side effects, target specificity, etc. At present, the peptide drug market is growing twice as fast as other drug markets. Currently, most of the peptides are manufactured by solid-phase peptide synthesis. During synthesis and transportation process, related structure im-purities such as amino acid deletion, amino acid insertion, incomplete removal of protecting groups, oxidation/reduction are easily generated. Many related structure impurities don’t have therapeutic effect; on the contrary they have toxic and side effect. In the paper, the analysis of related structure impurities in synthetic peptide medicines is systematically reviewed. This will be helpful to establish related regulation on quality control of medicine and improve quality of peptide medicine.