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由于多肽物质具有广泛的生物活性,因而是新药研制的理想起点。迄今为止应市的多肽药物为数甚少。究其原因,除许多活性多肽发现较晚外,多肽复杂的化学、生物学及药代动力学性质又使其具有许多特殊的问题。高分子量的多肽通常口服难以吸收,遇胃酶及血浆酶类不稳定且易被排泄。然而多肽药物的治疗潜力却促使人们去克服这些困难。研究多肽药物的程序通常是先选出一种多肽进行药理学研究,而后制备更有效、更稳定及选择性更强的类似物。也可能是高效及强选择性的拮抗剂。该研究的后期则主要针对研制能有效给药并能维持足够作用时间的药物—一般为口服剂,否则就有必要研制皮下或鼻腔吸收的缓释剂型。
Due to the wide range of biological activity of the polypeptide material, it is an ideal starting point for the development of new drugs. To date the market of peptide drugs is very small. The reason for this is that the complex chemical, biological and pharmacokinetic properties of peptides, in addition to the later discovery of many active peptides, have given rise to many unique problems. High molecular weight peptides are usually difficult to orally absorbed in case of peptic and plasma enzymes unstable and easily excreted. However, the therapeutic potential of peptide drugs has prompted people to overcome these difficulties. The procedure for studying peptide drugs is usually to first select a peptide for pharmacological studies and then to prepare more effective, stable and more selective analogues. It may also be an efficient and potent antagonist. The latter part of the study focused on the development of drugs that can be administered effectively and with sufficient duration of action - usually oral, or else it is necessary to develop sustained release dosage forms for subcutaneous or nasal absorption.