口服缓释、控释制剂的常用技术及临床应用

Common techniques and clinical applications of oral sustained-release and controlled release formulations

背景:新型缓释、控释制剂加速药物制剂的研究速度,使得药物剂型及制剂质量不断提高。目的:分析了目前临床上常用的口服缓释、控释制剂的常用技术及临床应用情况。方法:以"缓释,控释,生物制药,药物载体,高分子材料"或"delayed release,drug delivery carrier,polymer material;controlled release"为检索词,应用计算机检索CNKI和PubMed数据库中2000-02/2011-04关于口服缓释、控释药物的相关文章。选入文章内容与高分子药用材料及缓释、控释药物制剂技术及和临床应用有关,排除重复研究。结果与结论:理想的剂型是指药物对靶部位选择性高,且能推迟必要的药效时间,迅速而完全地排泄,尽量不对其他脏器与组织产生不良反应。在缓释制剂的设计中,需要充分考虑药物的水溶性、油水分配系数、化学稳定性以及蛋白结合率等理化性质和生物学性质对缓释制剂释药行为的控制;生理因素对缓释制剂的设计,如给药部位、胃肠蠕动、首过效应、血流供应、患者疾病状态、药物作用的靶器官等也需考虑。

BACKGROUND：Newtype sustained-release and controlled release formulations accelerate the development of drug formulations. OBJECTIVE：To summarize the techniques and clinical applications of currently used oral sustained-release and controlled-release formulations. METHODS：Using ＂sustained-release,controlled-release,biopharmaceutics,drug delivery,polymer＂ in Chinese of ＂delayed release,drug delivery carrier,polymer material,contraled release＂ in Eenlish as in the title and abstracts,a computer retrieval of CNKI and PubMed database at 2000-02/2011-04 was performed for articles on oral sustained-release and controlled-release drugs. Language was limited to English and Chinese. Articles related to the polymer medicinal materials,technology and clinical application of sustained-release and controlled-release drug formulations were included,repetitive articles were excluded. RESULTS：The ideal dosage form requires a high selectivity of drugs on the target site,efficacy in delaying the necessary time,then rapidly and completely excretes,has no adverse reactions to other organs and tissues. In the design of sustained-release formulations,it need to fully consider the water-solubility of drugs,oil-water partition coefficient,chemical stability,protein binding rate and other physical and chemical properties and biological properties. Physiological factors are still important for sustained-release preparations,such as site of administration,gastrointestinal peristalsis,first-pass effect,blood supply,patient＇s disease state,target organ.