药用高分子辅料做缓控释制剂辅料研究进展摘要:缓释制剂是将药物与高分子载体以物理或化学方法结合,使药物在释放介质中缓慢地非恒速释放,以便长时间保持治疗所需药物浓度而达到长效作用的一类制剂;控释制剂是药物通过控释衣膜在预定的时间内定时、定量、匀速地向外释放的一种剂型。
控释制剂除了具有缓释制剂的优点外,还拥有较缓释制剂更为平稳的血药浓度,而且控释制剂能够通过控制药物溶出的区域和时机实现药物的靶向释放和目的释放。
近些年,有一些新型高分子材料的应用和研究使缓控释制剂步入了定时、定向、定位、速效、高效、长效的精密化给药阶段。
本文围绕高分子材料在缓控释制剂中的应用重点阐述。
关键词:高分子材料、缓控释制剂、骨架Abstract: Sustained-release preparations are a type of preparation in which a drug and a macromolecular carrier are physically or chemically combined so that the drug is slowly and non-constantly released in a release medium so as to maintain a desired drug concentration for a long period of time to achieve a long-acting effect; The release preparation is a dosage form in which the drug is released to the outside by a controlled release film at a predetermined time, in a fixed amount, at a constant rate. In addition to the advantages of sustained-release preparations, controlled-release preparations have a more stable blood concentration than sustained-release preparations, and controlled-release preparations can achieve targeted release and purpose release of drugs by controlling the area and timing of drug dissolution. In recent years, the application and research of some new high-molecular materials have enabled the controlled-release preparations to enter a precise, time-dependent, targeted, fast-acting, high-efficiency, and long-lasting precision drug delivery phase. This article focuses on the application of macromolecular materials in controlled-release formulations.Keywords: Polymer materials;sustained-release preparations;skeletons1 骨架型缓控释系统骨架型缓控释系统制剂是指以一种或多种惰性固体材料作为骨架,将其与药物通过压制制成片状、颗粒状或其它形式的固形制剂。
根据其材料本身特性和微观物理结构控制制剂的释药速率不同,可将其分为不溶性骨架缓控释系统、亲水性凝胶骨架缓控释系统、微囊和微粒型控释制剂。
1.1 不溶性骨架缓控释系统不溶性骨架片的药物释放是液体穿透骨架, 将药物溶解, 然后从骨架的沟槽中扩散出来,一般适合于水溶性药物[1]。
常采用亲生物质高分子材料如无毒聚乙烯、聚氯乙烯、羟丙甲纤维素(HPMC)、聚乙烯吡咯烷酮(PVP)等作为骨架基质,结构支撑使药物填充其间,再加入丙酮等有机溶剂为润湿剂,对药剂进行制粒,压片。
骨架材料口服后不能被机体分解吸收,性质不变地从通过排遗排出体外。
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