Abrahams R A, Ronel S H
J Biomed Mater Res. 1975 May;9(3):355-66. doi: 10.1002/jbm.820090310.
Implantable, sustained release drug delivery devices offer benefits not obtained through oral ingestion or injection. These include delivery at a constant therapeutic rate, thus avoiding adverse intermittent and massive dose effects, as well as reliance upon patients taking their prescribed dosages. The drawbacks to their widespread acceptance have been their inability to maintain a zero-order release rate over an extended period of time and poor biocompatibility. Devices capable of satisfying these requirements have been developed and tested extensively for in vitro release of the narcotic antagonist cyclazocine. By using implant models prepared from Hydron, a hydrophilic polymer known to exhibit excellent tissue compatibility, we have found that the release rate could be precisely regulated by proper geometry, copolymer composition, concentration of ionogenic groups and cross-link density. Devices in such varied forms as capusles, barrier-film coated tablets and bulk polymerized rods have been tested in vitro for periods approaching 1 year.
可植入的缓释药物递送装置具有口服或注射给药方式所没有的优势。这些优势包括以恒定的治疗速率给药,从而避免不良的间歇性和大剂量效应,以及无需依赖患者按规定剂量服药。它们未能被广泛接受的缺点在于无法在较长时间内维持零级释放速率,以及生物相容性较差。能够满足这些要求的装置已针对麻醉拮抗剂环唑辛的体外释放进行了广泛研发和测试。通过使用由Hydron制备的植入模型(Hydron是一种已知具有优异组织相容性的亲水性聚合物),我们发现可以通过适当的几何形状、共聚物组成、离子ogenic基团的浓度和交联密度精确调节释放速率。胶囊、屏障膜包衣片和本体聚合棒等多种形式的装置已在体外进行了近1年的测试。