Conte U, Maggi L, Torre M L, Giunchedi P, La Manna A
Department of Pharmaceutical Chemistry, University of Pavia, Italy.
Biomaterials. 1993 Oct;14(13):1017-23. doi: 10.1016/0142-9612(93)90195-8.
A new dry-coated device for the release of drug after a programmable period of time is proposed. It is intended to be used mainly in the therapy of those diseases which depend on circadian rhythms. Some core formulations, characterized by different release rates and mechanisms (containing diltiazem hydrochloride or sodium diclofenac as model drugs), were coated by compression with different polymeric barrier layers (press-coated systems). The shell formulations tested contained either gellable or erodible polymers. The dissolution profiles of uncoated cores and press-coated devices were compared. The gellable and/or erodible characteristics (properties) of the barrier formulations were also examined by means of a penetrometer. The coatings prevent drug release from the core until the polymeric shell is completely eroded or swollen. This delay in release start is not influenced by the core composition and depends only on the shell formulation. Except for the time-lag, the release kinetics of the drug contained in the core are not significantly influenced by the presence of the erodible barrier, but can be widely modulated using a swellable polymeric shell.
提出了一种新型干包衣装置，可在可编程时间段后释放药物。它主要用于治疗那些依赖昼夜节律的疾病。一些以不同释放速率和机制为特征的核心制剂（以盐酸地尔硫卓或双氯芬酸钠为模型药物）通过用不同的聚合物阻挡层进行压制包衣（压制包衣系统）。测试的外壳制剂包含可胶凝或可侵蚀的聚合物。比较了未包衣核心和压制包衣装置的溶出曲线。还通过针入度计检查了阻挡制剂的可胶凝和/或可侵蚀特性（性质）。包衣可防止药物从核心释放，直到聚合物外壳完全侵蚀或溶胀。释放开始的这种延迟不受核心组成的影响，仅取决于外壳制剂。除了时间延迟外，核心中所含药物的释放动力学不受可侵蚀阻挡层存在的显著影响，但可以使用可溶胀的聚合物外壳进行广泛调节。
