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首页> 外文期刊>Journal of drug delivery science and technology >A novel core-shell chronotherapeutic system for the oral administration of ketoprofen
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A novel core-shell chronotherapeutic system for the oral administration of ketoprofen

机译：酮洛芬口服的新型核壳计时治疗系统

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The aim of a chronotherapeutic medicine is to tailor drug in vivo availability to circadian rhythms of diseases in order to reduce side effects and improve patient compliance. To counteract morning symptoms of early morning pathologies, a drug delivery system able to delay ketoprofen release after oral administration has been proposed. Particles made of a pectin matrix were produced by means of prilling; core-shell systems were produced covering the drug particles with Eudragit S100 (R). The systems developed, containing different drug/polymer ratios, were fully characterized in terms of drug content, efficiency of encapsulation, morphology and drug release kinetics. The results indicated that the loading of larger amounts of drug in the feed solution led to spherical and mono-disperse beads, with high encapsulation efficiency and a reduced drug delivery in gastric simulated fluids (22%). Finally, a further delay of drug release (7.3% released in simulated gastric fluid) was achieved applying to the drug/pectin core a shell of Eudragit S100 (R) (40% w/w) a gastro-resistant polymer. This core-shell platform exploits the different characteristics of the two selected polymers, i.e. pH dependent solubility of Eudragit S100 (R) and the peculiarities of pectin, degraded slowly in alkaline environment and selectively by the intestinal microflora in vivo. (C) 2015 Elsevier B.V. All rights reserved.
机译：计时治疗药物的目的是根据疾病的昼夜节律调整药物的体内利用率，以减少副作用并改善患者依从性。为了抵消清晨病理的早晨症状，已经提出了在口服给药后能够延迟酮洛芬释放的药物递送系统。由果胶基质制成的颗粒是通过造粒生产的。用Eudragit S100（R）制备了覆盖药物颗粒的核-壳系统。所开发的系统包含不同的药物/聚合物比率，在药物含量，包封效率，形态和药物释放动力学方面已得到充分表征。结果表明，进料溶液中大量药物的装载导致球形和单分散的珠粒，具有较高的包封效率，并减少了在胃模拟液中的药物递送（22％）。最终，将药物Eudragit S100（R）（40％w / w）的一种耐胃性聚合物的外壳加到药物/果胶芯上，进一步释放了药物（在模拟胃液中释放了7.3％）。该核-壳平台利用了两种选定聚合物的不同特征，即Eudragit S100（R）的pH依赖性溶解度和果胶的特性，它们在碱性环境中缓慢降解，并在体内被肠道菌群选择性地降解。 （C）2015 Elsevier B.V.保留所有权利。

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