Surface modified zeolite-based granulates for the sustained release of diclofenac sodium

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• 作者：Carla Serri^a ; Bruno de Gennaro^b ; Vincenzo Quagliariello^c ; Rosario Vincenzo Iaffaioli^c ; Giuseppe De Rosa^d ; Lilia Catalanotti^b ; Marco Biondi^d ; ^e ; ^{mabiondi@unina.it} ; Laura Mayol^d ; ^e
• 关键词：Zeolite ; Granulation ; Diclofenac ; Sustained release ; Cells
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：1 March 2017
• 年：2017
• 卷：99
• 期：Complete
• 页码：202-208
• 全文大小：527 K
• 卷排序：99

文摘

In this study, a granulate for the oral controlled delivery of diclofenac sodium (DS), an anionic sparingly soluble nonsteroidal anti-inflammatory drug, has been realized by wet granulation, using a surface modified natural zeolite (SMNZ) as an excipient. The surface modification of the zeolite has been achieved by means of a cationic surfactant, so as to allow the loading of DS through ionic interaction and bestow a control over the drug release mechanism. The granules possessed a satisfactory dosage uniformity, a flowability suitable for an oral dosage form manufacturing, along with a sustained drug release up to 9 h, driven by both ion exchange and transport kinetics. Furthermore, the obtained granulate did not elicit a significant cytotoxicity and could also induce a prolonged anti-inflammatory effect on RAW264.7 cells. Taking also into account that natural zeolites are generally abundant and economic, SMNZ can be considered as an attracting alternative excipient for the production of granules with sustained release features.