Serri Carla, de Gennaro Bruno, Quagliariello Vincenzo, Iaffaioli Rosario Vincenzo, De Rosa Giuseppe, Catalanotti Lilia, Biondi Marco, Mayol Laura
Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Piazza Pugliatti 1, Messina, Italy.
Dipartimento di Ingegneria Chimica, dei Materiali e della Produzione Industriale, Università di Napoli Federico II, Piazzale V. Tecchio 80, 80125 Napoli, Italy.
Eur J Pharm Sci. 2017 Mar 1;99:202-208. doi: 10.1016/j.ejps.2016.12.019. Epub 2016 Dec 22.
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 9h, 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.
在本研究中，通过湿法制粒实现了一种用于口服控释双氯芬酸钠（DS）的颗粒剂，DS是一种阴离子型微溶性非甾体抗炎药，使用表面改性天然沸石（SMNZ）作为辅料。沸石的表面改性通过阳离子表面活性剂实现，以便通过离子相互作用实现DS的负载，并控制药物释放机制。这些颗粒具有令人满意的剂量均匀性、适合口服剂型制造的流动性，以及由离子交换和传输动力学驱动的长达9小时的药物缓释效果。此外，所获得的颗粒剂不会引起显著的细胞毒性，还能对RAW264.7细胞产生延长的抗炎作用。考虑到天然沸石通常丰富且经济，SMNZ可被视为生产具有缓释特性颗粒剂的有吸引力的替代辅料。
