Oral controlled release formulation of diclofenac sodium by microencapsulation with ethyl cellulose
Oral controlled release formulation of diclofenac sodium by microencapsulation with ethyl cellulose
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DOI：
10.1080/0265204021000022734
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发表时间：
2002-01
影响因子：
3.9
通讯作者：
C. Sajeev;G. Vinay;R. Archna;R. Saha
中科院分区：
文献类型：
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作者：
C. Sajeev;G. Vinay;R. Archna;R. Saha
采用不同比例的乙基纤维素（EC）作为缓释材料，制备双氯芬酸钠（DFS）微囊控释制剂，并对其缓释效果进行评价。然后将配制的微胶囊压制成片剂以获得控释口服制剂。以环己烷为溶剂，采用相分离-凝聚法制备了不同比例EC的DFS微胶囊。采用美国药典2型溶出仪（USP 2000）（桨法）在三重蒸馏水中对微囊及其片剂的物理特性、体外释放模式进行了研究。制备的微胶囊为白色、自由流动的球形，粒径为49.94-52.72 μ m。DFS从微胶囊中释放的持续时间被认为是直接成比例的EC的比例，因此，涂层厚度。所有片剂在外观、药物含量均匀度、硬度、重量变化、脆碎度和厚度均匀度方面质量良好。微囊片在三重蒸馏水中的体外释放研究表明，微囊片的释药动力学为零级，释药时间超过24 h。药物释放量（t60）与微囊中EC的比例之间具有良好的相关性.在压片微囊的情况下，t60、EC比例、片重之间以及释放速率常数（K）与EC比例之间可以建立非常好的相关性。所有制剂均高度稳定，并在各批次中具有可重现的释放动力学。
The aim of this study was to formulate and evaluate microencapsulated controlled release preparations of diclofenac sodium (DFS) using different proportions of ethyl cellulose (EC) as the retardant material to extend the release. The formulated microcapsules were then compressed into tablets to obtain controlled release oral formulations. Phase separation-coacervation technique was employed to prepare microcapsules of DFS using different proportions of EC in cyclohexane. Physical characteristics of microcapsules and their tablets, in vitro release pattern of the designed microcapsules and their tablets prepared from them were studied using USP dissolution apparatus (USP 2000) type 2 (paddle method) in triple distilled water. The prepared microcapsules were white, free flowing and spherical in shape, with the particle size varying from 49.94-52.72 #119 m. The duration of DFS release from microcapsules was found to be directly proportional to the proportion of EC and, thus, coat thickness. All tablets were of good quality with respect to appearance, drug content uniformity, hardness, weight variation, friability and thickness uniformity. In vitro release study of the tabletted microcapsules in triple distilled water showed a zero order release kinetics and extended release beyond 24 h. A good correlation was obtained between drug release (t 60) and proportion of EC in the microcapsules. In the case of tabletted microcapsules, very good correlation could be established between t 60, proportion of EC, weight of the tablets and between release rate constant (K) and proportion of EC. All the formulations were highly stable and possessed reproducible release kinetics across the batches.