Alotaibi Hadyah Faleh, Elsamaligy Samar, Mahrous Gamal M, Bayomi Mohsen A, Mahmoud Hanaa Abdelmonem
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, Helwan University, Ain Helwan, Cairo, Egypt.
Saudi Pharm J. 2019 Mar;27(3):354-362. doi: 10.1016/j.jsps.2018.12.003. Epub 2018 Dec 7.
Diclofenac sodium (DS) a non-steroidal anti-inflammatory drug has a bitter taste and is a local stomach irritant. The aim of this study was to formulate taste masked DS orally dispersible tablets (ODTs) with targeted drug release in the intestine. Pellets of DS were designed using sugar sphere cores layered with DS followed by an enteric coat of Eudragit L100 and a second coat of Eudragit E100 for taste masking. The produced pellets had a high loading efficiency of 99.52% with diameters ranging from 493.7 to 638.9 µm. The prepared pellets were spherical with smooth surfaces on scanning electron microscopy examination. Pellets with the 12% enteric coat Eudragit L100 followed by 5% Eudragit E 100 resulted in 1.4 ± 0.5% DS release in simulated gastric fluid (SGF) and complete dissolution in simulated intestinal fluid (SIF). The pellets were then used to formulate ODTs. disintegration time of ODTs ranged from 20 ± 0.26 to 46 ± 0.27 s in simulated saliva fluid (SSF). Dissolution was less than 10% in SGF while complete drug release occurred in SIF. The release rate was higher for the optimized formulation (F12) in SIF than for the marketed product Voltaren® 25 mg tablets. The optimized ODTs formulation had a palatable highly acceptable taste.
双氯芬酸钠（DS）是一种非甾体抗炎药，有苦味且对胃部有局部刺激性。本研究的目的是制备具有肠道靶向释药功能的掩味双氯芬酸钠口腔崩解片（ODT）。采用糖球芯材包裹双氯芬酸钠制备微丸，随后依次包衣乙基纤维素（Eudragit）L100肠溶衣和Eudragit E100第二层包衣以实现掩味。制备的微丸载药效率高达99.52%，直径范围为493.7至638.9 µm。扫描电子显微镜检查显示，制备的微丸呈球形，表面光滑。包衣12% Eudragit L100肠溶衣后再包衣5% Eudragit E100的微丸在模拟胃液（SGF）中的双氯芬酸钠释放率为1.4±0.5%，在模拟肠液（SIF）中完全溶解。然后将这些微丸用于制备口腔崩解片。口腔崩解片在模拟唾液（SSF）中的崩解时间为20±0.26至46±0.27秒。在模拟胃液中溶出度小于10%，而在模拟肠液中药物完全释放。优化制剂（F12）在模拟肠液中的释放速率高于市售产品扶他林®25 mg片剂。优化后的口腔崩解片制剂口感良好，接受度高。
