Wang Xiuzhi, Wang Puxiu, Huang Chenglong, Lin Xiaoyang, Gong Haoyu, He Haibing, Cai Cuifang
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
Asian J Pharm Sci. 2017 May;12(3):266-278. doi: 10.1016/j.ajps.2016.11.003. Epub 2016 Dec 21.
Aspirin is apt to hydrolyze. In order to improve its stability, a new method has been developed involving the application of hot-melt sub- and outercoating combined with enteric aqueous coating. The main aim was to investigate the influence of these factors on the stability of ASA and understand how they work. Satisfactory storage stability were obtained when the aspirin tablet core coated with Eudragit L30D55 film was combined with glycerin monostearate (GMS) as an outercoat. Hygroscopicity testing indicated that the moisture penetrating into the tablet may result in a significant change in the physical properties of the coating film observed by scanning electron microscopy. Investigation of the compatibility between the drug and film excipients shows that the talc and methacrylic acid had a significant catalytic effect on ASA. A hypothesis was proposed that the hydrolysis of ASA enteric coated tablets (ASA-ECT) was mostly concentrated in the internal film and the interfaces between the film and tablet core. In conclusion, hot-melt coating technology is an alternative to subcoating or outercoating. Also, GMS sub-coating was a better choice for forming a stable barrier between the tablet core and the polymer coating layer, and increases the structure and chemical stability.
阿司匹林易于水解。为提高其稳定性，已开发出一种新方法，即采用热熔内包衣和外包衣结合肠溶水性包衣。主要目的是研究这些因素对阿司匹林稳定性的影响，并了解它们的作用方式。当用尤特奇L30D55薄膜包衣的阿司匹林片芯与单硬脂酸甘油酯（GMS）作为外包衣结合时，可获得令人满意的储存稳定性。吸湿试验表明，水分渗入片剂可能会导致通过扫描电子显微镜观察到的包衣膜物理性质发生显著变化。对药物与薄膜辅料之间相容性的研究表明，滑石粉和甲基丙烯酸对阿司匹林有显著的催化作用。提出了一个假设，即阿司匹林肠溶片（ASA-ECT）的水解主要集中在内膜以及膜与片芯之间的界面处。总之，热熔包衣技术是内包衣或外包衣的一种替代方法。此外，GMS内包衣是在片芯与聚合物包衣层之间形成稳定屏障的更好选择，并提高了结构和化学稳定性。
