a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , China.
b School of Functional food and Wine , Shenyang Pharmaceutical University Shenyang , Shenyang , China.
Drug Dev Ind Pharm. 2019 Jun;45(6):959-967. doi: 10.1080/03639045.2019.1583756. Epub 2019 Mar 20.
In this work, aspirin (ASP) sustained granules were prepared using micro-crystal coating and hot-melt granulation, respectively. In the process of micro-crystal coating, PVP was used to form the isolation layer and then coated with either Eudragit RS/RL30D or ethyl cellulose (EC) as sustained-release layers to prepare sustained granules (the granules from this method were denoted m-cG). And in the process of hot-melt granulation, the granules were obtained with stearyl alcohol as a binder and EC as matrix material to prepare sustained granules (the granules were denoted h-mG). The in vitro release of ASP sustained-release granules was investigated by dissolution apparatus and the stability of the granules was studied. Since both methods effectively prevented the hydrolysis of ASP, the sustained granules by micro-crystal coating and hot-melt granulation were stable. However, there was a clear difference in the in vitro release of h-mG and m-cG. The h-mG was completely released in 4 h, while the m-cG with EC as sustained-release layer released 80% in 24 h and the m-cG with the Eudragit RS/RL 30 D as sustained-release layer released completely in 5 h. The results showed that micro-crystal coating was more suitable for the preparation of ASP sustained granules, and the granules with EC as sustained layer could achieve a better sustained-release effect.
在这项工作中，分别采用微丸包衣和热熔挤出造粒法制备了阿司匹林（ASP）控释颗粒。在微丸包衣过程中，采用 PVP 形成隔离层，然后分别用 Eudragit RS/RL30D 或乙基纤维素（EC）作为控释层包衣制备控释颗粒（该方法得到的颗粒表示为 m-cG）。在热熔挤出造粒过程中，以硬脂醇为粘合剂，以 EC 为基质材料制备控释颗粒（该颗粒表示为 h-mG）。采用溶出仪考察了 ASP 控释颗粒的体外释放行为，研究了颗粒的稳定性。由于两种方法均能有效阻止 ASP 的水解，因此微丸包衣和热熔挤出造粒的控释颗粒均稳定。然而，h-mG 和 m-cG 的体外释放存在明显差异。h-mG 在 4 h 内完全释放，而以 EC 为控释层的 m-cG 在 24 h 内释放 80%，以 Eudragit RS/RL 30 D 为控释层的 m-cG 在 5 h 内完全释放。结果表明，微丸包衣更适合制备 ASP 控释颗粒，以 EC 为控释层的颗粒可以达到更好的控释效果。
