Cahyadi Christine, Chan Lai Wah, Heng Paul Wan Sia
GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, Singapore, Singapore.
GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, Singapore, Singapore.
Eur J Pharm Biopharm. 2015 Feb;90:30-7. doi: 10.1016/j.ejpb.2014.11.007. Epub 2014 Nov 15.
The Supercell coater was developed as an in-line small batch tablet coater which uses air-fluidization for tablet coating. Coating time is very much reduced, with improved heat and mass transfer. It was hypothesized that the quasi-continuous Supercell coating process was more suitable for the aqueous coating of tablets containing moisture-sensitive drugs. Acetylsalicylic acid (ASA) was used as the model drug in this study. The extent of ASA degradation in Supercell coating was compared against that of tablets coated using the conventional pan coater. Less than 0.3% of ASA was degraded at the end of the coating process using either coater. The extent of ASA degradation was found to be more pronounced during storage. The Supercell coated tablets exhibited comparable or smaller percentage of ASA degradation than the pan coated tablets at the end of a storage period of 6 months under accelerated stability conditions (40°C/75% RH) and 3 years under ambient conditions (25°C/50% RH). The extent and rate of ASA degradation during storage were dependent on the processing conditions employed during Supercell coating. Increase in temperature generally led to a reduction in ASA degradation, while increase in spray rate and coating level caused more degradation. Greater extent of ASA degradation was observed on the surface of pan coated tablets compared with Supercell coated tablets due to greater moisture contact and the slower and wetter coating process. Changes to the processing conditions also influenced the residual moisture content (0.55-2.86%) of the tablets. However, no direct correlation between the residual moisture content of the tablets after coating and the extent of ASA degradation during storage was found.
超级单元包衣机是作为一种在线小批量片剂包衣机开发的，它利用空气流化进行片剂包衣。包衣时间大大缩短，传热传质得到改善。据推测，准连续的超级单元包衣工艺更适合对含有对湿度敏感药物的片剂进行水性包衣。本研究中使用乙酰水杨酸（ASA）作为模型药物。将超级单元包衣中ASA的降解程度与使用传统锅式包衣机包衣的片剂进行了比较。使用任何一种包衣机在包衣过程结束时，ASA的降解率均低于0.3%。发现ASA的降解程度在储存期间更为明显。在加速稳定性条件（40°C/75%相对湿度）下储存6个月和在环境条件（25°C/50%相对湿度）下储存3年后，超级单元包衣的片剂与锅式包衣的片剂相比，ASA降解的百分比相当或更小。储存期间ASA降解的程度和速率取决于超级单元包衣过程中采用的加工条件。温度升高通常会导致ASA降解减少，而喷雾速率和包衣水平的增加会导致更多降解。与超级单元包衣的片剂相比，锅式包衣的片剂表面观察到更大程度的ASA降解，这是由于更大的水分接触以及更缓慢和更潮湿的包衣过程。加工条件的改变也会影响片剂的残留水分含量（0.55 - 2.86%）。然而，未发现包衣后片剂的残留水分含量与储存期间ASA降解程度之间存在直接相关性。
