藥物控制釋放（Controlled release）系統具有多項優點。然其製造時常因賦形劑與儲存的環境之不同，具有不同的藥物釋放特性及純度變化，進而影響製劑系統之品質。本研究乃是以美沙拉?（Mesalamine）為模式藥物，藉由耐受性試驗了解美沙拉?的化學安定性，將錠劑加入不同比例 Povidone K30 與 Sodium Starch Glycolate 製作核心錠劑後，以溶離試驗研究其對藥物釋放之影響。之後再以不同比例 Eudragit S100 與 Povidone K30 進行錠劑之膜衣包覆，以研究膜衣材質特性和溶離速率間的關係。另藉由加速安定性試驗，了解賦形劑是否對美沙拉?造成不良的影響。由以上實驗結果得知，在耐受性試驗中美沙拉?在酸、光照與加熱中較為安定，在鹼性與氧化中則較不安定。經由溶離試驗可得知，核心錠劑釋放的速度可經由不同比例的崩散劑與黏著劑達到不同核心藥物釋放速率，而以 Eudragit S100 與 Povidone K30 混和所形成的膜衣，以不同厚度或比例可達到控制藥物釋放曲線。利用加速安定性試驗分析美沙拉?在不同的儲存環境可能產生裂解狀況，並參考 ICH Q3B 得知本實驗所設計延釋劑型之化學安定性在加速安定性試驗下是符合規範的。 Controlled release system has a number of advantages, however various excipients and storage conditions might affect release characteristics as well as chemical structure integrity, and thus many affect system quality. The purpose of this study is to investigates stability of mesalamine by using forced-degradation, and then to study effects of core and coating excipients on drug release. Different percentages of povidone K30 and sodium starch glycolate were used in the core tablet. Various percentages of Eudragit S100 and Povidone K30 were coated on the core tablet to produce delayed-release formulations. The chemical stability of the coated tablet under accelerated stability condition was also evaluated. In summary, the forced degradation tests demonstrate that mesalamine is very stable in acid, UV and heat, but not stable in the base and H2O2. The dissolution results show that mesalamine release rates from core tablet can be controlled by binder and disintegrant. Different percentages and thickness of Eudragit S100 and Povidone K30 coating may control the release profile of the delayed-release formulations. By using accelerated stability condition, we can observe limited of mesalamine degradation and is acceptable according to ICH Q3B.
