隨著控釋劑型藥物的進展，控釋圓粒以其釋藥速率受生理因素影響小、副作用少以及同時可進行多種成分的組合等特有的優點，使其受到人們的重視，成為口服控釋製劑的發展趨勢。
本研究採用Ketoprofen當模式藥物，以膜衣包覆方式製備控釋圓粒。第一階段製作藥蕊圓粒，第二階段製作藥蕊圓粒控釋膜衣。首先分別以乙基纖維素 (EC)、羥丙基纖維素 (HPC-L) 當粘合劑，將Ketoprofen噴於惰性糖蕊圓粒上；藉此了解不同粘合劑製成的藥蕊對藥物釋放的影響，並選一配方分別使用Glatt迴旋流動床顆粒機和CF顆粒機設備，製備Ketoprofen之藥芯圓粒，探討不同機器對藥蕊釋藥速率的影響。
第二階段進行控釋膜衣的包覆，以乙基纖維素為主，分別與腸溶性膜衣材質虫膠 (Shellac) 或聚甲基丙烯酸 (Eudragit L) 當致孔劑，做為控釋圓粒外表包覆的材料；並利用不同聚合物的混合比率及包覆厚薄的程度，藉由不同pH溶媒的體外溶離試驗探討包覆的材料對控釋圓粒藥物的釋放影響效應；其物性方面則利用掃描式電子顯微鏡 (SEM)觀察不同配方組成圓粒之表面結構，並經由安定性試驗來了解控釋劑型配方中聚合物的安定性，對控釋劑型藥物的釋放影響效應。另外，本研究以健康人的體內試驗探討其血中濃度對時間的關係，最高血中濃度 (C max ) ，最高血中濃度時間 (T max)，和血中藥物濃度曲線下之面積 (AUC) 等藥動參數的資料，並與速放製劑之體內吸收的參數互相比較。根據研究結果顯示本控釋圓粒於體內確實有控釋效果。 This study was aimed to evaluate the effect of formulation as well preparation methods on controlled-release pellets. Ketoprofen (a less water soluble model drug) pellet formulations based on HPC-L or EC as core binders were prepared and evaluated. Moreover, the preparation methods of core pellets using Glatt Rotar Granulators and CF-Granulator were also compared.
Then core pellets were subsequently film-coated with EC as controlled
release polymer, and the released rates were adjusted by using enteric polymers
Eudragit-L or Shellac . The effects of film thickness on dissolution rates were
assessed.
The surface of pellets was examined by scanning electron microscopy (SEM), whereas the stability of pellets were evaluated by the accelerated test as well as dissolution method.
The pharmacokinetic studies using healthy human subjects indicate that the pellets indeed demonstrate controlled-release characteristics in vivo.
