Matrix system機轉製造控釋劑型藥物已廣泛被藥學界研究。以往之研究都著重在藥物劑型配方對於體外溶離之影響，然而劑型配方對於藥物在體內之表現影響則研究不多。所以本研究乃以Sulfinpyrazone為一模式藥物，以了解其由matrix錠劑中不同基質之體外溶離及體內吸收之狀況。本研究中之錠劑以濕粒法製成，錠劑中分別含有Hydroxypropylmethylcellulose (HPMC)或Glyceryl behenate (C-888)。而實驗之結果，HPMC及C-888含量較低的劑型具有較快之溶離速率，且不同基質的劑型其溶離曲線是不相同的，此結果證明體外的溶離的確會被劑型配方中的HPMC及C-888所影響。在以狗為模式動物之體內藥動試驗方面，將以含C-888為基質之Sulfinpyrazone控釋劑型與原廠（速放）製劑以動物試驗結果做比較，發現此控釋製劑具有較低之Cmax，較長之Tmax及相仿之AUC，顯示本製劑確有控釋效果，其緩釋效果並和體外緩釋溶離結果是一致的。 The major purpose of this study was to evaluate the effects of formulation variables on drug release from hydroxypropylmethylcellulose (HPMC) and glyceryl behenate(C-888) based matrix tablets. Sulfinpyrazone was used as model drug and beagle dog was used as the model animal. For the HPMC
based matrix tablets, drug release was found to be a function of HPMC concentration, with slower drug release for tablet containing higher amount of HPMC. Similar results were also observed for the C-888 based matrix tablets, i.e., drug release was also slower for tablet containing more C-888.
The animal results indicate that the in vitro and in vivo performance of model drug was correlated and the model drug can be sustained well by the C-888 based formulations.
