以Matrix system之方式製造控釋劑型藥物已被廣泛研究，先前之研究都著重在藥物劑型配方對於體外溶離之影響關係，然而劑型配方對藥物於體內表現之影響則研究不多。所以本研究乃以Nimesulide為一模式藥物，以狗為動物模式進行試驗，以瞭解matrix錠劑中HPMC 所含的量對體外溶離及體內吸收的影響及相關特性。本研究錠劑之製造是以溼粒法製成，並以IR錠劑(Immediate release)進行對照。實驗結果發現，所試驗的劑型其f1、f2顯示出並不相似，並且所含之HPMC聚合物之量較低者，有著較快之體外釋放。且其在體內具有較高之Cmax及較快之Tmax，此表示體內之藥物濃度與體外之溶離結果相關。 The oral controlled release formulations using matrix systems have been
studied extensively. Most of the studies have focused on the correlation
between formulation variable and in vitro dissolution of matrix system.
However, the effects of formulation variables on their in vivo performance
have not been fully explored.
In this study, Nimesulide was used as a model drug to illustrate how the
relative rates of in vitro dissolution/ in vivo absorption in dogs may be
affected by the HPMC concentration in the matrix tablets.
The various HPMC concentrations were used to study the matrix tablets were 20%
and 30%，and the IR formulation was used as a standard. A wet granulation
method was utilized to fabricate the matrix tablets. The results showed that
the formulation with lower HPMC concentration exhibited a faster release
rate. The lower HPMC concentration formulation showed higher
AUC、faster Tmax and higher Cmax in model animals. The in vivo result may be
reflected by their in vitro dissolution.
