Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.本發明係關於純度可為98.5－100%之二肽基肽酶IV抑制劑（本文稱作DPP－IV），其為一種能夠與特定賦形劑直接壓錠成為諸如具有所要硬度、崩解性及可接受之溶解特徵的錠劑及膠囊之固體形式劑型的高劑量藥物。DPP－IV原本並不可壓錠且因此存在調配問題。用於調配之賦形劑增強了藥物及製錠混合物的流動及緊密特性。最佳流動性有助於均一的沖模填充及重量控制。所用黏合劑確保了允許使用直接壓錠方法來壓縮DPP－IV之充分內聚特性。所產生之錠劑提供可接受之活體外溶解概況。
