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    • 5. 发明申请
    • AN ORAL PREPARATION HAVING IMPROVED BIOAVAILABILITY
    • 具有改善生物利用度的口头准备
    • WO2006057507A1
    • 2006-06-01
    • PCT/KR2005/003950
    • 2005-11-22
    • DONG WHA PHARM.IND.CO., LTDRYU, Jei ManCHO, Soon KiJUNG, Se HyunSEONG, Seung KyooCHO, Eun HeeAHN, Seok HoonKIM, Yun Jung
    • RYU, Jei ManCHO, Soon KiJUNG, Se HyunSEONG, Seung KyooCHO, Eun HeeAHN, Seok HoonKIM, Yun Jung
    • A61K47/30A61P19/10
    • C07D277/24A61K9/143A61K31/426
    • The present invention relates to an oral preparation of N-hydroxy-4- {5- [4- (5-isopropyl-2 -methyl- 1, 3-thiazol-4-yl)p henoxy] pentoxyl -benzamidine having improved bioavailability . More particularly, the present invention relates to an oral preparation comprising: N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-l, 3-thiazol-4- yl) phenoxy] pentoxy} -benzamidine or pharmaceutically acceptable salt thereof; and one or more carbonates selected from the group consisting of alkalimetal carbonate, alkalimetal bicarbonate and alkaline earth metal carbonate, and/or one or more disintegrants selected from the group consisting of sodium starch glycolate, carmellose calcium and croscarmellose sodium. The oral preparation according to the present invention inhibits gelation of N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-l, 3-thiazol-4-yl) p henoxy] pentoxy} -benzamidine or pharmaceutically acceptable salt thereof in the early stage of release, which increases dissolution rate and remarkably raises bioavailability.
    • 本发明涉及具有改善的生物利用度的N-羟基-4- {5- [4-(5-异丙基-2-甲基-1,3-噻唑-4-基)苯氧基]戊氧基 - 苄脒的口服制剂。 更具体地说,本发明涉及包含N-羟基-4- {5- [4-(5-异丙基-2-甲基-1,3-噻唑-4-基)苯氧基]戊氧基} - 苄脒的口服制剂 或其药学上可接受的盐; 和一种或多种选自碳酸亚烷基碳酸盐,碱金属碳酸氢盐和碱土金属碳酸盐的碳酸盐,和/或选自淀粉羟乙酸钠,羧甲纤维素钙和交联羧甲基纤维素钠的一种或多种崩解剂。 根据本发明的口服制剂抑制N-羟基-4- {5- [4-(5-异丙基-2-甲基-1,3-噻唑-4-基)苯氧基]戊氧基} - 苄脒或 其药学上可接受的盐在释放的早期阶段,其增加溶解速率并显着提高生物利用度。