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    • 7. 发明申请
    • PHARMACEUTICAL PREPARATIONS FOR THE CONTROLLED RELEASE OF 'beta'-LACTAM ANTIBIOTICS
    • 用于控制释放β-LACTAM抗生素的药物制剂
    • WO1998022091A1
    • 1998-05-28
    • PCT/IL1997000368
    • 1997-11-13
    • YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEMKATZHENDLER, IfatHOFFMAN, AmnonFRIEDMAN, Michael
    • YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
    • A61K09/10
    • A61K31/545A61K9/2027A61K9/205A61K9/2054A61K31/43A61K2300/00
    • The present invention relates to a pharmaceutical controlled-release oral drug delivery system comprising as active ingredient at least one beta -lactam antibiotic agent, having a specific absorption site in the small intestine in combination with a polymeric matrix, optionally further containing additional pharmaceutically acceptable constituents, wherein at least 50 % of the beta -lactam antibiotic agent are released from the matrix within from about 3 to about 4 hours from oral administration and the remainder of the pharmaceutical agent is released at a controlled rate. The drug delivery system according to the invention optionally further comprises a beta -lactamase inhibitor, preferably in combination with amoxicillin and/or amoxicillin trihydrate as the active ingredient. The polymeric matrix of the pharmaceutical controlled-release oral drug delivery system of the invention may be of hydrophilic and/or hydrophobic nature and the delivery system may further comprise pharmaceutically acceptable additive. The pharmaceutical controlled-release oral drug delivery system of the invention is preferably in dosage unit form.
    • 本发明涉及药物控释口服药物递送系统,其包含至少一种β-内酰胺抗生素作为活性成分,其在小肠中具有与聚合物基质组合的特异性吸收部位,任选地还含有另外的药学上可接受的成分 ,其中至少50%的β-内酰胺抗生素试剂在口服给药约3至约4小时内从基质释放,并且药物的其余部分以受控的速率释放。 根据本发明的药物递送系统任选地还包含β-内酰胺酶抑制剂,优选与阿莫西林和/或阿莫西林三水合物作为活性成分组合。 本发明的药物控释口服药物递送系统的聚合物基质可具有亲水性和/或疏水性质,并且递送系统还可包含药学上可接受的添加剂。 本发明的药物控释口服药物递送系统优选为剂量单位形式。