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Volumn 16, Issue 10, 2006, Pages 2632-2636

A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors

Author keywords

Absorption; Bioavailability; Cassette dosing; Claisen Ireland rearrangement; Clearance; Dual; Inhibitor; Metalloproteinase; MMP; Oral; Pharmacokinetics; Rheumatoid arthritis; TACE; TNF ; TNF484; Trocade

Indexed keywords

CIPEMASTAT; MATRIX METALLOPROTEINASE INHIBITOR; TNF 484; TUMOR NECROSIS FACTOR ALPHA CONVERTING ENZYME INHIBITOR;

EID: 33645892563     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.02.042     Document Type: Article
Times cited : (14)

References (17)
  • 15
    • 33645877893 scopus 로고    scopus 로고
    • note
    • PK cassette-dosing in rats. The experiment was performed in conscious, fed, permanently cannulated rats kept under standard conditions. For oral administration by gavage, a mixture of ethanol (3%) and cornoil was used as a vehicle (5 mL/kg), whereas for the intravenous route compounds were administered into the femoral vein as a solution in N-methyl-2-pyrrolidone (30%) in polyethylene glycol 200 (0.5 mL/kg). Plasma samples of approximately 70 μL were collected from the femoral artery for 24 h after iv administration and for 7 h after oral dosing. iv and po administration was in the same animals with a 48 h washout period between administrations. After acetonitrile precipitation of plasma samples (25 μL), parent drug concentrations in extracts were measured using a specific HPLC/MS method. Complete details of the procedure are given as supporting information.
  • 17
    • 33645844183 scopus 로고    scopus 로고
    • note
    • 50 was determined.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.