PHARMACOKINETICS OF DICLOFENAC SODIUM FOLLOWING INTRAVENOUS AND ORAL-ADMINISTRATION

被引:250
作者
WILLIS, JV
KENDALL, MJ
FLINN, RM
THORNHILL, DP
WELLING, PG
机构
[1] UNIV BIRMINGHAM,FAC MED & DENT,DEPT CLIN PHARMACOL,BIRMINGHAM B15 2TT,W MIDLANDS,ENGLAND
[2] UNIV BIRMINGHAM,FAC MED & DENT,DEPT THERAPEUT,BIRMINGHAM B15 2TT,W MIDLANDS,ENGLAND
[3] UNIV BIRMINGHAM,FAC MED & DENT,CTR COMP STUDIES,BIRMINGHAM B15 2TT,W MIDLANDS,ENGLAND
关键词
bioavailability; diclofenac; enteric coating; intravenous bolus administration; oral administration; plasma levels;
D O I
10.1007/BF00568201
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The pharmacokinetics of diclofenac were examined following single rapid intravenous injection and also following single oral doses to healthy female volunteers. After intravenous injection plasma levels of diclofenac fell rapidly and were below the limits of detection at 5.5 h postdosing. Individual drug profiles were described by a triexponential function and mean half-lives of the three exponential phases were 0.05, 0.26 and 1.1 h. After oral doses of enteric-coated tablets, the lag time between dosing and the appearance of drug in plasma varied between 1.0 and 4.5 h. However once drug absorption had commenced similar plasma drug profiles were obtained in different individuals. Peak plasma diclofenac levels ranged from 1.4 to 3.0 μg · ml-1. The mean terminal drug half-life in plasma was 1.8 h after oral doses. This value was not significantly greater than the value of 1.1 h following intravenous doses. Fifty percent of orally dosed diclofenac did not reach the systemic circulation due, predominantly, to first-pass metabolism. © 1979 Springer-Verlag.
引用
收藏
页码:405 / 410
页数:6
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