Königsson K, Törneke K, Engeland I V, Odensvik K, Kindahl H
Department of Obstetrics and Gynaecology, Centre for Reproductive Biology in Uppsala, Uppsala, Sweden.
Acta Vet Scand. 2003;44(3-4):153-9. doi: 10.1186/1751-0147-44-153.
The pharmacokinetics and the prostaglandin (PG) synthesis inhibiting effect of flunixin were determined in 6 Norwegian dairy goats. The dose was 2.2 mg/kg body weight administered by intravenous (i.v.). intramuscular (i.m.) and oral (p.o.) routes using a cross-over design. Plasma flunixin content was analysed by use of liquid chromatography and the PG synthesis was evaluated by measuring plasma 15-ketodihydro-PGF2alpha by a radioimmuno-assay. Results are presented as median (range). The elimination half-lives (t(1/2) x lambda) were 3.6 (2.0-5.0), 3.4 (2.6-6.8) and 4.3 (3.4-6.1) h for i.v., i.m. and p.o. administration, respectively. Volume of distribution at steady state (Vd(ss)) was 0.35 (0.23-0.4 1) L/kg and clearance (CL), 110 (60-160) mL/h/kg. The plasma concentrations after oral administration showed a double-peak phenomenon with the two peaks occurring at 0.37 (0.25-1) and 3.5 (2.5-5.0) h, respectively. Both peaks were in the same order of magnitude. Bioavailability was 79 (53-112) and 58 (35%-120)% for i.m. and p.o. administration, respectively. 15-Ketodihydro-PGF2, plasma concentrations decreased after flunixin administration independent of the route of administration.
在6只挪威奶山羊身上测定了氟尼辛的药代动力学和前列腺素(PG)合成抑制作用。剂量为2.2毫克/千克体重,采用交叉设计经静脉(i.v.)、肌肉(i.m.)和口服(p.o.)途径给药。通过液相色谱分析血浆氟尼辛含量,并通过放射免疫分析法测量血浆15-酮二氢-PGF2α来评估PG合成。结果以中位数(范围)表示。静脉注射、肌肉注射和口服给药的消除半衰期(t(1/2) x lambda)分别为3.6(2.0 - 5.0)、3.4(2.6 - 6.8)和4.3(3.4 - 6.1)小时。稳态分布容积(Vd(ss))为0.35(0.23 - 0.41)升/千克,清除率(CL)为110(60 - 160)毫升/小时/千克。口服给药后的血浆浓度呈现双峰现象,两个峰分别出现在0.37(0.25 - 1)和3.5(2.5 - 5.0)小时。两个峰的大小在同一数量级。肌肉注射和口服给药的生物利用度分别为79(53 - 112)%和58(35% - 120)%。氟尼辛给药后,无论给药途径如何,血浆15-酮二氢-PGF2α浓度均下降。