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Pharmacokinetics and Pharmacodynamic Effects of Flunixin after Intravenous Intramuscular and Oral Administration to Dairy Goats

机译:氟尼辛静脉肌肉和口服给药后对奶山羊的药代动力学和药效学作用

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摘要

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-PGF2α by a radioimmuno-assay. Results are presented as median (range). The elimination half-lives (t1/2·λ) 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 (Vdss) was 0.35 (0.23–0.41) 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-PGF2α plasma concentrations decreased after flunixin administration independent of the route of administration.
机译:在6只挪威乳山羊中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 mg / kg体重,采用交叉设计通过静脉内(i.v.),肌肉内(i.m.)和口服(p.o.)途径给药。通过液相色谱法分析血浆氟尼辛含量,并通过放射免疫法测定血浆15-酮二氢-PGF2α来评估PG的合成。结果以中位数(范围)表示。 i.v. i.m.的消除半衰期(t1 / 2·λ)为3.6(2.0-5.0),3.4(2.6-6.8)和4.3(3.4-6.1)h。和p.o.行政管理。稳态分布量(Vdss)为0.35(0.23-0.41)L / kg,清除率(CL)为110(60-160)mL / h / kg。口服后的血浆浓度出现双峰现象,两个峰分别出现在0.37(0.25-1)和3.5(2.5-5.0)h处。两个峰处于相同的数量级。下午的生物利用度为79(53–112)和58(35%–120)%。和p.o.行政管理。氟尼辛给药后15-Ketodihydro-PGF2α血浆浓度降低,与给药途径无关。

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