Abu-Basha E A, Idkaidek N M, Al-Shunnaq A F
Department of Veterinary Basic Medical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan.
Vet Res Commun. 2007 May;31(4):477-85. doi: 10.1007/s11259-006-3543-6.
A bioavailability and pharmacokinetics study of powder and liquid tilmicosin formulations was carried out in 18 healthy chickens according to a single-dose, two-period, two-sequence, crossover randomized design. The two formulations were Provitil and Pulmotil AC. Both drugs were administered to each chicken after an overnight fast on two treatment days separated by a 2-week washout period. A modified rapid and sensitive HPLC method was used for determination of tilmicosin concentrations in chicken plasma. Various pharmacokinetic parameters including area under plasma concentration-time curve (AUC(0-72)), maximum plasma concentration (C(max)), time to peak concentration (t(max)), elimination half-life (t(1/2beta)), elimination rate (k(el)), clearance (Cl(B)), mean residence time (MRT) and volume of distribution (V(d,area)) were determined for both formulations. The average means of AUC(0-72) for Provitil and Pulmotil AC were very close (24.24 +/- 3.86, 21.82 +/- 3.14 (microg x h)/ml, respectively), with no significant differences based on ANOVA. The relative bioavailability of Provitil as compared to Pulmotil AC was 111%. In addition, there were no significant differences in the C(max) (2.09 +/- 0.37, 2.12 +/- 0.40 microg/ml), tmax (3.99 +/- 0.84, 5.82 +/- 1.04 h), t(1/2beta) (47.4 +/- 9.32, 45.0 +/- 5.73 h), k(el) (0.021 +/- 0.0037, 0.022 +/- 0.0038 h(-1)), Cl(B) (19.73 +/- 3.73, 21.37 +/- 4.54ml/(min/kg)), MRT (71.20 +/- 12.87, 67.15 +/- 9.01 h) and V(d,area) (1024.8 +/- 87.5, 1009.8 +/- 79.5 ml/kg) between Pulmotil AC and Provitil, respectively. In conclusion, tilmicosin was rapidly absorbed and slowly eliminated after oral administration of single dose of tilmicosin aqueous and powder formulations. Provitil and Pulmotil AC can be used as interchangeable therapeutic agents.
根据单剂量、两周期、两序列、交叉随机设计，在18只健康鸡身上进行了替米考星粉剂和液体制剂的生物利用度和药代动力学研究。两种制剂分别为Provitil和Pulmotil AC。在两个治疗日，每只鸡在禁食过夜后给药，两个治疗日之间间隔2周的洗脱期。采用改良的快速灵敏高效液相色谱法测定鸡血浆中替米考星的浓度。测定了两种制剂的各种药代动力学参数，包括血浆浓度-时间曲线下面积（AUC(0 - 72)）、最大血浆浓度（C(max)）、达峰时间（t(max)）、消除半衰期（t(1/2β)）、消除速率（k(el)）、清除率（Cl(B)）、平均驻留时间（MRT）和分布容积（V(d,area)）。Provitil和Pulmotil AC的AUC(0 - 72)平均值非常接近（分别为24.24±3.86、21.82±3.14（μg·h）/ml），方差分析显示无显著差异。Provitil相对于Pulmotil AC的相对生物利用度为111%。此外，Pulmotil AC和Provitil之间的C(max)（2.09±0.37、2.12±0.40μg/ml）、tmax（3.99±0.84、5.82±1.04 h）、t(1/2β)（47.4±9.32、45.0±5.73 h）、k(el)（0.021±0.0037、0.022±0.0038 h⁻¹）、Cl(B)（19.73±3.73、21.37±4.54ml/(min/kg)）MRT（71.20±12.87、67.15±9.01 h）和V(d,area)（1024.8±87.5、1009.8±79.5 ml/kg）均无显著差异。总之，单剂量口服替米考星水剂和粉剂制剂后，替米考星吸收迅速，消除缓慢。Provitil和Pulmotil AC可作为可互换的治疗药物。
