替米考星(TMC),一种半合成大环内酯类抗生素,由于其广谱,在兽医学中被广泛使用,抑菌性能。经常在各种鸟类中施用,它也可能在鹅的标签外使用。该研究试图调查TMC的药代动力学,组织残留物,在鹅体内通过体内实验。这项研究涉及对15名健康成年男性的纵向开放研究,三个阶段分开一个月的冲洗期。鹅通过静脉注射TMC(IV,5mg/kg),皮下(SC,10mg/kg),和口服(PO,25mg/kg,连续五天)的路线,以特定的间隔抽取血样。还在预先指定的时间收集组织样品用于随后的分析。通过完全验证的HPLC方法定量鹅血浆中的TMC。对于PO和IV途径,将血浆浓度定量至4小时,在SC路线中长达10小时。在SC(87%)和PO(4%)途径之间观察到生物利用度的显著变化。身体提取率低至0.03,表明肝脏和肾脏消除TMC的能力最小。多次口服剂量显示没有血浆积聚,但是组织数据显示广泛的分布和长期的居住,长达120小时,尽管血浆半衰期很短,但仍具有持续的治疗效果。关于多次PO剂量,建议肝脏临时停药时间为6、7.5和8天,肌肉,和肾脏,分别,根据EMA为鸡中这些基质设定的MRL。总之,虽然在人口层面上不鼓励实际的口服给药,TMC的SC管理可能适合鹅,尽管羊群疗法不切实际。
Tilmicosin (TMC), a semi-synthetic macrolide antibiotic, is widely used in veterinary medicine due to its broad-spectrum, bacteriostatic properties. Frequently administered in various birds species, it is likely used off-label in
geese as well. The study sought to investigate TMC\'s pharmacokinetics, tissue residues, in
geese through in vivo experiments. The study involved longitudinal open studies on 15 healthy adult males, with three phases separated by one-month washout periods.
Geese were administered TMC through intravenous (IV, 5 mg/kg), subcutaneous (SC, 10 mg/kg), and oral (PO, 25 mg/kg for five consecutive days) routes, with blood samples drawn at specific intervals. Tissue samples were also collected for subsequent analysis at pre-assigned times. TMC in goose plasma was quantified by a fully validated HPLC method. Plasma concentrations were quantified up to 4 hr for the PO and IV routes, and up to 10 hr in the SC route. Significant variations in bioavailability were observed between SC (87%) and PO (4%) routes. The body extraction ratio was low at 0.03, suggesting minimal ability of the liver and kidneys to eliminate TMC. Multiple oral doses showed no plasma accumulation, but tissue data revealed extensive distribution and prolonged residence, up to 120 h, suggesting a sustained therapeutic effect despite the brief plasma half-life. Regarding the multiple PO doses, provisional withdrawal times of 6, 7.5, and 8 days were suggested for the liver, muscles, and kidneys, respectively, according to the MRL set for these matrices in chickens by EMA. In conclusion, while the practical oral administration is discouraged at the population level, SC administration of TMC may be appropriate for
geese, albeit impractical for flock therapy.