School of Life Science and Engineering, Foshan University, Foshan, China.
Foshan Nanhai Dongfang Aolong Pharmaceutical Co., Ltd, Foshan, China.
J Vet Pharmacol Ther. 2023 Jul;46(4):257-263. doi: 10.1111/jvp.13118. Epub 2023 Mar 21.
Microdialysis is a continuous direct sampling technique used in live animals to study pharmacokinetic (PK) characteristics of drugs directly in target organs. The antibiotic tilmicosin used to treat arthritis in chickens caused by Mycoplasma synoviae. However, the PK study of tilmicosin in chicken joint has not been reported. The aim of this study was to explore the PK characteristics and penetration of tilmicosin by microdialysis incorporated with High-Performance Liquid Chromatography Mass Spectrometry (HPLC-MS/MS). An articular cavity microdialysis sampling model was established by determining in vivo and in vitro recovery results. Tilmicosin was orally administered to chickens and flow rate testing combined with retro-dialysis were used to determine tilmicosin concentration in the target synovial space. HPLC-MS/MS quantification of tilmicosin from plasma and joint dialysate indicated that recovery was negatively correlated with flow rate and the optimal perfusion rate was determined to be 1.0 μL/min. The AUC, C , MRT and t in plasma were 4.6, 3.0, 2.2 and 1.6 times higher than in the joint dialysate, respectively, but T did not significantly differ. The penetration of tilmicosin from plasma to joint (AUC /AUC ) was 0.24 and indicated tilmicosin concentration in joints was much lower than that of plasma. Microdialysis technology provides a novel technique to study pharmacokinetics directly in target tissues and our study provides a reference for the clinical use of tilmicosin for treatment of M. synoviae infections in articular cavities.
微透析是一种连续直接采样技术，用于活体动物中，以直接在靶器官中研究药物的药代动力学（PK）特征。替米考星抗生素用于治疗由滑液支原体引起的鸡关节炎。然而，替米考星在鸡关节中的 PK 研究尚未报道。本研究旨在通过微透析与高效液相色谱-质谱联用（HPLC-MS/MS）探索替米考星的 PK 特征和穿透性。通过体内和体外回收率结果确定关节腔微透析采样模型。替米考星经口服给予鸡，通过流量测试和逆行透析来确定靶关节腔中替米考星的浓度。从血浆和关节透析液中 HPLC-MS/MS 定量替米考星表明，回收率与流速呈负相关，最佳灌注速率确定为 1.0 μL/min。AUC、C、MRT 和 t 在血浆中的值分别比在关节透析液中高 4.6、3.0、2.2 和 1.6 倍，但 T 没有显著差异。替米考星从血浆到关节的穿透率（AUC/AUC）为 0.24，表明关节中替米考星的浓度远低于血浆中的浓度。微透析技术为直接在靶组织中研究药代动力学提供了一种新的技术，我们的研究为替米考星在治疗关节腔滑液支原体感染中的临床应用提供了参考。
