Determination of tiamulin concentration in minipig plasma by LC-MS/MS and its application in pharmacokinetic studies of different formulations
10.11665/j.issn.1000-5048.2025032501
- VernacularTitle:LC-MS/MS法测定小型猪血浆中泰妙菌素浓度及其在不同制剂药代动力学研究中的应用
- Author:
Jiahui TU
1
;
Mei GENG
;
Qingming HOU
;
Xianhai LUO
;
Zhixia QIU
;
Cong WANG
Author Information
1. 中国药科大学创新药物药代动力学评价平台, 南京 210009;山东胜利生物工程有限公司, 济宁 272000;中牧实业股份有限公司, 北京 100070
- Publication Type:Journal Article 期刊文章
- Keywords:
tiamulin;
LC-MS/MS;
minipigs;
bioavailability;
pharmacokinetics
- From:
Journal of China Pharmaceutical University
2026;57(1):54-59
- CountryChina
- Language:Chinese
-
Abstract:
The present study aimed to establish an LC-MS/MS method for the quantification of tiamulin in minipig plasma and to further conduct a pharmacokinetic comparison of different formulations. The plasma samples were extracted with acetonitrile (meloxicam as internal standard), separated on a C18 column, and quantified by multiple reaction monitoring mode (ESI+). Sanyuan minipigs were used as experimental animals. Plasma samples were collected after intravenous injection (10 mg/kg) and intragastric administration (20 mg/kg). The method showed good linearity, with intra- and inter-batch RSD of 1.00%–8.13% and RE within ±15%. The extraction recovery, matrix effect and stability of the analytical methods met the relevant requirements. Tiamulin fumarate active pharmaceutical ingredient was intravenously administered, with c0 of about (4383.73±2676.78) ng/mL, AUC0-t of about (4803.50±965.68) h·ng/mL, t1/2 of about (4.66±1.68) h, and CL of about (2.14±0.46) L/(kg·h). Three tiamulin formulations were intragastrically administered, with cmax of (552.00±328.55), (545.00±136.97) and (590.60±237.02) ng/mL, tmax of (1.47±0.68), (0.69±0.75) and (0.72±0.72) h, and F of 24.85%, 15.28% and 16.97%, respectively. The validated method meets the requirements for biological sample analysis and is applicable for the pharmacokinetic evaluation of tiamulin formulations in minipigs.
