Comparison of tranexamic acid pharmacokinetics after intra-articular and intravenous administration in rabbits

• Published in: Pakistan journal of pharmaceutical sciences 2017-07, Vol.30 (4), p.1309-1316
• Main Authors: Rong, Gen-Xiang, Shen, Chen-Lin, Gui, Bin-Jie, Yin, Hao, Tang, Zhi
• Format: Article
• Language: English
• Subjects: Administration, Intravenous; Animal experimentation; Animals; Antifibrinolytic Agents - administration & dosage; Antifibrinolytic Agents - blood; Antifibrinolytic Agents - pharmacokinetics; Dosage and administration; Injections, Intra-Articular; Limit of Detection; Pharmacokinetics; Rabbits; Tranexamic acid; Tranexamic Acid - administration & dosage; Tranexamic Acid - blood; Tranexamic Acid - pharmacokinetics
• ISSN: 1011-601X

Tranexamic Acid (TXA) is commonly administered in total knee arthroplasty for reducing blood loss. There has been a growing interest in the topical use of TXA except intravenous use for prevention of bleeding in TKA. The aim of this study was to develop and validate a HPLC-MS method to detect TXA and apply to compare the pharmacokinetic profile of TXA after intravenous (IV) and topical intra-articular (IA) application of TXA at a dose of 20 mg/kg in rabbits. In order to prove intra-articular administration is better than that of intravenous administration from the point of rabbit pharmacokinetic. Two groups of rabbits (n=6/group) respectively received TXA intra-articularly or intravenously. Blood samples were collected at scheduled time. The concentration of TXA in plasma was determined by a validated HPLC-MS method. Excellent linearity was found between 0.015 and 70.0μg/ml with a lower limit of quantitation (LLOQ) of 0.015μg/ml (r>0.99); moreover, all the validation data including accuracy and precision (intra- and inter-day) were all within the required limits. The pharmacokinetic parameters in IA and IV group were: C : 30.65±3.31 VS 54.05± 6.21μg/ml (p