Journal Article

Pharmacokinetic Study of Enteric-Coated Sustained-Release Aspirin Tablets in Healthy Chinese Participants

Cong,Duanduan, Liu,Xiaohui, Qi,Wenyuan, Xue,Wei, Li,Kexin, Xu,Xiaoyu, Dong,Lingyun

2023

Overview

To study and compare the pharmacokinetic characteristics of enteric-coated sustained-release (EcSr) aspirin tablets with enteric-coated (Ec) aspirin tablets (Bayer S.p.A) in healthy Chinese participants. In this open, randomized, single-dose, three-way, crossover study, 18 healthy participants randomly received 100 mg EcSr tablets pre-prandially (a.c.), EcSr tablets post-prandially (p.c.), or Ec tablets a.c. in each period. The concentrations of acetylsalicylic acid (ASA) and salicylic acid (SA) in plasma were determined by the LC-MS/MS method, and the pharmacokinetic parameters were calculated using WinNonlin (version 8.1). The essential PK parameters under the three treatment conditions (ie Ec a.c., EcSr a.c. and EcSr p.c.) were as follows: C : 758.38±455.34, 222.77±98.04 and 194.54±61.19 ng, T : 6.75(2,16), 4.5(2,11) and 8.25(5,11) h, T : 0.43±0.08, 1.44±0.59 and 4.32±10.04 h, AUC : 1008.88±452.27, 918.04±238.40 and 845.55±183.25 h·ng/mL; C : 6409.38±2098.52, 2863.53±679.73 and 2913.75±853.27ng/mL, T : 7.25(2,24), 10(3.5-14) and 10(7,14) h, T1/2, SA: 2.21±0.46, 2.69±0.72 and 3.51±2.06h, AUC : 29,131.41±9376.23, 27,243.97±7465.16, 27,240.25±7444.67 h·ng/mL. When taking EcSr aspirin tablets, the 90% confidence intervals of the geometric mean ratios (pre-prandial/post-prandial) of AUC and AUC , C , AUC and AUC were within the range of 80.00%-125.00%. EcSr aspirin tablets showed less inter-individual variation in release and absorption than Ec aspirin tablets, which was well reflected by comparing essential PK parameters. Furthermore, meals had no significant effect on the pharmacokinetics of EcSr aspirin tablets.

• Publisher: Informa UK Limited,Dove Medical Press Limited,Dove,Dove Medical Press
• Subject: acetylsalicylic acid / Aspirin / Aspirin - pharmacokinetics / Chromatography, Liquid / Clinical Trial Report / Cross-Over Studies / Delayed-Action Preparations - pharmacokinetics / Drug Design, Development and Therapy / East Asian People / enteric-coated sustained-release / Healthy Volunteers / Humans / pharmacokinetics / RM1-950 / Salicylates / Salicylic Acid / Tablets, Enteric-Coated - pharmacokinetics / Tandem Mass Spectrometry / Therapeutics. Pharmacology