Drug Design, Development and Therapy (Aug 2023)
Pharmacokinetic Study of Enteric-Coated Sustained-Release Aspirin Tablets in Healthy Chinese Participants
Abstract
Duanduan Cong,1 Wenyuan Qi,1 Xiaohui Liu,1 Xiaoyu Xu,1 Lingyun Dong,2 Wei Xue,1,* Kexin Li1,* 1Clinical Trial Center, Beijing Hospital, National Center of Gerontology, Institute of Geriatric Medicine, Chinese Academy of Medical Sciences, Beijing Key Laboratory of Drug Clinical Risk and Personalized Medication Evaluation, Beijing, People’s Republic of China; 2Beijing Yeedozencom Healthcare Science & Technology Co., Ltd, Beijing, People’s Republic of China*These authors contributed equally to this workCorrespondence: Wei Xue; Kexin Li, Clinical Trial Centre (The North Building B4), Beijing Hospital, No. 1 Dahua Road, Dongdan, Dongcheng District, Beijing, 100730, People’s Republic of China, Tel +861085133632, Email [email protected]; [email protected]: 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.Patients and Methods: 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).Results: The essential PK parameters under the three treatment conditions (ie Ec a.c., EcSr a.c. and EcSr p.c.) were as follows: Cmax, ASA: 758.38± 455.34, 222.77± 98.04 and 194.54± 61.19 ng, Tmax, ASA: 6.75(2,16), 4.5(2,11) and 8.25(5,11) h, T1/2, ASA: 0.43± 0.08, 1.44± 0.59 and 4.32± 10.04 h, AUC0-t, ASA: 1008.88± 452.27, 918.04± 238.40 and 845.55± 183.25 h·ng/mL; Cmax, SA: 6409.38± 2098.52, 2863.53± 679.73 and 2913.75± 853.27ng/mL, Tmax, SA: 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, AUC0–t, SA: 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 AUC0-t, ASA and AUC0–∞, ASA, Cmax, SA, AUC0-t, SA and AUC0–∞, SA were within the range of 80.00%– 125.00%.Conclusion: 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.Keywords: acetylsalicylic acid, salicylic acid, enteric-coated sustained-release, pharmacokinetics
