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Bioavailavility Section

Pharmacokinetics and bioequivalence of ezetimibe tablet in healthy Chinese subjects under fasting and fed conditions 

Guan Liu, Hegui Yan, Baodong Yuan, and Gang Li

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Volume 63 (2025) p. 38 - 46

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 63 – No. 1/2025 (38-46)

Pharmacokinetics and bioequivalence of ezetimibe tablet in healthy Chinese subjects under fasting and fed conditions 

Guan Liu, Hegui Yan, Baodong Yuan, and Gang Li

Phase I Clinical Trial Center, Wuhan Pulmonary Hospital, Wuhan Institute of Tuberculosis Prevention and Control, Wuhan, Hubei Province, China
Objective: The purpose of this study is to evaluate the pharmacokinetics (PK) parameters of an ezetimibe 10 mg (test drug) and assess its bioequivalence to the branded reference product in healthy Chinese subjects under fasting and fed conditions.
Materials and methods: A single-center, randomized, open-label, four-period, two-sequence, full replicate crossover study was conducted in 88 healthy Chinese subjects under fasting or fed conditions. Subjects received a single oral dose of 10 mg ezetimibe tablet as test or reference formulation. There was a minimum 14-day washout period between each dose. Blood samples were collected at prescribed time intervals, the plasma concentration of free ezetimibe and total ezetimibe (ezetimibe + ezetimibe glucuronide) was determined by a validated ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method. Pharmacokinetik and bioavailability parameters were estimated via non-compartmental methods. Adverse events were also recorded.
Results: 40 and 48 eligible healthy subjects were enrolled in the fasted and fed study. Under fasting state, total ezetimibe with 90% confidence intervals (CIs) of C_max, AUC_0–t, and AUC_0–∞ were 87.17% (81.99 – 92.66%), 95.98% (92.38-99.72%), and 96.04% (91.37 – 100.95%), respectively. Under fed state, total ezetimibe with 90% confidence intervals (CIs) of C_max, AUC_0–t, and AUC_0–∞ were 98.71% (90.11 – 108.13%), 98.32% (94.71 – 102.06%), and 97.90% (92.68 – 103.42%), respectively. The 90% CIs of the ratio of geometric means (GMRs) of C_max, AUC_0–t, AUC_0–∞ of the test and reference formulation in both fasting and fed conditions fell within the conventional bioequivalence criteria of 0.80 – 1.25. No severe adverse events were observed.
Conclusion: The test and reference 10-mg ezetimibe tablets were bioequivalent under fasting and fed conditions in Chinese subjects. Both preparations showed good safety and tolerability.Correspondence to:
Baodong Yuan, MD, or Gang Li, MD
Phase I Clinical Trial Center
Wuhan Pulmonary Hospital
Wuhan Institute of Tuberculosis Prevention and Control
Wuhan 430030, China
Email: [email protected]; [email protected]

Bioavailability Section

Pharmacokinetic and bioequivalence study of apremilast tablets in healthy Chinese subjects under fasting and fed conditions 

Pan Lu, Fang Yao, Jie Wang, Yingxia He, Jun Liang, Xuejia Zhai, and Guan Liu

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42.00 $

Volume 64 (2026) p. 487 - 497

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 64 – No. 9/2026 (487-497)

Pharmacokinetic and bioequivalence study of apremilast tablets in healthy Chinese subjects under fasting and fed conditions 

Pan Lu¹, Fang Yao¹, Jie Wang¹, Yingxia He¹, Jun Liang¹, Xuejia Zhai²#³, and Guan Liu¹

¹PhaseI Clinical Research Center, Wuhan Pulmonary Hospital, ²Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, and ³Hubei Province Clinical Research Center for Precision Medicine for Critical Illness, Union Hospital, Wuhan, China
Apremilast is a pioneering oral selective phosphodiesterase-4 inhibitor for the treatment of psoriasis. To evaluate and compare the pharmacokinetic properties and bioavailability of apremilast tablets manufactured by Nanjing Haijing Pharmaceutical Company (Nanjing, China) with apremilast tablets certified by Celgene Europe B.V. (Utrecht, The Netherlands), we conducted a randomized, open-label, single-dose, two-period, crossover study in healthy Chinese subjects under fasted and fed conditions. Eligible subjects were randomly assigned to receive reference or test apremilast tablets in the first treatment period and the other formulation in the second period. Serial blood samples were collected for pharmacokinetic analysis. Adverse events were recorded. A total of 28 healthy subjects were enrolled in the fasting cohort and 36 subjects in the fed cohort. The 90% confidence intervals of the geometric mean ratios of the test to reference formulations were 91.56 – 106.18% for C_max, 96.08 – 108.18% for AUC_0–t, and 96.02 – 107.67% for AUC_0–∞ in the fasting cohort, and 95.15 – 107.05% for C_max, 105.13 – 113.45% for AUC_0–t, and 104.80 – 111.91% for AUC_0–∞ in the fed cohort, all of which were within the bioequivalence range of 80.00 – 125.00%. There were no serious adverse events. The results showed that the test and reference apremilast tablets were bioequivalent and well tolerated in healthy Chinese subjects under fasting and fed conditions.Correspondence to:
Guan Liu, MD
Phase | Clinical Research Center
Wuhan Pulmonary Hospital
Wuhan, People’s Republic of China
Email: [email protected]

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