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<p>The single-pill combination of rosuvastatin and ezetimibe effectively reduces low-density lipoprotein cholesterol (LDL-C), while the pharmacokinetics of the single-pill combination of rosuvastatin and ezetimibe at a dosage of 2.5&#xa0;mg/10&#xa0;mg are seldom reported. This study aimed to evaluate the pharmacokinetics of a single-pill combination of rosuvastatin and ezetimibe (2.5&#xa0;mg/10&#xa0;mg) in healthy Chinese adult subjects. In this open-label, two-period, phase I study, 16 healthy subjects were enrolled and were administered a single-pill combination of rosuvastatin and ezetimibe (2.5&#xa0;mg/10&#xa0;mg) on day (D) 1 (single-dose period) and D14 to D23 once daily (multiple-dose period) under fasting conditions. The plasma concentrations of free ezetimibe, total ezetimibe, and rosuvastatin were determined. The pharmacokinetic parameters, including peak plasma concentration (C<sub>max</sub>), area under the curve from zero to last measurement (AUC<sub>0–t</sub>), and area under the curve from zero to infinity (AUC<sub>0–∞</sub>), were subsequently calculated. During the single-dose period, the C<sub>max</sub>, AUC<sub>0-t</sub>, and AUC<sub>0-∞</sub> were 4.7 ± 2.8&#xa0;ng/mL, 99.6 ± 40.7&#xa0;h*ng/mL, and 97.1 ± 35.9&#xa0;h*ng/mL for free ezetimibe; 59.5 ± 27.6&#xa0;ng/mL, 564.7 ± 177.3&#xa0;h*ng/mL, and 580.5 ± 190.1&#xa0;h*ng/mL for total ezetimibe; and 2.7 ± 1.3&#xa0;ng/mL, 21.8 ± 11.3&#xa0;h*ng/mL, and 23.1 ± 11.5&#xa0;h*ng/mL for rosuvastatin, respectively. During the multiple-dose period, the C was 9.0 ± 4.6&#xa0;ng/mL for free ezetimibe, 77.0 ± 30.1&#xa0;ng/mL for total ezetimibe, and 3.1 ± 1.1&#xa0;ng/mL for rosuvastatin. LDL-C reached a reduction of 37.7 ± 9.0%, 44.4 ± 8.3%, and 16.0 ± 16.3% at D20, D23, and D28, respectively, compared with its level at D13 (all <i>P</i> &lt; 0.05). The total adverse event (AE) rate was 81.3%, and all these AEs were Grade I. The single-pill combination of rosuvastatin and ezetimibe (2.5&#xa0;mg/10&#xa0;mg) indicates a steady pharmacokinetic characteristic, a good lipid-lowering effect, and a safe profile in healthy Chinese subjects.</p>

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Pharmacokinetics of a single-pill combination of rosuvastatin and ezetimibe (2.5 mg/10 mg) in healthy Chinese subjects: an open-label, two-period, phase I study

  • 期刊论文

  • 发表日期：

    2025年11月28日

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  • Ying Wang,
  • Jiaxiang Ding,
  • Dongmei Cheng,
  • Yuzhou Ding,
  • Tonghao Zhang,
  • Wang Hu,
  • Xiaoni Wang,
  • Xu Zhu,
  • Yunqiu Xie,
  • Huan Zhou

摘要

The single-pill combination of rosuvastatin and ezetimibe effectively reduces low-density lipoprotein cholesterol (LDL-C), while the pharmacokinetics of the single-pill combination of rosuvastatin and ezetimibe at a dosage of 2.5 mg/10 mg are seldom reported. This study aimed to evaluate the pharmacokinetics of a single-pill combination of rosuvastatin and ezetimibe (2.5 mg/10 mg) in healthy Chinese adult subjects. In this open-label, two-period, phase I study, 16 healthy subjects were enrolled and were administered a single-pill combination of rosuvastatin and ezetimibe (2.5 mg/10 mg) on day (D) 1 (single-dose period) and D14 to D23 once daily (multiple-dose period) under fasting conditions. The plasma concentrations of free ezetimibe, total ezetimibe, and rosuvastatin were determined. The pharmacokinetic parameters, including peak plasma concentration (Cmax), area under the curve from zero to last measurement (AUC0–t), and area under the curve from zero to infinity (AUC0–∞), were subsequently calculated. During the single-dose period, the Cmax, AUC0-t, and AUC0-∞ were 4.7 ± 2.8 ng/mL, 99.6 ± 40.7 h*ng/mL, and 97.1 ± 35.9 h*ng/mL for free ezetimibe; 59.5 ± 27.6 ng/mL, 564.7 ± 177.3 h*ng/mL, and 580.5 ± 190.1 h*ng/mL for total ezetimibe; and 2.7 ± 1.3 ng/mL, 21.8 ± 11.3 h*ng/mL, and 23.1 ± 11.5 h*ng/mL for rosuvastatin, respectively. During the multiple-dose period, the C was 9.0 ± 4.6 ng/mL for free ezetimibe, 77.0 ± 30.1 ng/mL for total ezetimibe, and 3.1 ± 1.1 ng/mL for rosuvastatin. LDL-C reached a reduction of 37.7 ± 9.0%, 44.4 ± 8.3%, and 16.0 ± 16.3% at D20, D23, and D28, respectively, compared with its level at D13 (all P < 0.05). The total adverse event (AE) rate was 81.3%, and all these AEs were Grade I. The single-pill combination of rosuvastatin and ezetimibe (2.5 mg/10 mg) indicates a steady pharmacokinetic characteristic, a good lipid-lowering effect, and a safe profile in healthy Chinese subjects.