Pharmacokinetic Properties of Single- and Multiple-Dose Pitavastatin Calcium Tablets in Healthy Chinese Volunteers
Open accessAbstract
BACKGROUND: Pitavastatin is a newly developed 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor approved for the treatment of hyperlipidemia. Pharmacokinetic properties of pitavastatin have been studied previously. OBJECTIVE: To investigate the pharmacokinetic properties of pitavastatin in healthy Chinese volunteers after single-dose and multiple-dose administration. METHODS: An open-label, randomized, single-dose and multiple-dose study was conducted in healthy Chinese volunteers. The study included 4 stages, each separated with a 5-day washout period. A randomized, 3-way crossover design was carried out in Stages 1 to 3 for the single-dose study. Eligible subjects were randomized to receive a single 1 mg, 2 mg, or 4 mg pitavastatin calcium tablet. Blood samples were obtained predose and up to 36 hours following dosing. In Stage 4 the subjects received a 2-mg pitavastatin calcium tablet once daily for 6 days. At the last day of multiple dosing, blood samples were collected predose and up to 48 hours following dosing. Plasma pitavastatin was quantified by a validated liquid chromatography tandem mass spectrometry method. Tolerability was assessed by the adverse events, physical examination, 12-lead ECG, and laboratory tests. RESULTS: Twelve volunteers (6 male and 6 female) were enrolled in the study and 11 of them completed all 4 study stages. Following a single dose of 1 mg, 2 mg, and 4 mg, the mean (SD) Tmax values were 0.63 (0.17) hours, 0.65 (0.17) hours, and 0.79 (0.36) hours, respectively; the corresponding Cmax values were 66.80 (16.32) ng/mL, 106.09 (31.59) ng/mL, and 232.91 (66.42) ng/mL, respectively. AUC0-36 values were 190.04 (38.97) ng/mL/h, 307.87 (57.94) ng/mL/h, and 785.10 (166.08) ng/mL/h, respectively, whereas t1/2 values were 10.99 (2.70) hours, 9.52 (2.58) hours, and 10.38 (4.28) hours, respectively. The AUC and Cmax showed dose proportionality after single dosing according to linear-regression analysis. In the multiple-dose study, a rapid absorption (Tmax of 0.68 [0.20] hours) and marked peak concentration of 90.99 (36.88) ng/mL were observed. AUC0-48 and AUCss were 306.28 (130.02) ng/mL/h and 256.16 (116.34) ng/mL/h, respectively. The elimination half-life after multiple dosing was significantly prolonged, which amounted to 13.31 (2.58) hours. Comparison of the pharmacokinetic parameters between the male and female groups revealed no significant differences. CONCLUSIONS: In healthy Chinese volunteers, single dosing of 1 mg, 2 mg, and 4 mg pitavastatin resulted in linear plasma pharmacokinetic properties. Compared with single dosing, multiple dosing of pitavastatin showed different distribution and elimination characteristics. Sex did not appear to affect the pharmacokinetic properties of pitavastatin. Chictr.org identifier: ChiCTR-OO-13004294.
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Pitavastatin's indication as a fluconazole adjuvant is rationally conceivable.
“Of note, pitavastatin was shown to reach a peak blood concentration of 0.23 µg/ml following a single oral dose of 4 mg, suggesting that its indication as a fluconazole adjuvant is rationally conceivable28.”
From Repurposing approach identifies pitavastatin as a potent azole chemosensitizing agent effective against azole-resistant Candida species (2020) · cites this paper as [28]
Pitavastatin reaches a peak blood concentration of 0.23 μg/ml following a single oral dose of 4 mg.
“Of note, pitavastatin was shown to reach a peak blood concentration of 0.23 µg/ml following a single oral dose of 4 mg, suggesting that its indication as a fluconazole adjuvant is rationally conceivable28.”
From Repurposing approach identifies pitavastatin as a potent azole chemosensitizing agent effective against azole-resistant Candida species (2020) · cites this paper as [28]
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- Authors
- Luo, Z., Zhang, Y., Gu, J., Feng, P., & Wang, Y.
- Affiliations
- Sichuan University (CN)
- Jilin University (CN)
- Corresponding author
- Feng, Ping
- Venue
- Current Therapeutic Research
- Publisher
- Elsevier BV
- Published
- 2015-12
- Volume
- 77
- Pages
- 52-57
- ISSN
- 0011-393X (ISSN-L)
- PMC
- PMC4460194
- OpenAlex
- W1984200018
- Cited by
- 28
- References
- 30
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 1 · 2023: 4 · 2022: 1 · 2021: 4 · 2020: 6 · 2019: 5 · 2016: 1
- FWCI
- 0.34
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Current Therapeutic Research (publishedVersion, cc-by-nc-nd)
- Europe PMC (PubMed Central) (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Keywords
- pitavastatin, pharmacokinetics, single-dose administration, repeated dosing, statins, hyperlipidemia, dose proportionality, bioavailability, Chinese volunteers, adverse events, tolerability, drug safety, tablet formulation, elimination half-life, steady-state concentration, crossover design, washout period, liquid chromatography-tandem mass spectrometry
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