Single Ascending Dose Study to Assess Pharmacokinetic Linearity, Safety, and Tolerability of Trimetazidine - Modified Release in Healthy Human Subjects
Drug Research, ISSN: 2194-9387, Vol: 70, Issue: 10, Page: 472-477
2020
- 21Captures
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Metrics Details
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Article Description
Aim This study assessed the linearity of pharmacokinetics (PK) of trimetazidine (TMZ) modified-release tablets (indicated in adults as an add-on therapy for stable angina pectoris) and measured its renal elimination, safety, and tolerability in healthy subjects. Methods This was a randomized, open-label, single-ascending dose study in healthy subjects. Subjects were administered with a single dose of 35, 70, or 105 mg TMZ-modified release tablets (six subjects each). Pharmacokinetic evaluations and safety analysis were performed before the first dose and till 48 h post-first dose. Results Following administration of 35, 70, and 105 mg TMZ-modified release; the C (mean±SD) was 79.32 (±23.08), 153.17 (±23.08), and 199.67 (±23.08) ng/mL, the T was 5.42 (±0.49), 4.51 (±1.27), and 4.57 (±0.96) h, t was 7.75 (±1.62), 6.40 (±1.23), and 6.50 (±1.18) h, AUC was 1116.89 (±378.35), 1838.39 (±284.50), and 2504.84 (±348.35) ng.h/mL, CL was 13.70 (±2.24), 14.80 (±5.91), and 19.58 (±6.24) L·h and CL/F was 33.69 (±8.51), 38.85 (±6.15), and 42.74 (±7.10) L·h , respectively. Slope estimates for AUC , AUC , and C were less than 1. Corresponding 95% CI of the slope for the AUC parameters excluded 1, indicating that the deviation from dose-proportionality was statistically significant. Corresponding 95% CI of the slope for C included 1, indicating that the less than dose-proportional increase in C was not statistically significant. No significant adverse events were observed. Conclusion Substantial deviation from a dose-proportional increase in AUC and AUC suggested a non-linear PK for TMZ-modified release. Single dose of TMZ-modified release was well tolerated and safe.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85092119580&origin=inward; http://dx.doi.org/10.1055/a-1180-4357; http://www.ncbi.nlm.nih.gov/pubmed/32886932; http://www.thieme-connect.de/DOI/DOI?10.1055/a-1180-4357; https://dx.doi.org/10.1055/a-1180-4357; https://www.thieme-connect.de/products/ejournals/abstract/10.1055/a-1180-4357
Georg Thieme Verlag KG
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