Abstract | BACKGROUND: OBJECTIVE: The purpose of this trial was to compare the PK, BE and safety of a test 10 mg versus the reference 10 mg formulation of cloperastine under fasting and postprandial conditions in healthy Chinese volunteers. METHODS: A single-centre, randomised, open, double-cycle, self-crossover, single oral administration Phase I trial was performed in healthy Chinese volunteers. A total of 60 subjects were enrolled in either the fasting (28 subjects) or the postprandial condition (32 subjects). Subjects randomly received a single dose of the T or R preparation (10 mg dose). Plasma concentrations of cloperastine were analysed by a validated LC-MS/MS method. The primary endpoints of the PK parameters were the area under the plasma concentration-time curve from zero to 72 h (AUC0-72h), under the plasma concentration-time curve from zero to infinity (AUC0-∞) and the maximal plasma concentration (Cmax). The equivalence standard range (80.0-125.0%) was used to evaluate the BE of the two preparations. The safety parameter as secondary endpoint was mainly evaluated by the occurrence of adverse events (AEs). RESULTS: A total of 25 and 30 subjects in the fasting and postprandial conditions completed this clinical trial, respectively. The geometric mean ratio (GMR) of the T/R for the Cmax, AUC0-72h and AUC0-∞ were 102.1%, 103.8% and 104.0% in the fasting condition, respectively. In the postprandial condition, the GMR of the T/R for the Cmax, AUC0-72h and AUC0-∞ were 94.2%, 98.8% and 99.0%, respectively. All the values fell within the range (80.0-125.0%). The Cmax and AUC0-72h values of the T and R preparations in fasting and postprandial conditions were not statistically significant (P > 0.05). Furthermore, no serious adverse events (SAEs) occurred during the whole trial. CONCLUSIONS: The T and R preparations were bioequivalent under both conditions. Food has no significant effect on the absorption of cloperastine. Moreover, T and R preparations were well tolerated. The trial registration number (TRN) and date of registrations were CTR20212515, 13 October 2021.
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Authors | Hong-Yu Luo, Hui-Zhi Long, Zi-Wei Zhou, Shuo-Guo Xu, Feng-Jiao Li, Yan Cheng, Dan-Dan Wen, Ping Deng, Li-Chen Gao |
Journal | Drugs in R&D
(Drugs R D)
Vol. 22
Issue 4
Pg. 311-320
(Dec 2022)
ISSN: 1179-6901 [Electronic] New Zealand |
PMID | 36369609
(Publication Type: Randomized Controlled Trial, Clinical Trial, Phase I, Journal Article)
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Copyright | © 2022. The Author(s). |
Chemical References |
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Topics |
- Humans
- Therapeutic Equivalency
- Fasting
- Chromatography, Liquid
- Healthy Volunteers
- Tandem Mass Spectrometry
- Tablets
- China
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