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Background: Cloperastine is a preferred pivotal antibechic drug, mainly used for the cough caused by respiratory diseases. Previous studies have proved that it is effective and safe in the patients. Methods: The present phase I trial was designed to evaluate the pharmacokinetics (PK), bioequivalence (BE) and safety of 10 mg cloperastine in Chinese healthy subjects after single-dose administration under the fasting and postprandial conditions. A total of 60 subjects were enrolled in either the fasting (28 subjects) or postprandial group (32 subjects). A two-cycle test was carried out with an interval of 7 days. The whole blood samples were collected for the PK and BE analysis before and after administration (0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24, 36, 48 h). The primary endpoints of the PK parameters for BE trial were the area under the plasma concentration time curve from zero to t and 72 h (AUC0-t), the maximal plasma concentration (Cmax), and the safety parameters as secondary endpoints were mainly the occurrence of adverse events (AE), vital signs, physical examination, electrocardiogram, and laboratory tests before and after the trial. Results: A total of 25 and 30 subjects in the fasting and postprandial groups completed this clinical trial, respectively. The geometric mean ratio (GMR) of test/reference (T/R) for Cmax and AUC0-72h were 102.05 % and 103.80 % in the fasting trial, respectively. And their 90% confidence interval (CI) were 93.63 %~111.22 % and 95.74 %~112.54 %, respectively. In the postprandial condition, the GMR of T/R for Cmax and AUC0-72h were 94.20 % and 98.78 %, respectively. And their 90 % CI were 87.44 %~101.49 % and 93.53 %~104.33 %, respectively. All the values were fell within the range of 80.00 %~125.00 %. Furthermore, no adverse reactions (ADR) and serious adverse events (SAE) occurred during the whole clinical trial. Conclusions: The results of this trial showed that the T and R tablets were bioequivalent under both conditions. Moreover, both preparations were tolerated well.Clinical Trial Registration: http://www.chinadrugtrials.org.cn/m_index.html, CTR20212515