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Clinical Trial
. 2021 Jan;38(1):468-478.
doi: 10.1007/s12325-020-01542-4. Epub 2020 Nov 4.

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

Alberto Papi  1 , Andrea F D Di Stefano  2 , Milko Radicioni  3
Affiliations
Clinical Trial

Pharmacokinetics and Safety of Single and Multiple Doses of Oral N-Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study

Alberto Papi et al. Adv Ther. 2021 Jan.

Abstract

Introduction: Few studies have evaluated whether the pharmacokinetics of N-acetyl-cysteine (NAC) are different in Chinese and Caucasian individuals.

Methods: This single- and multiple-dose, single-centre, open-label, phase I clinical study was conducted in healthy adult volunteers. All participants received oral NAC 600-mg uncoated tablets, which were administered first as a single dose and, following a 48-h wash-out period, twice daily for 3 days. Blood and urine were collected after single- and multiple-dose NAC administration. Adverse event (AE) data were collected throughout the study.

Results: Fifteen Chinese and 15 Caucasian (mostly Italian) individuals (males 66.7%, mean age 36.8 years) participated in the study. Pharmacokinetic characteristics of NAC were similar in the two cohorts. Following both single- and multiple-dose administration, plasma concentration of NAC increased rapidly, reaching a peak at approximately 1.0 h. Maximum plasma concentration and extent of exposure were higher after multiple doses than after a single dose. The accumulation ratio was relatively consistent in both Chinese (mean ± standard deviation 1.5 ± 0.4) and Caucasian (1.4 ± 0.2) participants. The half-life was 15.4 h in Chinese and 18.7 h in Caucasian participants, and the fraction of NAC excreted in urine in the 36 h following administration was 3.7% in Chinese and 3.8% in Caucasian participants. Two Caucasian participants had a total of 3 AEs (headache, presyncope and dysmenorrhoea). No AEs occurred in Chinese participants.

Conclusions: The pharmacokinetic characteristics of NAC are similar in healthy Chinese and Caucasian individuals after single and repeated administration. NAC has a favourable tolerability profile.

Keywords: Caucasian; Chinese; Healthy volunteer; N-acetylcysteine; Pharmacokinetics; Phase I.

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Figures

Fig. 1
Fig. 1
Baseline-corrected plasma concentration of N-acetyl-cysteine: a Chinese participants; b Caucasian participants
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References

    1. Samuni Y, Goldstein S, Dean OM, Berk M. The chemistry and biological activities of N-acetylcysteine. Biochim Biophys Acta. 2013;1830(8):4117–4129. doi: 10.1016/j.bbagen.2013.04.016. - DOI - PubMed
    1. Sies H. Glutathione and its role in cellular functions. Free Radic Biol Med. 1999;27(9–10):916–921. doi: 10.1016/s0891-5849(99)00177-x. - DOI - PubMed
    1. Rodenstein D, DeCoster A, Gazzaniga A. Pharmacokinetics of oral acetylcysteine: absorption, binding and metabolism in patients with respiratory disorders. Clin Pharmacokinet. 1978;3(3):247–254. doi: 10.2165/00003088-197803030-00005. - DOI - PubMed
    1. Borgstrom L, Kagedal B, Paulsen O. Pharmacokinetics of N-acetylcysteine in man. Eur J Clin Pharmacol. 1986;31(2):217–222. doi: 10.1007/bf00606662. - DOI - PubMed
    1. Olsson B, Johansson M, Gabrielsson J, Bolme P. Pharmacokinetics and bioavailability of reduced and oxidized N-acetylcysteine. Eur J Clin Pharmacol. 1988;34(1):77–82. doi: 10.1007/bf01061422. - DOI - PubMed

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