The effect of food intake on the pk of rhein released from diacerein

Authors

  • Ming Huang The Second Affiliated Hospital of Soochow University, Clinical Pharmacology Laboratory https://orcid.org/0000-0003-1535-2095
  • Shun-lin Zong The Second Affiliated Hospital of Soochow University, Clinical Pharmacology Laboratory
  • Quan-ying Zhang The Second Affiliated Hospital of Soochow University, Clinical Pharmacology Laboratory

DOI:

https://doi.org/10.1590/s2175-97902019000418011

Keywords:

Diacerein capsule/pharmacokinetics, HPLC-MS/MS, High fat and calories diet

Abstract

Diacerein is a symptomatic slow-acting drug used for treating osteoarthritis. This drug is completely metabolized into the active metabolite rhein before reaching the systemic circulation. This study evaluated the effects of food on the pharmacokinetics of rhein released from diacerein in healthy Chinese subjects. This was a single-center, randomized, single-dose, open-label, two-period, cross-over study. Twentyfour healthy subjects were randomly selected to receive a single oral dose of 50 mg diacerein capsule in either fasted or fed state on two separate visits. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters were calculated using WinNonlin software. In the fasted and fed states, the main pharmacokinetic parameters of diacerein capsule were as follows: Cmax were (4471 ± 936), (3225 ± 755) ng/mL, t1/2 were (4.22 ± 0.42), (4.19 ± 1.05) h, tmax were (2.61 ± 1.25), (3.81 ± 1.29) h, AUC0-24 h were (24223 ± 4895), (24316 ± 5856) h·ng/mL, and AUC0-∞ were (24743 ± 5046), (25170 ± 6415) h·ng/mL. The absorption rate of diacerein capsule was obviously delayed by food intake but the absorption degree remained unaffected.

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Published

2021-03-02

How to Cite

Huang, M. ., Zong, S.- lin ., & Zhang, Q.- ying . (2021). The effect of food intake on the pk of rhein released from diacerein. Brazilian Journal of Pharmaceutical Sciences, 56, e18011. https://doi.org/10.1590/s2175-97902019000418011

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