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Determination of chidamide in rat plasma and cerebrospinal fluid.
- Source :
-
Regulatory toxicology and pharmacology : RTP [Regul Toxicol Pharmacol] 2018 Oct; Vol. 98, pp. 24-30. Date of Electronic Publication: 2018 Jul 06. - Publication Year :
- 2018
-
Abstract
- Chidamide is a new subtype-selective histone deacetylase inhibitor (HDACi), which has been approved for the treatment of recurrent or refractory peripheral T-cell lymphoma (PTCL) in China. However, there are few studies about the application of chidamide in PTCL with central nervous system (CNS) involvement. It is essential to investigate the penetration of chidamide in the blood brain barrier (BBB). LC-MS methods were established firstly to determine the concentration of chidamide in rat plasma and CSF. Then five rats were anaesthetized and the plasma and CSF samples were collected at the time of 5, 15, 30, 60, 120, 180, 240, 360 and 480 min after being administered 1 mg/kg chidamide by intravenous injection, respectively. All samples were analyzed with the established LC-MS method by using the precursor/product transitions (m/z) of 391.1/265.1 for chidamide and 441.1/138.2 for internal standard (IS). The PK parameters were calculated after both of the concentrations of chidamide in plasma and CSF were determined. The penetration ratio of chidamide in BBB ranged from 0.19% to 0.67%. Result indicated chidamide could pass through the BBB, enter into the CNS and have the potential to be utilized in PTCL with CNS involvement.<br /> (Copyright © 2018 Elsevier Inc. All rights reserved.)
- Subjects :
- Aminopyridines pharmacokinetics
Animals
Antineoplastic Agents pharmacokinetics
Benzamides pharmacokinetics
Histone Deacetylase Inhibitors pharmacokinetics
Male
Rats, Sprague-Dawley
Aminopyridines blood
Aminopyridines cerebrospinal fluid
Antineoplastic Agents blood
Antineoplastic Agents cerebrospinal fluid
Benzamides blood
Benzamides cerebrospinal fluid
Histone Deacetylase Inhibitors blood
Histone Deacetylase Inhibitors cerebrospinal fluid
Subjects
Details
- Language :
- English
- ISSN :
- 1096-0295
- Volume :
- 98
- Database :
- MEDLINE
- Journal :
- Regulatory toxicology and pharmacology : RTP
- Publication Type :
- Academic Journal
- Accession number :
- 30008379
- Full Text :
- https://doi.org/10.1016/j.yrtph.2018.07.001