Abstract
Our paper aimed to develop rapid, sensitive, and specific LC-MS/MS method for the quantification of niacin (NA) and its metabolite nicotinuric acid (NUA) in human plasma. Following protein precipitation with acetonitrile, the NA, NUA, and internal standard (5-fluorouracil) were separated on a Zorbax 300SB-C8 column (250 mm × 4.6 mm, 5 μm) with a mobile phase consisting of methanol-2 mM ammonium acetate (3 : 97, v/v) at a flow rate of 1 mL/min (split 1 : 1). A tandem mass spectrometer equipped with electrospray ionization source was used as the detector and operated in negative ion mode. The linear concentration ranges of the calibration curves were 5–800 ng/mL for NA and NUA. The intra-assay RSD for quality control (QC) samples were from 5.0% to 8.7% for NA, and 5.5% to 7.6% for NUA. The interassay RSD for QC samples were from 2.8% to 9.4% for NA, and 3.7% to 5.8% for NUA. The relative errors for QC samples were from −2.2% to 2.3% for NA, and −0.6% to 3.2% for NUA. The method was successfully applied to the investigation of the pharmacokinetic profiles of NA, NUA in human after single dose administration of Niacin extended-release/Simvastatin tablet (500 mg/10 mg).
Highlights
Atherogenic dyslipidemia is highly prevalent, especially in patients with insulin resistance and diabetes mellitus
It possesses the ability to decrease low density lipoprotein (LDL) cholesterol level and to increase high density lipoprotein (HDL) cholesterol level which led to its clinical use in the treatment of dyslipidemia and prevention of atherosclerosis [3]
It was found that a statin combined with NA can be an attractive option because both have excellent records of improving cardiovascular outcomes and can effectively correct all abnormalities of atherogenic dyslipidemia in patients especially those with diabetes [6]
Summary
Atherogenic dyslipidemia is highly prevalent, especially in patients with insulin resistance and diabetes mellitus. It was found that a statin combined with NA can be an attractive option because both have excellent records of improving cardiovascular outcomes and can effectively correct all abnormalities of atherogenic dyslipidemia in patients especially those with diabetes [6]. According to the US Food and Drug Administration (FDA) guidelines, a fixed dose combination of NA and SV for use in patients with complex lipid abnormalities has been approved in 2008 [4]. We developed a specific LC-MS/MS method for the quantification simultaneously of NA and NUA in human plasma after single dose oral administration of a pharmaceutical formulation containing Simvastatin 10 mg and Niacin 500 mg to healthy Chinese volunteers. We hope this study can be of help in substantiating the clinical use of Niacin extended-release/Simvastatin tablet in the treatment of human atherogenic dyslipidemia
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