Pharmacokinetic Study of Lovastatin/niacin Sustained-release Tablets in Healthy Chinese Volunteers_West China Medical Journal

Authors：

 LUOZhu , LIANGMao-zhi , WANGYing , YUQin , SHENQi ,  QINYong-ping

National Institute of Drug Clinical Trial/GCP Center, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P. R. China;

Corresponding?author：

QINYong-ping, Email: qinyping1@163.com

Keywords：

Lovastatin/niacin sustained-release tablets; High performance liquid chromatography-tandem mass spectrometry; Pharmacokinetics

DOI：

10.7507/1002-0179.20150540

Video：

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Objective To study the pharmacokinetics of lovastatin/niacin sustained-release tablets in healthy Chinese volunteers. Methods Eligible subjects were enrolled to receive a single dose of 20/500, 20/750 and 20/1 000 mg lovastatin/niacin sustained-release tablets and multiple dose of 20/1 000 mg lovastatin/niacin sustainedrelease tablets, one time per day, sustained for 5 days, respectively. Blood samples were obtained before dosing and up to 10, 20, 30, and 45 minutes, and 1 hour, 1.5, 2, 2.5, 3, 3.5, 4, 5, 7, 9, 12, and 15 hours after dosing. Niacin, niacinamide, nicotinuric acid and lovastatin were detected by high performance liquid chromatography-tandem mass spectrometry method. Results The peak concertration and the area under the plasma concentration-time curve (0-t) of nicotinuric acid had linear dynamics characteristics with the dosage when the dose of niacin was between 500 and 1 000 mg. After multiple dosing, pharmacokinetics parameters of nicotinuric acid and lovastatin were close. No significant diTherence was found between male and female subjects. Conclusion Lovastatin/niacin sustained-release tablets possess linear kinetics. Accumulation is not significant after multiple dosing. Gender doesn't affect the pharmacokinetics parameters.

Citation： LUOZhu, LIANGMao-zhi, WANGYing, YUQin, SHENQi, QINYong-ping. Pharmacokinetic Study of Lovastatin/niacin Sustained-release Tablets in Healthy Chinese Volunteers. West China Medical Journal, 2015, 30(10): 1881-1886. doi: 10.7507/1002-0179.20150540 Copy

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1. Abbott Laboratories. Advicor^® (niacin extended-release/lovastatin tablets)[EB/OL].[2014-07-01]. http://www.advicor.com/importantsafety-information.asp.
2. 廖冬雪, 秦永平, 龔曉麗, 等. LC-MS/MS法測定人血漿中洛伐他汀及其活性代謝物的含量[J]. 四川大學學報:醫學版, 2009, 40(4): 730-733.
3. 王磊, 秦永平, 龔曉麗, 等. HPLC-MS/MS法測定人血漿中煙酸及其代謝物[J]. 四川大學學報:醫學版, 2010, 41(6):1051-1054.
4. Pfuhl P, K?rcher U, H?ring N, et al. Simultaneous determination of niacin, niacinamide and nicotinuric acid in human plasma[J]. J Pharm Biomed Anal, 2005, 36(5):1045-1052.
5. Lauring B, Rosko K, Luo WL, et al. A comparison of the pharmacokinetics of two diTherent formulations of extended-release niacin[J]. Curr Med Res Opin, 2009, 25(1):15-22.
6. Zhang P, Sun Y, Shi G, et al. Quantification of niacin and its metabolite nicotinuric acid in human plasma by LC-MS/MS: application to a clinical trial of a fixed dose combination tablet of niacin extended-release/simvastatin (500 mg/10 mg) in healthy Chinese volunteers[J]. Int J Anal Chem, 2015:212437.
7. Liu M, Zhang D, Wang X, et al. Simultaneous quantification of niacin and its three main metabolites in human plasma by LCMS/MS[J]. J Chromatogr B Analyt Technol Biomed Life Sci, 2012, 904(2):107-114.
8. Menon R, Tolbert D, Cefali E. The comparative bioavailability of an extended-release niacin and lovastatin fixed dose combination tablet versus extended-release niacin tablet, lovastatin tablet and a combination of extended-release niacin tablet and lovastatin tablet[J]. Biopharm Drug Dispos, 2007, 28(6):297-306.
9. 王玉, 宋敏, 杭太俊, 等. 洛伐他汀煙酸緩釋片健康人體藥動學研究[J]. 中國新藥雜志, 2011, 41(5):433-439.
10. 葛苗苗, 衛樂樂, 方凱, 等. 煙酸緩釋片在健康人體的生物等效性[J]. 中國臨床藥理學雜志, 2011, 27(2):118-120.
11. 范新華, 屠永銳, 胡一橋. 自制復方洛伐他汀-煙酸緩釋片及其人體藥動學研究[J]. 世界臨床藥物, 2009, 30(12):739-745.
12. 王萍, 顧世芬, 楊德隆, 等. 煙酸緩釋片的人體藥代動力學及相對生物利用度[J]. 中國藥師, 2005, 8(2):94-96.
13. 舒成仁, 鄧彬, 周雪蘋, 等. 煙酸緩釋片的生物等效性研究[J]. 醫藥導報, 2011, 30(11):1432-1434.
14. Liu M, Wang XL, Zhang D, et al. Pharmacokinetics of niacin, simvastatin and their metabolites in healthy Chinese subjects after single and multiple doses of a fixed dose combination tablet of niacin extended release/simvastatin[J]. Drug Res (Stuttg), 2014, 64(6):296-300.
15. Wang XL, Liu M, Yang M, et al. Gender differences in pharmacokinetics of a combination tablet of niacin extendedrelease/simvastatin in healthy Chinese volunteers[J]. Eur J Drug Metab Pharmacokinet, 2014, 39(4):321-326.

West China Medical Journal

Pharmacokinetic Study of Lovastatin/niacin Sustained-release Tablets in Healthy Chinese Volunteers

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