雷诺嗪消旋体及其光学异构体的药动学研究

廖明琪; 李玲; 马海忠; 王婷<sup>*</sup>; 梁莉; 乔华

引用本文:	廖明琪,李玲,马海忠,王婷,梁莉,乔华.雷诺嗪消旋体及其光学异构体的药动学研究[J].中国现代应用药学,2014,31(11):1366-1370.
	LIAO Mingqi,LI Ling,MA Haizhong,WANG Ting,LIANG Li,QIAO Hua.Study on the Pharmacokinetics of Ranolazine and Its Optical Isomer[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(11):1366-1370.

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雷诺嗪消旋体及其光学异构体的药动学研究
廖明琪^1,2, 李玲^1,2, 马海忠^1,2, 王婷¹, 梁莉¹, 乔华¹
1.兰州大学第一医院，国家药物临床试验机构，兰州 730000;2.兰州大学药学院，兰州 730000

摘要:

目的研究雷诺嗪消旋体及其光学异构体在大鼠体内的药动学特点。方法采用高效液相色谱法测定给药后不同时间点大鼠血浆中雷诺嗪消旋体及其光学异构体的含量，并计算药动学参数。结果主要药动学参数如下：雷诺嗪消旋体低、中、高剂量的C_max分别为(3.404±0.442)，(5.858±0.422)和(8.186±0.625)mg·L^-1；T_max分别为(0.250±0.000)，(0.250±0.000)和(0.500±0.000)h；AUC_{0-12 h}分别为(7.033±0.757)，(13.055±1.665)和(20.899±2.965)mg·h·L^-1；t_1/2分别为(4.882±2.017)，(6.757±2.932)和(4.603±0.462)h；R-雷诺嗪低、中、高剂量的C_max分别为(1.144±0.193)，(3.999±0.830)和(5.987±0.321)mg·L^-1；T_max分别为(0.500±0.000)，(0.583±0.144)和(0.477±0.632)h；AUC_{0-12 h}分别为(4.182±0.555)，(8.831±1.092)和(13.517± 7.238)mg·h·L^-1 ；t_1/2分别为(4.420±0.694)，(3.430±0.773)和(4.221±2.881)h；S-雷诺嗪低、中、高剂量的C_max分别为(0.756± 0.227)，(2.786±0.269)和(4.769±0.501)mg·L^-1；T_max分别为(0.583±0.144)，(0.500±0.000)和(0.417±0.144)h；AUC_{0-12 h}分别为(3.696±0.821)，(6.695±0.888)和(9.976±0.314)mg·h·L^-1；t_1/2分别为(3.191±0.322)，(5.630±1.086)和(4.603±0.462)h。结论统计学结果表明，R-雷诺嗪和S-雷诺嗪的C_max、T_max、t_1/2、AUC_{0-12 h}均无显著性差异，雷诺嗪消旋体与不同光学异构体相比在体内有较好的吸收。

关键词: 雷诺嗪光学异构体药动学高效液相色谱法

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Study on the Pharmacokinetics of Ranolazine and Its Optical Isomer

LIAO Mingqi^1,2, LI Ling^1,2, MA Haizhong^1,2, WANG Ting¹, LIANG Li¹, QIAO Hua¹

1.National Institute for Drug Clinical Trial, The First Hospital of Lanzhou University, Lanzhou 730000, China;2.College of Pharmacy, Lanzhou University, Lanzhou 730000, China

Abstract:

OBJECTIVE To study the pharmacokinetics of ranolazine and its optical isomers in rat plasma. METHODS The concentrations of ranolazine in rats plasma at different time were determined by HPLC and the pharmacokinetic parameters were calculated. RESULTS The pharmacokinetic parmeters were as follows: the group of ranolazine: C_max (3.404±0.442), (5.858±0.422) and (8.186±0.625)mg·L^-1; T_max (0.250±0.000), (0.250±0.000) and (0.500±0.000)h; AUC_{0-12 h} (7.033±0.757), (13.055±1.665) and (20.899±2.965)mg·h·L^-1; T_1/2 (4.882±2.017), (6.757±2.932) and (4.603±0.462)h; the group of R-ranolazine: C_max (1.144±0.193), (3.999±0.830) and (5.987±0.321)mg·L^-1; T_max (0.500±0.000), (0.583±0.144) and (0.477±0.632)h; AUC_{0-12 h} (4.182±0.555), (8.831±1.092) and (13.517±7.238)mg·h·L^-1; T_1/2 (4.420±0.694), (3.430±0.773) and (4.221±2.881)h, the group of S-ranolazine C_max (0.756±0.227), (2.786±0.269) and (4.769±0.501)mg·L^-1; T_max (0.583±0.144), (0.500±0.000) and (0.417±0.144)h; AUC_{0-12 h} (3.696±0.821), (6.695±0.888) and (9.976±0.314)mg·h·L^-1; T_1/2 (3.191±0.322), (5.630±1.086) and (4.603±0.462)h. CONCLUSION Statistical results show that the value of C_max, T_max, T_1/2 and AUC of R-Ranolazine and S-Ranolazine has no significant difference. Ranolazine compared with different optical isomer has good absorption in the body.

Key words: ranolazine optical isomers pharmacokinetic HPLC