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采用高效液相色谱法研究中药丹参素(3,4-二羟基苯乳酸)在兔体内的药代动力学。

Pharmacokinetics of a Chinese traditional medicine, danshensu (3,4-dihydroxyphenyllactic acid), in rabbits using high-performance liquid chromatography.

作者信息

Zhao F Q, Zheng N X, Sato H, Adachi I, Horikoshi I

机构信息

Department of Hospital Pharmacy, Heilongjian Province Hospital, Harbin, China.

出版信息

Biol Pharm Bull. 1997 Mar;20(3):285-7. doi: 10.1248/bpb.20.285.

Abstract

An injectable solution of Danshen was prepared and its in vivo disposition was examined in rabbits. The presence of Danshensu, one of the active components of Danshen, in the obtained solution was confirmed by a simple high-performance liquid chromatographic (HPLC) method. The pharmacokinetics of Danshensu in rabbits was evaluated by the HPLC method for plasma Danshensu. The calibration curve for Danshensu was linear (r = 0.998) over the concentration range of 0.25-40.0 micrograms/ml. The intra-assay coefficients of variation (CVs) were 3.8, 3.1, and 3.1% at 1, 10, and 50 micrograms/ml, respectively, and the inter-assay CVs were 5.3, 5.3, and 2.9% at 1, 10, and 50 micrograms/ml, respectively. The analytical recovery of Danshensu in plasma averaged 95.2%. From the plasma concentration profile of Danshensu after its intravenous administration, the t1/2, mean residence time (MRT), Vdss, and Cltot were determined as 32 min, 48 min, 149 ml/kg, and 3.13 ml/min/kg, respectively.

摘要

制备了丹参注射液,并在兔体内研究了其体内处置情况。通过一种简单的高效液相色谱(HPLC)方法确认了所得溶液中丹参的活性成分之一丹酚酸B的存在。采用HPLC法测定血浆中丹酚酸B的含量,以评估丹酚酸B在兔体内的药代动力学。丹酚酸B的校准曲线在0.25 - 40.0微克/毫升的浓度范围内呈线性(r = 0.998)。在1、10和50微克/毫升时,批内变异系数(CVs)分别为3.8%、3.1%和3.1%,批间CVs在1、10和50微克/毫升时分别为5.3%、5.3%和2.9%。血浆中丹酚酸B的分析回收率平均为95.2%。根据丹酚酸B静脉给药后的血浆浓度曲线,确定其t1/2、平均驻留时间(MRT)、稳态分布容积(Vdss)和总清除率(Cltot)分别为32分钟、48分钟、149毫升/千克和3.13毫升/分钟/千克。

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