Wang Yuanqing, Yan Jianye, Li Shunxiang, Cai Xiong, Wang Wei, Luo Kun, Huang Dan, Gao Jiesheng
Department of Chemistry, Key Laboratory of Modernization of Chinese Medicine, Changsha, China ; Department of Biotechnology, Laboratory of Biotechnology and Engineering, School of Life Science and Technology, Central South University of Forestry and Technology, Changsha, China.
Department of Chemistry, Key Laboratory of Modernization of Chinese Medicine, Changsha, China.
Pharmacogn Mag. 2014 Jul;10(39):285-91. doi: 10.4103/0973-1296.137369.
Bushen Huoxue Qubi (BHQ) granules, a traditional Chinese medicine preparation, has been clinically used for the treatment of the blood stasis syndrome.
The main objective is to investigate whether the diseased condition would alter the pharmacokinetics and tissue distribution of tanshinone IIA in BHQ, which was given orally to the acute blood stasis rats.
The main bioactive constituent in BHQ, tanshinone IIA, was measured in the plasma and tissues of animals by the high performance liquid chromatography with ultraviolet detection. The analysis was successfully performed on an Agilent TC-C18 column (250 × 4.6 mm I.D., 5 μm) protected with a Octadecylsilane (ODS) guard column (10 × 4.6 mm I.D., 5 μm). The mobile phase was aqueous solution (A) (containing 0.40% aqueous acetic acid) and acetonitrile (B). The conditions of the solvent gradient elution were 35-40% (B) in 0-15 min, 40-42% (B) in 15-18 min and 42-70% (B) in 18-30 min at a flow rate of 1.0 mL/min. Detection was conducted with wavelength of 270 nm at 30°C.
Good linearity relationships were found (r (2)> 0.9955) over the investigated concentration range for bio-samples. Blood stasis was associated with significantly higher area under the concentration-time curve (AUC), the maximum plasma concentration (Cmax) and biological half-life (t1/2), lower total body clearance (CL) and apparent volume of distribution (Vd) of tanshinone IIA in plasma and higher AUC0-t of tanshinone IIA in the analyzed tissues of rats treated with BHQ.
Blood stasis could alter pharmacokinetics and tissue distribution of tanshinone IIA in BHQ.
补肾活血祛痹（BHQ）颗粒是一种中药制剂，已在临床上用于治疗血瘀证。
主要目的是研究疾病状态是否会改变急性血瘀大鼠口服BHQ后丹参酮IIA的药代动力学和组织分布。
采用高效液相色谱-紫外检测法测定动物血浆和组织中BHQ的主要生物活性成分丹参酮IIA。分析在Agilent TC-C18柱（250×4.6 mm内径，5μm）上成功进行，该柱由十八烷基硅烷（ODS）保护柱（10×4.6 mm内径，5μm）保护。流动相为水溶液（A）（含0.40%乙酸水溶液）和乙腈（B）。溶剂梯度洗脱条件为：0-15分钟内（B）为35-40%，15-18分钟内（B）为40-42%，18-30分钟内（B）为42-70%，流速为1.0 mL/分钟。在30℃下以270 nm波长进行检测。
在所研究的生物样品浓度范围内发现良好的线性关系（r（2）>0.9955）。血瘀与丹参酮IIA在血浆中的浓度-时间曲线下面积（AUC）、最大血浆浓度（Cmax）和生物半衰期（t1/2）显著升高、全身清除率（CL）和表观分布容积（Vd）降低以及BHQ处理的大鼠分析组织中丹参酮IIA的AUC0-t升高有关。
血瘀可改变BHQ中丹参酮IIA的药代动力学和组织分布。
