天龙通心方(TLTX)是由红景天、丹参、川芎等6味中药组方而成,临床主要用于气虚血瘀所致的胸痹。为探讨TLTX药效物质基础,并为给药方案提供依据,给予大鼠TLTX后对7种成分的血药浓度和药代特征进行了研究。建立了同时检测生物样品中7种化合物的高灵敏度LC-MS/MS分析方法,经过对线性、专属性、回收率、准确度、精密度和稳定性考察,所建立的分析方法符合临床前药代动力学研究要求。灌胃TLTX 4.5 g·kg^-1后在大鼠血浆中检出7种成分,并分别在给药后0.11~4.67 h达峰。各成分体内含量差异较大,其中红景天苷的药时曲线下面积明显高于其他成分,这表明该成分可能是复方中的主要起效成分,也从体内血药浓度角度说明了红景天为君药的科学性。
Tianlongtongxin (TLTX) formula is composed of six Chinese herbs including Rhodiola rosea L., Salviae Miltiorrhizae Radix et Rhizoma, Chuanxiong Rhizoma and so on. It has been mainly used in the treatment of chest-Bi syndrome in the clinics. To investigate the material foundation and provide reference for clinical dosage regimen, the pharmacokinetics of seven components in the rat plasma were studied after oral administration of TLTX. A high sensitive method was established to determine the seven active components from TLTX in rat plasma based on the LC-MS/MS technique. The method met the requirements of preclinical pharmacokinetic study, through the investigation of linearity, specificity, recovery, accuracy, precision and stability. After administration of TLTX at 4.5 g.kg-1 dose, all of the components were detectable in the plasma after 5 min, The concentration peaks were observed at 0.11-4.67 h respectively after administration with great difference in levels. The AUC of salidroside was significantly higher than other components, suggesting it as a main active component in TLTX formula. The observations provide scientific evidence for the rationality of salidroside as monarch drug in the formula.