红细胞负载丹参酮ⅡA磺酸钠给药系统的大鼠体内药动学研究

Study on pharmacokinetics of sodium tanshinone Ⅱ A sulfonate loaded erythrocyte delivery system in rats

目的建立大鼠血浆中丹参酮ⅡA磺酸钠(STS)检测的高效液相色谱法,并对红细胞负载STS给药系统静脉注射后大鼠体内药动学进行研究。方法 SD大鼠尾静脉注射载药红细胞液,给药剂量5.0 mg/kg,采用高效液相色谱法测定药物的质量浓度,以软件DAS 2.0拟合药动学参数。结果丹参酮ⅡA磺酸钠在0.25~25.00μg/mL范围内呈良好线性关系,回收率、精密度和稳定性均符合检测要求。大鼠尾静脉注射载药红细胞后,STS的t_(1/2α)为(0.139±0.54)h,t_(1/2β)为(3.268±1.10)h,C_(max)为(6.88±2.07)mg/L,AUC_(0-∞)为(10.19±0.72)(mg·h)/L。结论该方法简便准确,可用于STS血浆样品的含量测定和药动学研究。

Objective To establish a HPLC method for determination of sodium tanshinone ⅡA sulfonate in plasma and study on the pharmacokinetics of drug loaded erythrocyte after intravenous administration. Methods SD rats were given drug loaded erythrocyte solution via tail vein at a dose of 5.0 mg/kg, and the drug plasma concentration was determined by HPLC. The pharmacokinetics parameters were also calculated by DAS 2.0 software. Results A good linear relationship of sodium tanshinone Ⅱ A sulfonate was observed in the range of 0.25-25.00 μg/mL, and the results of recovery, precision and stability tests were suitable for drug analysis. After tail vein injection, pharmacokinetics parameters of sodium tanshinone ⅡA sulfonate were as follows： t1/2a = （0.139±0.54） h, t1/2B= （ 3.268± 1.10） h, Cmax = （6.88±2.07） mg/L, and AUC0-∞ = （10.19±0.72） （rag h）/L. Conclusion The established method is accurate, simple and could be used for determination of sodium tanshinone ⅡA sulfonate in plasma as well as pharmaeokinetic study.