排脓散汤剂和散剂中有效成分生物利用度的比较研究

Bioavailability of Effective Constituents in Decoction Versus Powder of Painong San

目的比较排脓散的汤剂与散剂中有效成分的药物代谢动力学参数,为排脓散的剂型选择提供依据。方法以栀子苷为内标,采用UPLC-MS/MS法测定大鼠血液中芍药苷、橙皮苷、新橙皮苷和柚皮苷的含量,用乙酸乙酯法提取后,制备样品,然后使用Themo Scientific Syncronis C 18色谱柱(2.1 mm×100 mm,2.7μm)在35℃下进行色谱分离,以水和乙腈为流动相,流速0.3 mL/min,进行负离子模式的多反应监测,用于测定血浆中标准品和内标。结果4种有效成分含量在0.2~500 ng/mL范围内与峰面积呈良好的线性关系,提取回收率、稳定性、精密度均良好且达到测定要求。大鼠经单次给药后,与汤剂比较,排脓散散剂可显著增加橙皮苷的生物利用度(P<0.05),而不能显著增加新橙皮苷、柚皮苷和芍药苷的生物利用度(P>0.05)。结论排脓散散剂的生物利用度可能更优于汤剂。

Objective To investigate the differences in pharmacokinetic parameters of effective constituents between the decoction and power of Painong San,and to provide a basis for selecting the dosage form of Painong San.Methods With geniposide as the internal standard,ultra-performance liquid chromatography-tandem mass spectrometry was used to determine the content of paeoniflorin,hesperidin,neohesperidin,and naringin in rat blood.Samples were prepared after extraction using ethyl acetate,and then chromatographic separation was performed on a Thermo Scientific Syncronis C 18 column(2.1 mm×100 mm,2.7μm)with a mobile phase of water and acetonitrile,at a temperature of 35℃and a flow rate of 0.3 mL/min.Multiple reaction monitoring with the negative ion mode was performed to measure the standard substances and the internal standard in plasma.Results The four effective constituents showed a good linear relationship with the peak area within the range of 0.2-500 ng/mL,with good extraction recovery,stability,and precision,which met the determination requirements.Compared with the decoction of Painong San after a single administration in rats,the powder significantly increased the bioavailability of hesperidin(P<0.05),with no significant increases in the bioavailability of neohesperidin,naringin,and paeoniflorin(P>0.05).Conclusion The powder of Painong San may have better bioavailability than the decoction.