目的依照International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use(ICH)指导原则,采用化学反应动力学和热力学方法研究野黄芩苷及灯盏花素注射液水溶液在不同pH值、温度、离子强度及初始质量浓度等条件下的降解反应的动力学特征,以研究野黄芩苷降解机制,比较其制剂与单体稳定性的差异,并考察临床使用条件对制剂稳定性的影响。方法采用HPLC法考察不同条件下野黄芩苷单体及灯盏花素注射液中其量随时间的变化,利用化学反应动力学的方法计算野黄芩苷在不同环境下的降解反应动力学参数,预测其半衰期(t1/2)和活化能。同时考察灯盏花素注射液与5种常用输液剂(0.9%生理盐水溶液、5%葡萄糖注射液、10%葡萄糖注射液、乳酸钠林格注射液、复方电解质葡萄糖注射液)的配伍稳定性。结果野黄芩苷单体及灯盏花素注射液在不同温度和酸碱条件下的降解反应均遵循一级动力学规律,25℃时其在中性水溶液环境中最稳定,单体t1/2为203.87 h,活化能为97.9 kJ/mol。在各种条件下,灯盏花素注射液水溶液中野黄芩苷的稳定性均优于单体。Na+、Cl.离子强度及溶液初始浓度对野黄芩苷降解速率无明显影响。灯盏花素注射液与5种输液剂配伍在30 d内均可观察到明显的质量浓度下降。结论野黄芩苷在中性水溶液中较为稳定,受温度、酸碱环境影响较大,初始质量浓度和离子对野黄芩苷稳定性的影响不明显,而灯盏花素注射液与5种常用输液剂配伍均不稳定。为有效地预测含野黄芩苷的中药制剂的稳定性变化提供了合理准确的依据,为含野黄芩苷的中药制剂的安全应用提供技术支持。 OBJECTIVE: To study the effects of different concentrations of scutellarin and breviscapine in aqueous solution at different pH values, temperature, ionic strength and initial pH using chemical reaction kinetics and thermodynamics in accordance with the guidelines of International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) Mass concentration and other degradation kinetic characteristics of the study to study the degradation mechanism of scutellarin, compare the stability of the preparation and monomer differences, and investigate the clinical conditions on the stability of the preparation. Methods The content of baicalin monomer and breviscapine injection under different conditions were measured by HPLC. The kinetic parameters of saikosalin degradation reaction under different environments were calculated by chemical reaction kinetics. Half-life (t1 / 2) and activation energy. At the same time, the compatibility of breviscapine injection with five kinds of commonly used infusion solution (0.9% saline solution, 5% glucose injection, 10% glucose injection, sodium lactate Ringer injection, compound electrolyte glucose injection) was investigated. Results The degradation reaction of saikosalin monomer and breviscapine injection under different temperature and acid-base conditions followed the first-order kinetics and was the most stable in neutral aqueous solution at 25 ℃. The monomer t1 / 2 was 203.87 h, the activation energy of 97.9 kJ / mol. Under various conditions, the stability of scutellarin in the solution of breviscapine injection is better than the monomer. The ionic strength of Na +, Cl. And the initial concentration of the solution had no significant effect on the degradation rate of baicalin. Breviscapine injection with 5 kinds of infusion solution compatibility within 30 d were observed in the mass concentration decreased significantly. Conclusion Scutellaria baicalensis is relatively stable in neutral aqueous solution, and is greatly affected by temperature, acid and alkali environment. The initial concentration and ions have no obvious effect on the stability of Scutellaria baicalensis, but Breviscapine injection and 5 commonly used infusion solutions Compatibility is not stable. This study provides a reasonable and accurate basis for predicting the change of stability of traditional Chinese medicine preparations containing wild baicalin effectively and provides technical support for the safe application of traditional Chinese medicine preparations containing wild baicalin.