Abstract

Hydroxysafflor yellow A (HSYA) is the main bioactive ingredient of XBJ injection. At first, the stability of HSYA in solution and in a Xuebijing injection was investigated, then the mechanisms of the increased stability of HSYA in the XBJ injection were investigated to provide useful information on clinical safety. HSYA stability was investigated as a function of pH and temperature in aqueous solution and an XBJ injection, following the guidelines from the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use. Products were identified by UPLC-MS/MS. HSYA reaction followed first-order kinetics under all conditions. The half-life of HSYA in XBJ was almost 40 times longer than in aqueous solution. The activation energies of HSYA reaction in aqueous solution and XBJ were calculated to be 78.53 and 92.90 kJ∙mol−1 by using Arrhenius equation. The results indicated that HSYA was more stable in XBJ than in aqueous solution. Two products were identified and the mechanism was intra-molecular nucleophilic substitution. The excellent stability of HSYA in XBJ injection partly due to the micelles formed in the injection. The study may provide clues for compatibility in TCM prescription and also provide useful information for further preparation technology research of HSYA and assessment of clinical safety of XBJ.

Highlights

  • Hydroxysafflor yellow A (HSYA) is a pharmacologically active chalcone found in Flos Carthami, a medicinal and edible herb from Eurasia

  • Under weak to moderate with previous findings [27], we found that the flavanone-chalcone isomerization equilibrium was alkaline conditions, the hydroxyl group at C-20 is ionized firstly, followed by intra-molecular regulated by alkalinity of the buffer

  • HSYA and the other with previous findings [27], we found that the flavanone-chalcone isomerization equilibrium was four active ingredients (PF, DSS, ferulic acid degradation (FA) and Sen I) of XBJ were detected in EEX while dextrose was regulated byWSX

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Summary

Introduction

Hydroxysafflor yellow A (HSYA) is a pharmacologically active chalcone found in Flos Carthami, a medicinal and edible herb from Eurasia. Stability of active ingredients of herbal drugs is one of important factors affecting the quality, safety and efficacy of herbal drugs [12]. HSYA may have thermo and stability anddegrade may degrade best of there are few reports on the chemical stability of in aqueous solution or in XBJ. As an important our knowledge, there are few reports on the chemical stability of HSYA in aqueous solution or in TCM injection, the therapeutic efficacythe andtherapeutic safety of XBJ haveand caused extensive concern. Theabove parameters associated with the degradation of HSYA infor aqueous solution and XBJ under condition were estimated. The effects of WSX and EEX into and four bioactive ingredients of XBJ (PF), injection was separated on an SPE column water-soluble. HSYA degradation pathways and the factors underlying its influenced stability in XBJ were proposed

Method
The pH Profile of HSYA
The Temperature Profile of HSYA Stability
Mass Balance
Factors that Stabilize HSYA in XBJ Injection
Methods
Sample Preparation
Measurement of HSYA Stability at Different pHs
Measurement of HSYA Stability at Different Temperatures
Characterization of Degradation Products
The Effects of XBJ Components on HSYA Stability
Conclusions
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