Evaluating the spectrum-effect profiling and pharmacokinetics of Tieshuang Anshen Prescription with better sedative-hypnotic effect based on Fe2+ than Hg2+ - 03/09/21
, Guoxiang Sun a, ⁎ Bienvenue sur EM-consulte, la référence des professionnels de santé.
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Abstract |
Although Zhusha Anshen Pill (ZSASP) is a commonly used traditional prescription for insomnia, the safety of cinnabar in the formula has always been controversial since its initial application in medical fields. Here, we developed a new prescription, Tieshuang Anshen Prescription (TSASP), by improving ZSASP with Fe2+ instead of Hg2+. Besides, TSASP was further optimized by establishing and testing the HPLC fingerprint and its sedative-hypnotic effect of formulas with different compatibility ratios and performing correlation spectrum analysis. The safety of TSASP was also evaluated by HE staining of liver and kidney. In addition, a validated and robust UHPLC-MS/MS method was established to demonstrate the pharmacokinetic characteristics of berberine, palmatine, jatrorrhizine, ligustilide, catalpol, loganin, liquiritin and liquiritigenin after oral administration of TSASP. Our study originally provides a new non-toxic prescription, TSASP, with better sedative-hypnotic effect in comparison with ZSASP, revealing that Fe2+ could replace Hg2+ to eliminate its toxicity and play a sedative role. Meanwhile, we believe that our pharmacokinetics results may contribute valuable reference to both TSASP’s specific mechanism of action and its further clinical efficacy and effectiveness research.
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Highlights |
• | Fe2+ was substituted for Hg2+ to remove toxicity, playing a sedative-hypnotic role. |
• | Tieshuang Anshen Prescription (TSASP) was proved to be safe for liver and kidney. |
• | Spectrum-effect relationship analysis was established for optimizing TSASP. |
• | TSASP has a better sedative-hypnotic effect than Zhusha Anshen Pill. |
• | A rapid and reliable UHPLC-MS/MS method was established for pharmacokinetics of TSASP. |
Abbreviations : BBR, CTP, DG, DH, DZP, FAC, GC, GRA, HE, HL, IS, JAT, LGN, LIG, LLOQ, LQG, LQT, MLR, MRM, NLT, PAL, PPV, QC, RFP, RSD, RT, TCM, TS, TSASP, TST, ZSASP
Keywords : Sedative-hypnotic effect, Fingerprint, Spectrum-effect relationship, Tieshuang Anshen Prescription, Pharmacokinetics
Plan
Vol 141
Article 111923- septembre 2021 Retour au numéro
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