Comparative pharmacokinetics of six major compounds in normal and insomnia rats after oral administration of Ziziphi Spinosae Semen aqueous extract / 药物分析学报

Ziziphi Spinosae Semen (ZSS), a traditional Chinese medicine, is used in clinics for the treatment ofinsomnia in China and other Asian countries. Herein, we described for the first time a comparative pharmacokinetics study of the six major compounds of ZSS in normal control (NC) and para-chlor-ophenylalanine (PCPA)-induced insomnia model (IM) rats that were orally administered the aqueous extract of ZSS. An ultra-high-performance liquid chromatography coupled with quadrupole orbitrap mass (UHPLC-Q-Orbitrap-MS) method was developed and validated for the simultaneous determination of coclaurine, magnoflorine, spinosin, 6'''-feruloylspinosin, jujuboside A (JuA), and jujuboside B (JuB) in ZSS in rat plasma. The established approach was successfully applied to a comparative pharmacokinetic study. The systemic exposures of spinosin and 6'''-feruloylspinosin were decreased in the IM group compared to the NC group, while plasma clearance (CL) was significantly increased. The Tmax values of JuA and JuB in IM rats were significantly lower than those in NC rats. The T1/2 of JuA in the IM group was significantly accelerated. The pharmacokinetic parameters of coclaurine and magnoflorine were not evidently affected between the two groups. These results indicate that the pathological state of insomnia altered the plasma pharmacokinetics of spinosin, 6'''-feruloylspinosin, JuA, and JuB in the ZSS aqueous extract, providing an experimental basis for the role of ZSS in insomnia treatment. The comparative pharmacokinetics-based UHPLC-Q-Orbitrap-MS using full-scan mode can therefore provide a reliable and suitable means for the screening of potentially effective substances applied as quality markers of ZSS.

Study on Changes of Extraction Rates of Forsythiaside A and Forsythin in Forsythia suspense Compatible with Other Medicinal Materials of Menshi Huwei Formula before and after Decoction / 中国药房

OBJECTIVE： To investigate the changes of extraction rates of forsythiaside A and forsythin in Forsythia suspensa compatible with other medicinal material of Menshi huwei formula before and after decoction. METHODS： HPLC method was used to determine the extraction amounts and to calculate the extraction rates of forsythiaside A and forsythin in F. suspensa （5 g×7 doses）， F. suspensa （5 g×7 doses） compatible with Pinelliae rhizoma praeparatum cum zingibere et alumine （PRZA）， Menshi huwei formula [including 6 ingredients as F. suspense （5 g×7 doses）， PRZA] after decocted with water. The determination was performed on Diamonsil C18 column with mobile phase consisted of acetonitrile-0.2％ formic acid solution （gradient elution）. The detection wavelength was set at 278 nm， and the column temperature was 30 ℃. The flow rate was 1.0 mL/min. RESULTS： The linear range of forsythiaside A and forsythin were 0.61-6.1， 0.246-2.46 μg （r＝0.999 7， 0.999 9）， respectively； RSDs of precision， stability （within 20 h） and reproducibility tests were all lower than 2％ （n＝6）. Average recovery rates were 96.10％-99.37％ （RSD≤2.36％，n＝6） respectively. In F. suspensa， extraction rates of forsythiaside A and forsythin were 96.90％ and 66.67％. In F. suspensa compatible with PRZA， extraction rates of them were 101.61％ and 54.55％. In Menshi huwei formula， extraction rates of them were 98.39％ and 84.85％. CONCLUSIONS： After F. suspensa is compatible with PRZA， the extraction rates of forsythiaside A is increased while forsythin is decreased. After compatible with other medicinal material in Menshi huwei formula， extraction rates of both are increased slightly.

Simultaneous Determination of 4 Kinds of Effective Components in Volatile Oil of Forsythia suspensa by QAMS / 中国药房

OBJECTIVE： To establish a method for simultaneous determination of α-pinene， β-pinene， limonene and α-terpineol in volatile oil of Forsythia suspensa. METHODS： GC method was adopted. The determination was performed on HP-5 capillary column through temperature-programmed route. The inlet temperature was 230 ℃， and detector temperature was 250 ℃； split sampling was applied （split ratio of 8 ∶ 1）； the air flow rate was 300 mL/min， the hydrogen flow rate was 30   mL/min， the tail gas flow rate was 30 mL/min， and the injection volume was 1 μL. Using limonene as internal reference， relative correction factors of α-pinene， β-pinene and α-terpineol were established， and the reproducibility of relative correction factors were investigated by using different chromatographs and columns， and chromatographic peak location of components was measured. The contents of above components were calculated with QAMS， and then compared with the results of external standard method. RESULTS： The linear range of α-pinene， β-pinene， limonene and α-terpineol were 16.5-990.0， 38.1-2 287.5， 8.2-491.2， 2.4-142.5  μg/mL， respectively （r≥0.999 1）. RSDs of precision， reproducibility and stability tests were all lower than 3％ （n＝6）. Average recoveries were 99.7％-105.5％（RSD＜4％，n＝9）. Compared with limonene （1.00），the average relative correction factors of α-pinene， β-pinene and α-terpineol were 0.91，0.86 and 1.11（n＝3）； relative retention time were 0.69-0.74， 0.81-0.86， 1.25-1.35（RSD＜3％，n＝3）. By using different chromatographs and columns， RSDs of relative correction factors were 0.21％-4.65％（n＝6）. Compared with external standard method， determination results of above 4 components were consistent （the absolute value of relative error were all less than 7％）. CONCLUSIONS： QAMS can be used for simultaneous determination of 4 kinds of effective components in volatile oil from F. suspensa.

Comprehensive Quality Evaluation of Flos Farfarae from Different Habitats / 中国中医药信息杂志

Objective To compare the quality of Flos Farfarae from different habitats, and provide basis for the utilization and development of Tussilago farfara. Methods The contents of rutin and tussilagone were determinated by HPLC, the 100-bud dry weight and bud color were weighed and observed. And the data of different samples were compared and statistical analysed. Results The content of rutin, tussilagone and 100-bud dry weight in Flos Farfarae from different place has a significant difference, and there was a significant positive correlation between rutin and tussilagone. Principal component and factor analysis showed that the quality of Flos Farfarae from Yushe, Ningwu, Guangling was better than other areas. Conclusion The quality of Flos Farfarae from different areas is difference, and wild T. farfara in Yushe, Ningwu, Guangling could be used as high quality germplasm.

Compatability chemistry of acid-alkaline pair medicine of Ephedra sinica and Glycyrrhiza uralencis in Maxing Shigan decoction / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the change regularity of ephedrine and glyrihhzine acid in Ephedra sinila and Glycyrrhiza uralencis pair medicines and in Maxing Shigan decoction.</p><p><b>METHOD</b>The contents of ephedrine and glycyrrhizic acid were determined by HPLC in samples of E. sinica extracts, G. uralencis extracts, pair medicines extracts of Maxing Shigao decoction sinica and G. uralencis, and extracts of E. sinica.</p><p><b>RESULT</b>There were no significant difference in ephedrine contents amoung different samples; the contents of glycyrrhizic acid were lower in decoctions of Maxing Shigan decoction than in G. uralencis decoction and pair medicines extracts.</p><p><b>CONCLUSION</b>Macromolecular complex was NOT formed by ephedrine and Glycyrrhizic acid in decoctions containing pair medicines of E. sinica and G. uralencis.</p>

Compatibility chemistry of acid-alkaline pair medicine of Dahuang and Huangbai in Dahuang Xiaoshi decoction / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the change pattern of alkaline and acid components of Dahuang and Huangbai amoung different combinations in Dahuang Xiaoshi decotion.</p><p><b>METHOD</b>The contents of anthraquinones and berberine were determined by HPLC in samples of Dahuang extracts, Huangbai extracts, Dahuang and Huangbai pair medicine extracts, and extracts of whole recipe.</p><p><b>RESULT</b>The contents of anthraquinones and berberine were decreased with the changes of combinations: from component medicinal material alone to pair medicines, and to whole recipe. the change pattern was more apparent in water decoctions than in ethanol extracts.</p><p><b>CONCLUSION</b>The contents of alkaline and acid components are changed with different extract methods and different combinations.</p>

Compatability chemistry of acid-alkaline pair medicine of dahuang and Fuzi in Dahuang Fuzi decoction / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the change pattern of alkaline and acid components of Dahuang and Fuzi in different combinations.</p><p><b>METHOD</b>The contents of anthraquinones and aconite alkaloids were determined by HPLC in samples of Dahuang extracts, Fuzi extracts, Dahuang and Fuzi pair medicines extracts, and extracts of whole recipe.</p><p><b>RESULT</b>As for Dahuang, the contents of anthraquinones were decreased with changes of combination: higher contents were in decoctions of Dahuang alone, lower contents were in decoctions of pair medicines, and the lowest contents were in decoctions of whole recipe. As for Fuzi, monoester aconite alkaloids could be detected in water extracts, and both biester and monoester aconite alkaloids could be detected in ethanol extracts. The contents of aconite alkaloids were decreased with changes of combinations: from Fuzi alone to pair medicines, and to whole recipe. The change pattern was more apparent when extracted in water decoction.</p><p><b>CONCLUSION</b>The contents of alkaline and acid components are changed with different extract methods and different combinations.</p>

Compatability chemistry of acid-alkaline pair medicine of Fuzi and Gancao in Sini decoction / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the change pattern of alkaline and acid components of Fuzi and gancao amoung different combinations in Sini Decotion.</p><p><b>METHOD</b>The contents of aconite alkaloids and glycyrrhizic acid were determined by HPLC in samples of Fuzi extracts, gancao extracts, Fuzi and gancao pair medicines extracts, and extracts of whole recipe.</p><p><b>RESULT</b>As for Fuzi, monoester aconite alkaloids could be detected in water extracts, and both biester and monoester aconite alkaloids could be detected in ethanol extracts. The contents of aconite alkaloids were decreased with changes of combinations: from Fuzi alone to pair medicines, and to whole recipe. The change pattern was more apparent when extracted in water decoction. As for Gancao, the glycyrrhizic acid was lowered from single medicine to pair medicines, and to whole recipe.</p><p><b>CONCLUSION</b>The contents of alkaline and acid components were changed with different extract methods and different combinations of Fuzi and Gancao.</p>

Studies on chemical structure of complexes compounds formed by acid and alkaline components of pair medicines in decoction / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical structures of macromolecular complexes formed by aconitine and glycyrrhizic acid, aconitine and rhein, berberine and rhein, ephedrine and glycyrrhizic acid in decoctions.</p><p><b>METHOD</b>The binding energy of reactants and products was determined by X-ray spectrography, the ground level charge distribution of products was caculated by density function theory of quantum chemistry.</p><p><b>RESULT</b>The binding energy of aconitine and glycyrrhizic acid, aconitine and rhein, berberine and rhein were changed after reaction. The characteristic atoms in the molecular structures of acid components have higher positive electric charge, while the ones in alkaline components have higher negative charge.</p><p><b>CONCLUSION</b>Aconitine and glycyrrhizic acid, aconitine and rhein, berberine and rhein can form macromolecular complexes, ephedrine and glycyrrhizic acid can not.</p>

Research on compatibility chemistry of acid-alkaline pair medicines in formulas of traditional Chinese medicine / 中国中药杂志

Compatibility chemistry of acid-alkaline pair medicines in formulas of traditional Chinese medicine (TCM) is an important research field which should merit to pay attention. The ideas and methods in prescription compatibility research on formulas containing alkaline-acid pair medicines were summarized from the aspect of chemical groups of alkaline and acid ingredients; the research results were introduced and analyzed; the research meaning was elaborated; and the expectation of the field was viewed.