| The purpose of this study was to discuss the effect of Rheum palmatum and Radix scutelariae after processing with wine on change and pharmacokinetics,tissue distribution in rat of effect ingredients,which provided a theoretical foundation and experimental data for the study of wine processing mechanism.1、To develop and validate the HPLC method for simultaneous determination of eight components(aloe-emodin,rhein,emodin,chrysophanol,physcion,gallic acid,Sennoside B,Sennoside A)in crude and wine processed Rheum palmatum.An Kromasil-C18 column(250×4.6mm,5μm)was used with a flow rate of 1 ml/min.Mobile phase was composed of acetonitrile(A)and 0.1%aqueous acetic acid(B)using a gradient elution of 0-5min,2%A;5-12min,10%A→15%A;12-20min,15%A→20%A;20-30min,20%A→22%A;30min-55min,22%A→68%A;55min-65min,68%A;65min-70min,68%A→80%A;70min-80min,80%A;80min-84min,80%A→2%A;84min-85min,2%A.Detection wavelengths were set at 254 nm.As a result,After a large rice wine made five free anthraquinone(aloe-emodin,rhein,emodin,chrysophanol and emodin)content increased significantly,and combined with the type the anthraquinone(sennoside A and senna glycosides B)as rhubarbthe medium induced diarrhea stronger role ingredient by the wine made after content decreases.To develop and validate the UPLC method for simultaneous determination of eleven flavonoids(baicalin,wogonoside,baicalein,wogonin,oroxylin A,chrysin,scutellarin,oroxylin A-7-O-glucuronide,scutellarein,apigenin,apigenin-7-glucuronide)in crude and wine processed Radix scutellariae.An Waters ACQUITY UPLC BEH C18(100 mm×2.1 mm;i.d.,1.7 μm)was used with a flow rate of 0.2 ml/min.Mobile phase was composed of(A)aqueous formic acid(0.01%,v/v)and(B)methanol using a gradient elution of 15%-35%B at 0-3 min;35%B,at 3-12 min;35%-50%B,at 12-14 min;50%B,at 14-28 min;50%-15%B,at 28-28.5 min;15%B,at 28.5-30 min.Detection wavelengths were set at 275 nm.As a result,the content of baicalin,wogonoside,oroxylin A-7-O-glucuronide,scutellarin and apigenin-7-glucuronide was lower inthe crude,but higher in the processed.However,the content of baicalein,wogonin,oroxylin A,chrysin,scutellarein and apigenin was higher in the crude,but lower in the processed.2、A sensitive and specific method was developed for the determination of aloe-emodin,rhein and emodin in rats plasma.Separation was performed on a kromsail C18 column(150mm×4.6mm,i.d.:5μm)with 3mmoI/L ammonium acetate-methanol(25:75,v/v)as the mobile phase.The linear range of 2.9-2900 ng/mL,24-24000 ng/mL,0.5-500 ng/mL;correlation coefficients(r)were greater than 0.99;average recovery of each component and the internal standard(71.2-88.8)%RSD<11.7%;compared three kinds of anthraquinones in vivo pharmacokinetics of orally administered rhubarb raw products/wine products extract differences in adoption of this Law,the results showed that,except rheinig rhubarb uncooked food and wine products,aloe emodin and emodin drug of-concentration curve quite different extension of aloe emodin and emodin Tmax in varying degrees,Cmax compared with raw goods group high,AUC0-t increased in varying degrees,but the half-life of T1/2 have fewer;’the rhein pharmacokinetic parameters change little,half-life T1/2,Cmax and AUC0-t was no significant differenceshort time to peak Tmax than goods group.A rapid,sensitive and selective liquid chromatography/tandem mass spectrometry method(LC-MS/MS)was developed and for simultaneous determination 10 active compounds(baicalin,wogonoside,baicalein,wogonin,oroxylinA,chrysin,scutellarin,oroxylinA-7-O-glucuronide,scutellarein and apigenin)in rat plasma.Separation was performed on an Waters ACQUITY UPLC BEH C18 column(1.7 μm,2.1×100 mm)protected by a Van Guard BEH C18 column(1.7 μm,2.1x5 mm).Mobile phase was composed of(A)aqueous formic acid(0.1%,v/v)and(B)methanol using a gradient elution of 35%-50%B,at 0-1 min;50%-90%B,at 1-8 min;90%-35%B,at 8-8.5 min;35%B,at 8.5-10 min.The linear range of 54.37-5220 ng/mL,163.1-15660 ng/mL,731.8-70260 ng/mL,15.3-1470 ng/mL,2.38-228.6 ng/mL,153.87-14772 ng/mL,2.4-230ng/mL,48.75-4680 ng/mL,335.3-32190 ng/mL,337.8-32430 ng/mL;correlation coefficients(r)were greater than 0.993;each component and the average recovery of the internal standard(71.2-89.7)%RSD ≤ 11.9%;As a result,after being given wine processed Radix scutellariae extracts,it took less time for baicalin,oroxylinA-7-O-glucuronide,wogonoside,oroxylin A and wogonin to reach the peak concentration,indicating that it could promote the absorption of these analytes.The t1/2 of baicalin,wogonoside,oroxylin A-7-O-glucuronide was increased remarkably,indicating that it could postpone the elimination of baicalin,wogonoside,oroxylin A-7-O-glucuronide and might prolong the potency of them in vivo.3、A sensitive and specific method was developed for the determination of aloe-emodin,rhein and emodin in rat tissue(heart,lung,brain,liver,kidney).Separation was performed on a kromsail C18 column(150mmx4.6mm,i.d.:5μm)with 3mmol/L ammonium acetate-methanol(25:75,v/v)as the mobile phase.The linear range of the three components in various tissues were 2.9-2900 ng/mL,24-24000 ng/mL,2-2000 ng/mL;correlation coefficients(r)were greater than 0.99;each component and the internal standard.the average recoveries(70.5-95.8)%RSD ≤ 11.8%;compared orally administered rhubarb raw products/wine products extract three kinds of anthraquinones in vivo tissue distribution differences in adoption of this Law,the resultsfound that oral administration of rat the rhubarb raw products/wine products extract,aloe-emodin,rhein and distribution in animals rapidly 15min after the administration,can be detected in the organs of the organizations to a higher leveldrug concentration.Aloe emodin,rhein,emodin were not detected in the brain,Description aloe emodin,rhein,emodin can not penetrate the blood-brain barrier.Distribution of each component in the organizations after the rats were given large rice wine products.A rapid,sensitive and selective liquid chromatography/tandem mass spectrometry method(LC-MS/MS)was developed and for simultaneous determination 10 active compounds(baicalin,wogonoside,baicalein,wogonin,oroxylinA,chrysin,scutellarin,oroxylinA-7-O-glucuronide,scutellarein and apigenin)in rat tissue(heart,lung,spleen,liver,kidney).Separation was performed on an Waters ACQUITY UPLC BEH C18 column(1.7 μm,2.1×100 mm)protected by a Van Guard BEH C18 column(1.7 μm,2.1×5mm).Mobile phase was composed of(A)aqueous formic acid(0.1%,v/v)and(B)methanol using a gradient elution of 35%-50%B,at 0-1 min;50%-90%B,at 1-8 min;90%-35%B,at 8-8.5 min;35%B,at 8.5-10 min.each component,the average recoveries(70.0-110.7)%between;using irrigation compared Act gastric administration skullcap raw products/wine products of the extract 10 kinds of flavonoids in different tissue distribution in vivo and found that oral administration skullcap wine products,can significantly increase the bAICALEIN,oroxylin a,skullcap glycosides,scutellarein,scutellarin,oroxylin a-7-O-glucuronide,wogonoside in rat lung tissue distribution,and chrysin,wogonin,apigenin in the lung tissue the distribution compared with little change in raw product.In this thesis,using a variety of analytical methods on the above two drugs with wine flavor representative-Rhubarb,Scutellaria research,we can draw preliminary summary:two with wine can affect the taste of traditional Chinese medicine and the effects of changes in the composition in rats the pharmacokinetics and biodistribution of the results for clinical application rhubarb,Scutellaria wine products focus on treating illness to provide a scientific basis,but whether the "wine Sunburn by lifting" concocted theory still needs further study are consistent.This topic is Pieces cooked with wine class mechanism provides a certain research ideas and experimental evidence. |
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