| AbstractSini Decoction(SND), from Treatise on Exogenous Febrile Diseases, iscomposed of Asdix Aconiti Praeparata, Anizoma Zingiberis and RadixGlycyrrhizae Praeparata. Aconiti, heavy acrid fiavour and great hot nature,has the effect of warming and tonifying kidneym. Its effect is pompt butnot lasting. Zingiberis can warm and tonify spleenW and its effect islasting but not prompt. The combination of these two drugs, assisted byglycyrrhizae gives a prompt and lasting effect. Sini Decoction canrecuperate the depleted yang and rescue the patient from danger, main1y forcases of exhaustion of yang-energy, manifested as deadly cold of limbs,sunken and feeble pulse.Objective: to study the effective fraction of SN'D bypharmacokinetics(PK)-pharmacody method, to study thepharmacological substance of SND, to reveal the comPatibility law of SND.Methods: (l) Preparation of SNDf Radix Aconiti Praeparata,Rhizoma Zingiberis and Radix Glycyrrhizae Praeparata are extractedrespectively, merged into SND. (2) Purification of SNDf SND is purified bymacroporous resin D,,,' (3) Pharmaceutical evaluation of the purification fThe alkaloids in Radix Aconiti Praeparata, glycyrrhizic acid, liquiritigenin,isoliquiritigenin in Radix Glycyrrhizae Praeparata, and some markercomponents in Rhizoma Zingiberis are identified by TLC(Thin LayerChromatography). The fingerprint chromatograms and content of aconitine-type alkaloids(including doub1e ester-type alkaloids and their hydrolysates )are inspected and determined by HPLC (High Pefformance LiquidChromatography). (4) Pharmacological evaluation of the purification f Theindexes include myocardiac contraction, cardiac output, heart rate of frog's3separated heart and the content of nitric oxide (NO), which cal1 dilate bloodvessel and remedy shock. (5) The method of determining the pIasl11aconcentration by HPLC is developed. (6) PK-PD study f Three dogs areintramuscular injected with the purification. The bIood is got from thighartery befOre the injection and at different moments after injectio11. Thecontents of aconitine-type alkaloids and NO of the same moment's serumare determined. After the data are processed by MCPKI, PharmacokineticPC Program, the parameters are caculated and the correlation is studiedbetween the plasma concentration and the NO net growth rate duri11g 0~6hr.Results: (l) The optimum factors of purifing SND' The concentrationof SND extraction is 0.5g/ml, the eluating ethanol concentration is 70%, andthe flow rate is lml/min.The absorption recovery of aconitine-type alkaloidsis 83 .97%, while the weight of the dried purification is 5.23% of the total. (2)The pharmaceutical study shows the thi1l layer chromatograms of the SNDpurification and those of SND are almost the same. The purification keepsaconitine-type alkaloids in Radix Aconiti Praeparata, glycyrrhizic acid,Iiquiriti8enin, isoliquiritigenin in Radix Glycyrrhizae Praeparata and markercomponents in Rhizoma Zingiberis. High performance liquid chromatogran1of the purification is basically the same as that of SND, while the co11tent ofaconitine-type alkaloids is 0.0243mg/ml determined by HPLC. (3) TI1epharmacoIogical experiments proved that the SND purification can promotemyocardiac contraction and cardiac output, lower the heart rate of frog'sseparated heart, raise siSniflcantly the content of NO in serum of micetreated by Metaraminol. (4) The regression equation of acol1itine refCrel1cestandard in serum determined by HPLC is Y=42667. l l982X-28l7. l33, r=0 9995, the linear range is l~20 P g/ml. The precision and accuracy of t11emethod can meet the needs of the experiment. (5) The data of PK and PDcan be botl1 described by one compartme11t open model witl1 first order4absorption. The parameters of two methods are similar. The regressionequation of the plasma concentration and the NO net growth rate during0--6hr is Y=0.4478X-0.ll23, r=0.9939, showing the corre... |
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