| Cyclovirobuxine D(CB)is an alkaloid extracted from the Department of boxwood plants Buxus(Buxus microphylla Sieb.Et Zucc.Var.Sinica Rehd.Et Wils.)and from the same plant.CB used to treat chest pain,coronary heart disease,cardiac arrhythmias and other cardiovascular diseases caused by blood stasis.However,the further research and application of CB is limited for its poor solubility in water and its low bioavailability in vivo,and its efficacy for treating cardiovascular disease can not give full play.Therefore,this paper prepared CBHP in order to improve the solubility and the oral bioavailability of CB.This paper established a pre-column derivatization of HPLC-FLD method for the content determination of CB,and studied CBHP from the physical and chemical properties,pharmacokinetics and in the intestinal absorption.This paper mainly includes the following sections:The first section of this paper prepared the CBHP and characterized its physicochemical properties.This paper established a pre-column derivatization of HPLC-FLD method for the content determination ofCBHP,and the physical and chemical properties of CB were characterized from the appearance,solubility,partition coefficient,particle size and Zeta potential,infrared spectroscopy,differential scanning calorimetry.CBHP increase significantly the solubility of CB in water.The average particle size and Zeta potential of CBHP was about 160 nm,-24 mV,and the experiments of IR and DSC indicated CBHP was prepared successfully.The second section of this paper investigated the in vivo pharmacokinetics dynamics of CBHP in rats.This paper established a pre-column derivatization of HPLC-FLD method for the content determination of plasma samples of CBHP and studied the pharmacokinetics profile of CBHP in rats.The experimental showed that the CBHP extended half-life in rats,reduced the clearance rate,increased the in vivo retention time.The relative bioavailability of CBHP is 443.87 %,which showed that the CBHP significantly improved the oral bioavailability of CB.The third section of this paper studied the intestinal absorption of CBHP in SD rats.This paper established a pre-column derivatization of HPLC-FLD method for the content determination of in the intestinal absorption liquid of CBHP,and investigated the absorption of CBHP in the duodenum,jejunum,ileum and colon.The experimental showed that CBHP and CB are best absorbed in the ileum and CBHP significantly improved the absorption of CB in the small intestine of rat. |
PDF Full Text Request