Preparation of chrysin-phospholipid complex and its pharmacokinetic behaviors / 中成药

ABSTRACT

AIM To prepare the chrysin-phospholipid complex and to investigate its pharmacokinetic behaviors.METHODS Solvent evaporation method was used for preparing the complex.With preparation temperature,preparation time,chrysin concentration and drug-lipid ratio (chrysin-phospholipid) as influencing factors,together with recombination rate as an evaluation index,the preparation was optimized by orthogonal test.The obtained complex was analyzed by X-ray diffraction,differential scanning calorimetry,1H-NMR and 31P-NMR,whose solubility was examined as well.SD rats were intragastrically administered with chrysin and its phospholipid complex,respectively.The blood concentration of chrysin was detected by HPLC,after which the pharmacokinetic parameters were calculated.RESULTS The optimal conditions were determined to be 40 ℃ for preparation temperature,2 h for preparation time,20 mg/mL for chrysin concentration,and 1 ∶ 2 for drug-lipid ratio,the recombination rate was close to 100％.Chrysin existed in an amorphous state in the phospholipid complex,which was a new phase rather than physical mixture (chrysin-phosphatidylcholine),and no new chemical bond was generated.Phospholipid complex could significantly increase chrysin's apparent solubility in water and n-octanol,the Cmax,AUC0-t and AUC0-∞ were also obviously increased as compared with raw medicine.CONCLUSION Phospholipid complex can improve both the solubility of chrysin and its oral bioavailability.