栀子苷磷脂复合物的制备及评价

摘要

采用溶剂挥发法制备栀子苷磷脂复合物(GE-PLC),以提高栀子苷的口服生物利用度,并利用单因素试验优化制备工艺.采用UV,IR和DSC对GE-PLC进行表征,并测定了大鼠口服给药的药动学参数.结果表明:优化的制备工艺为以无水乙醇为反应溶剂,栀子苷与磷脂的质量比m(栀子苷):m(磷脂)=1:4,栀子苷质量浓度16.7mg/mL,40℃条件下反应1.5h.物性表征显示栀子苷与磷脂未形成新的化合物,GE-PLC的脂溶性约为栀子苷的15倍.药动学结果显示GE-PLC的药时曲线下面积为栀子苷的1.63倍.GE-PLC制备工艺稳定且复合率较高,脂溶性得到明显改善,促进了栀子苷的吸收,可见磷脂复合物对水溶性好、膜渗透性差的药物提高生物利用度有较好的作用.%To improve the oral bioavailability of geniposide, geniposide phospholipids complex (GE-PLC) was prepared by solvent evaporation method,and the preparation technology was optimized by single factor test. Then the products were evaluated by UV, IR and DSC. Moreover,the pharmacokinetic parameters of rats were calculated after oral administration.The results showed that the optimal preparation procedures of GE-PLC were as follows :anhydrous ethanol was used as reaction medium,the quality ratio of GE to phospholipid was 1:4,reaction concentration of GE was 16.7 mg/mL,reaction temperature and time were 40 ℃ and 1.5 h respectively.The physicochemical properties indicated that there were no new compounds formed during preparation process and the lipid solubility of GE-PLC was about 15 times higher than that of GE.The AUC of GE-PLC was 1.63 times as large as GE.The preparation technology of GE-PLC was stable and the recombination rate was enhanced.In addition,the lipid solubility of GE was enhanced significantly and drug absorption was promoted. These results demonstrated phospholipids complex could improve the bioavailability of drugs which had good water-solubility and poor membrane permeability.