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目的研究葛根素壳聚糖微球在大鼠体内药动学过程,为葛根素壳聚糖微球的药效学研究提供参考。方法采用乳化-交联法制备葛根素壳聚糖微球,高效液相色谱法测定葛根素在大鼠体内血药浓度,使用3P97药动学软件计算药动学参数。结果葛根素壳聚糖微球的粒径范围为20~40μm,平均粒径为27.8μm,葛根素的包封率为65.8%,载药量为29.0%。葛根素壳聚糖微球在大鼠体内药动学过程均符合二室模型,微球中葛根素的达峰时间明显比葛根素样品推迟,药-时曲线下面积AUC比葛根素样品大,说明葛根素壳聚糖微球有缓释作用。结论以壳聚糖为载体,采用乳化-交联法制备葛根素壳聚糖微球具有缓释作用。
Objective To study the pharmacokinetics of puerarin chitosan microspheres in rats and provide reference for the pharmacodynamics study of puerarin chitosan microspheres. Methods The puerarin chitosan microspheres were prepared by emulsion-crosslinking method. The plasma concentrations of puerarin in rats were determined by HPLC. Pharmacokinetic parameters were calculated by 3P97 pharmacokinetic software. Results The particle size range of puerarin chitosan microspheres was 20-40 μm, the average particle size was 27.8 μm, the encapsulation efficiency of puerarin was 65.8% and the drug loading was 29.0%. The pharmacokinetics of puerarin chitosan microspheres in rats were in accordance with the two-compartment model. The peak time of puerarin in microspheres was obviously delayed than that of puerarin. The area under curve of drug-time curve was larger than that of puerarin, Description of puerarin chitosan microspheres slow release. Conclusion Chitosan as a carrier, prepared by emulsion - crosslinking puerarin chitosan microspheres with sustained-release effect.