目的 制备及表征葛根素壳聚糖/海藻酸钠口服纳米粒（Pur-CS/SA-NPs），并进行药动学研究。方法 采用自组装法制备Pur-CS/SA-NPs，对Pur-CS/SA-NPs混悬液和冻干粉的形态、粒径、多分散指数（PDI）、Zeta电位、包封率、载药量、微观结构等进行表征；建立葛根素LC-MS/MS分析方法，测定大鼠口服给予Pur-CS/SA-NPs后血浆中葛根素的浓度，考察其药动学特征。结果 Pur-CS/SA-NPs混悬液和冻干粉的形态结构完整，其中Pur-CS/SA-NPs混悬液的粒径为（208.327±1.870）nm，PDI为0.131±0.006，包封率为（89.056±1.680）%，载药量为（44.528±0.840）%，Pur-CS/SA-NPs冻干粉的粒径为（260.000±0.475）nm，Zeta电位为（47.300±0.208）mV，包封率为（86.234±0.873）%，载药量为（43.117±0.234）%，无新化学键和晶体形成；Pur-CS/SA-NPs的药时曲线下面积（AUC_0～24和AUC_0～∞）、达峰时间（t_max）、达峰浓度（C_max）分别为（833.067±132.546）mg·h/L、（844.919±154.768）mg·h/L、（1.000±0.098）h、（236.318±36.864）mg/L，葛根素的AUC_0～24、AUC_0～∞、t_max、C_max分别为（250.087±32.156）mg·h/L、（250.091±28.398）mg·h/L、（0.500±0.031）h、（191.830±17.963）mg/L，Pur-CS/SA-NPs的AUC_0～24、AUC_0～∞、t_max、C_max分别为葛根素的3.331、3.378、2.000、1.232倍。结论 自组装法制备的Pur-CS/SA-NPs形态结构稳定，口服给药后药物在体内的AUC_0～24、AUC_0～∞、t_max均显著增大，循环时间也相对延长，显著提高了葛根素的生物利用度。

Objective To prepare and characterize puerarin chitosan/sodium alginate oral nanoparticles (Pur-CS/SA-NPs) and conduct its pharmacokinetics studies. Methods Pur-CS/SA-NPs were prepared by self-assembly method, the morphology, particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, drug loading and microstructure of Pur-CS/SA-NPs suspension and lyophilized powder were characterized. To determine the concentration of puerarin in plasma after oral administration of nanoparticles to rats, an LC-MS/MS analysis method for puerarin was established, and its pharmacokinetic characteristics were investigated. Results The morphology, structure and texture of Pur-CS/SA-NPs suspension and lyophilized powder were complete and fine, no new chemical bonds and crystals were formed. The particle size, PDI, Zeta potential, encapsulation efficiency, and drug loading of Pur-CS/SA-NPs suspension were (208.327 ±1.870) nm, 0.131 ±0.006, (89.056 ±1.680)% and (44.528 ±0.840)%, respectively. The particle size, Zeta potential, encapsulation efficiency and drug loading of Pur-CS/SA-NPs lyophilized powder were (260.000 ±0.475) nm, (47.300 ±0.208) mV, (86.234 ±0.873)% and (43.117 ±0.234)%, respectively. The AUC_0-24, AUC_0-∞, t_max and C_max of Pur-CS/SA-NPs were (833.067 ±132.546) mg∙h/L, (844.919 ±154.768) mg∙h/L, (1.000 ±0.098) h and (236.318 ±36.864) mg/L, respectively. The AUC_0-24, AUC_0-∞, t_max and C_max of puerarin were (250.087 ±32.156) mg∙h/L, (250.091 ±28.398) mg∙h/L, (0.500 ±0.031) h and (191.830 ±17.963) mg/L, respectively. The AUC_0-24, AUC_0-∞, t_max and C_max of Pur-CS/SA-NPs were 3.331, 3.378, 2.000, and 1.232 times of puerarin, respectively. Conclusion The structure of Pur-CS/SA-NPs prepared by self-assembly method is stable. After oral administration, the AUC_0-24, AUC_0-∞ and t_max of the drug in the body are significantly increased, and the circulation time is relatively extended, which significantly improve bioavailability of puerarin.

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国家重点研发计划中医药现代化研究重点专项（2017YFC1702904）；国家重点研发计划中医药现代化研究重点专项（2018ZX09721002）；江西省教育厅科技计划项目（GJJ170718）；中药学一流学科科研项目（JXSYLXK-ZHYAO049）