黄芩苷纳米晶体微丸的制备及其药代动力学初步研究  

Preparation of baicalin nanocrystal pellets and preliminary study on its pharmacokinetics

作　　者：靳世英[1,2] 袁海龙[2] 靳士晓[1,2] 吕青远[2] 白金霞[1,2] 韩晋[2] 

机构地区：[1]成都中医药大学药学院,四川成都611730 [2]解放军302医院,北京100039

出　　处：《中国中药杂志》2013年第8期1156-1159,共4页China Journal of Chinese Materia Medica

基　　金：北京市自然科学基金项目(7122176)

摘　　要：目的:该研究制备了黄芩苷纳米晶体(baicalin nanocrystal,BC-NC),并进行了大鼠体内药物动力学研究。方法:采用探头超声结合高压均质法制备黄芩苷纳米混悬剂,然后通过流化干燥工艺将其脱水干燥成固体微丸,考察纳米晶体的形态、粒径分布、Zeta电位。以黄芩苷为指标成分,采用HPLC测定大鼠灌胃给药后的血药浓度,用DAS 2.0药动学软件计算药代动力学参数。结果:黄芩苷纳米晶体在扫描电镜下呈不规则颗粒状,平均粒径(248±6)nm,多分散指数(PI)为(0.181±0.065),Zeta电位为(-32.3±1.8)mV。BC-NC达峰浓度(Cmax)为(16.51±1.73)mg.L-1,0～24 h的药时曲线下面积(AUC)增加为(206.96±21.23)mg.L-1.h,与黄芩苷原料药及物理混合物相比均有显著性提高(P<0.01)。结论:通过高压均质及流化干燥工艺制得的黄芩苷纳米晶体能显著提高药物体内生物利用度,有望进一步制成口服固体制剂。Objective： To prepare baicalin nanocrystal （BC-NC） and evaluate its pharmacokinetics in rats. Method： Baicalin nanosuspensions （BC-NS） were prepared by the high pressure homogenization technology combined with ultrasonic, and then BC-NS were solidificated into BC-NC pellets by removing the water through fluid-bed drying. Its morphology, mean diameter and Zeta-potential were determined. An HPLC method was employed to determine the concentration of baicalin in plasma, and the bioavailability of the nanocrystal was compared with the reference group by oral administration in Wistar rats. Result： The nanocrystals observed by scanning electron microscopy were irregular granulated, and the mean particle sizes of BC-NC were （248± 6 ） nm. Its polydispersity index （PI） and zeta-potential were （0. 181±0. 065）, （ -32. 3 ± 1.8） mV, respectively. The pharmacokinetic parameters showed that the Cmaxwas （16. 54± 1.73） mg ·L^-1 and the AUC0.24h was （206. 96±21.23） mg ·L^-1· h, which were significantly enhanced com- pared with the baicalin bulk and baicalin physical mixture （BC-PM） formulation, respectively （P 〈 0.01 ）. Conclusion： Baicalin nanoerystal can significantly improve the bioavailability of baicalin.

关 键 词：黄芩苷 纳米晶体 高压均质 流化干燥 药代动力学 

分 类 号：R286[医药卫生—中药学]