黄芩苷纳米晶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].
作者信息
Jin Shi-Ying, Yuan Hai-Long, Jin Shi-Xiao, Lv Qing-Yuan, Bai Jin-Xia, Han Jin
机构信息
School of Pharmaceutical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu 611730, China.
出版信息
Zhongguo Zhong Yao Za Zhi. 2013 Apr;38(8):1156-9.
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 C(max) was (16.54 +/- 1.73) mg x L(-1) and the AUC(0-24 h) was (206.96 +/- 21.23) mg x L(-1) x h, which were significantly enhanced compared with the baicalin bulk and baicalin physical mixture (BC-PM) formulation, respectively (P < 0.01).
CONCLUSION
Baicalin nanocrystal can significantly improve the bioavailability of baicalin.
目的
制备黄芩苷纳米晶体（BC-NC）并评价其在大鼠体内的药代动力学。
方法
采用高压均质技术结合超声法制备黄芩苷纳米混悬液（BC-NS），然后通过流化床干燥除水将BC-NS固化成BC-NC微丸。测定其形态、平均粒径和Zeta电位。采用高效液相色谱法测定血浆中黄芩苷的浓度，并通过Wistar大鼠口服给药，将纳米晶体与参比组的生物利用度进行比较。
结果
扫描电子显微镜观察到的纳米晶体为不规则颗粒状，BC-NC的平均粒径为（248±6）nm。其多分散指数（PI）和Zeta电位分别为（0.181±0.065）、（-32.3±1.8）mV。药代动力学参数显示，Cmax为（16.54±1.73）mg·L-1，AUC(0-24 h)为（206.96±21.23）mg·L-1·h，分别与黄芩苷原料药和黄芩苷物理混合物（BC-PM）制剂相比显著提高（P<0.01）。
结论
黄芩苷纳米晶体可显著提高黄芩苷的生物利用度。
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