黄芩苷类脂纳米囊制剂的制备及大鼠口服药物动力学

doi:10.6040/j.issn.1671-7554.0.2015.303

山东大学学报（医学版） ›› 2016, Vol. 54 ›› Issue (1): 22-28.doi: 10.6040/j.issn.1671-7554.0.2015.303

黄芩苷类脂纳米囊制剂的制备及大鼠口服药物动力学

穆军^1,2,单丽娜³,翟英杰²,翟光喜²

1.胜利石油管理局胜北医院药剂科, 山东东营 257064;
2.山东大学药学院药剂教研室, 山东济南 250012;
3.胜利石油管理局胜北医院中医科, 山东东营 257064

收稿日期:2015-03-20 出版日期:2016-01-11 发布日期:2016-01-11
通讯作者: 翟光喜. E-mail:zkyjd@sdu.edu.cn E-mail:zkyjd@sdu.edu.cn

Preparation and pharmacokinetics of baicalin lipid nanocapsules

MU Jun^1,2, SHAN Lina³, ZHAI Yingjie², ZHAI Guangxi²

1. Department of Pharmacy, Shengbei Hospital, Shengli Petroleum Administrative Bureau, Dongying 257064, Shandong, China;
2. Department of Pharmaceutics, College of Pharmaceutical Science, Shangdong University, Jinan 250012, Shandong, China;
3. Department of Traditional Chinese Medicine, Shengbei Hospital, Shengli Petroleum Administrative Bureau, Dongying 257064, Shandong, China

Received:2015-03-20 Online:2016-01-11 Published:2016-01-11

摘要/Abstract

摘要： 目的制备黄芩苷类脂纳米囊(BA-LNC)并考察其理化性质和大鼠口服药物动力学。方法以中链甘油三酯(MCT)为油相,聚乙二醇单硬脂酸酯(Solutol HS15)为表面活性剂,卵磷脂为助乳化剂,采用相转化法制备类脂纳米囊(LNC),以包封率(EE)和载药量(DL)为指标,通过单纯形网格法对处方因素进行优化,采用响应面法对实验结果进行处理,得最优处方。采用Wistar大鼠研究BA-LNC制剂的口服药物动力学。结果制备的BA-LNC包封率为92.58%,载药量为1.69%。在透射电镜下BA-LNC呈类球形,分散良好,无粘连,平均粒径为(84.2±1.7)nm,多分散指数为0.201,Zeta电位为(-13.2±0.62)mV,制剂可显著延长药物在体内的滞留时间,增大其口服吸收。结论 BA-LNC可显著增大黄芩苷的口服生物利用度。

关键词: 黄芩苷, 类脂纳米囊, 单纯形网格法, 相转化法

Abstract: Objective To prepare the novel baicalin-lipid nanocapsules(BA-LNC)and to detect the physical and chemical properties and the pharmacokinetics. Methods With the medium chain triglyceride(MCT)as oil phase,polyethylene glycol monostearate as surface active agent, lecithin as auxiliary emulsifier, lipid nanocapsules(LNC)were prepared by the phase inversion method and evaluated with encapsulation efficiency(EE)and drug loading(DL). The formulation was optimized by the simplex lattice method and the optimal prescription was obtained by a response surface method. The pharmacokinetic study was also conducted in Wistar rats to explore the potential of LNC as carriers of baicalin. Results The EE was 92.58% and the DL was 1.69%. Under the transmission electron microscope, BA-LNC was spherical without adhesion. The average particle size was(84.2±1.7)nm with the polydispersity index being 0.201, and the Zeta potential was(-13.2±0.62)mV. BA-LNC could significantly prolong the residence time of drug in vivo, and obviously improve the oral absorption of baicalin. Conclusion The prepared lipid nanocapsules can obviously increase the oral bioavailability of baicalin.

Key words: Baicalin, Phase inversion-based method, Simplex lattice, Lipid nanocapsules

中图分类号:

R944.1

穆军,单丽娜,翟英杰,翟光喜. 黄芩苷类脂纳米囊制剂的制备及大鼠口服药物动力学[J]. 山东大学学报（医学版）, 2016, 54(1): 22-28.

MU Jun, SHAN Lina, ZHAI Yingjie, ZHAI Guangxi. Preparation and pharmacokinetics of baicalin lipid nanocapsules[J]. JOURNAL OF SHANDONG UNIVERSITY (HEALTH SCIENCES), 2016, 54(1): 22-28.

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黄芩苷类脂纳米囊制剂的制备及大鼠口服药物动力学

Preparation and pharmacokinetics of baicalin lipid nanocapsules

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