作者：赵安权¹, 王倩倩¹, 李佳¹, 樊萌春², 贺英菊¹

作者单位：1. 四川大学华西药学院, 四川 成都 610041;
2. 贵州椿树中药科技有限公司, 贵州 贵阳 550005

关键词：绿原酸; 磷脂复合物; 固体分散体; 溶出度; 药动学; 口服生物利用度

摘要：

为研究绿原酸磷脂复合物固体分散体(CA-PC-SD)的体外溶出以及体内药动学规律,采用HPLC法考察CAPC-SD的体外溶出,大鼠灌胃后测定其血药浓度,并采用DAS 2.0软件分析计算药动学参数。结果显示:CA-PC-SD显著改善绿原酸磷脂复合物(CA-PC)的溶出效果,相较于原料药(CA)其相对生物利用度提高2.12倍。表明CA-PCSD能显著改善CA-PC的体外溶出特性以及CA的口服生物利用率。

Dissolution behavior in vitro and pharmacokinetic profile of chlorogenic acid phospholipid complex solid dispersion in rats

ZHAO Anquan¹, WANG Qianqian¹, LI Jia¹, FAN Mengchun², HE Yingju¹

1. West China School of Pharmacy, Sichuan University, Chengdu 610041, China;
2. Guizhou Chunshu Chinese Medicine Technology Co., Ltd., Guiyang 550005, China

Abstract: To study the chlorogenic acid phospholipid complex solid dispersion (CA-PC-SD)dissolution behavior of CA in vitro and pharmacokinetics of CA in the rats. The dissolution behavior of CA-PC-SD in vitro and plasma concentration of CA in rats was determined by HPLC. The pharmacokinetic parameters were estimated by DAS VER2.0 software. Results show that in vitro dissolution of CA-PC-SD is obviously greater than CA-PC. The oral bioavailability of CA-PC-SD is increased 2.12 times than CA. CA-PC-SD can significantly improve dissolution characters of CA-PC in vitro as well as the oral bioavailability of CA in rats.

Keywords: chlorogenic acid; phospholipid complex; solid dispersion; dissolution; pharmacokinetics; oral bioavailability

2015, 41(1): 54-57  收稿日期: 2014-3-15;收到修改稿日期: 2014-5-17

基金项目: 

作者简介: 赵安权(1989-),男,湖南常德市人,硕士研究生,专业方向为药剂学。

参考文献

[1] 吴江涛. 绿原酸的生物活性及其应用[J]. 现代农业科技,2009(19):349-350.
[2] 江永南,莫红缨,陈济民. 淫羊霍黄酮磷脂复合物大鼠体内药动学[J]. 中国医院药学杂志,2002,22(10):105-08.
[3] 黄毅,闫明,康爱荣,等. 阿苯达唑固体分散体体外溶出和大鼠体内药动学研究[J]. 中国新药杂志,2009,18(23):2259-2263.
[4] Silav T D, Arantes V T, Resende J A, et al. Preparation and characterization of solid dispersion of simvastain[J]. Drug Dev Ind Pharm,2010,14(6):312-317.
[5] 夏枚,张亚兰,高敬轩,等. 绿原酸生物粘附微球的制备及体外释放特性研究[J]. 华西药学杂志,2012,27(2):153-155.
[6] Vertzoni M V, Reppas C, Archontaki H A. Optimized determination of lycopene in canine plasma using reversed phase high performance liquid chromatograph y[J]. J Chromatogr B,2005,819(1):149-154.
[7] 国家药典委员会.中华人民共和国药典[S].北京:中国医药科技出版社,2010.
[8] 龚显峰,李述溪,赵学玲,等. 葛根素固体分散体的制备及大鼠体内生物利用度研究[J]. 黑龙江医药,2009,22(2):157-160.