Self-Nanoemulsifying Drug Delivery System of Tetrandrine for Improved Bioavailability: Physicochemical Characterization and Pharmacokinetic Study.
Self-Nanoemulsifying Drug Delivery System of Tetrandrine for Improved Bioavailability: Physicochemical Characterization and Pharmacokinetic Study.
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用于改善生物利用度的粉防己碱自纳米乳化给药系统的理化表征和药代动力学研究
DOI：
10.1155/2018/6763057
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发表时间：
2018
影响因子：
--
通讯作者：
Huang X
中科院分区：
文献类型：
--
作者：
Liu C;Lv L;Guo W;Mo L;Huang Y;Li G;Huang X
The main purpose of this study was to investigate the potential of self-nanoemulsified drug delivery system (SNEDDS) to improve the oral bioavailability of tetrandrine (Tet). SNEDDS was developed by using rational blends of excipients with good solubilizing ability for Tet which was selected based on solubility studies. Further ternary phase diagram was constructed to determine the self-emulsifying region. The optimal formulation with the best self-nanoemulsified and solubilization ability consisted of 40% (w/w) oleic acid as oil, 15% (w/w) SPC and 30% (w/w) Cremophor RH-40 as surfactant, and 15% (w/w) PEG400 as cosurfactant. The average droplet size and zeta-potential of the optimal Tet SNEDDS were 19.75±0.37 nm and 1.87±0.26 mv, respectively. The dissolute rate of Tet SNEDDS in various dissolution media was remarkably faster than Tet commercial tablet. Moreover, in vivo pharmacokinetic study results show that significant increase (p≤ 0.05) in the peak concentration (Cmax) and the area under the curve (AUC) of Tet was observed after the oral administration of Tet SNEDDS and the absorption of Tet from SNEDDS resulted in approximately 2.33-fold increase in oral bioavailability compared with the commercial tablet. Our research suggests that the prepared Tet SNEDDS could be a good candidate for improved the dissolution and oral bioavailability of Tet.
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DOI：
10.2147/dddt.s103169
发表时间：
2016
期刊：
Drug design, development and therapy
影响因子：
--
作者：
Guo K;Cang J
通讯作者：
Cang J
影响因子：
16.1
作者：
Porter, Christopher J. H.;Pouton, Colin W.;Charman, William N.
通讯作者：
Charman, William N.
影响因子：
2.9
作者：
Qiu, Wei;Zhang, Ai-Li;Tian, Ye
通讯作者：
Tian, Ye
影响因子：
5.2
作者：
Chen, Qian-Zhao;Li, Yang;He, Bai-Cheng
通讯作者：
He, Bai-Cheng
影响因子：
5.8
作者：
Pang, LH;Hoult, JRS
通讯作者：
Hoult, JRS