Preparation and in vitro evaluation of dabigatran etexilate nanoemulsion
10.11665/j.issn.1000-5048.20160610
- VernacularTitle:达比加群酯纳米乳的制备及体外评价
- Author:
Yajie ZHANG
1
;
Xiaoqing LIU
;
Min CHEN
;
Fujuan CHAI
;
Chunli ZHENG
;
Jianping LIU
Author Information
1. 中国药科大学药剂学教研室
- Publication Type:Journal Article
- Keywords:
dabigatran etexilate;
nanoemulsion;
pseudo-ternary diagrams;
orthogonal design;
weakly basic drug;
in vitro evaluation
- From:
Journal of China Pharmaceutical University
2016;47(6):688-693
- CountryChina
- Language:Chinese
-
Abstract:
The purpose of this study was to prepare dabigatran etexilate nanoemulsion to improve bioavailability of dabigatran etexilate, a poorly water-soluble drug. The physicochemical properties and the stability of dabigatran etexilate nanoemulsion were investigated. Equilibrium solubility of dabigatran etexilate in commonly used oil materials for nanoemulsion were determined for selection. Then, surfactant and co-surfactant were chosen based upon the plooted pseudo-ternary diagrams. The formulation and preparation process were further optimized with orthogonal design. As a result, the dabigatran etexilate nanoemulsion was formulated based on the system consisting of Oil Acid/Labrafac Lipophile WL1394/Cremophor RH40/Transcutol P/H2O. The dabigatran etexilate nanoemulsion was found to have a mean diameter of(57. 5±0. 2)nm, Zeta potential of -(20. 9±1. 4)mV, and the drug encapsulation efficiency of(85. 2±1. 0)%. Besides, the droplet size, stability constant and drug content of the nanoemulsion was found to have no significant changes in at least 3 months under room temperature. In conclusion, the uniform and stable dabigatran etexilate nanoemulsion with a clear and translucent appearance was obtained after the optimization of formulation and preparation process. Thus nanoemulsion could be a promising way for the improvement of bioavailability of dabigatran etexilate and other poorly water-soluble drugs.
