Preparation and Evaluation of Atorvastatin Calcium and Ezetimibe Self-microemulsifying Tablets
- VernacularTitle:复方阿托伐他汀钙依泽麦布自微乳化片剂的制备与评价
- Author:
Ying ZHENG
1
;
Meiyuan WU
Author Information
1. 岱山县中医院药剂科 浙江舟山316200
- Keywords:
Atorvastatin calcium;
Estazolam;
Self-microemulsifying drug delivery system;
Tablets;
Pseudo-ternary phase dia-gram;
In vitro dissolution
- From:
China Pharmacist
2017;20(11):1987-1992
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To prepare the self-microemulsifying drug delivery system (SMEDDS) and relevant tablets of atorvastatin calcium and ezetimibe(Ato-Eze),and investigate the in vitro release of Ato-Eze SMEDDS tablets. Methods:The solubility and excip-ient compatibility of Ato and Eze in different excipients were investigated. The pseudo-ternary phase diagram composed of different oil phase,emulsifier and co-emulsifier was used to obtain the self-emulsifying area. The morphology,particle size distribution and zeta po-tential of microemulsion were determined by a dilution method. The optimal formula of Ato-Eze SMEDDS was prepared into tablets. The drug release profiles of the commercial formula,Ato-Eze SMEDDS and Ato-Eze SMEDDS tablets were compared. Results:The op-timal formula was as follows:propylene glycol monocaprylate as the oil phase,Solutol HS 15 as the surfactant and polyethylene glycol 600 as the co-surfactant with the best ratio of 5 :3.75:1.25. Ato-Eze SMEDDS was a clear and transparent microemulsion solution with homogeneous small spheres as seen under a transmission electron microscope. The particle size and zeta potential of Ato-Eze SMEDDS was(44.2 ± 19.5) nm and( -24.1 ± 1.3) mV,respectively. The in vitro release profile indicated that the accumulated re-lease of Ato-Eze SNEDDS and the tablets reached up to nearly 100% in 45 min. Conclusion: Ato-Eze SMEDDS tablets can signifi-cantly improve the in vitro dissolution rates of the two drugs,and the preparation process is simple and feasible.
