Preparation of Clopidogrel Bisulfate Tablets and Optimization of the Formulation and Technology
10.6039/j.issn.1001-0408.2015.31.36
- VernacularTitle:硫酸氢氯吡格雷片的制备及其处方工艺优化
- Author:
Xia SUN
;
Xue WANG
;
Qingming GUO
;
Wei XIAO
- Publication Type:Journal Article
- Keywords:
Clopidogrel bisulfate tablet;
Formulation;
Technology;
Orthogonal test;
Optimization
- From:
China Pharmacy
2015;26(31):4429-4432
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To prepare Clopidogrel bisulfate tablets,and to optimize its formulation and technology. METHODS:The single factor test and compatibility test were used to optimize the fillers,disintegrating agents,adhesive,lubricants and prepa-ration technology;using sticking situation and disintegration time as indexes,the orthogonal test was used to optimize the amount of disintegrating agents [low substituted hydroxypropyl cellulose(L-HPC)],lubricants(hydrogenated vegetable oil and PEG6000), and the optimal technology was validated. The dissolution of prepared tablet and imported tablet(Plavix)in water,pH 2.0 hydro-chlorate buffer,pH 4.5 phosphate buffer(PBS)and pH 6.8 PBS were investigated,and influential factor test was conducted. RE-SULTS:Clopidogrel bisulfate tablets were prepared with dry granulating. The optimal formulation (1 000 tablets) was as follows as clopidogrel bisulfate 97.8 g,mannitol 84 g,amylum pregelatinisatum 36 g,L-HPC 8 g,hydrogenated vegetable oil 8 g, PEG6000 6 g;no tablet compressing sticking situation was found in prepared tablets and it owned medium disintegration time;ac-cumulative dissolution curves of prepared tablets in 4 kinds of medium were similar to those of Plavix;there were no significant dif-ference in results of influential factor test between prepared tablet and Plavix. CONCLUSIONS:Clopidogrel bisulfate tablets are prepared successfully,and the formulation is reasonable,practical,stable and controllable in quality.
