Optimization of Mirabegron Sustained-release Tablets by Central Composite Design-response Surface Meth-od
10.6039/j.issn.1001-0408.2017.01.29
- VernacularTitle:星点设计-响应面法优化米拉贝隆缓释片处方
- Author:
Bin XU
;
Yuwei PU
;
Wei ZHOU
;
Yimei DING
;
Dingqiang LU
- Keywords:
Mirabegron;
Sustained-release tablet;
Central composite design-response surface method;
Formulation optimiza-tion;
Accumulative release rate
- From:
China Pharmacy
2017;28(1):110-114
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To optimize the formulation of Mirabegron sustained-release tablets. METHODS:Using polyethylene oxide(PEO)and hydroxypropylmethyl cellulose(HPMC K4M)as the sustained release matrix,Mirabegron sustained-release tab-lets were prepared by powder direct compression technology. Using 1,3,5,7 h accumulative release rate as indexes,the amounts of PEO,HPMC K4M and OPADRY? were optimized by composite design-response surface method,and then validated. Accumula-tive release rates of sustained-release tablet and original tablet (MyrbetriqTM) were compared in different pH mediums (water,pH 1.0 simulated gastric fluid,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution) at different rotation rates (100,50 r/min),and similiar factor f2 was calculated to fit drug release model of sustained-release tablet. RESULTS:In the optimized firmu-lation each Mirabegron sustained-release tablet contained mirabegron 25 mg,PEO 108.02 mg,HPMC K4M 21.69 mg,OPADRY? 2.27%. Relative error of accumulative release rates at 1,3,5,7 h to predicted value were 4.78%,3.48%,0.69% and -1.41%, respectively. f2 of release curves of sustained-release tablet and original tablet were higher than 65 in different pH medium at differ-ent rotation rates. The drug release of sustained-release tablet was fitted to zero-order release equation. CONCLUSIONS:Mirabe-gron sustained-release tablet by optimized technology is similar to original tablet in drug release behavior.
