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星点设计-响应面法优化米拉贝隆缓释片处方
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| 篇名： | 星点设计-响应面法优化米拉贝隆缓释片处方 |
| TITLE： | |
| 摘要： | 目的：优化米拉贝隆缓释片处方。方法：采用聚氧乙烯（PEO）和羟丙甲基纤维素（HPMC K4M）为缓释骨架材料，以粉末直压法制备米拉贝隆缓释片。以1、3、5、7 h的累积释放度为指标，采用星点设计-响应面法优化处方中PEO、HPMC K4M和包衣液（OPADRY®）的用量，并进行验证。比较所制缓释片与原研片（MyrbetriqTM）在不同pH介质（水、pH 1.0的人工胃液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液）中不同转速（100、50 r/min）下的累积释放度，计算相似因子f2，拟合缓释片的释药模型。结果：优化处方中每片米拉贝隆缓释片含米拉贝隆25 mg、PEO 108.02 mg、HPMC K4M 21.69 mg、OPADRY® 2.27％；其1、3、5、7 h的累积释放度与预测值的相对误差分别为4.78％、3.48％、0.69％、－1.41％。所制缓释片与原研片在不同pH介质中和不同转速下释放曲线的f2均大于65；缓释片释药符合零级释药特征。结论：优化处方制备的米拉贝隆缓释片与原研片的释放行为相似。 |
| 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 tablets 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. Accumulative 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 firmulation 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 different rotation rates. The drug release of sustained-release tablet was fitted to zero-order release equation. CONCLUSIONS： Mirabegron sustained-release tablet by optimized technology is similar to original tablet in drug release behavior. |
| 期刊： | 2017年第28卷第1期 |
| 作者： | 徐斌，浦雨伟，周卫，丁逸梅，卢定强 |
| AUTHORS： | XU Bin，PU Yuwei，ZHOU Wei，DING Yimei，LU Dingqiang |
| 关键字： | 米拉贝隆；缓释片；星点设计-响应面法；处方优化；累积释放度 |
| KEYWORDS： | Mirabegron； Sustained-release tablet； Central composite design-response surface method； Formulation optimization； Accumulative release rate |
| 阅读数： | 1058 次 |
| 本月下载数： | 17 次 |
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