星点设计-响应面法优化米拉贝隆缓释片处方

发布时间：2018-08-20 14:56

【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p H介质(水、p H 1.0的人工胃液、p H 4.5醋酸盐缓冲液、p H 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p H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 Milabelon sustained-release tablets. Methods: Milabelon sustained-release tablets were prepared by direct pressing of polyoxyethylene (PEO) and hydroxypropylmethyl cellulose (HPMC K 4M) as sustained-release matrix materials. Based on the cumulative release rate for 7 h, PEOHPMC K4M and OPADRYL? were optimized by star design-response surface method (RSM). The amount used is verified. The cumulative release rates of (MyrbetriqTM) in different pH medium (pH 4.5 acetate buffer solution, pH 6.8 phosphate buffer) in different pH medium (100 渭 m 50 r/min) were compared between the prepared sustained-release tablets and the original laminated tablets. The similarity factor f 2 was calculated and the drug release model of sustained-release tablets was fitted. Results: each Milabelon sustained-release tablet contained 25 mg / g PEO 108.02 mg / g of Mira Belon, and the relative error between the cumulative release and the predicted value was 4.783.480.691.41 and 1.41, respectively, and the score of OPADRYN was 2.27.The relative error of the cumulative release rate and the predicted value was 4.78 ~ 3.480.691.41, and the relative error between the cumulative release and the predicted value was 4.78 ~ 3.480.69 ~ 1.41, and the relative error between the cumulative release and the predicted value was 4.78 ~ 3.480.691.41. The release curves of sustained-release tablets and original tablets were higher than 65 in different pH media and at different rotational speeds, and the release of sustained-release tablets was in accordance with the characteristics of zero-order release. Conclusion: the release behavior of Milabelon sustained-release tablets prepared by optimized formulation is similar to that of original tablets.
【作者单位】：南京工业大学药学院;江苏省药物研究所有限公司;中国药科大学药学院;
【分类号】：R943

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