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采用响应面法对氟比洛芬进行天然胶基缓释骨架片的配方和评价。

Formulation and evaluation of natural gum-based sustained release matrix tablets of flurbiprofen using response surface methodology.

机构信息

Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.

出版信息

Drug Dev Ind Pharm. 2009 Dec;35(12):1470-8. doi: 10.3109/03639040903025848.

Abstract

BACKGROUND

This research work was done to design oral sustained release matrix tablets of water-insoluble drug, flurbiprofen, using natural gums as the matrix polymers and to evaluate the drug release characteristics using response surface methodology. The central composite design for two factors at five levels each was employed to systematically optimize drug release profile.

METHOD

Matrix tablets were prepared by direct compression technique. Xanthan and acacia gums were taken as the independent variables. Fourier transform infrared spectroscopy studies were also performed to find out the stability of drug during the direct compression and to check the interactions between polymers and drug. Percent drug release in 2 hours and percent drug release in 8 hours were taken as response variables (Y1 and Y2, respectively).

RESULTS

Both the polymers were found to have significant effect on the drug release. Polynomial mathematical models, generated for the response variables using multiple linear regression analysis, were found to be statistically significant (P < 0.05). Contour plots were drawn to depict the relationship between response variables and independent variables.

CONCLUSION

The formulated matrix tablets followed zero-order kinetics with negligible drug release in 0.1 N HCl at pH 1.2, which was the objective of this study to produce a formulation avoiding the gastric effects of flurbiprofen.

摘要

背景

本研究旨在设计一种水不溶性药物氟比洛芬的口服缓释基质片,使用天然胶作为基质聚合物,并采用响应面法评价药物释放特性。采用两因素五水平的中心复合设计,系统优化药物释放曲线。

方法

采用直接压片技术制备基质片。黄原胶和阿拉伯胶作为自变量。还进行了傅里叶变换红外光谱研究,以确定药物在直接压片过程中的稳定性,并检查聚合物与药物之间的相互作用。以 2 小时和 8 小时的药物释放百分率(分别为 Y1 和 Y2)作为响应变量。

结果

两种聚合物均对药物释放有显著影响。使用多元线性回归分析生成的响应变量的多项式数学模型在统计学上具有显著性(P<0.05)。绘制了轮廓图以描绘响应变量与自变量之间的关系。

结论

所制备的基质片符合零级动力学,在 pH 1.2 的 0.1N HCl 中药物释放可忽略不计,这是本研究的目的,即生产一种避免氟比洛芬胃作用的制剂。

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