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多组分羟丙基甲基纤维素基质片剂中的聚合物渗透阈值

Polymer Percolation Threshold in Multi-Component HPMC Matrices Tablets.

作者信息

Maghsoodi Maryam, Barghi Leila

机构信息

School of Pharmacy and Drug applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Adv Pharm Bull. 2011;1(1):27-33. doi: 10.5681/apb.2011.004. Epub 2011 Jul 20.

Abstract

INTRODUCTION

The percolation theory studies the critical points or percolation thresholds of the system, where one component of the system undergoes a geometrical phase transition, starting to connect the whole system.The application of this theory to study the release rate of hydrophilic matrices allows to explain the changes in release kinetics of swellable matrix type system and results in a clear improvement of the design of controlled release dosage forms.

METHODS

In this study, the percolation theory has been applied to multi-component hydroxypropylmethylcellulose (HPMC) hydrophilic matrices. Matrix tablets have been prepared using phenobarbital as drug, magnesium stearate as a lubricant employing different amount of lactose and HPMC K4M as a filler and matrix forming material, respectively. Ethylcelullose (EC) as a polymeric excipient was also examined. Dissolution studies were carried out using the paddle method.In order to estimate the percolation threshold, the behaviour of the kinetic parameters with respect to thevolumetric fraction of HPMC at time zero, was studied.

RESULTS

In both HPMC/lactose and HPMC/EC/lactose matrices, from the point of view of the percolation theory, the optimum concentration for HPMC, to obtain a hydrophilic matrix system for the controlled release of phenobarbital is higher than 18.1% (v/v) HPMC. Above 18.1% (v/v) HPMC, an infinite cluster of HPMC would be formed maintaining integrity of the system and controlling the drug release from the matrices. According to results, EC had no significant influence on the HPMC percolation threshold.

CONCLUSION

This may be related to broad functionality of the swelling hydrophilic matrices.

摘要

引言

渗流理论研究系统的临界点或渗流阈值,在该点系统的一个组分经历几何相变,开始连接整个系统。将该理论应用于研究亲水性基质的释放速率,可以解释可溶胀基质型系统释放动力学的变化,并显著改进控释剂型的设计。

方法

在本研究中,渗流理论已应用于多组分羟丙基甲基纤维素(HPMC)亲水性基质。以苯巴比妥为药物,硬脂酸镁为润滑剂,分别使用不同量的乳糖和HPMC K4M作为填充剂和基质形成材料制备基质片剂。还考察了乙基纤维素(EC)作为聚合物辅料的情况。采用桨法进行溶出度研究。为了估计渗流阈值,研究了动力学参数在时间为零时相对于HPMC体积分数的行为。

结果

从渗流理论的角度来看,在HPMC/乳糖和HPMC/EC/乳糖基质中,获得用于苯巴比妥控释的亲水性基质系统的HPMC最佳浓度高于18.1%(v/v)HPMC。高于18.1%(v/v)HPMC时,将形成HPMC的无限簇,维持系统的完整性并控制药物从基质中的释放。根据结果,EC对HPMC渗流阈值没有显著影响。

结论

这可能与溶胀亲水性基质的广泛功能有关。

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