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含具有塑性/脆性和塑性/塑性变形特性辅料的二元混合片剂渗滤阈值的比较研究

Comparison studies on the percolation thresholds of binary mixture tablets containing excipients of plastic/brittle and plastic/plastic deformation properties.

作者信息

Amin Mohd C I, Fell John T

机构信息

Department of Pharmacy, Faculty of Allied Health Sciences, Universiti Kebangsaan, Malaysia, Kuala Lumpur, Malaysia.

出版信息

Drug Dev Ind Pharm. 2004;30(9):937-45. doi: 10.1081/ddc-200034998.

Abstract

Percolation theory has been used with great interest in understanding the design and characterization of dosage forms. In this study, work has been carried out to investigate the behavior of binary mixture tablets containing excipients of similar and different deformation properties. The binary mixture tablets were prepared by direct compression using lactose, polyvinyl chloride (PVC), Eudragit RS 100, and microcrystalline cellulose (MCC). The application of percolation theory on the relationships between compactibility, Pmax, or compression susceptibility (compressibility), gamma, and mixture compositions reveals the presence of percolation thresholds even for mixtures of similar deformation properties. The results showed that all mixture compositions exhibited at least one discreet change in the slope, which was referred to as the percolation threshold. The PVC/Eudragit RS100 mixture compositions showed significant percolation threshold at 80% (w/w) PVC loading. Two percolation thresholds were observed from a series of binary mixtures containing similar plastic deformation materials (PVC/MCC). The percolation thresholds were determined at 20% (w/w) and 80% (w/w) PVC loading. These are areas where one of the components percolates throughout the system and the properties of the tablets are expected to experience a sudden change. Experimental results, however, showed that total disruption of the tablet physical properties at the specified percolation thresholds can be observed for PVC/lactose mixtures at 20-30% (w/w) loading while only minor changes in the tablets' strength for PVC/MCC or PVC/Eudragit RS 100 mixtures were observed.

摘要

渗流理论在理解剂型的设计和特性方面引起了极大的兴趣。在本研究中,已开展工作来研究含有具有相似和不同变形特性辅料的二元混合物片剂的行为。二元混合物片剂通过直接压片法制备,使用了乳糖、聚氯乙烯(PVC)、丙烯酸树脂RS 100和微晶纤维素(MCC)。将渗流理论应用于可压性、最大压力(Pmax)或压缩敏感性(压缩性)、γ与混合物组成之间的关系,结果表明即使对于具有相似变形特性的混合物也存在渗流阈值。结果显示,所有混合物组成的斜率至少有一个离散变化,这被称为渗流阈值。PVC/丙烯酸树脂RS100混合物组成在PVC含量为80%(w/w)时表现出显著的渗流阈值。从一系列含有相似塑性变形材料(PVC/MCC)的二元混合物中观察到两个渗流阈值。渗流阈值在PVC含量为20%(w/w)和80%(w/w)时确定。在这些区域,其中一种组分贯穿整个体系渗透,预计片剂的性质会发生突然变化。然而,实验结果表明,对于PVC/乳糖混合物,在含量为20 - 30%(w/w)时,在指定的渗流阈值处可观察到片剂物理性质的完全破坏,而对于PVC/MCC或PVC/丙烯酸树脂RS 100混合物,仅观察到片剂强度有微小变化。

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