Investigation of the influence of particle size on the excipient percolation thresholds of HPMC hydrophilic matrix tablets.
Investigation of the influence of particle size on the excipient percolation thresholds of HPMC hydrophilic matrix tablets.
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研究粒径对 HPMC 亲水骨架片赋形剂渗滤阈值的影响。
DOI：
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发表时间：
2007
期刊：
影响因子：
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通讯作者：
I. Caraballo
中科院分区：
文献类型：
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作者：
Antonia Miranda;M. Millán;I. Caraballo
在我们研究组之前的论文中，在惰性基质的情况下，发现药物渗透阈值和相对药物粒径（药物/赋形剂）之间存在线性关系。本文的目的是研究亲水性基质中颗粒尺寸对赋形剂渗滤阈值的影响。这种影响会对这些控释装置的释放行为产生重要影响。使用 KCl/洛苯扎利二钠作为药物，HPMC K4M 作为基质形成材料，采用六种不同的赋形剂/药物粒度比（范围从 0.42 至 4.16）制备骨架片。研究的制剂载药量在 20-90% (w/w) 范围内。为了估计渗滤阈值，研究了零时间时动力学参数相对于每种组分的体积分数的行为。获得的结果支持组分渗滤阈值（药物或赋形剂）与其相对粒径（在药物渗滤阈值的情况下为药物/赋形剂或在赋形剂渗滤阈值的情况下为赋形剂/药物）之间存在线性关系。这种关系对于不同的药物、赋形剂和系统（惰性或亲水性骨架片）是有效的。
In previous papers of our research group, a linear relationship between the drug percolation threshold and the relative drug particle size (drug/excipient) has been found, in the case of the inert matrices. The objective of the present paper is to investigate the influence of the particle size on the excipient percolation threshold in the case of hydrophilic matrices. This influence can have important consequences on the release behaviour of these controlled release devices. Matrix tablets have been prepared using KCl/Lobenzarit Disodium as drugs and HPMC K4M as matrix forming material, employing six different excipient/drug particle size ratios (ranging from 0.42 to 4.16). The formulations studied contain a drug loading in the range of 20-90% (w/w). In order to estimate the percolation threshold, the behaviour of the kinetic parameters with respect to the volumetric fraction of each component at time zero, was studied. The obtained results support the existence of a linear relationship between a component percolation threshold (drug or excipient) and its relative particle size (drug/excipient in the case of the drug percolation threshold or excipient/drug in the case of the excipient percolation threshold). This relationship is valid for different drugs, excipients and systems (inert or hydrophilic matrix tablets).