Abstract
Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the burst effect increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms.
Highlights
IntroductionHydrophilic matrices are the most widely used sustained-release oral dosage forms
Hydrophilic matrices are the most widely used sustained-release oral dosage forms.Their advantages lie primarily in the flexibility of dissolution behaviour, the low cost of the tableting process, and the availability of numerous swelling polymeric carriers differing in their origin [1]
While the USP results showed that the Neusilin® US2 (NEU) was unsuitable for formulating HPMC matrices due to much faster drug release, the biorelevant dynamic dissolution test did not confirm these findings and partially mitigated the differences between the filler’s influence
Summary
Hydrophilic matrices are the most widely used sustained-release oral dosage forms Their advantages lie primarily in the flexibility of dissolution behaviour, the low cost of the tableting process, and the availability of numerous swelling polymeric carriers differing in their origin [1]. It is available under several trademarks, and its linear polysaccharide molecules differ in the degree of substitution, ratio of side groups, final molecular weight, and solution viscosity. These parameters significantly affect the drug’s liberation from HPMC-based matrix systems and influence standard processes such as surface hydration, swelling, and gel layer formation [3]. In combination with API and other pharmaceutical excipients, HPMC co-participates in the dissolution behaviour of the final matrix system, characterized by the drug’s dissolution rate, kinetics, and release mechanism, including the diffusion of API molecules through the surface gel layer, erosion, or a combination of both processes [4]
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